ChEMBL ligand: CHEMBL54 (Dolpin, Dozic, Fortunan, Haldol, Haldol solutab, Haloperidol, Haloperidol decanoate impurity, haloperidol-, Kentace, Keselen, MCN-JR-1625, NSC-170973, NSC-615296, R-1625, Serenace)
3-beta-hydroxysteroid-delta(8),delta(7)-isomerase in Human [ChEMBL: CHEMBL4931] [UniProtKB: Q15125] There should be some charts here, you may need to enable JavaScript!
α1A-adrenoceptor/Alpha-1a adrenergic receptor in Human [ChEMBL: CHEMBL229] [GtoPdb: 22] [UniProtKB: P35348] Alpha-1a adrenergic receptor in Bovine [ChEMBL: CHEMBL4892] [UniProtKB: P18130] α1A-adrenoceptor/Alpha-1a adrenergic receptor in Rat [ChEMBL: CHEMBL319] [GtoPdb: 22] [UniProtKB: P43140] There should be some charts here, you may need to enable JavaScript!
α1B-adrenoceptor/Alpha-1b adrenergic receptor in Rat [ChEMBL: CHEMBL315] [GtoPdb: 23] [UniProtKB: P15823] There should be some charts here, you may need to enable JavaScript!
α1D-adrenoceptor/Alpha-1d adrenergic receptor in Human [ChEMBL: CHEMBL223] [GtoPdb: 24] [UniProtKB: P25100] There should be some charts here, you may need to enable JavaScript!
α2A-adrenoceptor/Alpha-2a adrenergic receptor in Human [ChEMBL: CHEMBL1867] [GtoPdb: 25] [UniProtKB: P08913] There should be some charts here, you may need to enable JavaScript!
α2B-adrenoceptor/Alpha-2b adrenergic receptor in Human [ChEMBL: CHEMBL1942] [GtoPdb: 26] [UniProtKB: P18089] There should be some charts here, you may need to enable JavaScript!
α2C-adrenoceptor/Alpha-2c adrenergic receptor in Human [ChEMBL: CHEMBL1916] [GtoPdb: 27] [UniProtKB: P18825] There should be some charts here, you may need to enable JavaScript!
AP-2 complex subunit sigma in Rat [ChEMBL: CHEMBL1697667] [UniProtKB: P62744] There should be some charts here, you may need to enable JavaScript!
β1-adrenoceptor/Beta-1 adrenergic receptor in Rat [ChEMBL: CHEMBL3252] [GtoPdb: 28] [UniProtKB: P18090] There should be some charts here, you may need to enable JavaScript!
β2-adrenoceptor/Beta-2 adrenergic receptor in Rat [ChEMBL: CHEMBL3754] [GtoPdb: 29] [UniProtKB: P10608] There should be some charts here, you may need to enable JavaScript!
C-8 sterol isomerase in Saccharomyces cerevisiae S288c [ChEMBL: CHEMBL3224] [UniProtKB: P32352] There should be some charts here, you may need to enable JavaScript!
D1 receptor/Dopamine D1 receptor in Human [ChEMBL: CHEMBL2056] [GtoPdb: 214] [UniProtKB: P21728] Dopamine D1 receptor in Pig [ChEMBL: CHEMBL5067] [UniProtKB: P50130] D1 receptor/Dopamine D1 receptor in Rat [ChEMBL: CHEMBL265] [GtoPdb: 214] [UniProtKB: P18901] There should be some charts here, you may need to enable JavaScript!
Dopamine D2 receptor in Chlorocebus aethiops [ChEMBL: CHEMBL5456] [UniProtKB: P52702] D2 receptor/Dopamine D2 receptor in Human [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416] Dopamine D2 receptor in Bovine [ChEMBL: CHEMBL3998] [UniProtKB: P20288] D2 receptor/Dopamine D2 receptor in Rat [ChEMBL: CHEMBL339] [GtoPdb: 215] [UniProtKB: P61169] There should be some charts here, you may need to enable JavaScript!
Dopamine D3 receptor in Chlorocebus aethiops [ChEMBL: CHEMBL2304406] [UniProtKB: P52703] D3 receptor/Dopamine D3 receptor in Human [ChEMBL: CHEMBL234] [GtoPdb: 216] [UniProtKB: P35462] D3 receptor/Dopamine D3 receptor in Rat [ChEMBL: CHEMBL3138] [GtoPdb: 216] [UniProtKB: P19020] There should be some charts here, you may need to enable JavaScript!
D4 receptor/Dopamine D4 receptor in Human [ChEMBL: CHEMBL219] [GtoPdb: 217] [UniProtKB: P21917] D4 receptor/Dopamine D4 receptor in Rat [ChEMBL: CHEMBL3361] [GtoPdb: 217] [UniProtKB: P30729] There should be some charts here, you may need to enable JavaScript!
D5 receptor/Dopamine D5 receptor in Human [ChEMBL: CHEMBL1850] [GtoPdb: 218] [UniProtKB: P21918] There should be some charts here, you may need to enable JavaScript!
DAT/Dopamine transporter in Rat [ChEMBL: CHEMBL338] [GtoPdb: 927] [UniProtKB: P23977] There should be some charts here, you may need to enable JavaScript!
GluN1/GluN2A/GluN2B/GluN2C/GluN2D/GluN3B/GluN3A/Glutamate NMDA receptor in Rat [ChEMBL: CHEMBL1907608] [GtoPdb: 455, 456, 457, 458, 459, 461, 460] [UniProtKB: P35439, Q00959, Q00960, Q00961, Q62645, Q8VHN2, Q9R1M7] There should be some charts here, you may need to enable JavaScript!
GluN2B/Glutamate [NMDA] receptor subunit epsilon 2 in Mouse [ChEMBL: CHEMBL3442] [GtoPdb: 457] [UniProtKB: Q01097] There should be some charts here, you may need to enable JavaScript!
Kv11.1/HERG in Human [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809] There should be some charts here, you may need to enable JavaScript!
H1 receptor/Histamine H1 receptor in Human [ChEMBL: CHEMBL231] [GtoPdb: 262] [UniProtKB: P35367] H1 receptor/Histamine H1 receptor in Rat [ChEMBL: CHEMBL4701] [GtoPdb: 262] [UniProtKB: P31390] Histamine H1 receptor in Guinea pig [ChEMBL: CHEMBL3943] [UniProtKB: P31389] There should be some charts here, you may need to enable JavaScript!
H2 receptor/Histamine H2 receptor in Human [ChEMBL: CHEMBL1941] [GtoPdb: 263] [UniProtKB: P25021] There should be some charts here, you may need to enable JavaScript!
HLA class I histocompatibility antigen A-3 in Human [ChEMBL: CHEMBL2632] [UniProtKB: P04439] There should be some charts here, you may need to enable JavaScript!
Human immunodeficiency virus type 1 protease in Human immunodeficiency virus 1 [ChEMBL: CHEMBL243] [UniProtKB: Q72874] There should be some charts here, you may need to enable JavaScript!
Human rhinovirus A protease in Human rhinovirus sp. [ChEMBL: CHEMBL2857] [UniProtKB: Q4U254] There should be some charts here, you may need to enable JavaScript!
μ receptor/Mu opioid receptor in Human [ChEMBL: CHEMBL233] [GtoPdb: 319] [UniProtKB: P35372] There should be some charts here, you may need to enable JavaScript!
M1 receptor/Muscarinic acetylcholine receptor M1 in Human [ChEMBL: CHEMBL216] [GtoPdb: 13] [UniProtKB: P11229] M1 receptor/Muscarinic acetylcholine receptor M1 in Rat [ChEMBL: CHEMBL276] [GtoPdb: 13] [UniProtKB: P08482] There should be some charts here, you may need to enable JavaScript!
M2 receptor/Muscarinic acetylcholine receptor M2 in Rat [ChEMBL: CHEMBL309] [GtoPdb: 14] [UniProtKB: P10980] There should be some charts here, you may need to enable JavaScript!
M5 receptor/Muscarinic acetylcholine receptor M5 in Human [ChEMBL: CHEMBL2035] [GtoPdb: 17] [UniProtKB: P08912] There should be some charts here, you may need to enable JavaScript!
N-acetyltransferase Eis in Mycobacterium tuberculosis [ChEMBL: CHEMBL3879870] [UniProtKB: P9WFK7] There should be some charts here, you may need to enable JavaScript!
NET/Norepinephrine transporter in Human [ChEMBL: CHEMBL222] [GtoPdb: 926] [UniProtKB: P23975] There should be some charts here, you may need to enable JavaScript!
ABCB1/P-glycoprotein 1 in Human [ChEMBL: CHEMBL4302] [GtoPdb: 768] [UniProtKB: P08183] There should be some charts here, you may need to enable JavaScript!
Plasmodium falciparum [ChEMBL: CHEMBL364] There should be some charts here, you may need to enable JavaScript!
K2P2.1/Potassium channel subfamily K member 2 in Human [ChEMBL: CHEMBL2321615] [GtoPdb: 514] [UniProtKB: O95069] There should be some charts here, you may need to enable JavaScript!
Prion protein in Human [ChEMBL: CHEMBL4869] [UniProtKB: P04156] There should be some charts here, you may need to enable JavaScript!
5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Human [ChEMBL: CHEMBL214] [GtoPdb: 1] [UniProtKB: P08908] 5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Rat [ChEMBL: CHEMBL273] [GtoPdb: 1] [UniProtKB: P19327] There should be some charts here, you may need to enable JavaScript!
5-HT1B receptor/Serotonin 1b (5-HT1b) receptor in Rat [ChEMBL: CHEMBL3459] [GtoPdb: 2] [UniProtKB: P28564] There should be some charts here, you may need to enable JavaScript!
5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Human [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223] Serotonin 2a (5-HT2a) receptor in Pig [ChEMBL: CHEMBL2490] [UniProtKB: P50129] Serotonin 2a (5-HT2a) receptor in Bovine [ChEMBL: CHEMBL3446] [UniProtKB: Q75Z89] 5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Rat [ChEMBL: CHEMBL322] [GtoPdb: 6] [UniProtKB: P14842] There should be some charts here, you may need to enable JavaScript!
5-HT2B receptor/Serotonin 2b (5-HT2b) receptor in Human [ChEMBL: CHEMBL1833] [GtoPdb: 7] [UniProtKB: P41595] There should be some charts here, you may need to enable JavaScript!
5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Human [ChEMBL: CHEMBL225] [GtoPdb: 8] [UniProtKB: P28335] 5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Rat [ChEMBL: CHEMBL324] [GtoPdb: 8] [UniProtKB: P08909] There should be some charts here, you may need to enable JavaScript!
5-HT3A/Serotonin 3a (5-HT3a) receptor in Mouse [ChEMBL: CHEMBL4972] [GtoPdb: 373] [UniProtKB: P23979] There should be some charts here, you may need to enable JavaScript!
5-HT6 receptor/Serotonin 6 (5-HT6) receptor in Human [ChEMBL: CHEMBL3371] [GtoPdb: 11] [UniProtKB: P50406] There should be some charts here, you may need to enable JavaScript!
5-HT7 receptor/Serotonin 7 (5-HT7) receptor in Human [ChEMBL: CHEMBL3155] [GtoPdb: 12] [UniProtKB: P34969] 5-HT7 receptor in Mouse [GtoPdb: 12] [UniProtKB: P32304] 5-HT7 receptor/Serotonin 7 (5-HT7) receptor in Rat [ChEMBL: CHEMBL3223] [GtoPdb: 12] [UniProtKB: P32305] There should be some charts here, you may need to enable JavaScript!
SERT/Serotonin transporter in Human [ChEMBL: CHEMBL228] [GtoPdb: 928] [UniProtKB: P31645] SERT/Serotonin transporter in Rat [ChEMBL: CHEMBL313] [GtoPdb: 928] [UniProtKB: P31652] There should be some charts here, you may need to enable JavaScript!
Sigma-1 receptor in Guinea pig [ChEMBL: CHEMBL4153] [UniProtKB: Q60492] There should be some charts here, you may need to enable JavaScript!
σ2/Sigma intracellular receptor 2 in Human [ChEMBL: CHEMBL4105907] [GtoPdb: 2553] [UniProtKB: Q5BJF2] σ2/Sigma intracellular receptor 2 in Rat [ChEMBL: CHEMBL4105864] [GtoPdb: 2553] [UniProtKB: Q5U3Y7] There should be some charts here, you may need to enable JavaScript!
sigma non-opioid intracellular receptor 1/Sigma opioid receptor in Human [ChEMBL: CHEMBL287] [GtoPdb: 2552] [UniProtKB: Q99720] sigma non-opioid intracellular receptor 1/Sigma opioid receptor in Rat [ChEMBL: CHEMBL3602] [GtoPdb: 2552] [UniProtKB: Q9R0C9] There should be some charts here, you may need to enable JavaScript!
Transporter in Rat [ChEMBL: CHEMBL6184] [UniProtKB: Q63380] There should be some charts here, you may need to enable JavaScript!
Urokinase plasminogen activator surface receptor in Human [ChEMBL: CHEMBL4883] [UniProtKB: Q03405] There should be some charts here, you may need to enable JavaScript!
Vesicular acetylcholine transporter in Rat [ChEMBL: CHEMBL2125] [GtoPdb: 1013] [UniProtKB: Q62666] There should be some charts here, you may need to enable JavaScript!
Zinc finger protein 664 in Guinea pig [ChEMBL: CHEMBL4105757] [UniProtKB: Q60493] There should be some charts here, you may need to enable JavaScript!
5-HT1D receptor in Human [GtoPdb: 3] [UniProtKB: P28221] There should be some charts here, you may need to enable JavaScript!
Kir3.2 in Mouse [GtoPdb: 435] [UniProtKB: P48542] There should be some charts here, you may need to enable JavaScript!
Kv10.1 in Human [GtoPdb: 570] [UniProtKB: O95259] There should be some charts here, you may need to enable JavaScript!

DB	Assay description	Assay Type	Standard value	Standard parameter	Original value	Original units	Original parameter	Reference
3-beta-hydroxysteroid-delta(8),delta(7)-isomerase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4931] [UniProtKB: Q15125]
ChEMBL	Affinity for human EMP expressed in ERG2 deficient strain of Saccharomyces cerevisiae using [3H]ifenprodil or (+)-[3H]pentazocine as radioligand	B	6.72	pKi	190	nM	Ki	J Med Chem (2005) 48: 4754-4764 [PMID:16033255]
α1A-adrenoceptor/Alpha-1a adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL229] [GtoPdb: 22] [UniProtKB: P35348]
ChEMBL	Binding Assay: Binding assay using 5-HT2A, Dopamine D2, SERT, αA1, 5-HT2C and H1 Receptors.	B	7.96	pKi	11	nM	Ki	US-8598119-B2. Methods and compositions for sleep disorders and other disorders (2013)
Alpha-1a adrenergic receptor in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4892] [UniProtKB: P18130]
ChEMBL	Affinity towards Alpha-1A adrenergic receptor in membranes from bovine frontal cortex using [3H]prazosin	B	7.7	pIC50	20	nM	IC50	J Med Chem (1998) 41: 2010-2018 [PMID:9622542]
α1A-adrenoceptor/Alpha-1a adrenergic receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL319] [GtoPdb: 22] [UniProtKB: P43140]
ChEMBL	Binding affinity towards Alpha-1A adrenergic receptor in rat denuded thoracic aorta	B	7.76	pKd	17.38	nM	Kd	Bioorg Med Chem Lett (2003) 13: 175-178 [PMID:12482418]
ChEMBL	DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)	B	7.55	pKi	28	nM	Ki	DrugMatrix in vitro pharmacology data
ChEMBL	DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)	B	7.17	pIC50	68	nM	IC50	DrugMatrix in vitro pharmacology data
α1B-adrenoceptor/Alpha-1b adrenergic receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL315] [GtoPdb: 23] [UniProtKB: P15823]
ChEMBL	DRUGMATRIX: Alpha-1B adrenergic receptor radioligand binding (ligand: prazosin)	B	8.31	pKi	4.95	nM	Ki	DrugMatrix in vitro pharmacology data
ChEMBL	DRUGMATRIX: Alpha-1B adrenergic receptor radioligand binding (ligand: prazosin)	B	8.05	pIC50	8.94	nM	IC50	DrugMatrix in vitro pharmacology data
α1D-adrenoceptor/Alpha-1d adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL223] [GtoPdb: 24] [UniProtKB: P25100]
ChEMBL	DRUGMATRIX: Alpha-1D adrenergic receptor radioligand binding (ligand: prazosin)	B	7.39	pKi	41	nM	Ki	DrugMatrix in vitro pharmacology data
ChEMBL	DRUGMATRIX: Alpha-1D adrenergic receptor radioligand binding (ligand: prazosin)	B	7.08	pIC50	84	nM	IC50	DrugMatrix in vitro pharmacology data
α2A-adrenoceptor/Alpha-2a adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1867] [GtoPdb: 25] [UniProtKB: P08913]
ChEMBL	DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)	B	5.73	pKi	1865	nM	Ki	DrugMatrix in vitro pharmacology data
ChEMBL	DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)	B	5.3	pIC50	4973	nM	IC50	DrugMatrix in vitro pharmacology data
α2B-adrenoceptor/Alpha-2b adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1942] [GtoPdb: 26] [UniProtKB: P18089]
ChEMBL	DRUGMATRIX: Alpha-2B adrenergic receptor radioligand binding (ligand: Rauwolscine)	B	6.21	pKi	618	nM	Ki	DrugMatrix in vitro pharmacology data
ChEMBL	DRUGMATRIX: Alpha-2B adrenergic receptor radioligand binding (ligand: Rauwolscine)	B	5.87	pIC50	1354	nM	IC50	DrugMatrix in vitro pharmacology data
α2C-adrenoceptor/Alpha-2c adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1916] [GtoPdb: 27] [UniProtKB: P18825]
ChEMBL	DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)	B	6.57	pKi	268	nM	Ki	DrugMatrix in vitro pharmacology data
ChEMBL	DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)	B	5.73	pIC50	1845	nM	IC50	DrugMatrix in vitro pharmacology data
AP-2 complex subunit sigma in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1697667] [UniProtKB: P62744]
ChEMBL	Displacement of [3H]-DTG from rat sigma2 receptor by liquid scintillation counting	B	7.62	pKi	24.2	nM	Ki	J Med Chem (2011) 54: 1555-1564 [PMID:21348515]
β1-adrenoceptor/Beta-1 adrenergic receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3252] [GtoPdb: 28] [UniProtKB: P18090]
ChEMBL	Binding affinity against beta-1 adrenergic receptor in rat brain using [3H]DHA	B	5	pIC50	>10000	nM	IC50	J Med Chem (1986) 29: 1628-1637 [PMID:2875184]
β2-adrenoceptor/Beta-2 adrenergic receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3754] [GtoPdb: 29] [UniProtKB: P10608]
ChEMBL	Binding affinity against beta-2 adrenergic receptor in rat brain using [3H]DHA	B	5	pIC50	>10000	nM	IC50	J Med Chem (1986) 29: 1628-1637 [PMID:2875184]
C-8 sterol isomerase in Saccharomyces cerevisiae S288c (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3224] [UniProtKB: P32352]
ChEMBL	Affinity for ERG2 of Saccharomyces cerevisiae using [3H]ifenprodil or (+)-[3H]pentazocine radioligand	B	9.3	pKi	0.5	nM	Ki	J Med Chem (2005) 48: 4754-4764 [PMID:16033255]
D1 receptor/Dopamine D1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2056] [GtoPdb: 214] [UniProtKB: P21728]
ChEMBL	Binding affinity towards human Dopamine receptor D1	B	6.57	pKi	270	nM	Ki	J Med Chem (2004) 47: 1303-1314 [PMID:14998318]
ChEMBL	Displacement of [3H]SCH23390 from human dopamine D1 receptor by liquid scintillation counting	B	6.92	pKi	120	nM	Ki	Bioorg Med Chem Lett (2014) 24: 4294-4297 [PMID:25070422]
ChEMBL	Binding affinity to human cloned dopamine D1 receptor	B	6.92	pKi	120	nM	Ki	Bioorg Med Chem (2008) 16: 7291-7301 [PMID:18595716]
ChEMBL	Inhibition of human dopamine D1 receptor	B	6.97	pKi	107	nM	Ki	J Med Chem (2011) 54: 2529-2591 [PMID:21413808]
ChEMBL	Binding affinity for human recombinant dopamine receptor D1	B	7.09	pKi	82	nM	Ki	J Med Chem (2004) 47: 4155-4158 [PMID:15293986]
ChEMBL	DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)	B	7.26	pKi	55	nM	Ki	DrugMatrix in vitro pharmacology data
ChEMBL	Compound was tested for the binding affinity against human cloned Dopamine receptor D1 by radioligand ([3H]SCH-23390) binding assay	B	7.31	pKi	49	nM	Ki	J Med Chem (1996) 39: 2764-2772 [PMID:8709107]
ChEMBL	Displacement of [3H]SCH233930 from human D1 receptor expressed in HEK cells	B	7.6	pKi	25	nM	Ki	Bioorg Med Chem Lett (2011) 21: 3622-3626 [PMID:21555222]
GtoPdb	-	-	8.2	pKi	-	-	-	Nature (1991) 350: 614-9 [PMID:1826762]; J Psychopharmacol (Oxford) (2009) 23: 65-73 [PMID:18308814]
ChEMBL	Displacement of [3H]SCH23390 from human dopamine D1 receptor	B	8.21	pKi	6.17	nM	Ki	Bioorg Med Chem Lett (2009) 19: 6059-6062 [PMID:19796944]
ChEMBL	DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)	B	6.96	pIC50	110	nM	IC50	DrugMatrix in vitro pharmacology data
Dopamine D1 receptor in Pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5067] [UniProtKB: P50130]
ChEMBL	Displacement of [3H]SCH23390 from dopamine D1 receptor in pig striatal membranes	B	7.01	pKi	98	nM	Ki	J Med Chem (2010) 53: 7219-7228 [PMID:20839776]
ChEMBL	Displacement of [3H]SCH23390 from D1 receptor from porcine cerebral cortex homogenates	B	7.03	pKi	93	nM	Ki	J Med Chem (2011) 54: 4896-4903 [PMID:21599022]
ChEMBL	Displacement of [3H]SCH 23390 from pig dopamine D1 receptor in striatal membrane	B	7.03	pKi	93	nM	Ki	J Med Chem (2011) 54: 7911-7919 [PMID:21999579]
ChEMBL	Displacement of [3H]SCH23390 from porcine striatal membranes D1 receptor by competitive binding assay	B	8.02	pKi	9.5	nM	Ki	Bioorg Med Chem Lett (2014) 24: 3753-3756 [PMID:25047579]
D1 receptor/Dopamine D1 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL265] [GtoPdb: 214] [UniProtKB: P18901]
ChEMBL	Tested for binding affinity towards rat striatal dopamine receptor D1 using [3H]-SCH- 23390 as radioligand	B	6.33	pKi	467	nM	Ki	J Med Chem (1994) 37: 3523-3533 [PMID:7932581]
ChEMBL	Inhibition of [3H]SCH-23390 binding to rat Dopamine receptor D1	B	6.44	pKi	359	nM	Ki	J Med Chem (2005) 48: 1709-1712 [PMID:15771415]
ChEMBL	Binding affinity to dopamine D1 receptor in rat striatum by liquid scintillation counting method	B	6.5	pKi	318	nM	Ki	J Med Chem (2018) 61: 372-384 [PMID:29220177]
ChEMBL	Displacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometry	B	6.5	pKi	318	nM	Ki	J Med Chem (2009) 52: 151-169 [PMID:19072656]
ChEMBL	Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate	B	6.5	pKi	318	nM	Ki	J Med Chem (2002) 45: 344-359 [PMID:11784139]
ChEMBL	Inhibition of [3H]-SCH- 23390 binding to rat dopamine D1 receptor	B	6.5	pKi	318	nM	Ki	J Med Chem (2005) 48: 1705-1708 [PMID:15771414]
ChEMBL	In vitro binding affinity towards Dopamine receptor D1 in rat tissue homogenate using [3H]-SCH- 23390 as radioligand	B	6.5	pKi	318	nM	Ki	J Med Chem (2004) 47: 143-157 [PMID:14695828]
ChEMBL	Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate	B	6.5	pKi	316.23	nM	Ki	J Med Chem (2002) 45: 344-359 [PMID:11784139]
ChEMBL	In vitro affinity against Dopamine receptor D1	B	6.7	pKi	199.53	nM	Ki	J Med Chem (2000) 43: 4678-4693 [PMID:11101359]
ChEMBL	In vitro ability to displace [3H]SCH-23390 binding from Dopamine 1 (D1) receptor in rat striatal membrane.	B	6.8	pKi	158.49	nM	Ki	J Med Chem (1999) 42: 2774-2797 [PMID:10425088]
ChEMBL	Binding affinity measured at the Dopamine receptor D1 by the inhibition of [3H]SCH-23390 binding to rat striatum using unlabeled apomorphine for nonspecific binding.	B	6.84	pKi	145	nM	Ki	J Med Chem (1998) 41: 5402-5409 [PMID:9876110]
ChEMBL	Inhibition constant for in vitro inhibition of [3H]-SCH- 23390 binding to striatal membranes Dopamine receptor D1	B	7.01	pKi	97.72	nM	Ki	Bioorg Med Chem Lett (1995) 5: 579-584
ChEMBL	Compound was evaluated for its affinity (pKi) to inhibit [3H]SCH-23390 binding to the Dopamine receptor D1	B	7.01	pKi	97.72	nM	Ki	J Med Chem (1991) 34: 2242-2247 [PMID:1676759]
ChEMBL	Inhibition of [3H]-SCH- 23390 binding to dopamine receptor D1 rat striatal membrane	B	7.01	pKi	97.72	nM	Ki	J Med Chem (1994) 37: 2564-2573 [PMID:7914540]
ChEMBL	In vitro binding affinity against Dopamine receptor D1 in rat striatal tissue	B	7.12	pKi	76	nM	Ki	J Med Chem (1993) 36: 2107-2114 [PMID:8101877]
ChEMBL	Binding affinity against dopamine receptor D1	B	7.12	pKi	75.86	nM	Ki	J Med Chem (1994) 37: 519-525 [PMID:7907148]
ChEMBL	Binding Affinity was determined against Dopamine receptor D1 in rat striatal membranes using [3H]- SCH 23390 radioligand.	B	7.15	pKi	70.79	nM	Ki	J Med Chem (2000) 43: 599-608 [PMID:10691686]
ChEMBL	Displacement of [3H]SCH-23390 from dopamine D1 receptor in rat brain	B	7.24	pKi	58.08	nM	Ki	Bioorg Med Chem (2007) 15: 7361-7367 [PMID:17869521]
ChEMBL	Binding affinity was measured against dopamine receptor D1 in rat using [3H]SCH-23390 as radioligand	B	7.33	pKi	47	nM	Ki	J Med Chem (1994) 37: 1964-1970 [PMID:8027978]
ChEMBL	Ability to displace [3H]-SCH- 23390 (0.2 nM) from corpus striatum of rat Dopamine receptor D1	B	7.54	pKi	29	nM	Ki	J Med Chem (2003) 46: 265-283 [PMID:12519065]
ChEMBL	Binding affinity towards Dopamine receptor D1	B	7.62	pKi	24	nM	Ki	J Med Chem (1987) 30: 1433-1454 [PMID:3039136]
ChEMBL	Affinity for Dopamine receptor D1	B	7.7	pKi	20	nM	Ki	Bioorg Med Chem Lett (1998) 8: 983-988 [PMID:9871525]
ChEMBL	Inhibitory concentration against rat striatal dopamine (D1) sensitive adenylate cyclase activity	F	6.26	pIC50	550	nM	IC50	J Med Chem (1987) 30: 1906-1910 [PMID:2888899]
ChEMBL	Binding affinity towards Dopamine receptor D1 in rat membranes using [3H]SCH-23390 as radioligand	B	6.47	pIC50	337	nM	IC50	J Med Chem (1991) 34: 3360-3365 [PMID:1662725]
ChEMBL	Binding affinity towards D1 CNS receptor of rat corpus striatum using [3H]SCH-23390 as radioligand	B	7.44	pIC50	36	nM	IC50	J Med Chem (1999) 42: 2235-2244 [PMID:10377229]
ChEMBL	Inhibitory binding of [3H]SCH-23390 to Dopamine receptor D1 in membranes from rat corpus striatum	B	7.44	pIC50	36	nM	IC50	J Med Chem (1997) 40: 4146-4153 [PMID:9406603]
Dopamine D2 receptor in Chlorocebus aethiops (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5456] [UniProtKB: P52702]
ChEMBL	Displacement of [3H]-YM 09151 from african green monkey Dopamine receptor D2	B	8.3	pKi	5	nM	Ki	J Med Chem (1995) 38: 4950-4952 [PMID:8523409]
ChEMBL	Displacement of [3H]YM-09151 from recombinant African green monkey Dopamine receptor D2	B	8.32	pKi	4.8	nM	Ki	J Med Chem (1995) 38: 2251-2255 [PMID:7783157]
D2 receptor/Dopamine D2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416]
ChEMBL	Displacement of PPHT-red from SNAP-tagged human D2LR expressed in CHOK1 cell membranes by TR-FRET assay	B	9.31	pKd	0.49	nM	Kd	J Med Chem (2019) 62: 9488-9520 [PMID:31580666]
ChEMBL	Displacement of [3H]spiroperidol from human cloned dopaminergic D2 receptor expressed in rat C6 cells	B	5.19	pKi	6400	nM	Ki	J Med Chem (2008) 51: 7602-7613 [PMID:19053888]
ChEMBL	Tested for affinity against cloned mammalian dopamine autoreceptor (DA) D2 receptors expressed in CHO-K1 cells using [3H]spiperone as radioligand	B	6.66	pKi	>217	nM	Ki	J Med Chem (1994) 37: 2735-2753 [PMID:8064801]
ChEMBL	Displacement of the radioligand [3H]spiperone from the cloned human Dopamine receptor D2 long expressed in CHO cells	B	7.74	pKi	18	nM	Ki	Bioorg Med Chem Lett (2002) 12: 1327-1330 [PMID:11992769]
ChEMBL	Displacement of [3H]N-methylspiperone from human dopamine D2 receptor by PDSP assay	B	8.02	pKi	9.6	nM	Ki	Bioorg Med Chem (2016) 24: 2060-2071 [PMID:27032890]
ChEMBL	Displacement of [3H]N-methylspiperone from human dopamine D2 receptor assessed as inhibition constant	B	8.02	pKi	9.6	nM	Ki	J Med Chem (2023) 66: 10060-10079 [PMID:37421373]
ChEMBL	In vitro binding affinity at human cloned Dopamine receptor D2L expressed in Sf9 cell membranes	B	8.07	pKi	8.5	nM	Ki	J Med Chem (2002) 45: 5136-5149 [PMID:12408724]
ChEMBL	Displacement of [3H]-spiperone from human D2s receptor expressed in CHO-K1 cells membrane incubated for 1 hr by microbeta liquid scintillation counting analysis	B	8.13	pKi	7.41	nM	Ki	Eur J Med Chem (2023) 252: 115285-115285 [PMID:37027998]
ChEMBL	Antagonism of dopamine-stimulated [35S]GTP-gamma-S binding against human Dopamine receptor D2 in CHO cells	F	8.15	pKi	7	nM	Ki	J Med Chem (2000) 43: 3923-3932 [PMID:11052797]
ChEMBL	Displacement of [3H]-N-methylspiperone from D2 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method	B	8.2	pKi	6.33	nM	Ki	J Med Chem (2021) 64: 17239-17258 [PMID:34797051]
ChEMBL	Displacement of [3H]-N-methylspiperone from D2 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method	B	8.2	pKi	6.31	nM	Ki	J Med Chem (2021) 64: 17239-17258 [PMID:34797051]
ChEMBL	Displacement of [3H]spiperone from human D2S receptor expressed in CHO-K1 cells by radioligand competitive binding analysis	B	8.21	pKi	6.22	nM	Ki	J Nat Prod (2020) 83: 127-133 [PMID:31933369]
ChEMBL	Displacement of [3H]spiperone from human D2S receptor expressed in CHO-K1 cells by radioligand competitive binding analysis	B	8.21	pKi	6.17	nM	Ki	J Nat Prod (2020) 83: 127-133 [PMID:31933369]
ChEMBL	Displacement of [3H]methylspiperonee from recombinant human D2 receptor expressed in HEK293 cells cell membranes after 60 mins by liquid scintillation counting method	B	8.23	pKi	5.9	nM	Ki	Bioorg Med Chem Lett (2018) 28: 2039-2049 [PMID:29730027]
ChEMBL	In vitro binding affinity towards Dopamine receptor D2L, using [3H]spiroperidol radioligand in Sf9 baculovirus expression.	B	8.25	pKi	5.6	nM	Ki	J Med Chem (2000) 43: 270-277 [PMID:10649982]
ChEMBL	Displacement of [3H]N-methylspiperone from dopamine D2 receptor (unknown origin)	B	8.25	pKi	5.58	nM	Ki	Bioorg Med Chem Lett (2020) 30: 127305-127305 [PMID:32631525]
ChEMBL	Displacement of [3H]-N-Methylspiperone from human dopamine D2 receptor expressed in stable fibroblast cells incubated for 90 mins by microbeta counting method	B	8.25	pKi	5.58	nM	Ki	Bioorg Med Chem (2020) 28: 115578-115578 [PMID:32631561]
ChEMBL	Displacement of [3H]YM-09151-2 from human dopamine D2S receptor in membrane suspensions by liquid scintillation counter	B	8.29	pKi	5.09	nM	Ki	Bioorg Med Chem (2008) 16: 8875-8881 [PMID:18793859]
ChEMBL	Displacement of [3H]spiperone from human dopamine D2 receptor short form expressed in CHO cells	B	8.3	pKi	5.01	nM	Ki	J Med Chem (2007) 50: 5103-5108 [PMID:17880057]
ChEMBL	Binding affinity on human Dopamine receptor D2 expressed in CHO cells using radioligand [3H]-YM 09151	B	8.32	pKi	4.8	nM	Ki	J Med Chem (1997) 40: 1-3 [PMID:9016321]
ChEMBL	Displacement of [3H]-raclopride from human D2 receptor expressed in HEK cells incubated for 1 hr by Cheng-Prusoff analysis based microbeta scintillation counting method	B	8.35	pKi	4.5	nM	Ki	Eur J Med Chem (2019) 180: 383-397 [PMID:31325785]
ChEMBL	Displacement of [3H]-raclopride from recombinant human D2 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting analysis	B	8.35	pKi	4.5	nM	Ki	Eur J Med Chem (2019) 166: 144-158 [PMID:30703658]
ChEMBL	Displacement of [3H]spiroperidol from human cloned dopamine D2L receptor by liquid scintillation counting	B	8.38	pKi	4.2	nM	Ki	Bioorg Med Chem (2009) 17: 758-766 [PMID:19081257]
ChEMBL	Displacement of [3H]spiroperidol from human cloned dopamine D2L receptor expressed in rat C6 cells	B	8.38	pKi	4.2	nM	Ki	J Med Chem (2008) 51: 5813-5822 [PMID:18800769]
ChEMBL	Displacement of [3H]N-methylspiperone from human recombinant dopamine D2 receptor expressed in CHOK1 cells incubated for 60 mins by scintillation counting method	B	8.4	pKi	4	nM	Ki	Eur J Med Chem (2015) 92: 221-235 [PMID:25557493]
ChEMBL	Displacement of [3H]N-methylspiperone from human recombinant D2 receptor expressed in CHO-K1 cell membrane after 60 mins by liquid scintillation counting analysis	B	8.4	pKi	4	nM	Ki	J Med Chem (2014) 57: 4543-4557 [PMID:24805037]
ChEMBL	In vitro binding affinity towards Dopamine receptor D2 in human using [3H]-spiperone as radioligand	B	8.43	pKi	3.7	nM	Ki	J Med Chem (2004) 47: 143-157 [PMID:14695828]
ChEMBL	Potency was measured by the displacement of [3H]spiperone binding to human D2 dopaminergic receptor	B	8.44	pKi	3.6	nM	Ki	Bioorg Med Chem Lett (1997) 7: 1207-1212
ChEMBL	Displacement of [3H]-N-methylspiperone from human dopamine D2 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysis	B	8.45	pKi	3.55	nM	Ki	J Med Chem (2021) 64: 7778-7808 [PMID:34011153]
ChEMBL	Displacement of [3H]N-Methylspiperone from dopamine D2 receptor (unknown origin)	B	8.45	pKi	3.55	nM	Ki	Bioorg Med Chem Lett (2014) 24: 576-579 [PMID:24365159]
ChEMBL	Displacement of [3H]N-Methylspiperone from dopamine D2 receptor (unknown origin)	B	8.46	pKi	3.5	nM	Ki	Bioorg Med Chem Lett (2014) 24: 576-579 [PMID:24365159]
ChEMBL	Displacement of [3H]spiperone from human cloned dopamine receptor D2 long expressed in CHO cells	B	8.48	pKi	3.3	nM	Ki	Eur J Med Chem (2007) 42: 1044-1048 [PMID:17316913]
ChEMBL	Displacement of [3H]Spiperone from human D2S receptor expressed in CHOK1 cell membranes measured after 120 mins	B	8.49	pKi	3.25	nM	Ki	Eur J Med Chem (2019) 180: 673-689 [PMID:31357129]
ChEMBL	Displacement of [3H]spiperone from D2 receptor	B	8.52	pKi	3	nM	Ki	Bioorg Med Chem Lett (2009) 19: 5552-5555 [PMID:19720528]
ChEMBL	Displacement of [3H]spiperone form human dopamine D2 receptor by liquid scintillation counting	B	8.52	pKi	3	nM	Ki	Bioorg Med Chem Lett (2010) 20: 2983-2986 [PMID:20347298]
ChEMBL	Displacement of [3H]raclopride from human D2L receptor expressed in CHO cells after 60 mins by scintillation proximity assay	B	8.52	pKi	3	nM	Ki	Bioorg Med Chem Lett (2012) 22: 5134-5140 [PMID:22677319]
ChEMBL	In vitro binding affinity at human cloned dopamine receptor D2 (long) stably expressed in CHO cells by [3H]spiperone displacement.	B	8.52	pKi	3	nM	Ki	Bioorg Med Chem Lett (2003) 13: 405-408 [PMID:12565939]
ChEMBL	Inhibition of human dopamine D2 receptor	B	8.55	pKi	2.84	nM	Ki	J Med Chem (2011) 54: 2529-2591 [PMID:21413808]
ChEMBL	Binding affinity to dopamine D2S receptor (unknown origin) by radioligand displacement assay	B	8.58	pKi	2.61	nM	Ki	Bioorg Med Chem Lett (2022) 59: 128573-128573 [PMID:35063632]
ChEMBL	Displacement of [3H]spiroperidol from human cloned dopamine D2L receptor	B	8.59	pKi	2.6	nM	Ki	J Med Chem (2007) 50: 5043-5047 [PMID:17850060]
ChEMBL	Inhibition of [3H]-spiperone binding to human Dopamine receptor D2	B	8.6	pKi	2.5	nM	Ki	J Med Chem (2005) 48: 1709-1712 [PMID:15771415]
ChEMBL	Binding affinity for human recombinant dopamine D2 receptor	B	8.66	pKi	2.2	nM	Ki	J Med Chem (2004) 47: 4155-4158 [PMID:15293986]
ChEMBL	DRUGMATRIX: Dopamine D2L radioligand binding (ligand: [3H] Spiperone)	B	8.66	pKi	2.2	nM	Ki	DrugMatrix in vitro pharmacology data
ChEMBL	Displacement of [3H]-raclopride from human D2LR expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method	B	8.7	pKi	2	nM	Ki	Eur J Med Chem (2018) 145: 790-804 [PMID:29407591]
ChEMBL	Displacement of [3H]spiroperidol from human recombinant Dopamine D2 long receptor	B	8.7	pKi	2	nM	Ki	J Med Chem (2007) 50: 4214-4221 [PMID:17649988]
ChEMBL	In vitro inhibitory constant against [3H]spiperone binding to human dopamine D2 receptor expressed in CHO cells	B	8.7	pKi	2	nM	Ki	J Med Chem (2005) 48: 6855-6869 [PMID:16250644]
ChEMBL	Binding affinity to human D2 receptor	B	8.71	pKi	1.97	nM	Ki	Bioorg Med Chem Lett (2020) 30: 127053-127053 [PMID:32107165]
ChEMBL	Displacement of [3H]spiperone from human dopamine D2 receptor at low affinity state expressed in HEK293 cells	B	8.72	pKi	1.9	nM	Ki	J Med Chem (2010) 53: 2510-2520 [PMID:20155917]
ChEMBL	Displacement of [3H]-methylspiperone from recombinant human D2 receptor expressed in CHOK1 cell membranes measured after 60 mins by microbeta counting method	B	8.73	pKi	1.86	nM	Ki	Eur J Med Chem (2020) 191: 112149-112149 [PMID:32105980]
ChEMBL	Displacement of [3H]-methylspiperone from human D2 receptor transfected in CHO-K1 cells measured after 60 mins by scintillation counting method	B	8.73	pKi	1.86	nM	Ki	J Med Chem (2021) 64: 12603-12629 [PMID:34436892]
ChEMBL	Ability to displace [3H]spiperone from human cloned Dopamine receptor D2 expressed in CHO K-1 cells in vitro.	B	8.8	pKi	1.6	nM	Ki	J Med Chem (1997) 40: 2688-2693 [PMID:9276014]
ChEMBL	Binding affinity against cloned human dopamine receptor D2 expressed in Chinese hamster ovary (CHO) K-1 cells by displacement of [3H]spiperone.	B	8.8	pKi	1.6	nM	Ki	J Med Chem (1997) 40: 4026-4029 [PMID:9406594]
GtoPdb	-	-	8.8	pKi	-	-	-	J Pharmacol Exp Ther (1994) 268: 417-26 [PMID:8301582]; Eur J Pharmacol (1994) 266: 79-85 [PMID:7907989]; Eur J Pharmacol (1992) 225: 331-7 [PMID:1354163]; Eur J Pharmacol (1995) 290: 29-36 [PMID:7664822]; Pharmacol Biochem Behav (1994) 49: 567-71 [PMID:7862709]
ChEMBL	Displacement of [3H]SCH23390 from human D2long receptor expressed in CHO cells	B	8.82	pKi	1.5	nM	Ki	J Med Chem (2011) 54: 4896-4903 [PMID:21599022]
ChEMBL	Binding affinity for Dopamine receptor D2 by displacement of [3H]-spiperone	B	8.82	pKi	1.5	nM	Ki	Bioorg Med Chem Lett (2000) 10: 509-512 [PMID:10743959]
ChEMBL	Displacement of [3H]spiperone from human DRD2 Long receptor expressed in chinese hamster CHO cells by radioligand binding assay	B	8.82	pKi	1.5	nM	Ki	J Med Chem (2011) 54: 7911-7919 [PMID:21999579]
ChEMBL	Displacement of [3H]methylspiperone from human D2L receptor expressed in HEK cell membrane after 90 mins by scintillation counting analysis	B	8.85	pKi	1.4	nM	Ki	J Med Chem (2014) 57: 3450-3463 [PMID:24666157]
ChEMBL	Ability to displace [3H]spiperone from human dopamine receptor D2 stably expressed in CHO cells.	B	8.85	pKi	1.4	nM	Ki	J Med Chem (1997) 40: 2374-2385 [PMID:9240352]
ChEMBL	Binding affinity to human cloned dopamine D2 receptor	B	8.85	pKi	1.4	nM	Ki	Bioorg Med Chem (2008) 16: 7291-7301 [PMID:18595716]
ChEMBL	Binding affinity towards human Dopamine receptor D2	B	8.85	pKi	1.4	nM	Ki	J Med Chem (2004) 47: 1303-1314 [PMID:14998318]
ChEMBL	Displacement of [3H]spiperone from human Dopamine receptor D2 expressed in CHO cells	B	8.85	pKi	1.4	nM	Ki	J Med Chem (1996) 39: 1943-1945 [PMID:8642551]
ChEMBL	Binding affinity for dopamine receptor D2 determined using [3H]spiperone	B	8.85	pKi	1.4	nM	Ki	Bioorg Med Chem Lett (2001) 11: 2345-2349 [PMID:11527728]
ChEMBL	Binding affinity towards cloned human Dopamine receptor D2 stably expressed in CHO cells was evaluated using [3H]spiperone as radioligand	B	8.85	pKi	1.4	nM	Ki	J Med Chem (1996) 39: 1941-1942 [PMID:8642550]
ChEMBL	Displacement of [3H]-methylspiperone from human D2 receptor expressed in CHO-K1 cells after 60 mins by scintillation counting	B	8.85	pKi	1.4	nM	Ki	J Med Chem (2017) 60: 7483-7501 [PMID:28763213]
ChEMBL	Binding affinity for human dopamine receptor D2 long	B	8.89	pKi	1.3	nM	Ki	J Med Chem (2005) 48: 694-709 [PMID:15689154]
ChEMBL	Binding affinity to dopamine D2	B	8.95	pKi	1.12	nM	Ki	J Med Chem (2007) 50: 489-500 [PMID:17266201]
ChEMBL	Displacement of [125I]ABN from human dopamine D2 long receptor expressed in HEK293 cells after 60 mins by gamma counting	B	8.96	pKi	1.1	nM	Ki	Bioorg Med Chem (2010) 18: 5291-5300 [PMID:20542439]
ChEMBL	Displacement of [3H]spiperone from human D2short receptor expressed in CHO cells	B	8.96	pKi	1.1	nM	Ki	J Med Chem (2011) 54: 4896-4903 [PMID:21599022]
ChEMBL	Displacement of [3H]spiperone from human DRD2 short receptor expressed in chinese hamster CHO cells by radioligand binding assay	B	8.96	pKi	1.1	nM	Ki	J Med Chem (2011) 54: 7911-7919 [PMID:21999579]
ChEMBL	Displacement of [3H]N-methylspiperone from human dopamine D2 receptor by liquid scintillation counting	B	8.96	pKi	1.1	nM	Ki	Bioorg Med Chem (2009) 17: 1716-1723 [PMID:19155177]
ChEMBL	Displacement of [3H]Spiperone from human dopamine D2 long receptor expressed in CHO cells	B	8.96	pKi	1.1	nM	Ki	J Med Chem (2010) 53: 7219-7228 [PMID:20839776]
ChEMBL	Displacement of [3H]spiperone from human dopamine D2 receptor at high affinity state expressed in HEK293 cells	B	9	pKi	1	nM	Ki	J Med Chem (2010) 53: 2510-2520 [PMID:20155917]
ChEMBL	Binding affinity towards Dopamine type 2 receptor was determined by displacement assays using [3H]-YM 09151 as the competitive ligand	B	9	pKi	1	nM	Ki	Bioorg Med Chem Lett (2002) 12: 3111-3115 [PMID:12372513]
ChEMBL	Displacement of [3H]N-methylspiperone from human D2 receptor expressed in HEK cells	B	9	pKi	1	nM	Ki	Bioorg Med Chem Lett (2011) 21: 3622-3626 [PMID:21555222]
ChEMBL	Binding affinity towards mouse LtK- cells transfected with human D2 receptor using [3H]spiperone	B	9	pKi	1	nM	Ki	Bioorg Med Chem Lett (1995) 5: 219-222
ChEMBL	Displacement of [3H]spiperone from human dopamine D2L receptor expressed in CHO cells	B	9.02	pKi	0.96	nM	Ki	ACS Med Chem Lett (2015) 6: 882-887 [PMID:26288260]
ChEMBL	Cataleptogenic effect against cloned human Dopamine receptor D2 in male Sprague-Dawley rats in a bar test	B	9.05	pKi	0.89	nM	Ki	Bioorg Med Chem Lett (2003) 13: 3779-3782 [PMID:14552778]
ChEMBL	Displacement of [3H]spiperone from human Dopamine receptor D2	B	9.05	pKi	9.05	nM	pKi	J Med Chem (2004) 47: 497-508 [PMID:14736232]
ChEMBL	Displacement of [3H]N-methylspiperone from human dopamine D2 receptor by liquid scintillation counting	B	9.05	pKi	0.89	nM	Ki	Bioorg Med Chem Lett (2014) 24: 4294-4297 [PMID:25070422]
ChEMBL	In vitro ability to inhibit the binding of [3H]spiperone to cloned human Dopamine receptor D2 using apomorphine induced climbing test in male Swiss mice	B	9.05	pKi	0.89	nM	Ki	Bioorg Med Chem Lett (2003) 13: 3779-3782 [PMID:14552778]
ChEMBL	Displacement of [3H]Spiperone from human dopamine D2 short receptor expressed in CHO cells	B	9.06	pKi	0.87	nM	Ki	J Med Chem (2010) 53: 7219-7228 [PMID:20839776]
ChEMBL	Displacement of [3H]spiperone from human D2 receptor transfected in HEK cells	B	9.07	pKi	0.85	nM	Ki	J Med Chem (2014) 57: 4368-4381 [PMID:24779610]
ChEMBL	Displacement of [3H]spiperone from human D2short receptor stably expressed in CHO cell membranes by competitive binding assay	B	9.07	pKi	0.85	nM	Ki	Bioorg Med Chem Lett (2014) 24: 3753-3756 [PMID:25047579]
ChEMBL	In vitro binding affinity against human D2 dopamine receptor in CHO cells by [3H]spiperone displacement.	B	9.08	pKi	0.84	nM	Ki	Bioorg Med Chem Lett (1998) 8: 725-730 [PMID:9871530]
ChEMBL	Displacement of [3H]spiperone from human D2long receptor stably expressed in CHO cell membranes by competitive binding assay	B	9.09	pKi	0.81	nM	Ki	Bioorg Med Chem Lett (2014) 24: 3753-3756 [PMID:25047579]
ChEMBL	In vitro binding affinity for Dopamine receptor D2	B	9.1	pKi	0.79	nM	Ki	Bioorg Med Chem Lett (2001) 11: 1313-1316 [PMID:11392544]
ChEMBL	Binding Assay: Binding assay using 5-HT2A, Dopamine D2, SERT, αA1, 5-HT2C and H1 Receptors.	B	9.15	pKi	0.7	nM	Ki	US-8598119-B2. Methods and compositions for sleep disorders and other disorders (2013)
ChEMBL	Inhibition of [3H]raclopride binding to Dopamine receptor D2	B	9.18	pKi	0.66	nM	Ki	J Med Chem (1996) 39: 4421-4429 [PMID:8893836]
ChEMBL	Displacement of [3H]spiperone human cloned dopamine D2 receptor	B	9.22	pKi	0.6	nM	Ki	Bioorg Med Chem Lett (2007) 17: 4873-4877 [PMID:17588750]
ChEMBL	Binding affinity towards dopamine receptor D2	B	9.22	pKi	0.6	nM	Ki	Bioorg Med Chem Lett (2004) 14: 585-589 [PMID:14741248]
ChEMBL	Displacement of [3H]spiperone from human cloned D2 receptor by in vitro binding assay	B	9.22	pKi	0.6	nM	Ki	Medchemcomm (2011) 2: 1194-1200
ChEMBL	Displacement of [3H]spiperone from human D2 receptor	B	9.22	pKi	0.6	nM	Ki	Eur J Med Chem (2014) 71: 237-249 [PMID:24316025]
ChEMBL	Displacement of [3H]spiperone from human cloned dopamine D2 receptor	B	9.22	pKi	0.6	nM	Ki	Bioorg Med Chem Lett (2009) 19: 6059-6062 [PMID:19796944]
ChEMBL	Displacement of [3H]spiperone from human cloned dopamine D2 receptor	B	9.22	pKi	0.6	nM	Ki	J Med Chem (2008) 51: 6085-6094 [PMID:18783204]
ChEMBL	Tested for binding affinity towards human D2L receptor using [3H]spiperone as radioligand	B	9.3	pKi	0.5	nM	Ki	J Med Chem (1994) 37: 3523-3533 [PMID:7932581]
ChEMBL	Displacement of PPHT-red from SNAP-tagged human D2LR expressed in CHOK1 cell membranes by TR-FRET assay	B	9.33	pKi	0.47	nM	Ki	J Med Chem (2019) 62: 9488-9520 [PMID:31580666]
ChEMBL	Displacement of [3H]spiperone from CHO-K1 cell membranes expressing human dopamine receptor D2	B	9.36	pKi	0.44	nM	Ki	J Med Chem (1993) 36: 3929-3936 [PMID:7902870]
ChEMBL	Displacement of [3H]raclopride from human dopamine D2A receptors expressed in LtK cells	B	9.36	pKi	0.44	nM	Ki	Bioorg Med Chem Lett (1999) 9: 2167-2172 [PMID:10465538]
ChEMBL	Displacement of [3H]spiperone from human D2long receptor expressed in CHO cell membranes by radioligand binding assay	B	9.38	pKi	0.42	nM	Ki	Bioorg Med Chem (2017) 25: 5084-5094 [PMID:28666858]
ChEMBL	Displacement of [3H]N-methylspiperone from human D2L receptor expressed in HEK293T cells co-expressing CRE-Luc incubated for 60 mins by microbeta scintillation counting method	B	9.58	pKi	0.26	nM	Ki	Eur J Med Chem (2021) 214: 113190-113190 [PMID:33548637]
ChEMBL	Displacement of [3H]spiperone from human D2short receptor expressed in CHO cell membranes by radioligand binding assay	B	9.6	pKi	0.25	nM	Ki	Bioorg Med Chem (2017) 25: 5084-5094 [PMID:28666858]
ChEMBL	Displacement of [3H]quinpirole from Dopamine receptor D2	B	9.8	pKi	0.16	nM	Ki	J Med Chem (1996) 39: 4421-4429 [PMID:8893836]
ChEMBL	Displacement of [3H]quinpirole from human dopamine D2A receptors expressed in LtK cells	B	9.8	pKi	0.16	nM	Ki	Bioorg Med Chem Lett (1999) 9: 2167-2172 [PMID:10465538]
ChEMBL	Antagonist activity at dopamine D2 receptor (unknown origin)	B	9.92	pKi	0.12	nM	Ki	J Med Chem (2020) 63: 15187-15217 [PMID:33111525]
ChEMBL	Binding affinity towards human Dopamine receptor D2 using [3H]spiroperidol as radioligand	B	9.92	pKi	0.12	nM	Ki	J Med Chem (2002) 45: 5727-5735 [PMID:12477356]
ChEMBL	Antagonist activity at dopamine D2 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of [35S]GTPgammaS binding by scintillation proximity assay	F	6.26	pIC50	550	nM	IC50	Bioorg Med Chem (2013) 21: 856-868 [PMID:23332346]
ChEMBL	Antagonist activity at D2 receptor (unknown origin) after 40 mins by [35S]GTP-gammaS binding assay in presence of quinpirole	F	6.39	pIC50	410	nM	IC50	Bioorg Med Chem (2014) 22: 5838-5846 [PMID:25308766]
ChEMBL	DRUGMATRIX: Dopamine D2L radioligand binding (ligand: [3H] Spiperone)	B	8.18	pIC50	6.59	nM	IC50	DrugMatrix in vitro pharmacology data
ChEMBL	Binding affinity towards human Dopamine receptor D2	B	8.31	pIC50	4.9	nM	IC50	J Med Chem (1999) 42: 2235-2244 [PMID:10377229]
ChEMBL	In vitro binding affinity at human cloned Dopamine receptor D2 by [3H]spiroperidol displacement.	B	8.39	pIC50	4.1	nM	IC50	J Med Chem (1998) 41: 4903-4909 [PMID:9822559]
ChEMBL	Binding affinity to dopamine receptor D2 cloned from human, using [3H]- YM09151 as competitive ligand	B	8.4	pIC50	4	nM	IC50	J Med Chem (2000) 43: 3923-3932 [PMID:11052797]
ChEMBL	Antagonist activity at human dopamine D2 short receptor transiently expressed in HEK293 cells assessed as inhibition of beta-arrestin recruitment after 6 hrs by chemiluminescence assay	B	9.15	pIC50	0.71	nM	IC50	J Med Chem (2014) 57: 4861-4875 [PMID:24831693]
ChEMBL	Antagonist activity at human dopamine D2 short receptor transiently expressed in HEK293 cells assessed as inhibition of beta-arrestin recruitment after 6 hrs by chemiluminescence assay	B	9.15	pIC50	0.7	nM	IC50	J Med Chem (2014) 57: 4861-4875 [PMID:24831693]
ChEMBL	Antagonist activity against human D2LR expressed in CHOK1 cells assessed as inhibition of pergolide-induced beta-arrestin translocation by beta-galactosidase based beta-arrestin recruitment assay	B	9.8	pIC50	0.16	nM	IC50	J Med Chem (2014) 57: 7042-7060 [PMID:25126833]
Dopamine D2 receptor in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3998] [UniProtKB: P20288]
ChEMBL	Binding affinity towards dopamine receptor D2 was determined by displacement of [3H]spiroperidol from bovine nucleus caudate membranes.	B	7.7	pKi	20	nM	Ki	J Med Chem (1987) 30: 814-819 [PMID:2883318]
ChEMBL	Binding towards Dopamine receptor D2 expressed in CHO-K1 cells using [3H]U-86170	B	9.15	pKi	0.7	nM	Ki	J Med Chem (1993) 36: 3188-3196 [PMID:8230107]
ChEMBL	Evaluated for binding towards Dopamine receptor D2 using [3H]-spiperone as radioligand, in cloned mammalian receptors expressed in CHO-K1 cells	B	9.52	pKi	0.3	nM	Ki	J Med Chem (1993) 36: 3188-3196 [PMID:8230107]
ChEMBL	Competition in vitro with the dopamine receptor D2 antagonist [3H]spiperone, for binding sites on calf caudate membranes.	B	7.52	pIC50	30	nM	IC50	J Med Chem (1993) 36: 912-918 [PMID:8096548]
ChEMBL	Affinity towards Dopamine receptor D2 in membranes from bovine striatum using [3H]raclopride	B	8.92	pIC50	1.2	nM	IC50	J Med Chem (1998) 41: 2010-2018 [PMID:9622542]
D2 receptor/Dopamine D2 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL339] [GtoPdb: 215] [UniProtKB: P61169]
ChEMBL	Compound was evaluated for in vitro binding affinity towards Dopamine receptor D2 in rat striatum using [3H]- spiperone as radioligand	B	8	pKi	10	nM	Ki	J Med Chem (1992) 35: 2712-2715 [PMID:1353116]
ChEMBL	Binding affinity measured at the Dopamine receptor D2 by the inhibition of [3H]methylspiperone binding to rat striatum using unlabeled haloperidol for nonspecific binding.	B	8.01	pKi	9.8	nM	Ki	J Med Chem (1998) 41: 5402-5409 [PMID:9876110]
ChEMBL	Binding affinity for dopamine receptor D2 long expressed in Sf9 cells using [125I]IABN radioligand	B	8.12	pKi	7.6	nM	Ki	J Med Chem (2001) 44: 1815-1826 [PMID:11356115]
ChEMBL	Tested in vitro for its ability to inhibit [3H]spiperone binding to Dopamine receptor D2 in rat striatal membrane	B	8.3	pKi	5.01	nM	Ki	Bioorg Med Chem Lett (1997) 7: 913-918
ChEMBL	Inhibition of [3H]-spiperone 23390 binding to dopamine receptor D2 rat striatal membrane	B	8.3	pKi	5.01	nM	Ki	J Med Chem (1994) 37: 2564-2573 [PMID:7914540]
ChEMBL	Inhibition constant for in vitro inhibition of [3H]spiperone binding to striatal membranes Dopamine receptor D2	B	8.3	pKi	5.01	nM	Ki	Bioorg Med Chem Lett (1995) 5: 579-584
ChEMBL	Compound was evaluated for its affinity (pKi) to inhibit [3H]spiperone binding to the Dopamine receptor D2	B	8.3	pKi	5.01	nM	Ki	J Med Chem (1991) 34: 2242-2247 [PMID:1676759]
GtoPdb	-	-	8.3	pKi	-	-	-	Nature (1990) 347: 146-51 [PMID:1975644]
ChEMBL	Compound was tested for its binding affinity towards Dopamine receptor D2 using [3H]spiperone from rat striatum	B	8.32	pKi	4.8	nM	Ki	J Med Chem (1998) 41: 1557-1560 [PMID:9572880]
ChEMBL	In vitro binding affinity towards Dopamine receptor D2 in rat tissue homogenate using [3H]-spiperone as radioligand	B	8.32	pKi	4.8	nM	Ki	J Med Chem (2004) 47: 143-157 [PMID:14695828]
ChEMBL	Inhibition of [3H]spiperone binding to rat dopamine D2 receptor	B	8.32	pKi	4.8	nM	Ki	J Med Chem (2005) 48: 1705-1708 [PMID:15771414]
ChEMBL	Half-maximal inhibition of [3H]spiperone binding to Dopamine receptor D2 in rat striatal homogenate	B	8.32	pKi	4.8	nM	Ki	J Med Chem (2002) 45: 344-359 [PMID:11784139]
ChEMBL	Half-maximal inhibition of [3H]spiperone binding to Dopamine receptor D2 in rat striatal homogenate	B	8.32	pKi	4.79	nM	Ki	J Med Chem (2002) 45: 344-359 [PMID:11784139]
ChEMBL	Displacement of [3H]YM-09151-2 from rat striatum D2 receptor	B	8.36	pKi	4.37	nM	Ki	J Med Chem (2007) 50: 865-876 [PMID:17300168]
ChEMBL	In vitro Dopamine receptor D2 affinity by using [3H]-Spiperone as the radioligand in rat limbic system at 1 uM concentration of compound	B	8.4	pKi	4	nM	Ki	J Med Chem (1987) 30: 1818-1823 [PMID:2888898]
ChEMBL	In vitro binding affinity for dopamine receptor D2 of rat nucleus accumbens labeled with [3H]spiperone	B	8.4	pKi	4	nM	Ki	J Med Chem (1987) 30: 1100-1105 [PMID:2884314]
ChEMBL	In vitro ability to displace [3H]spiperone binding from dopamine receptor D2 in rat striatal membrane.	B	8.48	pKi	3.31	nM	Ki	J Med Chem (1999) 42: 2774-2797 [PMID:10425088]
ChEMBL	Compound was measured for the inhibition of [3H]spiperone binding to striatal membrane Dopamine receptor D2	B	8.48	pKi	3.31	nM	Ki	Bioorg Med Chem Lett (1998) 8: 3571-3576 [PMID:9934473]
ChEMBL	Affinity against Dopamine receptor D2	B	8.48	pKi	3.31	nM	Ki	J Med Chem (2000) 43: 4678-4693 [PMID:11101359]
ChEMBL	Binding affinity towards Dopamine receptor D2 in rat frontal striatum using [3H]spiperone	B	8.53	pKi	2.95	nM	Ki	Bioorg Med Chem Lett (2003) 13: 175-178 [PMID:12482418]
ChEMBL	Inhibitory constant against dopamine D2 receptor using 0.2 nM [3H]-spiperone	B	8.57	pKi	2.69	nM	Ki	J Med Chem (2005) 48: 266-273 [PMID:15634021]
ChEMBL	Displacement of [3H]spiperone from dopamine D2 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometry	B	8.59	pKi	2.6	nM	Ki	J Med Chem (2009) 52: 151-169 [PMID:19072656]
ChEMBL	Displacement of [3H]-spiperone from DRD2 in rat striatum by scintillation counting	B	8.6	pKi	2.5	nM	Ki	J Med Chem (2016) 59: 9960-9966 [PMID:27739690]
ChEMBL	Displacement of [3H]-spiperone from dopamine D2 receptor in rat striatum by scintillation counting method	B	8.64	pKi	2.3	nM	Ki	Eur J Med Chem (2015) 90: 1-9 [PMID:25461306]
ChEMBL	Binding affinity to the dopamine receptor D2L in rat brain membranes	B	8.66	pKi	2.2	nM	Ki	J Med Chem (1999) 42: 3342-3355 [PMID:10464021]
ChEMBL	Binding Affinity was determined against Dopamine receptor D2 in rat striatal membranes using [3H]- spiperone radioligand.	B	8.67	pKi	2.14	nM	Ki	J Med Chem (2000) 43: 599-608 [PMID:10691686]
ChEMBL	Displacement of [3H]-spiperone from dopamine D2 receptor in rat strriatum after 15 mins by liquid scintillation counting method	B	8.68	pKi	2.1	nM	Ki	J Med Chem (2018) 61: 372-384 [PMID:29220177]
ChEMBL	Displacement radioligand form dopamine D2 receptor in rat striatum by liquid scintillation counting	B	8.68	pKi	2.1	nM	Ki	Eur J Med Chem (2011) 46: 433-438 [PMID:21055848]
ChEMBL	Inhibition of [3H]spiroperidol binding to Dopamine receptor D2 of rat striatal membranes	B	8.71	pKi	1.95	nM	Ki	J Med Chem (1998) 41: 1574-1580 [PMID:9572883]
ChEMBL	Displacement of [3H]spiperone (0.5 nM) from rat corpus striatum dopamine D2 receptor	B	8.72	pKi	1.9	nM	Ki	J Med Chem (2003) 46: 265-283 [PMID:12519065]
ChEMBL	Tested for binding affinity towards rat striatal D2 receptor using [3H]spiperone as radioligand	B	8.73	pKi	1.86	nM	Ki	J Med Chem (1994) 37: 3523-3533 [PMID:7932581]
ChEMBL	In vitro Dopamine receptor D2 affinity by using [3H]spiperone as the radioligand in rat limbic system at 1 uM concentration of compound; value may range from 0.7 to 3.5	B	8.74	pKi	1.8	nM	Ki	J Med Chem (1987) 30: 1818-1823 [PMID:2888898]
ChEMBL	Displacement of [3H]spiperone from Dopamine receptor D2 of rat corpora striata synaptic membranes	B	8.77	pKi	1.7	nM	Ki	Bioorg Med Chem Lett (1997) 7: 1327-1330
ChEMBL	Displacement of [3H]nemonapride from Rattus norvegicus (rat) chimeric dopamine D2 trunk/D2 tail receptor transfected in african green monkey COS7 cells after 1 hr by beta scintillation counting	B	8.79	pKi	1.63	nM	Ki	Med Chem Res (2004) 13: 25-33
ChEMBL	Ability to displace [3H]spiperone from D2 dopamine receptor isolated from the striata of male Wistar rats	B	8.82	pKi	1.5	nM	Ki	Bioorg Med Chem Lett (1995) 5: 1245-1250
ChEMBL	Displacement of [3H]-Spiperone from Dopamine receptor D2 in rat striatum	B	8.85	pKi	1.4	nM	Ki	J Med Chem (1988) 31: 1934-1940 [PMID:2902226]
ChEMBL	Ability to inhibit the [3H]spiperone binding to striatum Dopamine receptor D2 was determined in rat	B	8.85	pKi	1.4	nM	Ki	J Med Chem (1987) 30: 2099-2104 [PMID:2889830]
ChEMBL	Affinity against the dopamine receptor D2 using [3H]spiperinone.	B	8.85	pKi	1.4	nM	Ki	J Med Chem (1995) 38: 4211-4222 [PMID:7473548]
ChEMBL	Binding affinity to rat Dopamine receptor D2 expressed in CHO cells was determined using [125 I ] iodosulpride as radioligand	B	8.96	pKi	1.1	nM	Ki	J Med Chem (1996) 39: 2764-2772 [PMID:8709107]
ChEMBL	Binding affinity was measured against dopamine (D2) receptor in rat using [3H]spiperone as radioligand	B	8.96	pKi	1.1	nM	Ki	J Med Chem (1994) 37: 1964-1970 [PMID:8027978]
ChEMBL	Displacement of [3H]nemonapride from Rattus norvegicus (rat) wild type dopamine D2 receptor transfected in african green monkey COS7 cells after 1 hr by beta scintillation counting	B	9	pKi	1.01	nM	Ki	Med Chem Res (2004) 13: 25-33
ChEMBL	In vitro binding affinity against Dopamine D2 receptor in rat striatal tissue.	B	9.06	pKi	0.88	nM	Ki	J Med Chem (1993) 36: 2107-2114 [PMID:8101877]
ChEMBL	Binding affinity against dopamine D2 receptor	B	9.06	pKi	0.87	nM	Ki	J Med Chem (1994) 37: 519-525 [PMID:7907148]
ChEMBL	Binding affinity towards dopamine receptor D2 in rat striatal membranes	B	9.1	pKi	0.8	nM	Ki	J Med Chem (2001) 44: 4431-4442 [PMID:11728188]
ChEMBL	Binding affinity towards Dopamine receptor D2	B	9.12	pKi	0.75	nM	Ki	J Med Chem (1987) 30: 1433-1454 [PMID:3039136]
ChEMBL	Displacement of [3H]NPA from rat brain Dopamine receptor D2	B	9.15	pKi	0.71	nM	Ki	J Med Chem (1996) 39: 143-148 [PMID:8568801]
ChEMBL	Displacement of [3H]NPA from rat brain Dopamine receptor D2	B	9.15	pKi	0.71	nM	Ki	J Med Chem (1996) 39: 143-148 [PMID:8568801]
ChEMBL	Evaluated for binding towards Dopamine receptor D2 using [3H]N-0437 as radioligand from rat striatal membrane	B	9.15	pKi	0.7	nM	Ki	J Med Chem (1993) 36: 3188-3196 [PMID:8230107]
ChEMBL	In vitro by displacement of [3H]raclopride from Dopamine receptor D2 on rat striatal membrane	B	9.2	pKi	0.63	nM	Ki	J Med Chem (1997) 40: 586-593 [PMID:9046349]
ChEMBL	Binding affinity was evaluated against Dopamine receptor D2 on rat striatum using [3H]spiperone as radioligand; ND = Not determined	B	9.23	pKi	0.59	nM	Ki	J Med Chem (1998) 41: 2765-2778 [PMID:9667967]
ChEMBL	Displacement of [3H]spiperone from dopamine D2 receptor in rat brain	B	9.3	pKi	0.5	nM	Ki	Bioorg Med Chem (2007) 15: 7361-7367 [PMID:17869521]
ChEMBL	In vitro binding affinity towards dopamine receptor D2 in rat striatal membranes by [3H]sulpiride displacement.	B	9.33	pKi	0.47	nM	Ki	J Med Chem (1993) 36: 3073-3076 [PMID:7901415]
ChEMBL	Binding affinity against dopamine receptor D2 from rat corpus striatum by using radioligand [3H]sulpiride	B	9.33	pKi	0.47	nM	Ki	J Med Chem (1993) 36: 1488-1495 [PMID:8496917]
ChEMBL	Binding affinity towards dopamine D2 receptors in rat brain synaptosomal preparations	B	9.43	pKi	0.37	nM	Ki	J Med Chem (1994) 37: 1060-1062 [PMID:7909336]
ChEMBL	Compound was evaluated for its binding affinity with Dopamine receptor D2 using membranes prepared from rat striatum	B	9.43	pKi	0.37	nM	Ki	J Med Chem (1998) 41: 1997-2009 [PMID:9622541]
ChEMBL	Inhibition of [3H]spiperone binding to rat striatal membrane Dopamine receptor D2	B	9.48	pKi	0.33	nM	Ki	J Med Chem (1990) 33: 1155-1163 [PMID:1969484]
ChEMBL	Affinity for Dopamine receptor D2	B	9.7	pKi	0.2	nM	Ki	Bioorg Med Chem Lett (1998) 8: 983-988 [PMID:9871525]
ChEMBL	Binding affinity towards dopamine receptor D2 by displacing [3H]spiperone radioligand in rat striatum	B	9.7	pKi	0.2	nM	Ki	J Med Chem (1992) 35: 552-558 [PMID:1346653]
ChEMBL	Binding towards Dopamine receptor D2 using [3H]spiperone from rat striatal membrane	B	9.7	pKi	0.2	nM	Ki	J Med Chem (1993) 36: 3188-3196 [PMID:8230107]
ChEMBL	Binding affinity was determined against Dopamine receptor D2 using [3H]spiperone	B	9.7	pKi	0.2	nM	Ki	J Med Chem (1995) 38: 4198-4210 [PMID:7473547]
ChEMBL	In vitro binding affinity was measured by displacement of [3H]- raclopride from D2 receptor isolated from the striata of male Dawley rats	B	7.4	pIC50	40	nM	IC50	J Med Chem (1994) 37: 2552-2563 [PMID:7914539]
ChEMBL	Inhibition of [3H]raclopride binding at Dopamine receptor D2 from rat striata.	B	7.4	pIC50	40	nM	IC50	J Med Chem (1996) 39: 149-157 [PMID:8568802]
ChEMBL	Binding affinity towards Dopamine receptor D2 was determined in rat striatal homogenate using [3H]- spiperone as radioligand	B	7.48	pIC50	33	nM	IC50	J Med Chem (1996) 39: 4044-4057 [PMID:8831770]
ChEMBL	In vitro affinity towards D2 receptor using [3H]spiroperidol as radioligand in striatum	B	7.49	pIC50	32.7	nM	IC50	J Med Chem (1994) 37: 2308-2314 [PMID:7914536]
ChEMBL	Compound was measured for affinity at dopamine receptor D2 labeled with [3H]spiroperidol radioligand in striatum tissue	B	7.7	pIC50	20	nM	IC50	J Med Chem (1991) 34: 1068-1072 [PMID:1672156]
ChEMBL	Affinity for dopamine receptor D2 binding sites by its ability to displace [3H]spiperone from rat striatum.	B	7.74	pIC50	18	nM	IC50	J Med Chem (1995) 38: 1119-1131 [PMID:7707315]
ChEMBL	In vitro binding affinity for Dopamine D2 receptor of rat using [3H]YM-09151 as radioligand	B	7.76	pIC50	17.5	nM	IC50	J Med Chem (2002) 45: 4655-4668 [PMID:12361392]
ChEMBL	Inhibition of [3H]methylspiperone binding to rat striatal membrane Dopamine receptor D2	B	7.86	pIC50	13.7	nM	IC50	J Med Chem (1998) 41: 5402-5409 [PMID:9876110]
ChEMBL	In vitro binding affinity at Dopamine receptor D2 in rat by displacing [3H]- spiperone from rat striatal membrane	B	7.92	pIC50	12	nM	IC50	J Med Chem (1985) 28: 1263-1269 [PMID:4040977]
ChEMBL	In vitro ability to inhibit the binding of [3H]spiperone to dopamine receptor D2 in rat striatal membranes.	B	7.92	pIC50	12	nM	IC50	J Med Chem (1990) 33: 1155-1163 [PMID:1969484]
ChEMBL	Inhibitory binding of [3H]spiperone to Dopamine receptor D2 in membranes from rat corpus striatum	B	8.12	pIC50	7.5	nM	IC50	J Med Chem (1997) 40: 4146-4153 [PMID:9406603]
ChEMBL	Compound was tested for the inhibition of [3H]spiperone binding to dopamine receptor D2	B	8.12	pIC50	7.5	nM	IC50	J Med Chem (1992) 35: 1092-1101 [PMID:1348090]
ChEMBL	Binding affinity towards Dopamine receptor D2 binding site using [3H]spiroperidol.	B	8.12	pIC50	7.5	nM	IC50	J Med Chem (1995) 38: 1998-2008 [PMID:7783131]
ChEMBL	Binding affinity towards Dopamine receptor D2 of rat corpus striatum using [3H]spiperone as radioligand	B	8.12	pIC50	7.5	nM	IC50	J Med Chem (1999) 42: 2235-2244 [PMID:10377229]
ChEMBL	Compound was tested in vitro for its affinity towards rat striatal Dopamine receptor D2 labeled with [3H]- spiperone	B	8.15	pIC50	7	nM	IC50	J Med Chem (1986) 29: 359-369 [PMID:2869146]
ChEMBL	In vitro inhibitory concentration against radioligand [3H]spiperone binding to rat striatal dopamine receptor D2	B	8.15	pIC50	7	nM	IC50	J Med Chem (1992) 35: 4516-4525 [PMID:1361578]
ChEMBL	Inhibition of [3H](S)-sulpiride binding in striatal homogenates of rat brain	B	8.22	pIC50	6	nM	IC50	J Med Chem (1988) 31: 2027-2033 [PMID:3172140]
ChEMBL	Compound was tested for its binding affinity towards Dopamine receptor D2 by using [3H]domperidone as radioligand	B	8.26	pIC50	5.5	nM	IC50	J Med Chem (1991) 34: 3360-3365 [PMID:1662725]
ChEMBL	Affinity towards Dopamine receptor D2 was evaluated in rat striatal membrane using [3H]spiperone as radioligand	B	8.32	pIC50	4.8	nM	IC50	J Med Chem (1996) 39: 4928-4934 [PMID:8960552]
ChEMBL	Binding affinity to rat Dopamine receptor D2 expressed in CHO cells was determined using [125 I ] iodosulpride as radioligand	B	8.32	pIC50	4.8	nM	IC50	J Med Chem (1996) 39: 3195-3202 [PMID:8759642]
ChEMBL	Neuroleptic activity in terms of [3H]spiroperidol binding in rat striatal membrane to Dopamine receptor D2	B	8.37	pIC50	4.24	nM	IC50	J Med Chem (1991) 34: 194-197 [PMID:1671414]
ChEMBL	Ability to inhibit the specific binding of [3H]- spiroperidol to Dopamine receptor D2 in rat striatal membrane preparation by 50%	B	8.37	pIC50	4.24	nM	IC50	J Med Chem (1987) 30: 1906-1910 [PMID:2888899]
ChEMBL	Compound was evaluated In vitro for its activity by binding to Dopamine receptor D2 in the rat brain using [3H]NPA as radioligand.	B	8.51	pIC50	3.1	nM	IC50	J Med Chem (1991) 34: 1860-1866 [PMID:1676427]
ChEMBL	Displacement of [3H]spiroperidol from D2 dopamine receptor	B	8.6	pIC50	2.5	nM	IC50	J Med Chem (1994) 37: 1320-1325 [PMID:8176710]
ChEMBL	Inhibition of 0.1 nM of [125I]- (S)-N-(1-Ethyl-pyrrolidin-2-ylmethyl)-5-iodo-2-methoxy-benzamide binding in striatal homogenates of rat brain	B	8.92	pIC50	1.2	nM	IC50	J Med Chem (1988) 31: 2027-2033 [PMID:3172140]
ChEMBL	In vivo binding affinity against dopamine (D2) receptor in rat caudate-putamen tissue using [3H]nemonapride as radioligand	B	10.12	pIC50	0.07	nM	IC50	Bioorg Med Chem Lett (2003) 13: 4015-4017 [PMID:14592497]
Dopamine D3 receptor in Chlorocebus aethiops (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2304406] [UniProtKB: P52703]
ChEMBL	Displacement of [3H]-YM 09151 from african monkey Dopamine receptor D3	B	8.52	pKi	3	nM	Ki	J Med Chem (1995) 38: 4950-4952 [PMID:8523409]
D3 receptor/Dopamine D3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL234] [GtoPdb: 216] [UniProtKB: P35462]
ChEMBL	Intrinsic activity against dopamine receptor D3 by Eu-GTP binding assay	F	6.5	pKd	316.23	nM	Kd	J Med Chem (2005) 48: 7919-7922 [PMID:16335915]
ChEMBL	Binding affinity of compound towards Dopamine receptor D3 using [3H]spiperone (1.2 nM) ligand in cortex was determined	B	6.94	pKi	115	nM	Ki	J Med Chem (1997) 40: 952-960 [PMID:9083484]
ChEMBL	Binding affinity to human D3 receptor expressed in CHO cells assessed as inhibition constant by scintillation counting method	B	7.27	pKi	53.7	nM	Ki	Bioorg Med Chem (2023) 78: 117132-117132 [PMID:36542960]
ChEMBL	Displacement of [3H]N-methylspiperone from human D3 receptor expressed in HEK cells	B	7.54	pKi	29	nM	Ki	Bioorg Med Chem Lett (2011) 21: 3622-3626 [PMID:21555222]
ChEMBL	Displacement of the radioligand [3H]YM-09151-2 from cloned human Dopamine receptor D3 expressed in CHO cells	B	7.6	pKi	25	nM	Ki	Bioorg Med Chem Lett (2002) 12: 1327-1330 [PMID:11992769]
ChEMBL	Displacement of [3H]-SCH23390 from D3 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method	B	7.64	pKi	22.91	nM	Ki	J Med Chem (2021) 64: 17239-17258 [PMID:34797051]
ChEMBL	Displacement of [3H]-SCH23390 from D3 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method	B	7.64	pKi	22.7	nM	Ki	J Med Chem (2021) 64: 17239-17258 [PMID:34797051]
ChEMBL	Binding affinity towards human Dopamine receptor D3	B	7.68	pKi	21	nM	Ki	J Med Chem (2004) 47: 1303-1314 [PMID:14998318]
ChEMBL	Inhibition of [3H]7-OH-DPAT binding to Dopamine D3 receptor expressed in Sf9 cells	B	7.74	pKi	18	nM	Ki	J Med Chem (2005) 48: 1705-1708 [PMID:15771414]
ChEMBL	Displacement of [3H]Spiperone from D3 receptor (unknown origin) transfected in HEK293T cells after 50 mins by liquid scintillation counting analysis	B	7.79	pKi	16.04	nM	Ki	Bioorg Med Chem (2014) 22: 5838-5846 [PMID:25308766]
ChEMBL	Displacement of [3H]spiroperidol from cloned human dopamine receptor D3 in CHO cell membrane	B	7.8	pKi	16	nM	Ki	J Med Chem (2005) 48: 7919-7922 [PMID:16335915]
ChEMBL	Displacement of [3H]spiroperidol from human cloned dopamine D3 receptor	B	7.8	pKi	16	nM	Ki	J Med Chem (2007) 50: 5043-5047 [PMID:17850060]
ChEMBL	Binding affinity to dopamine D3 receptor (unknown origin) by radioligand displacement assay	B	7.87	pKi	13.5	nM	Ki	Bioorg Med Chem Lett (2022) 59: 128573-128573 [PMID:35063632]
ChEMBL	Displacement of [125I]ABN from human dopamine D3 receptor expressed in HEK293 cells after 60 mins by gamma counting	B	7.9	pKi	12.7	nM	Ki	Bioorg Med Chem (2010) 18: 5291-5300 [PMID:20542439]
ChEMBL	Displacement of [3H]spiperone from human dopamine D3 receptor	B	7.94	pKi	11.48	nM	Ki	Bioorg Med Chem Lett (2009) 19: 6059-6062 [PMID:19796944]
ChEMBL	Inhibition of human dopamine D3 receptor	B	7.98	pKi	10.4	nM	Ki	J Med Chem (2011) 54: 2529-2591 [PMID:21413808]
ChEMBL	Binding affinity for human dopamine receptor D3	B	8	pKi	10	nM	Ki	J Med Chem (2005) 48: 694-709 [PMID:15689154]
ChEMBL	Displacement of [3H]spiperone from human dopamine D3 expressed in CHO cell membrane	B	8.08	pKi	8.32	nM	Ki	J Med Chem (2007) 50: 489-500 [PMID:17266201]
ChEMBL	Binding affinity towards Chinese hamster ovary cells transfected with human D3 receptor using [3H]spiperone	B	8.1	pKi	7.94	nM	Ki	Bioorg Med Chem Lett (1995) 5: 219-222
ChEMBL	Binding affinity for human recombinant dopamine receptor D3	B	8.11	pKi	7.8	nM	Ki	J Med Chem (2004) 47: 4155-4158 [PMID:15293986]
ChEMBL	Displacement of [3H]Spiperone from human dopamine D3 receptor expressed in CHO cells	B	8.12	pKi	7.5	nM	Ki	J Med Chem (2010) 53: 7219-7228 [PMID:20839776]
ChEMBL	DRUGMATRIX: Dopamine D3 radioligand binding (ligand: [3H] Spiperone)	B	8.16	pKi	6.84	nM	Ki	DrugMatrix in vitro pharmacology data
ChEMBL	Displacement of [3H]spiperone from human dopamine D3 receptor expressed in CHO cells	B	8.17	pKi	6.8	nM	Ki	ACS Med Chem Lett (2015) 6: 882-887 [PMID:26288260]
ChEMBL	Binding towards Dopamine receptor D3 expressed in CHO-K1 cells using [3H]spiperone	B	8.19	pKi	6.4	nM	Ki	J Med Chem (1993) 36: 3188-3196 [PMID:8230107]
ChEMBL	Displacement of [3H]YM-09151-2 from human cloned dopamine D3 receptor expressed in CHO cells	B	8.19	pKi	6.4	nM	Ki	Eur J Med Chem (2007) 42: 1044-1048 [PMID:17316913]
ChEMBL	Displacement of [3H]spiperone from human D3 receptor expressed in CHO cells	B	8.2	pKi	6.3	nM	Ki	J Med Chem (2011) 54: 4896-4903 [PMID:21599022]
ChEMBL	Displacement of [3H]spiperone from human dopamine D3 receptor expressed in chinese hamster CHO cells by radioligand binding assay	B	8.2	pKi	6.3	nM	Ki	J Med Chem (2011) 54: 7911-7919 [PMID:21999579]
ChEMBL	Displacement of [3H]spiperone from human D3 receptor expressed in CHO-K1 cells by radioligand competitive binding analysis	B	8.24	pKi	5.75	nM	Ki	J Nat Prod (2020) 83: 127-133 [PMID:31933369]
ChEMBL	Displacement of [3H]N-methylspiperone from human dopamine D3 receptor by liquid scintillation counting	B	8.26	pKi	5.5	nM	Ki	Bioorg Med Chem (2009) 17: 1716-1723 [PMID:19155177]
ChEMBL	Displacement of [3H]spiperone from human D3 receptor expressed in CHO-K1 cells by radioligand competitive binding analysis	B	8.29	pKi	5.16	nM	Ki	J Nat Prod (2020) 83: 127-133 [PMID:31933369]
ChEMBL	In vitro ability to inhibit the binding of [3H]7-OH-DPAT to cloned human Dopamine receptor D3 using apomorphine induced climbing test in male Swiss mice	B	8.34	pKi	4.6	nM	Ki	Bioorg Med Chem Lett (2003) 13: 3779-3782 [PMID:14552778]
ChEMBL	Displacement of [3H]N-methylspiperone from human dopamine D3 receptor by liquid scintillation counting	B	8.34	pKi	4.6	nM	Ki	Bioorg Med Chem (2012) 20: 1291-1297 [PMID:22245230]
ChEMBL	Cataleptogenic effect against cloned human Dopamine receptor D3 in male Sprague-Dawley rats in a bar test	B	8.34	pKi	4.57	nM	Ki	Bioorg Med Chem Lett (2003) 13: 3779-3782 [PMID:14552778]
ChEMBL	Displacement of [3H]7-OH-DPAT from human Dopamine receptor D3	B	8.34	pKi	8.34	nM	pKi	J Med Chem (2004) 47: 497-508 [PMID:14736232]
ChEMBL	Inhibition of [125I]iodosulpiride binding to human Dopamine receptor D3	B	8.36	pKi	4.4	nM	Ki	J Med Chem (2005) 48: 1709-1712 [PMID:15771415]
ChEMBL	Displacement of [3H]-N-methylspiperone from human dopamine D3 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysis	B	8.36	pKi	4.4	nM	Ki	J Med Chem (2021) 64: 7778-7808 [PMID:34011153]
ChEMBL	Displacement of [3H]raclopride from Dopamine receptor D3	B	8.56	pKi	2.74	nM	Ki	J Med Chem (1996) 39: 4421-4429 [PMID:8893836]
ChEMBL	Ability to displace [3H]spiperone (0.3 nM) from CHO cells of human Dopamine receptor D3	B	8.57	pKi	2.7	nM	Ki	J Med Chem (2003) 46: 265-283 [PMID:12519065]
ChEMBL	Displacement of [3H]spiperone from human D3 receptor stably expressed in CHO cell membranes by competitive binding assay	B	8.59	pKi	2.6	nM	Ki	Bioorg Med Chem Lett (2014) 24: 3753-3756 [PMID:25047579]
GtoPdb	-	-	8.6	pKi	-	-	-	J Pharmacol Exp Ther (1994) 268: 417-26 [PMID:8301582]; Eur J Pharmacol (1992) 225: 331-7 [PMID:1354163]; Pharmacol Biochem Behav (1994) 49: 567-71 [PMID:7862709]; J Psychopharmacol (Oxford) (2009) 23: 65-73 [PMID:18308814]
ChEMBL	Binding affinity to human cloned dopamine D3 receptor	B	8.6	pKi	2.5	nM	Ki	Bioorg Med Chem (2008) 16: 7291-7301 [PMID:18595716]
ChEMBL	Displacement of [3H]N-methylspiperone from human dopamine D3 receptor by liquid scintillation counting	B	8.6	pKi	2.5	nM	Ki	Bioorg Med Chem Lett (2014) 24: 4294-4297 [PMID:25070422]
ChEMBL	Displacement of [3H]spiperone from human D3 receptor expressed in CHO cell membranes by radioligand binding assay	B	8.64	pKi	2.3	nM	Ki	Bioorg Med Chem (2017) 25: 5084-5094 [PMID:28666858]
ChEMBL	Ability to displace [3H]spiperone from human cloned Dopamine receptor D3 expressed in CHO K-1 cells in vitro.	B	8.66	pKi	2.2	nM	Ki	J Med Chem (1997) 40: 2688-2693 [PMID:9276014]
ChEMBL	Displacement of [125I]iodosulpiride from human Dopamine receptor D3 expressed in CHO cells	B	8.66	pKi	2.2	nM	Ki	J Med Chem (2003) 46: 4377-4392 [PMID:14521403]
ChEMBL	Binding affinity against cloned human dopamine receptor D3 expressed in Chinese hamster ovary (CHO) K-1 cells by displacement of [3H]spiperone.	B	8.66	pKi	2.2	nM	Ki	J Med Chem (1997) 40: 4026-4029 [PMID:9406594]
ChEMBL	Binding affinity towards cloned human Dopamine receptor D3 stably expressed in CHO cells was evaluated using [3H]spiperone as radioligand	B	8.7	pKi	2	nM	Ki	J Med Chem (1996) 39: 1941-1942 [PMID:8642550]
ChEMBL	Displacement of [3H]methylspiperone from human D3 receptor expressed in HEK293 cell membrane after 90 mins by scintillation counting analysis	B	8.7	pKi	2	nM	Ki	J Med Chem (2014) 57: 3450-3463 [PMID:24666157]
ChEMBL	Displacement of [3H]spiperone from human Dopamine receptor D3 expressed in CHO cells	B	8.7	pKi	2	nM	Ki	J Med Chem (1996) 39: 1943-1945 [PMID:8642551]
ChEMBL	Ability to displace [3H]spiperone from human dopamine receptor D3 (hD3) receptor stably expressed in HEK293 cells.	B	8.7	pKi	2	nM	Ki	J Med Chem (1997) 40: 2374-2385 [PMID:9240352]
ChEMBL	Displacement of [3H]spiperone from human dopamine D3 receptor expressed in CHO cells	B	8.8	pKi	1.58	nM	Ki	J Med Chem (2007) 50: 5103-5108 [PMID:17880057]
ChEMBL	Displacement of [3H]N-methylspiperone from human D3 receptor expressed in HEK293T cells co-expressing CRE-Luc incubated for 60 mins by microbeta scintillation counting method	B	8.95	pKi	1.12	nM	Ki	Eur J Med Chem (2021) 214: 113190-113190 [PMID:33548637]
ChEMBL	Displacement of [3H]-spiperone from CHO-K1 cell membranes expressing human dopamine 3 receptors	B	9.02	pKi	0.96	nM	Ki	J Med Chem (1993) 36: 3929-3936 [PMID:7902870]
ChEMBL	Displacement of [3H]7OH-DPAT from dopamine D3 receptor expressed in Sf9 cells by scintillation spectrometry	B	9.05	pKi	0.9	nM	Ki	J Med Chem (2009) 52: 151-169 [PMID:19072656]
ChEMBL	Tested for binding affinity towards human D3 receptor using [3H]spiperone as radioligand	B	9.16	pKi	0.69	nM	Ki	J Med Chem (1994) 37: 3523-3533 [PMID:7932581]
ChEMBL	DRUGMATRIX: Dopamine D3 radioligand binding (ligand: [3H] Spiperone)	B	7.7	pIC50	20	nM	IC50	DrugMatrix in vitro pharmacology data
ChEMBL	Binding affinity towards human Dopamine receptor D3	B	8	pIC50	10	nM	IC50	J Med Chem (1999) 42: 2235-2244 [PMID:10377229]
ChEMBL	Antagonist activity at human dopamine D3 opioid receptor expressed in HEK293T cells assessed as GalphaoA activation preincubated with compound in D-PBS for 3 hrs followed by coelenterazine addition for 5 mins once again compound addition for 10 mins by BRET assay	F	8.46	pIC50	3.47	nM	IC50	J Med Chem (2021) 64: 7778-7808 [PMID:34011153]
ChEMBL	Antagonist activity at SNAP-tagged human D3R receptor transfected in HEK293T cells coexpressing wild type Galpha-oA, venus-tagged Gbeta-1 (156 to 239 residues), venus-tagged Ggamma2 (1 to 155 residues) and Rluc8 fused masGRK3ct assessed as Galpha-oA activation using coelenterazine as substrate incubated for 40 mins in presence of quinpirole by BRET based GPA assay	F	8.56	pIC50	2.75	nM	IC50	J Med Chem (2023) 66: 10304-10341 [PMID:37467430]
ChEMBL	Antagonist activity at D3 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins in presence of quinpirole by BRET analysis	F	8.6	pIC50	2.54	nM	IC50	J Med Chem (2023) 66: 1809-1834 [PMID:36661568]
ChEMBL	Antagonist activity at D3 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins in presence of quinpirole by BRET analysis	F	8.6	pIC50	2.51	nM	IC50	J Med Chem (2023) 66: 1809-1834 [PMID:36661568]
ChEMBL	Antagonist activity against D3R in human U2OS cells assessed as inhibition of (+)-PD128907-induced beta-arrestin translocation by beta-galactosidase based beta-arrestin recruitment assay	B	10.22	pIC50	0.06	nM	IC50	J Med Chem (2014) 57: 7042-7060 [PMID:25126833]
ChEMBL	Antagonist activity at SNAP-tagged human D3R receptor transfected in HEK293T cells coexpressing wild type Galpha-oA, venus-tagged Gbeta-1 (156 to 239 residues), venus-tagged Ggamma2 (1 to 155 residues) and Rluc8 fused masGRK3ct assessed as Galpha-oA activation using coelenterazine as substrate incubated for 40 mins in presence of quinpirole by BRET based GPA assay	F	8.56	pEC50	2.76	nM	EC50	J Med Chem (2023) 66: 10304-10341 [PMID:37467430]
D3 receptor/Dopamine D3 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3138] [GtoPdb: 216] [UniProtKB: P19020]
GtoPdb	-	-	7	pKi	-	-	-	Nature (1990) 347: 146-51 [PMID:1975644]
ChEMBL	Binding affinity for dopamine receptor D3 expressed in Sf9 cells using [125I]IABN the radioligand.	B	7.33	pKi	47	nM	Ki	J Med Chem (2001) 44: 1815-1826 [PMID:11356115]
ChEMBL	Binding affinity towards Dopamine receptor D3 of rat using [3H]spiroperidol as radioligand	B	7.55	pKi	28	nM	Ki	J Med Chem (2002) 45: 5727-5735 [PMID:12477356]
ChEMBL	Displacement of [3H]PD 128907 from rat ventral striatal membrane dopamine D3-like receptor	B	7.62	pKi	24	nM	Ki	Bioorg Med Chem Lett (2006) 16: 443-446 [PMID:16290142]
ChEMBL	Half-maximal inhibition of [3H]7-OH-DPAT binding to Dopamine receptor D3 in rat tissue homogenate	B	7.74	pKi	18.2	nM	Ki	J Med Chem (2002) 45: 344-359 [PMID:11784139]
ChEMBL	Half-maximal inhibition of [3H]-7-OH-DPAT binding to Dopamine receptor D3 in rat tissue homogenate	B	7.74	pKi	18	nM	Ki	J Med Chem (2002) 45: 344-359 [PMID:11784139]
ChEMBL	In vitro binding affinity towards Dopamine receptor D3 in Sf9 cell membranes using [3H]7-OH-DPAT as radioligand	B	7.74	pKi	18	nM	Ki	J Med Chem (2004) 47: 143-157 [PMID:14695828]
ChEMBL	Tested for binding affinity against dopamine receptor D3 expressed in Sf9 cells.	B	7.84	pKi	14.3	nM	Ki	J Med Chem (1993) 36: 1499-1500 [PMID:8098771]
ChEMBL	Displacement of [3H]-7-OH-DPAT from dopamine D3 receptor in rat olfactory tubercle by scintillation counting method	B	8.06	pKi	8.8	nM	Ki	Eur J Med Chem (2015) 90: 1-9 [PMID:25461306]
ChEMBL	Binding affinity to rat Dopamine receptor D3 expressed in CHO cells was determined using [125 I] iodosulpride as radioligand	B	8.19	pKi	6.4	nM	Ki	J Med Chem (1996) 39: 2764-2772 [PMID:8709107]
ChEMBL	Displacement of [3H]-7-OH-DPAT from DRD3 in rat olfactory tubercle by scintillation counting	B	8.21	pKi	6.1	nM	Ki	J Med Chem (2016) 59: 9960-9966 [PMID:27739690]
ChEMBL	Displacement radioligand form dopamine D3 receptor in rat olfactory tubercle by liquid scintillation counting	B	8.24	pKi	5.8	nM	Ki	Eur J Med Chem (2011) 46: 433-438 [PMID:21055848]
ChEMBL	Displacement of [3H]nemonapride from Rattus norvegicus (rat) chimeric dopamine D3 trunk/D3 tail receptor transfected in african green monkey COS7 cells after 1 hr by beta scintillation counting	B	8.25	pKi	5.57	nM	Ki	Med Chem Res (2004) 13: 25-33
ChEMBL	Displacement of [3H]nemonapride from Rattus norvegicus (rat) wild type dopamine D3 receptor transfected in african green monkey COS7 cells after 1 hr by beta scintillation counting	B	8.3	pKi	5.04	nM	Ki	Med Chem Res (2004) 13: 25-33
ChEMBL	Binding affinity towards baculovirus expressed rat dopamine D3 receptors	B	8.52	pKi	3	nM	Ki	J Med Chem (1994) 37: 1060-1062 [PMID:7909336]
D4 receptor/Dopamine D4 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL219] [GtoPdb: 217] [UniProtKB: P21917]
ChEMBL	DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)	B	6.7	pKi	198	nM	Ki	DrugMatrix in vitro pharmacology data
ChEMBL	Displacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cells	B	6.99	pKi	103	nM	Ki	Eur J Med Chem (2007) 42: 1044-1048 [PMID:17316913]
ChEMBL	Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells	B	7.38	pKi	42	nM	Ki	Bioorg Med Chem Lett (2002) 12: 1327-1330 [PMID:11992769]
ChEMBL	Displacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method	B	7.58	pKi	26.3	nM	Ki	J Med Chem (2021) 64: 17239-17258 [PMID:34797051]
ChEMBL	Displacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method	B	7.58	pKi	26.3	nM	Ki	J Med Chem (2021) 64: 17239-17258 [PMID:34797051]
ChEMBL	Displacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation counting	B	7.9	pKi	12.7	nM	Ki	Bioorg Med Chem (2009) 17: 1716-1723 [PMID:19155177]
ChEMBL	Binding affinity towards human dopamine-4.2 receptor	B	7.96	pKi	11	nM	Ki	J Med Chem (2004) 47: 1303-1314 [PMID:14998318]
ChEMBL	Displacement of [3H]spiperone from human Dopamine receptor D4	B	7.98	pKi	7.98	nM	pKi	J Med Chem (2004) 47: 497-508 [PMID:14736232]
ChEMBL	Cataleptogenic effect against cloned human dopamine receptor D4 in male Sprague-Dawley rats in a bar test	B	7.98	pKi	10.47	nM	Ki	Bioorg Med Chem Lett (2003) 13: 3779-3782 [PMID:14552778]
ChEMBL	In vitro ability to inhibit the binding of [3H]spiperone to cloned human dopamine receptor D4 using apomorphine induced climbing test in male Swiss mice	B	8	pKi	10	nM	Ki	Bioorg Med Chem Lett (2003) 13: 3779-3782 [PMID:14552778]
ChEMBL	Inhibition of human dopamine D4 receptor	B	8.1	pKi	7.94	nM	Ki	J Med Chem (2011) 54: 2529-2591 [PMID:21413808]
ChEMBL	Binding affinity for human recombinant dopamine receptor D4.2	B	8.14	pKi	7.3	nM	Ki	J Med Chem (2004) 47: 4155-4158 [PMID:15293986]
ChEMBL	Binding affinity on human Dopamine receptor D4 expressed in CHO cells using radioligand [3H]-YM 09151	B	8.14	pKi	7.3	nM	Ki	J Med Chem (1997) 40: 1-3 [PMID:9016321]
ChEMBL	Binding affinity for Dopamine receptor D4	B	8.14	pKi	7.3	nM	Ki	J Med Chem (2005) 48: 694-709 [PMID:15689154]
ChEMBL	Displacement of [3H]-YM 09151 from human Dopamine receptor D4	B	8.15	pKi	7	nM	Ki	J Med Chem (1995) 38: 4950-4952 [PMID:8523409]
ChEMBL	Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells	B	8.2	pKi	6.31	nM	Ki	J Med Chem (2007) 50: 5103-5108 [PMID:17880057]
ChEMBL	Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in chinese hamster CHO cells by radioligand binding assay	B	8.2	pKi	6.3	nM	Ki	J Med Chem (2011) 54: 7911-7919 [PMID:21999579]
ChEMBL	Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells	B	8.2	pKi	6.3	nM	Ki	J Med Chem (2011) 54: 4896-4903 [PMID:21599022]
ChEMBL	Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane	B	8.22	pKi	6.03	nM	Ki	J Med Chem (2007) 50: 489-500 [PMID:17266201]
ChEMBL	Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells	B	8.22	pKi	6	nM	Ki	J Med Chem (2010) 53: 7219-7228 [PMID:20839776]
ChEMBL	Displacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assay	B	8.23	pKi	5.9	nM	Ki	Bioorg Med Chem Lett (2014) 24: 3753-3756 [PMID:25047579]
ChEMBL	Binding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligand	B	8.3	pKi	5	nM	Ki	Bioorg Med Chem Lett (2002) 12: 3111-3115 [PMID:12372513]
ChEMBL	Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK cells	B	8.3	pKi	5	nM	Ki	Bioorg Med Chem Lett (2011) 21: 3622-3626 [PMID:21555222]
ChEMBL	Binding affinity measured at the Dopamine receptor D4 by the inhibition of [3H]spiperone binding to human recombinant CHO cells using unlabeled haloperidol for nonspecific binding.	B	8.37	pKi	4.3	nM	Ki	J Med Chem (1998) 41: 5402-5409 [PMID:9876110]
ChEMBL	Potency was measured by the displacement of [3H]-spiperone binding to human D4 dopaminergic receptor	B	8.42	pKi	3.8	nM	Ki	Bioorg Med Chem Lett (1997) 7: 1207-1212
ChEMBL	Displacement of [3H]YM-09151-2 from human Dopamine receptor D4.2 expressed in baculovirus Sf9 cells	B	8.44	pKi	3.6	nM	Ki	Bioorg Med Chem Lett (1997) 7: 1327-1330
ChEMBL	Binding affinity to human cloned dopamine D4 receptor	B	8.48	pKi	3.3	nM	Ki	Bioorg Med Chem (2008) 16: 7291-7301 [PMID:18595716]
ChEMBL	In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.	B	8.48	pKi	3.3	nM	Ki	Bioorg Med Chem Lett (1998) 8: 725-730 [PMID:9871530]
ChEMBL	Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.	B	8.64	pKi	2.3	nM	Ki	J Med Chem (1997) 40: 2374-2385 [PMID:9240352]
ChEMBL	Inhibition of human dopamine D4 receptor	B	8.64	pKi	2.3	nM	Ki	J Med Chem (2017) 60: 7233-7243 [PMID:28489950]
ChEMBL	Displacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cells	B	8.64	pKi	2.3	nM	Ki	J Med Chem (1996) 39: 1943-1945 [PMID:8642551]
ChEMBL	Binding affinity towards cloned human Dopamine receptor D4 stably expressed in CHO cells was evaluated using [3H]spiperone as radioligand	B	8.64	pKi	2.3	nM	Ki	J Med Chem (1996) 39: 1941-1942 [PMID:8642550]
ChEMBL	In vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranes	B	8.66	pKi	2.2	nM	Ki	J Med Chem (2002) 45: 5136-5149 [PMID:12408724]
ChEMBL	Binding towards dopamine receptor D4 expressed in CHO-K1 cells using [3H]spiperone	B	8.66	pKi	2.2	nM	Ki	J Med Chem (1993) 36: 3188-3196 [PMID:8230107]
ChEMBL	Ability to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitro	B	8.66	pKi	2.2	nM	Ki	J Med Chem (1997) 40: 2688-2693 [PMID:9276014]
ChEMBL	Binding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperone	B	8.66	pKi	2.2	nM	Ki	J Med Chem (1997) 40: 4026-4029 [PMID:9406594]
ChEMBL	Binding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligand	B	8.68	pKi	2.1	nM	Ki	J Med Chem (1996) 39: 2764-2772 [PMID:8709107]
ChEMBL	Antagonism of dopamine-stimulated [35S]GTP-gamma-S binding against human Dopamine receptor D4 in CHO cells	F	8.7	pKi	2	nM	Ki	J Med Chem (2000) 43: 3923-3932 [PMID:11052797]
ChEMBL	In vitro ability to inhibit [3H]6b binding to human Dopamine receptor D4.4	B	8.72	pKi	1.9	nM	Ki	Bioorg Med Chem Lett (2004) 14: 5095-5098 [PMID:15380206]
ChEMBL	In vitro binding affinity for Dopamine receptor D4	B	8.8	pKi	1.58	nM	Ki	Bioorg Med Chem Lett (2001) 11: 1313-1316 [PMID:11392544]
GtoPdb	-	-	8.8	pKi	-	-	-	Eur J Pharmacol (1993) 236: 483-6 [PMID:8102973]; Pharmacol Biochem Behav (1994) 49: 567-71 [PMID:7862709]; J Psychopharmacol (Oxford) (2009) 23: 65-73 [PMID:18308814]
ChEMBL	Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysis	B	8.84	pKi	1.43	nM	Ki	J Med Chem (2021) 64: 7778-7808 [PMID:34011153]
ChEMBL	In vitro ability to inhibit [3H]spiperone binding to human Dopamine receptor D4.4	B	8.85	pKi	1.4	nM	Ki	Bioorg Med Chem Lett (2004) 14: 5095-5098 [PMID:15380206]
ChEMBL	In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.	B	9	pKi	1	nM	Ki	J Med Chem (2000) 43: 270-277 [PMID:10649982]
ChEMBL	Binding affinity towards human Dopamine receptor D4.2 in CHO cells	B	9	pKi	1	nM	Ki	J Med Chem (1996) 39: 4044-4057 [PMID:8831770]
ChEMBL	Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand	B	9.13	pKi	0.74	nM	Ki	J Med Chem (2002) 45: 5727-5735 [PMID:12477356]
ChEMBL	DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)	B	6.25	pIC50	563	nM	IC50	DrugMatrix in vitro pharmacology data
ChEMBL	Binding affinity towards human D4.2 receptor	B	8.19	pIC50	6.5	nM	IC50	J Med Chem (1999) 42: 2235-2244 [PMID:10377229]
ChEMBL	Inhibitory concentration against human Dopamine receptor D4.2 in CHO cells	B	8.22	pIC50	6	nM	IC50	J Med Chem (1996) 39: 4044-4057 [PMID:8831770]
ChEMBL	Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand	B	8.3	pIC50	5	nM	IC50	J Med Chem (2000) 43: 3923-3932 [PMID:11052797]
ChEMBL	In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.	B	8.89	pIC50	1.3	nM	IC50	J Med Chem (1998) 41: 4903-4909 [PMID:9822559]
ChEMBL	Agonist activity was calculated in calcium flux assay using HEK293 cells co-transfected with human Dopamine receptor D4.4 and Galphaqo5	F	5	pEC50	>10000	nM	EC50	Bioorg Med Chem Lett (2004) 14: 5095-5098 [PMID:15380206]
ChEMBL	Agonistic activity against human Dopamine receptor D4.2 using [35S]GTP-gamma-S binding assay	F	7.77	pEC50	17	nM	EC50	Bioorg Med Chem Lett (2003) 13: 2921-2924 [PMID:14611858]
D4 receptor/Dopamine D4 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3361] [GtoPdb: 217] [UniProtKB: P30729]
ChEMBL	Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting	B	8	pKi	10	nM	Ki	Bioorg Med Chem Lett (2014) 24: 4294-4297 [PMID:25070422]
D5 receptor/Dopamine D5 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1850] [GtoPdb: 218] [UniProtKB: P21918]
GtoPdb	-	-	6.3	pKi	-	-	-	Nature (1991) 350: 614-9 [PMID:1826762]
ChEMBL	Compound was tested for the Binding affinity against Human cloned Dopamine receptor D5 by Radio ligand ([3H]SCH-23390) binding assay	B	6.59	pKi	260	nM	Ki	J Med Chem (1996) 39: 2764-2772 [PMID:8709107]
ChEMBL	Binding affinity for human recombinant dopamine receptor D5	B	7.24	pKi	58	nM	Ki	J Med Chem (2004) 47: 4155-4158 [PMID:15293986]
ChEMBL	Displacement of [3H]SCH233930 from human D5 receptor expressed in HEK cells	B	7.32	pKi	48	nM	Ki	Bioorg Med Chem Lett (2011) 21: 3622-3626 [PMID:21555222]
ChEMBL	Inhibition of human dopamine D5 receptor	B	7.42	pKi	38	nM	Ki	J Med Chem (2011) 54: 2529-2591 [PMID:21413808]
DAT/Dopamine transporter in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL338] [GtoPdb: 927] [UniProtKB: P23977]
ChEMBL	Inhibitory constant towards reuptake of [125I]-12 from dopamine transporter in rat striatal membranes	B	6	pKi	>1000	nM	Ki	J Med Chem (1994) 37: 1535-1542 [PMID:8182712]
GluN1/GluN2A/GluN2B/GluN2C/GluN2D/GluN3B/GluN3A/Glutamate NMDA receptor in Rat (target type: PROTEIN COMPLEX GROUP) [ChEMBL: CHEMBL1907608] [GtoPdb: 455, 456, 457, 458, 459, 461, 460] [UniProtKB: P35439, Q00959, Q00960, Q00961, Q62645, Q8VHN2, Q9R1M7]
ChEMBL	Binding affinity was measured against phencyclidine (PCP) receptor in rat using [3H]TCP as radioligand	B	5	pKi	>10000	nM	Ki	J Med Chem (1994) 37: 1964-1970 [PMID:8027978]
GluN2B/Glutamate [NMDA] receptor subunit epsilon 2 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3442] [GtoPdb: 457] [UniProtKB: Q01097]
ChEMBL	Displacement of [3H]ifenprodil from GluN2B in mouse LTK cells assessed as inhibition constant measured after 120 mins by scintillation counting method	B	7.89	pKi	13	nM	Ki	J Med Chem (2023) 66: 4999-5020 [PMID:36946301]
Kv11.1/HERG in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809]
ChEMBL	Displacement of [3H]Astemizole from hERG expressed in HEK293 cells at 10 uM	B	6.29	pKi	512	nM	Ki	Bioorg Med Chem Lett (2006) 16: 5303-5308 [PMID:16908150]
ChEMBL	Binding affinity to human ERG expressed in HEK293 cells by whole cell patch clamp method	B	6.92	pKi	120	nM	Ki	J Med Chem (2009) 52: 151-169 [PMID:19072656]
ChEMBL	Inhibitory concentration against IKr potassium channel	B	5.85	pIC50	1400	nM	IC50	Bioorg Med Chem Lett (2004) 14: 4771-4777 [PMID:15324906]
ChEMBL	Inhibition of human ERG expressed in HEK293 cells measured after 30 mins by FluxOR dye based FLIPR TETRA assay	B	5.94	pIC50	1160	nM	IC50	J Med Chem (2020) 63: 5734-5751 [PMID:32392053]
ChEMBL	Inhibition of human ERG expressed in CHO cells after 30 mins by Rb+ flux assay	B	5.96	pIC50	1100	nM	IC50	Bioorg Med Chem Lett (2012) 22: 5134-5140 [PMID:22677319]
ChEMBL	Inhibition of human ERG expressed in HEK293 cells coexpressing Kir2.3 after 30 mins by FluxOR based FLIPR assay	B	6.64	pIC50	230	nM	IC50	J Nat Prod (2012) 75: 1210-1214 [PMID:22694270]
ChEMBL	Inhibition of K+ channel activity in CHO cells expressing HERG Kv11.1	B	7.49	pIC50	32	nM	IC50	Bioorg Med Chem Lett (2003) 13: 1829-1835 [PMID:12729675]
ChEMBL	Inhibition of human ERG expressed in CHO cells by whole cell patch clamp technique	B	7.52	pIC50	30.2	nM	IC50	Bioorg Med Chem (2008) 16: 6252-6260 [PMID:18448342]
ChEMBL	Inhibition of human Potassium channel HERG expressed in mammalian cells	B	7.52	pIC50	30.2	nM	IC50	Bioorg Med Chem Lett (2003) 13: 2773-2775 [PMID:12873512]
ChEMBL	Inhibitory concentration against potassium channel HERG	B	7.52	pIC50	30.2	nM	IC50	Bioorg Med Chem Lett (2005) 15: 2886-2890 [PMID:15911273]
ChEMBL	Inhibition of human voltage-gated potassium channel subunit Kv11.1 (ERG K+ channel) in open state	F	7.55	pIC50	28.18	nM	IC50	Bioorg Med Chem Lett (2005) 15: 1737-1741 [PMID:15745831]
ChEMBL	Inhibition of human ERG in MCF7 cells	B	7.55	pIC50	28.18	nM	IC50	Eur J Med Chem (2009) 44: 1926-1932 [PMID:19110341]
ChEMBL	K+ channel blocking activity in human embryonic kidney cells expressing HERG Kv11.1	F	7.55	pIC50	28.1	nM	IC50	J Med Chem (2002) 45: 3844-3853 [PMID:12190308]
ChEMBL	Inhibition of hERG K channel	F	7.57	pIC50	27	nM	IC50	Cardiovasc Res (2011) 91: 53-61 [PMID:21300721]
ChEMBL	Inhibition of human ERG	B	7.57	pIC50	26.92	nM	IC50	Eur J Med Chem (2011) 46: 618-630 [PMID:21185626]
ChEMBL	Inhibition of human ERG channel	B	7.57	pIC50	26.8	nM	IC50	J Med Chem (2009) 52: 4266-4276 [PMID:19534531]
ChEMBL	Inhibition of human ERG channel	B	7.57	pIC50	26.8	nM	IC50	J Med Chem (2009) 52: 4266-4276 [PMID:19534531]
ChEMBL	Inhibition of human ERG	B	8	pIC50	10	nM	IC50	J Med Chem (2013) 56: 8955-8971 [PMID:23919353]
H1 receptor/Histamine H1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL231] [GtoPdb: 262] [UniProtKB: P35367]
GtoPdb	-	-	6.1	pKi	-	-	-	Psychopharmacology (Berl.) (1996) 124: 57-73 [PMID:8935801]; Neuropsychopharmacology (2003) 28: 519-26 [PMID:12629531]
ChEMBL	Binding Assay: Binding assay using 5-HT2A, Dopamine D2, SERT, αA1, 5-HT2C and H1 Receptors.	B	6.11	pKi	780	nM	Ki	US-8598119-B2. Methods and compositions for sleep disorders and other disorders (2013)
ChEMBL	Binding affinity towards human histamine H1 receptor	B	6.14	pKi	730	nM	Ki	J Med Chem (2004) 47: 1303-1314 [PMID:14998318]
ChEMBL	Binding affinity to human cloned histamine H1 receptor	B	6.36	pKi	440	nM	Ki	Bioorg Med Chem (2008) 16: 7291-7301 [PMID:18595716]
ChEMBL	Displacement of [3H]pyrilamine from human H1 receptor by liquid scintillation counting	B	6.36	pKi	440	nM	Ki	Bioorg Med Chem (2012) 20: 1291-1297 [PMID:22245230]
ChEMBL	Displacement of [3H]Pyrilamine from human histamine H1 receptor by liquid scintillation counting	B	6.36	pKi	440	nM	Ki	Bioorg Med Chem Lett (2014) 24: 4294-4297 [PMID:25070422]
ChEMBL	DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)	B	6.49	pKi	323	nM	Ki	DrugMatrix in vitro pharmacology data
ChEMBL	DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)	B	5.56	pIC50	2781	nM	IC50	DrugMatrix in vitro pharmacology data
H1 receptor/Histamine H1 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4701] [GtoPdb: 262] [UniProtKB: P31390]
ChEMBL	Compound was tested for the binding affinity against rat cortical H1 receptor by Radio ligand [3H]pyrilamine binding assay.	B	5.68	pKi	2100	nM	Ki	J Med Chem (1996) 39: 2764-2772 [PMID:8709107]
ChEMBL	Half-maximal inhibition of [3H]pyrilamine binding to Histamine H1 receptor in rat frontal cortex homogenate	B	6.42	pKi	384	nM	Ki	J Med Chem (2002) 45: 344-359 [PMID:11784139]
ChEMBL	In vitro binding affinity towards Histamine H1 receptor of rat frontal cortex homogenate by using radioligand [3H]pyrilamine	B	6.42	pKi	384	nM	Ki	J Med Chem (2004) 47: 143-157 [PMID:14695828]
ChEMBL	Displacement of [3H]mepyramine from H1R in rat brain	B	5.7	pIC50	>2000	nM	IC50	Proc Natl Acad Sci U S A (2007) 104: 3456-3459 [PMID:17360666]
ChEMBL	Binding affinity towards histamine H1 receptor from rat brain membranes using [3H]mepyramine as radioligand	B	6	pIC50	>1000	nM	IC50	J Med Chem (1999) 42: 2235-2244 [PMID:10377229]
ChEMBL	Inhibitory binding of [3H]mepyramine to histamine H1 receptors in rat brain membranes	B	6	pIC50	>1000	nM	IC50	J Med Chem (1997) 40: 4146-4153 [PMID:9406603]
Histamine H1 receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3943] [UniProtKB: P31389]
ChEMBL	Displacement of [3H]pyrilamine from histaminergic H1 receptor guinea pig cerebellum	B	6.4	pKi	398.11	nM	Ki	J Med Chem (2007) 50: 5103-5108 [PMID:17880057]
H2 receptor/Histamine H2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1941] [GtoPdb: 263] [UniProtKB: P25021]
ChEMBL	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	B	5.94	pKi	1147	nM	Ki	DrugMatrix in vitro pharmacology data
ChEMBL	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	B	5.93	pIC50	1166	nM	IC50	DrugMatrix in vitro pharmacology data
HLA class I histocompatibility antigen A-3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2632] [UniProtKB: P04439]
ChEMBL	Binding affinity to human biotinylated HLA-A2 by surface plasmon resonance assay	B	5	pKd	<10000	nM	Kd	Bioorg Med Chem Lett (2018) 28: 2837-2841 [PMID:30077568]
Human immunodeficiency virus type 1 protease in Human immunodeficiency virus 1 (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL243] [UniProtKB: Q72874]
ChEMBL	Binding affinity to HIV-1 protease	B	4	pKi	100000	nM	Ki	J Med Chem (1994) 37: 1769-1778 [PMID:8021917]
ChEMBL	Binding affinity for HIV-1 protease	B	7	pKi	100	nM	Ki	J Med Chem (1991) 34: 2305-2314 [PMID:1875332]
Human rhinovirus A protease in Human rhinovirus sp. (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2857] [UniProtKB: Q4U254]
ChEMBL	The compound was tested for its affinity against HIV-2 protease	B	7	pKi	100	nM	Ki	J Med Chem (1991) 34: 2305-2314 [PMID:1875332]
μ receptor/Mu opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL233] [GtoPdb: 319] [UniProtKB: P35372]
ChEMBL	Displacement of [3H]-DAMGO from human MOR expressed in CHOK1 cell membranes incubated for 60 mins by liquid scintillation counting method	B	5	pKi	>10000	nM	Ki	J Med Chem (2020) 63: 2434-2454 [PMID:31743642]
ChEMBL	Displacement of [3H]DAMGO from human mu opioid receptor expressed in HEK293 cell membrane incubated for 60 mins by radioligand binding assay	B	5.61	pKi	2470	nM	Ki	J Med Chem (2021) 64: 7778-7808 [PMID:34011153]
ChEMBL	DRUGMATRIX: Opiate mu (OP3, MOP) radioligand binding (ligand: [3H] Diprenorphine)	B	6	pKi	992	nM	Ki	DrugMatrix in vitro pharmacology data
ChEMBL	DRUGMATRIX: Opiate mu (OP3, MOP) radioligand binding (ligand: [3H] Diprenorphine)	B	5.61	pIC50	2443	nM	IC50	DrugMatrix in vitro pharmacology data
ChEMBL	Agonist activity at human MOR expressed in CHOK1 cells assessed as stimulation of cAMP accumulation incubated for 45 mins by HTRF assay	F	5	pEC50	>10000	nM	EC50	J Med Chem (2020) 63: 2434-2454 [PMID:31743642]
M1 receptor/Muscarinic acetylcholine receptor M1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL216] [GtoPdb: 13] [UniProtKB: P11229]
ChEMBL	Binding affinity to human cloned muscarinic M1 receptor	B	5.8	pKi	1600	nM	Ki	Bioorg Med Chem (2008) 16: 7291-7301 [PMID:18595716]
ChEMBL	Displacement of [3H]QNB from human M1 receptor by liquid scintillation counting	B	5.8	pKi	1600	nM	Ki	Bioorg Med Chem (2012) 20: 1291-1297 [PMID:22245230]
ChEMBL	Inhibition of binding of 1.0 nM [3H]pirenzepine to cloned human Muscarinic acetylcholine receptor M1 expressed in membranes from CHO-K1 cells	B	5.26	pIC50	5500	nM	IC50	J Med Chem (1999) 42: 2235-2244 [PMID:10377229]
ChEMBL	Inhibitory binding of [3H]pirenzepine to human Muscarinic acetylcholine receptor M1 in membranes from CHO-K1 cells	B	5.26	pIC50	5500	nM	IC50	J Med Chem (1997) 40: 4146-4153 [PMID:9406603]
M1 receptor/Muscarinic acetylcholine receptor M1 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL276] [GtoPdb: 13] [UniProtKB: P08482]
ChEMBL	Half-maximal inhibition of [3H]QNB binding to Muscarinic acetylcholine receptor M1 in rat frontal cortex homogenate	B	5	pKi	>10000	nM	Ki	J Med Chem (2002) 45: 344-359 [PMID:11784139]
ChEMBL	In vitro binding affinity towards M1 receptor of rat frontal cortex homogenate by using radioligand [3H]QNB	B	5	pKi	>10000	nM	Ki	J Med Chem (2004) 47: 143-157 [PMID:14695828]
ChEMBL	Binding affinity was measured against muscarinic (M1) receptor in rat using [3H]pirenzepine as radioligand	B	5.67	pKi	2140	nM	Ki	J Med Chem (1994) 37: 1964-1970 [PMID:8027978]
ChEMBL	Compound was tested for the binding affinity against rat cortical Muscarinic acetylcholine receptor M1 by Radio ligand [3H]pirenzepine binding assay.	B	5.74	pKi	1800	nM	Ki	J Med Chem (1996) 39: 2764-2772 [PMID:8709107]
M2 receptor/Muscarinic acetylcholine receptor M2 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL309] [GtoPdb: 14] [UniProtKB: P10980]
ChEMBL	Binding affinity was measured against muscarinic (M2) receptor at 10 uM in rat using [3H]QN as radioligand	B	5.21	pKi	6120	nM	Ki	J Med Chem (1994) 37: 1964-1970 [PMID:8027978]
ChEMBL	Compound was tested for the binding affinity against rat heart Muscarinic acetylcholine receptor M2 by quinuclidinyl binding assay.	B	5.6	pKi	2500	nM	Ki	J Med Chem (1996) 39: 2764-2772 [PMID:8709107]
ChEMBL	Inhibition of [3H]N-methylscopolamine binding to Muscarinic acetylcholine receptor M2 of rat heart membranes	B	6.62	pKi	238	nM	Ki	J Med Chem (1998) 41: 1574-1580 [PMID:9572883]
M5 receptor/Muscarinic acetylcholine receptor M5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2035] [GtoPdb: 17] [UniProtKB: P08912]
ChEMBL	DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)	B	5.55	pKi	2795	nM	Ki	DrugMatrix in vitro pharmacology data
ChEMBL	DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)	B	5.41	pIC50	3890	nM	IC50	DrugMatrix in vitro pharmacology data
N-acetyltransferase Eis in Mycobacterium tuberculosis (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3879870] [UniProtKB: P9WFK7]
ChEMBL	Competitive inhibition of Mycobacterium tuberculosis Eis assessed as reduction in Eis-mediated kanamycin acetylation preincubated for 10 mins followed by substrate addition and measured for 2 to 5 mins using acetyl-CoA as substrate in presence of kanamycin by Lineweaver-Burk plot analysis	B	6.41	pKi	390	nM	Ki	RSC Med Chem (2021) 12: 1894-1909 [PMID:34825186]
ChEMBL	Inhibition of Mycobacterium tuberculosis Eis assessed as Eis-mediated kanamycin acetylation preincubated for 10 mins followed by substrate addition and measured for 2 to 5 mins using acetyl-CoA as substrate in presence of kanamycin by UV-Vis spectroscopy analysis	B	6.41	pIC50	390	nM	IC50	RSC Med Chem (2021) 12: 1894-1909 [PMID:34825186]
NET/Norepinephrine transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL222] [GtoPdb: 926] [UniProtKB: P23975]
ChEMBL	Displacement of [3H]Nisoxetine from human Norepinephrine transporter by liquid scintillation counting	B	5.26	pKi	5500	nM	Ki	Bioorg Med Chem Lett (2014) 24: 4294-4297 [PMID:25070422]
ChEMBL	DRUGMATRIX: Norepinephrine Transporter radioligand binding (ligand: [125I] RTI-55)	B	5.74	pKi	1820	nM	Ki	DrugMatrix in vitro pharmacology data
ChEMBL	DRUGMATRIX: Norepinephrine Transporter radioligand binding (ligand: [125I] RTI-55)	B	5.74	pIC50	1836	nM	IC50	DrugMatrix in vitro pharmacology data
ABCB1/P-glycoprotein 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4302] [GtoPdb: 768] [UniProtKB: P08183]
ChEMBL	High affinity constant at binding site of human P-Glycoprotein (P-gp) in two-affinity model	B	6.7	pKi	200	nM	Ki	J Med Chem (2002) 45: 5671-5686 [PMID:12477351]
ChEMBL	Concentration required for 50% inhibition at binding site of human P-Glycoprotein (P-gp) in one-affinity model	B	5.28	pIC50	5300	nM	IC50	J Med Chem (2002) 45: 5671-5686 [PMID:12477351]
Plasmodium falciparum (target type: ORGANISM) [ChEMBL: CHEMBL364]
ChEMBL	Antiplasmodial activity against Plasmodium falciparum D10 after 72 hrs by SYBR green assay	F	5	pIC50	10000	nM	IC50	Nat Chem Biol (2009) 5: 765-771 [PMID:19734910]
ChEMBL	Antiplasmodial activity against Plasmodium falciparum HB3 after 72 hrs by SYBR green assay	F	5.1	pIC50	7943.28	nM	IC50	Nat Chem Biol (2009) 5: 765-771 [PMID:19734910]
ChEMBL	Antiplasmodial activity against Plasmodium falciparum 7G8 after 72 hrs by SYBR green assay	F	5.3	pIC50	5011.87	nM	IC50	Nat Chem Biol (2009) 5: 765-771 [PMID:19734910]
ChEMBL	Antiplasmodial activity against Plasmodium falciparum Dd2 after 72 hrs by SYBR green assay	F	5.3	pIC50	5011.87	nM	IC50	Nat Chem Biol (2009) 5: 765-771 [PMID:19734910]
ChEMBL	Antiplasmodial activity against Plasmodium falciparum 3D7 after 72 hrs by SYBR green assay	F	5.5	pIC50	3162.28	nM	IC50	Nat Chem Biol (2009) 5: 765-771 [PMID:19734910]
ChEMBL	Antiplasmodial activity against Plasmodium falciparum GB4 after 72 hrs by SYBR green assay	F	5.5	pIC50	3162.28	nM	IC50	Nat Chem Biol (2009) 5: 765-771 [PMID:19734910]
ChEMBL	Antiplasmodial activity against Plasmodium falciparum W2 after 72 hrs by SYBR green assay	F	5.7	pIC50	1995.26	nM	IC50	Nat Chem Biol (2009) 5: 765-771 [PMID:19734910]
K2P2.1/Potassium channel subfamily K member 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2321615] [GtoPdb: 514] [UniProtKB: O95069]
ChEMBL	Inhibition of of human TREK1 expressed in whole COS cells assessed as reduction in channel currents	B	5.26	pIC50	5500	nM	IC50	J Med Chem (2016) 59: 5149-5157 [PMID:26588045]
Prion protein in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4869] [UniProtKB: P04156]
ChEMBL	Half maximal inhibition of Prion protein PrPsc formation was assayed in ScN2a cells	B	5	pEC50	>10000	nM	EC50	J Med Chem (2003) 46: 3563-3564 [PMID:12904059]
5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL214] [GtoPdb: 1] [UniProtKB: P08908]
ChEMBL	Binding affinity to human cloned 5HT1A receptor	B	5.44	pKi	3600	nM	Ki	Bioorg Med Chem (2008) 16: 7291-7301 [PMID:18595716]
ChEMBL	Displacement of [3H] 8-OH-DPAT from human 5-HT1A receptor by liquid scintillation counting	B	5.44	pKi	3600	nM	Ki	Bioorg Med Chem Lett (2014) 24: 4294-4297 [PMID:25070422]
ChEMBL	Binding affinity for 5-hydroxytryptamine 1A receptor determined using [3H]8-OH-DPAT as radioligand	B	5.55	pKi	2800	nM	Ki	Bioorg Med Chem Lett (2001) 11: 2345-2349 [PMID:11527728]
ChEMBL	Displacement of [3H]-8-OH-DPAT from human 5-HT1AR expressed in HEK293 cell membranes after 1 hr by microbeta counting method	B	5.77	pKi	1703	nM	Ki	Eur J Med Chem (2018) 145: 790-804 [PMID:29407591]
GtoPdb	-	-	5.8	pKi	-	-	-	Eur J Pharmacol (1998) 355: 245-56 [PMID:9760039]; J Pharmacol Exp Ther (1997) 280: 1241-9 [PMID:9067310]; Psychopharmacology (Berl.) (1996) 124: 57-73 [PMID:8935801]; J Pharmacol Exp Ther (1998) 286: 1341-55 [PMID:9732398]
ChEMBL	Affinity towards 5-hydroxytryptamine 1A receptor in membranes from bovine hippocampus using [3H]OH-DPAT	B	5.82	pIC50	1500	nM	IC50	J Med Chem (1998) 41: 2010-2018 [PMID:9622542]
5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL273] [GtoPdb: 1] [UniProtKB: P19327]
ChEMBL	Binding affinity measured at the 5-hydroxytryptamine 1A receptor by the inhibition of [3H]8-OH-DPAT binding to rat cortex using unlabeled buspirone for nonspecific binding.	B	5.08	pKi	8400	nM	Ki	J Med Chem (1998) 41: 5402-5409 [PMID:9876110]
ChEMBL	Compound was evaluated for in vitro binding affinity towards 5-hydroxytryptamine 1A receptor in rat hippocampus using [3H]8-OH-DPAT as radioligand	B	5.24	pKi	5750	nM	Ki	J Med Chem (1992) 35: 2712-2715 [PMID:1353116]
ChEMBL	In vitro binding affinity towards 5-hydroxytryptamine receptor 1A receptor by using [3H]8-OH-DPAT in rat hippocampal membranes.	B	5.62	pKi	2390	nM	Ki	J Med Chem (2000) 43: 270-277 [PMID:10649982]
ChEMBL	Compound was tested for the Binding affinity against rat hippocampal 5-hydroxytryptamine 1A receptor by Radio ligand [3H]8-OH-DPAT binding assay.	B	5.72	pKi	1900	nM	Ki	J Med Chem (1996) 39: 2764-2772 [PMID:8709107]
ChEMBL	Displacement of [3H]8OH-DPAT from 5HT1A receptor in CRL:CD(SD)BR-COBS rat hippocampus by scintillation spectrometry	B	5.74	pKi	1800	nM	Ki	J Med Chem (2009) 52: 151-169 [PMID:19072656]
ChEMBL	Ability to displace [3H]-8-OH-DPAT from serotonergic 5-hydroxytryptamine 1A receptor	B	5.74	pKi	1800	nM	Ki	Bioorg Med Chem Lett (1995) 5: 1245-1250
ChEMBL	Displacement of [3H]OH-DPAT from rat cortex 5HT1A receptor	B	5.77	pKi	1698.24	nM	Ki	J Med Chem (2007) 50: 865-876 [PMID:17300168]
ChEMBL	Binding affinity towards 5-hydroxytryptamine 1A receptor of rat brain synaptosomal preparations	B	6	pKi	>1000	nM	Ki	J Med Chem (1994) 37: 1060-1062 [PMID:7909336]
ChEMBL	Compound was evaluated for its binding affinity with 5-hydroxytryptamine 1A receptor using membranes prepared from rat cerebral cortex	B	6	pKi	>1000	nM	Ki	J Med Chem (1998) 41: 1997-2009 [PMID:9622541]
ChEMBL	The compound was tested binding affinity against 5-hydroxytryptamine 1A receptor from rat brain using [3H]8-OH-DPAT as radioligand at 10e-6 M.	B	6.3	pKi	>500	nM	Ki	J Med Chem (1999) 42: 3342-3355 [PMID:10464021]
ChEMBL	Binding affinity was determined against 5-hydroxytryptamine 1A receptor using [3H]WB-4101	B	6.4	pKi	401	nM	Ki	J Med Chem (1995) 38: 4198-4210 [PMID:7473547]
ChEMBL	Affinity against the 5-hydroxytryptamine receptor 1A using [3H]WB-4101.	B	6.4	pKi	401	nM	Ki	J Med Chem (1995) 38: 4211-4222 [PMID:7473548]
ChEMBL	The compound was tested for its binding affinity towards 5-hydroxytryptamine 1A receptor by displacing [3H]WB-4101 radioligand in rat hippocampus	B	6.4	pKi	401	nM	Ki	J Med Chem (1992) 35: 552-558 [PMID:1346653]
ChEMBL	Binding affinity towards serotonin 5-HT1A receptor was determined in rat hippocampus using [3H]8-OH-DPAT as ligand	B	5.15	pIC50	7079	nM	IC50	J Med Chem (1996) 39: 4044-4057 [PMID:8831770]
ChEMBL	In vitro affinity towards 5-hydroxytryptamine 1A receptor using [3H]8-OH-DPAT as radioligand in hippocampus	B	5.15	pIC50	7079	nM	IC50	J Med Chem (1994) 37: 2308-2314 [PMID:7914536]
ChEMBL	In vitro binding affinity was measured on serotonergic 5-hydroxytryptamine 1A receptor by displacement of [3H]- tetralin	B	5.15	pIC50	7000	nM	IC50	J Med Chem (1994) 37: 2552-2563 [PMID:7914539]
ChEMBL	Inhibition of [3H]8-OH-DPAT binding at serotonin 5-hydroxytryptamine 1A receptor from rat hippocampus tissue.	B	5.15	pIC50	7000	nM	IC50	J Med Chem (1996) 39: 149-157 [PMID:8568802]
ChEMBL	Compound was measured for affinity at 5-hydroxytryptamine 1A receptor labeled with [3H]8-OH-DPAT radioligand in hippocampus tissue	B	5.21	pIC50	6210	nM	IC50	J Med Chem (1991) 34: 1068-1072 [PMID:1672156]
ChEMBL	Binding affinity towards 5-hydroxytryptamine 1A receptor binding site using [3H]8-OH-DPAT.	B	5.49	pIC50	3200	nM	IC50	J Med Chem (1995) 38: 1998-2008 [PMID:7783131]
ChEMBL	In vitro binding affinity for serotonin 5-hydroxytryptamine 1A receptor fof rat cerebral cortex using [3H]8-OH-DPAT as radioligand	B	5.7	pIC50	1993	nM	IC50	J Med Chem (2002) 45: 4655-4668 [PMID:12361392]
ChEMBL	Binding affinity to 5-hydroxytryptamine 1A receptor in the rat brain using [3H]8-hydroxy-2-(di-n-propylamine)tetralin as radioligand.	B	6	pIC50	>1000	nM	IC50	J Med Chem (1991) 34: 1860-1866 [PMID:1676427]
ChEMBL	Inhibitory concentration against binding of 5-hydroxytryptamine 1A receptor from striata of male Wistar rats by displacement of [3H]8-OH-DPAT	B	6	pIC50	>1000	nM	IC50	Bioorg Med Chem Lett (2000) 10: 509-512 [PMID:10743959]
5-HT1B receptor/Serotonin 1b (5-HT1b) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3459] [GtoPdb: 2] [UniProtKB: P28564]
ChEMBL	Affinity towards 5-hydroxytryptamine 1B receptor in membranes from rat frontal cortex using [3H]5-HT	B	5	pIC50	>10000	nM	IC50	J Med Chem (1998) 41: 2010-2018 [PMID:9622542]
5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223]
ChEMBL	Inhibition of [125I]R91150 binding to human 5-hydroxytryptamine 2A receptor	B	6.36	pKi	435	nM	Ki	J Med Chem (2005) 48: 1709-1712 [PMID:15771415]
ChEMBL	Displacement of [3H]ketanserin from human cloned 5HT2A receptor	B	6.78	pKi	165.96	nM	Ki	Bioorg Med Chem Lett (2009) 19: 6059-6062 [PMID:19796944]
ChEMBL	Displacement of [3H]ketanserin from human cloned 5-HT2A receptor by in vitro binding assay	B	6.78	pKi	165.96	nM	Ki	Medchemcomm (2011) 2: 1194-1200
ChEMBL	Displacement of [3H]ketanserin from human cloned 5HT2A receptor	B	6.78	pKi	165.96	nM	Ki	J Med Chem (2008) 51: 6085-6094 [PMID:18783204]
ChEMBL	Binding affinity towards serotonin 5-hydroxytryptamine 2A receptor	B	6.78	pKi	165.96	nM	Ki	Bioorg Med Chem Lett (2004) 14: 585-589 [PMID:14741248]
ChEMBL	Displacement of [3H]ketanserin from human 5-HT2A receptor	B	6.78	pKi	165.96	nM	Ki	Eur J Med Chem (2014) 71: 237-249 [PMID:24316025]
ChEMBL	Displacement of [3H]ketanserin human cloned serotonin 5HT2A receptor	B	6.78	pKi	165.96	nM	Ki	Bioorg Med Chem Lett (2007) 17: 4873-4877 [PMID:17588750]
ChEMBL	In vitro binding affinity towards 5-hydroxytryptamine 2A receptor in human using [3H]ketanserin as radioligand	B	6.89	pKi	130	nM	Ki	J Med Chem (2004) 47: 143-157 [PMID:14695828]
ChEMBL	Displacement of [3H]Ketanserin from human 5-HT2A receptor by liquid scintillation counting	B	6.92	pKi	120	nM	Ki	Bioorg Med Chem Lett (2014) 24: 4294-4297 [PMID:25070422]
ChEMBL	Binding affinity to human cloned 5HT2A receptor	B	6.92	pKi	120	nM	Ki	Bioorg Med Chem (2008) 16: 7291-7301 [PMID:18595716]
ChEMBL	Binding affinity towards human 5-HT2A receptor in BEK cells	B	6.97	pKi	108	nM	Ki	J Med Chem (1996) 39: 4044-4057 [PMID:8831770]
ChEMBL	Displacement of [3H]ketanserin from human 5HT2A receptor expressed in CHO cells	B	7	pKi	100	nM	Ki	J Med Chem (2007) 50: 5103-5108 [PMID:17880057]
ChEMBL	Binding Assay: Binding assay using 5-HT2A, Dopamine D2, SERT, αA1, 5-HT2C and H1 Receptors.	B	7	pKi	100	nM	Ki	US-8598119-B2. Methods and compositions for sleep disorders and other disorders (2013)
ChEMBL	Displacement of [3H]-ketanserin from human 5-HT2AR expressed in CHO-K1 cell membranes after 1.5 hrs by microbeta counting method	B	7.05	pKi	89	nM	Ki	Eur J Med Chem (2018) 145: 790-804 [PMID:29407591]
GtoPdb	-	-	7.3	pKi	-	-	-	Psychopharmacology (Berl.) (1996) 124: 57-73 [PMID:8935801]; J Pharmacol Exp Ther (1998) 286: 1341-55 [PMID:9732398]; Neuropsychopharmacology (2003) 28: 519-26 [PMID:12629531]; J Pharmacol Exp Ther (2004) 310: 943-51 [PMID:15102927]; J Psychopharmacol (Oxford) (2009) 23: 65-73 [PMID:18308814]
ChEMBL	Binding affinity towards human serotonin 5-hydroxytryptamine 2A receptor	B	7.6	pKi	25	nM	Ki	J Med Chem (2004) 47: 1303-1314 [PMID:14998318]
ChEMBL	Displacement of [3H]-ketanserin from human human 5-HT2A receptor transfected in CHO-K1 cells measured after 60 mins by scintillation counting method	B	7.64	pKi	22.91	nM	Ki	J Med Chem (2021) 64: 12603-12629 [PMID:34436892]
ChEMBL	DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2A radioligand binding (ligand: [3H] Ketanserin)	B	7.68	pKi	21	nM	Ki	DrugMatrix in vitro pharmacology data
ChEMBL	Inhibitory concentration against human 5-HT2A receptor in BEK cells	B	6.54	pIC50	288	nM	IC50	J Med Chem (1996) 39: 4044-4057 [PMID:8831770]
ChEMBL	DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2A radioligand binding (ligand: [3H] Ketanserin)	B	7.12	pIC50	75	nM	IC50	DrugMatrix in vitro pharmacology data
Serotonin 2a (5-HT2a) receptor in Pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2490] [UniProtKB: P50129]
ChEMBL	Displacement of [3H]Ketanserin from 5-HT2 receptor in pig cortex membranes	B	7.52	pKi	30	nM	Ki	J Med Chem (2010) 53: 7219-7228 [PMID:20839776]
Serotonin 2a (5-HT2a) receptor in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3446] [UniProtKB: Q75Z89]
ChEMBL	Affinity towards 5-hydroxytryptamine 2A receptor in membranes from bovine frontal cortex using [3H]ketanserin	B	7.52	pIC50	30	nM	IC50	J Med Chem (1998) 41: 2010-2018 [PMID:9622542]
5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL322] [GtoPdb: 6] [UniProtKB: P14842]
ChEMBL	Half-maximal inhibition of [3H]- Ketanserin binding to 5-hydroxytryptamine 2A receptor in rat cerebral cortex homogenate	B	6.78	pKi	165.96	nM	Ki	J Med Chem (2002) 45: 344-359 [PMID:11784139]
ChEMBL	Inhibition of [3H]ketanserin binding to rat 5-hydroxytryptamine 2A receptor	B	6.79	pKi	164	nM	Ki	J Med Chem (2005) 48: 1705-1708 [PMID:15771414]
ChEMBL	Half-maximal inhibition of [3H]ketanserin binding to 5-hydroxytryptamine 2A receptor in rat cerebral cortex homogenate	B	6.79	pKi	164	nM	Ki	J Med Chem (2002) 45: 344-359 [PMID:11784139]
ChEMBL	Displacement of [3H]ketanserin from 5HT2A receptor in CRL:CD(SD)BR-COBS rat cortex by scintillation spectrometry	B	6.79	pKi	164	nM	Ki	J Med Chem (2009) 52: 151-169 [PMID:19072656]
ChEMBL	In vitro binding affinity towards 5-hydroxytryptamine 2A receptor in rat tissue homogenate using [3H]ketanserin as radioligand	B	6.79	pKi	164	nM	Ki	J Med Chem (2004) 47: 143-157 [PMID:14695828]
ChEMBL	Compound was tested for the Binding affinity against rat frontal cortex 5-hydroxytryptamine 2A receptor by Radio ligand [3H]ketanserin binding assay.	B	7.06	pKi	87	nM	Ki	J Med Chem (1996) 39: 2764-2772 [PMID:8709107]
ChEMBL	Displacement of [3H]ketanserin from rat cortex 5HT2A receptor	B	7.08	pKi	83.18	nM	Ki	J Med Chem (2007) 50: 865-876 [PMID:17300168]
ChEMBL	Binding affinity measured at the 5-hydroxytryptamine 2A receptor by the inhibition of [3H]ketanserin binding to rat cortex using unlabeled mianserin for nonspecific binding.	B	7.12	pKi	75	nM	Ki	J Med Chem (1998) 41: 5402-5409 [PMID:9876110]
ChEMBL	Binding affinity towards 5-hydroxytryptamine 2A receptor using [3H]ketanserin	B	7.28	pKi	52.48	nM	Ki	Bioorg Med Chem Lett (2003) 13: 175-178 [PMID:12482418]
ChEMBL	In vitro affinity against serotonin 5-hydroxytryptamine 2A receptor	B	7.28	pKi	52.48	nM	Ki	J Med Chem (2000) 43: 4678-4693 [PMID:11101359]
ChEMBL	Inhibitory constant on 5-hydroxytryptamine 2A receptor of Rat frontal cortex	B	7.28	pKi	52.48	nM	Ki	J Med Chem (2002) 45: 54-71 [PMID:11754579]
ChEMBL	In vitro binding affinity at serotonin 5-hydroxytryptamine 2A receptor in rat cortical membrane	B	7.31	pKi	49	nM	Ki	J Med Chem (2002) 45: 5136-5149 [PMID:12408724]
ChEMBL	In vitro ability to displace [3H]ketanserin from 5-hydroxytryptamine 2A receptor in rat brain.	B	7.35	pKi	45	nM	Ki	J Med Chem (1996) 39: 143-148 [PMID:8568801]
ChEMBL	Displacement of [3H]-ketanserin from rat brain 5-hydroxytryptamine 2A receptor	B	7.35	pKi	44.67	nM	Ki	J Med Chem (1996) 39: 143-148 [PMID:8568801]
GtoPdb	-	-	7.4	pKi	-	-	-	J Pharmacol Exp Ther (1998) 286: 85-90 [PMID:9655845]
ChEMBL	Displacement of [3H]ketanserin from 5HT2A receptor in rat brain	B	7.46	pKi	34.67	nM	Ki	Bioorg Med Chem (2007) 15: 7361-7367 [PMID:17869521]
ChEMBL	In vitro ability to displace [3H]ketanserin binding from 5-hydroxytryptamine 2A receptor in rat striatal membrane.	B	7.7	pKi	19.95	nM	Ki	J Med Chem (1999) 42: 2774-2797 [PMID:10425088]
ChEMBL	Compound was measured for the inhibition of [3H]ketanserin binding to rat frontal cortex membrane (5-HT2A receptor)	B	7.7	pKi	19.95	nM	Ki	Bioorg Med Chem Lett (1998) 8: 3571-3576 [PMID:9934473]
ChEMBL	Inhibition constant for in vitro inhibition of [3H]ketanserin binding to rat frontal cortex membranes 5-hydroxytryptamine 2A receptor	B	7.7	pKi	19.95	nM	Ki	Bioorg Med Chem Lett (1995) 5: 579-584
ChEMBL	Serotonergic activity of the compound.	B	7.7	pKi	19.95	nM	Ki	J Med Chem (2000) 43: 3233-3243 [PMID:10966742]
ChEMBL	Inhibition of [3H]ketanserin binding to 5-hydroxytryptamine 2A receptor rat frontal cortex membrane	B	7.7	pKi	19.95	nM	Ki	J Med Chem (1994) 37: 2564-2573 [PMID:7914540]
ChEMBL	Tested in vitro for its ability to inhibit [3H]ketanserin binding to 5-hydroxytryptamine 2A receptor in rat frontal cortex membranes	B	7.7	pKi	19.95	nM	Ki	Bioorg Med Chem Lett (1997) 7: 913-918
ChEMBL	In vitro affinity towards 5-hydroxytryptamine 2A receptor using [3H]spiroperidol as radioligand in cortex	B	6.89	pIC50	129	nM	IC50	J Med Chem (1994) 37: 2308-2314 [PMID:7914536]
ChEMBL	In vitro binding affinity for serotonin 5-hydroxytryptamine 2A receptor of rat cerebral cortex using [3H]ketanserin as radioligand	B	6.9	pIC50	125	nM	IC50	J Med Chem (2002) 45: 4655-4668 [PMID:12361392]
ChEMBL	Inhibition of [3H]ketanserin binding to rat frontal cortex membrane 5-hydroxytryptamine 2A receptor	B	6.98	pIC50	104	nM	IC50	J Med Chem (1998) 41: 5402-5409 [PMID:9876110]
ChEMBL	Binding affinity towards 5-hydroxytryptamine 2A receptor from rat frontal cortex using [3H]ketanserin as radioligand	B	7.26	pIC50	55	nM	IC50	J Med Chem (1999) 42: 2235-2244 [PMID:10377229]
ChEMBL	Inhibition of [3H]ketanserin binding to 5-hydroxytryptamine 2A receptor from rat brain	B	7.26	pIC50	55	nM	IC50	J Med Chem (1997) 40: 4146-4153 [PMID:9406603]
ChEMBL	Binding affinity towards 5-hydroxytryptamine 2A receptor binding site using [3H]ketanserin.	B	7.26	pIC50	55	nM	IC50	J Med Chem (1995) 38: 1998-2008 [PMID:7783131]
5-HT2B receptor/Serotonin 2b (5-HT2b) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1833] [GtoPdb: 7] [UniProtKB: P41595]
ChEMBL	DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)	B	5.88	pKi	1305	nM	Ki	DrugMatrix in vitro pharmacology data
GtoPdb	-	-	6.4	pKi	-	-	-	Naunyn Schmiedebergs Arch Pharmacol (1998) 357: 17-24 [PMID:9459568]
ChEMBL	DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)	B	5.69	pIC50	2050	nM	IC50	DrugMatrix in vitro pharmacology data
5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL225] [GtoPdb: 8] [UniProtKB: P28335]
ChEMBL	Displacement of [3H]mesulergine from human cloned 5HT2C receptor	B	5.14	pKi	7244.36	nM	Ki	J Med Chem (2008) 51: 6085-6094 [PMID:18783204]
ChEMBL	Displacement of [3H]mesulergine from human 5HT2C receptor	B	5.14	pKi	7244.36	nM	Ki	Bioorg Med Chem Lett (2009) 19: 6059-6062 [PMID:19796944]
ChEMBL	Binding affinity towards serotonin 5-hydroxytryptamine 2C receptor	B	5.14	pKi	7244.36	nM	Ki	Bioorg Med Chem Lett (2004) 14: 585-589 [PMID:14741248]
ChEMBL	Displacement of [3H]mesulergine human cloned serotonin 5HT2C receptor	B	5.14	pKi	7244.36	nM	Ki	Bioorg Med Chem Lett (2007) 17: 4873-4877 [PMID:17588750]
ChEMBL	Binding affinity towards human serotonin 5-hydroxytryptamine 2C receptor	B	5.3	pKi	>5000	nM	Ki	J Med Chem (2004) 47: 1303-1314 [PMID:14998318]
ChEMBL	Binding affinity to human cloned 5HT2C receptor	B	5.33	pKi	4700	nM	Ki	Bioorg Med Chem (2008) 16: 7291-7301 [PMID:18595716]
ChEMBL	Inhibitory constant was determined on 5-hydroxytryptamine 2C receptor of Bovine choroid plexus	B	5.34	pKi	4570.88	nM	Ki	J Med Chem (2002) 45: 54-71 [PMID:11754579]
ChEMBL	In vitro affinity against serotonin (5-hydroxytryptamine 2C) receptor	B	5.34	pKi	4570.88	nM	Ki	J Med Chem (2000) 43: 4678-4693 [PMID:11101359]
ChEMBL	Binding Assay: Binding assay using 5-HT2A, Dopamine D2, SERT, αA1, 5-HT2C and H1 Receptors.	B	5.4	pKi	3949	nM	Ki	US-8598119-B2. Methods and compositions for sleep disorders and other disorders (2013)
ChEMBL	In vitro ability to displace [3H]mesulergine binding from 5-hydroxytryptamine 2C receptor from bovine choroid plexus.	B	5.6	pKi	2511.89	nM	Ki	J Med Chem (1999) 42: 2774-2797 [PMID:10425088]
ChEMBL	DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2C radioligand binding (ligand: [3H] Mesulergine)	B	5.76	pKi	1753	nM	Ki	DrugMatrix in vitro pharmacology data
ChEMBL	Affinity towards 5-hydroxytryptamine 2C receptor in membranes from pig choroid plexus using [3H]N-methyl-mesulergine	B	5	pIC50	>10000	nM	IC50	J Med Chem (1998) 41: 2010-2018 [PMID:9622542]
ChEMBL	DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2C radioligand binding (ligand: [3H] Mesulergine)	B	5.48	pIC50	3347	nM	IC50	DrugMatrix in vitro pharmacology data
5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL324] [GtoPdb: 8] [UniProtKB: P08909]
ChEMBL	Displacement of [3H]Mesulergine from rat 5-HT2C receptor by liquid scintillation counting	B	5.33	pKi	4700	nM	Ki	Bioorg Med Chem Lett (2014) 24: 4294-4297 [PMID:25070422]
ChEMBL	Binding affinity towards 5-HT2C receptor from rat using [3H]mesulergine as radioligand	B	6	pIC50	>1000	nM	IC50	J Med Chem (1999) 42: 2235-2244 [PMID:10377229]
ChEMBL	Inhibition of [3H]mesulergine binding to 5-hydroxytryptamine 2C receptor in rat brain membranes	B	6	pIC50	>1000	nM	IC50	J Med Chem (1997) 40: 4146-4153 [PMID:9406603]
5-HT3A/Serotonin 3a (5-HT3a) receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4972] [GtoPdb: 373] [UniProtKB: P23979]
ChEMBL	Compound was tested for the Binding affinity against N1e-115 neuroblastoma 5-hydroxytryptamine 3 receptor by Radio ligand [3H]GR-65630 binding assay.	B	5	pKi	>10000	nM	Ki	J Med Chem (1996) 39: 2764-2772 [PMID:8709107]
5-HT6 receptor/Serotonin 6 (5-HT6) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3371] [GtoPdb: 11] [UniProtKB: P50406]
ChEMBL	Binding affinity to human cloned 5HT6 receptor	B	5.22	pKi	6000	nM	Ki	Bioorg Med Chem (2008) 16: 7291-7301 [PMID:18595716]
ChEMBL	Binding affinity towards human 5-hydroxytryptamine 6 receptor	B	5.3	pKi	>5000	nM	Ki	J Med Chem (2003) 46: 2795-2812 [PMID:12825922]
ChEMBL	Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method	B	5.97	pKi	1083	nM	Ki	Eur J Med Chem (2018) 145: 790-804 [PMID:29407591]
5-HT7 receptor/Serotonin 7 (5-HT7) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3155] [GtoPdb: 12] [UniProtKB: P34969]
ChEMBL	Displacement of [3H]-5-carboxyamidotryptamine from human 5HT7 receptor by liquid scintillation counting method	B	5.95	pKi	1122.02	nM	Ki	Bioorg Med Chem (2016) 24: 3671-3679 [PMID:27364609]
ChEMBL	Displacement of [3H]-5-carboxyamidotryptamine from human 5HT7 receptor by liquid scintillation counting method	B	5.96	pKi	1100	nM	Ki	Bioorg Med Chem (2016) 24: 3671-3679 [PMID:27364609]
ChEMBL	Displacement of [3H]-5-CT from human 5-HT7R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method	B	6.39	pKi	408	nM	Ki	Eur J Med Chem (2018) 145: 790-804 [PMID:29407591]
ChEMBL	Displacement of [3H]LSD from human 5HT7 receptor expressed in CHO cells	B	6.5	pKi	316.23	nM	Ki	J Med Chem (2007) 50: 5103-5108 [PMID:17880057]
GtoPdb	-	-	6.6	pKi	-	-	-	Br J Pharmacol (1997) 122: 126-32 [PMID:9298538]
5-HT7 receptor in Mouse [GtoPdb: 12] [UniProtKB: P32304]
GtoPdb	-	-	6.3	pKi	-	-	-	Mol Pharmacol (1993) 44: 229-36 [PMID:8394987]
5-HT7 receptor/Serotonin 7 (5-HT7) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3223] [GtoPdb: 12] [UniProtKB: P32305]
ChEMBL	Binding affinity towards rat 5-hydroxytryptamine 7 receptor	B	6.58	pKi	263	nM	Ki	J Med Chem (2003) 46: 2795-2812 [PMID:12825922]
GtoPdb	-	-	6.6	pKi	-	-	-	Eur J Pharmacol (1996) 317: 417-23 [PMID:8997630]; J Pharmacol Exp Ther (1994) 268: 1403-10 [PMID:7908055]; Proc Natl Acad Sci USA (1993) 90: 8547-51 [PMID:8397408]
SERT/Serotonin transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL228] [GtoPdb: 928] [UniProtKB: P31645]
ChEMBL	Binding affinity to human SERT	B	5.74	pKi	1800	nM	Ki	Bioorg Med Chem (2008) 16: 7291-7301 [PMID:18595716]
ChEMBL	Displacement of [3H]Citalopram from human Serotonin transporter by liquid scintillation counting	B	5.74	pKi	1800	nM	Ki	Bioorg Med Chem Lett (2014) 24: 4294-4297 [PMID:25070422]
ChEMBL	DRUGMATRIX: Transporter, Serotonin (5-Hydroxytryptamine) (SERT) radioligand binding (ligand: [3H] Paroxetine)	B	5.74	pKi	1799	nM	Ki	DrugMatrix in vitro pharmacology data
ChEMBL	Binding Assay: Binding assay using 5-HT2A, Dopamine D2, SERT, αA1, 5-HT2C and H1 Receptors.	B	6	pKi	>1000	nM	Ki	US-8598119-B2. Methods and compositions for sleep disorders and other disorders (2013)
ChEMBL	DRUGMATRIX: Transporter, Serotonin (5-Hydroxytryptamine) (SERT) radioligand binding (ligand: [3H] Paroxetine)	B	5.47	pIC50	3386	nM	IC50	DrugMatrix in vitro pharmacology data
SERT/Serotonin transporter in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL313] [GtoPdb: 928] [UniProtKB: P31652]
ChEMBL	In vitro binding affinity for serotonin reuptake sites in rat frontal cortex membranes by [3H]paroxetine displacement.	B	6	pKi	>1000	nM	Ki	Bioorg Med Chem Lett (2003) 13: 405-408 [PMID:12565939]
Sigma-1 receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4153] [UniProtKB: Q60492]
ChEMBL	Displacement of [3H]-(+)-pentazocine from guinea pig brain membrane sigma 1 receptor assessed as inhibition constant measured after 120 mins by scintillation counting method	B	7.11	pKi	78	nM	Ki	J Med Chem (2023) 66: 4999-5020 [PMID:36946301]
ChEMBL	Displacement of [3H](+)pentazocine from sigma-1 receptor in Cavia porcellus (guinea pig) brain membranes	B	8.04	pKi	9.2	nM	Ki	Med Chem Res (2005) 14: 158-168
ChEMBL	Displacement of [3H]-(+)-pentazocine from guinea pig Sigma1-receptor after 120 mins by liquid scintillation counting method	B	8.18	pKi	6.6	nM	Ki	Medchemcomm (2016) 7: 317-326
ChEMBL	Displacement of [3H]-(+)-pentazocine from sigma1 receptor in guinea pig brain membranes after 120 mins by scintillation counting method	B	8.18	pKi	6.6	nM	Ki	J Med Chem (2019) 62: 893-907 [PMID:30543421]
ChEMBL	Displacement of [3H]-(+)-pentazocine from sigma1 receptor in guinea pig brain cortex membranes after 120 mins by scintillation counting method	B	8.18	pKi	6.6	nM	Ki	Eur J Med Chem (2016) 121: 712-726 [PMID:27366902]
ChEMBL	Displacement of (+)-[3H]pentazocine from guinea pig brain cortex sigma1 receptor by scintillation analyzer	B	8.18	pKi	6.6	nM	Ki	Eur J Med Chem (2015) 90: 797-808 [PMID:25528334]
ChEMBL	Displacement of [3H]-(+)-pentazocine from sigma-1 receptor in guinea pig brain cortex membranes after 120 mins by scintillation counting analysis	B	8.18	pKi	6.6	nM	Ki	J Med Chem (2014) 57: 2884-2894 [PMID:24617836]
ChEMBL	Displacement of [3H]-(+)-pentazocine from sigma1 receptor in guinea pig brain membrane measured by competitive radioligand receptor binding assay	B	8.18	pKi	6.6	nM	Ki	Eur J Med Chem (2022) 230: 114079-114079 [PMID:35033825]
ChEMBL	Displacement of [3H]-(+)-pentazocine from sigma-1 receptor in guinea pig brain cortex membranes	B	8.18	pKi	6.6	nM	Ki	J Med Chem (2014) 57: 6845-6860 [PMID:25062506]
ChEMBL	Displacement of [3H]-(+)-Pentazocine from sigma1 receptor in guinea pig brain cortex membranes after 120 mins by scintillation counting analysis	B	8.18	pKi	6.6	nM	Ki	Medchemcomm (2016) 7: 2368-2380
ChEMBL	Displacement of [3H](+)-Pentazocine from sigma 1 receptor in guinea pig brain membranes after 120 mins by scintillation counting analysis	B	8.18	pKi	6.6	nM	Ki	J Med Chem (2016) 59: 5505-5519 [PMID:27156565]
ChEMBL	Displacement of [3H]-(+)-pentazocine from sigma1 receptor in guinea pig brain membrane by scintillation counting	B	8.2	pKi	6.3	nM	Ki	Bioorg Med Chem (2011) 19: 393-405 [PMID:21126878]
ChEMBL	Displacement of [3H]-pentazocine from sigma1 receptor in guinea pig brain membrane incubated for 120 mins by liquid scintillation counting method	B	8.2	pKi	6.3	nM	Ki	Eur J Med Chem (2021) 210: 112950-112950 [PMID:33148494]
ChEMBL	Displacement of [3H]-(+)-pentazocine from Sigma1 receptor in guinea pig cortex membranes incubated for 120 mins by scintillation counting method	B	8.2	pKi	6.3	nM	Ki	Eur J Med Chem (2020) 190: 112138-112138 [PMID:32070917]
ChEMBL	Displacement of [3H]-(+)pentazocine from sigma-1 receptor in guinea pig brain membranes after 120 mins by scintillation counting method	B	8.2	pKi	6.3	nM	Ki	ACS Med Chem Lett (2020) 11: 651-656 [PMID:32435366]
ChEMBL	Displacement of [3H]-(+)-pentazocine from sigma1 receptor in guinea pig brain membranes incubated for 120 mins by scintillation counting method	B	8.2	pKi	6.3	nM	Ki	Bioorg Med Chem (2020) 28: 115245-115245 [PMID:31843460]
ChEMBL	Displacement of [3H](+)-pentazocine from sigma 1 receptor in guinea pig brain by scintillation analyzer	B	8.2	pKi	6.3	nM	Ki	Bioorg Med Chem (2011) 19: 3141-3151 [PMID:21531141]
ChEMBL	Displacement of [3H]-(+)-pentazocine from sigma 1 receptor in guinea pig brain homogenates after 180 mins by solid scintillation counting	B	8.2	pKi	6.3	nM	Ki	Bioorg Med Chem (2012) 20: 257-269 [PMID:22136765]
ChEMBL	Displacement of [3H]-(+)-pentazocine from sigma1 receptor in guinea pig brain membrane by competitive radioligand receptor binding assay	B	8.2	pKi	6.3	nM	Ki	Eur J Med Chem (2022) 230: 114113-114113 [PMID:35065412]
ChEMBL	Displacement of [3H]-(+)-pentazocine from sigma1 receptor in guinea pig brain cortex membranes measured after 120 mins by scintillation counting method	B	8.2	pKi	6.3	nM	Ki	Eur J Med Chem (2022) 237: 114359-114359 [PMID:35468513]
ChEMBL	Displacement of [3H](+)-Pentazocine from sigma 1 receptor in guinea pig brain membranes after 120 mins by scintillation counting analysis	B	8.2	pKi	6.3	nM	Ki	Bioorg Med Chem (2013) 21: 1844-1856 [PMID:23462714]
ChEMBL	Displacement of [3H]-(+)-pentazocine from sigma1 receptor in guinea pig brain cortex membranes incubated for 120 mins by scintillation counting method	B	8.2	pKi	6.3	nM	Ki	Eur J Med Chem (2019) 177: 47-62 [PMID:31129453]
ChEMBL	Displacement of (+)-pentazocine from sigma-1 receptor in guinea pig brain cortex membrane after 120 mins by scintillation counting	B	8.2	pKi	6.3	nM	Ki	Eur J Med Chem (2013) 69: 490-497 [PMID:24095744]
ChEMBL	Displacement of [3H]-(+)pentazocine from sigma-1 receptor in guinea pig brain membranes after 120 mins by scintillation counting method	B	8.2	pKi	6.3	nM	Ki	Bioorg Med Chem (2019) 27: 3559-3567 [PMID:31255496]
ChEMBL	Displacement of [3H]-(+)-pentazocine from sigma1 receptor in guinea pig brain cortex membranes incubated for 120 mins by solid scintillation counting method	B	8.2	pKi	6.3	nM	Ki	Bioorg Med Chem (2019) 27: 115146-115146 [PMID:31648876]
ChEMBL	Displacement of [3H]-(+)-Pentazocine from sigma1 receptor in guniea pig brain cortex membranes by scintillation counting analysis	B	8.2	pKi	6.3	nM	Ki	Bioorg Med Chem Lett (2015) 25: 5748-5751 [PMID:26531150]
ChEMBL	Displacement of [3H](+)-pentazocine from sigma1 receptor in guinea pig brain membranes after 180 mins by scintillation counting method	B	8.2	pKi	6.3	nM	Ki	Bioorg Med Chem (2014) 22: 6638-6646 [PMID:25458498]
ChEMBL	Displacement of (+)-pentazocine from sigma1 receptor in guinea pig brain cortex membrane by scintillation counting analysis	B	8.2	pKi	6.3	nM	Ki	Eur J Med Chem (2014) 83: 526-533 [PMID:24996139]
ChEMBL	Displacement of [3H](+)-pentazocine from sigma 1 receptor in guinea pig brain membranes after 150 mins by liquid scintillation spectrometry	B	8.2	pKi	6.3	nM	Ki	Medchemcomm (2016) 7: 327-331
ChEMBL	Displacement of [3H]-(+)-Pentazocine from sigma1 receptor in guinea pig brain homogenate incubated for 120 mins by solid scintillation counting analysis	B	8.2	pKi	6.3	nM	Ki	Eur J Med Chem (2016) 116: 136-146 [PMID:27061977]
ChEMBL	Displacement of [3H](+)-Pentazocine from sigma 1 receptor in guinea pig brain membranes after 120 mins by scintillation counting analysis	B	8.2	pKi	6.3	nM	Ki	Medchemcomm (2017) 8: 975-981 [PMID:30108812]
ChEMBL	Displacement of [3H]-(+)-pentazocine from sigma-1 receptor in guinea pig brain cortex membranes incubated for 120 mins measured for 5 mins by scintillation counting method	B	8.2	pKi	6.3	nM	Ki	Eur J Med Chem (2018) 144: 672-681 [PMID:29289890]
ChEMBL	Displacement of [3H]-(+)-Pentazocine from sigma 1 receptor in guinea pig brain cortex membranes after 120 mins by scintillation counting analysis	B	8.2	pKi	6.3	nM	Ki	Bioorg Med Chem (2018) 26: 501-508 [PMID:29254894]
ChEMBL	Displacement of [3H](+)-Pentazocine from sigma 1 receptor in guinea pig brain membranes after 120 mins by scintillation counting analysis	B	8.2	pKi	6.3	nM	Ki	Bioorg Med Chem (2017) 25: 5365-5372 [PMID:28797770]
ChEMBL	Displacement of [3H]-pentazocine from sigma1 receptor in guinea pig brain membranes after 120 mins by liquid scintillation counting	B	8.2	pKi	6.3	nM	Ki	Bioorg Med Chem (2017) 25: 4778-4799 [PMID:28764962]
ChEMBL	Displacement of [3H]-(+)-pentazocine from sigma1 receptor in guinea pig brain membrane measured after 120 mins by scintillation counting method	B	8.2	pKi	6.3	nM	Ki	J Med Chem (2022) 65: 12292-12318 [PMID:36084304]
ChEMBL	Displacement of [3H]-(+)-pentazocine from sigma1 receptor in guinea pig brain membrane measured after 120 mins by solid scintillation counting method	B	8.2	pKi	6.3	nM	Ki	Eur J Med Chem (2021) 219: 113443-113443 [PMID:33901806]
ChEMBL	Displacement of [3H](+)-pentazocine from sigma1 receptor guinea pig brain after 180 mins scintillation counting	B	8.2	pKi	6.3	nM	Ki	Bioorg Med Chem (2010) 18: 8005-8015 [PMID:20965739]
ChEMBL	Displacement of [3H]-(+)-pentazocine from sigma 1 receptor in guinea pig brain cortex membranes	B	8.2	pKi	6.3	nM	Ki	Bioorg Med Chem (2014) 22: 4277-4284 [PMID:24913984]
ChEMBL	Displacement of [3H]-(+)-pentazocine from sigma1 receptor in guinea pig brain cortex membranes incubated for 120 mins by solid scintillation counting method	B	8.2	pKi	6.3	nM	Ki	Eur J Med Chem (2019) 180: 268-282 [PMID:31319263]
ChEMBL	Displacement of [3H]-(+)-pentazocine from sigma-1 receptor in guinea pig brain homogenates	B	8.22	pKi	6	nM	Ki	J Med Chem (2012) 55: 8953-8957 [PMID:23013229]
ChEMBL	Displacement of [3H]pentazocine from guinea pig sigma1 receptor measured after 90 mins by microbeta scintillation counting method	B	8.4	pKi	4	nM	Ki	Bioorg Med Chem Lett (2016) 26: 5689-5694 [PMID:27839919]
ChEMBL	Displacement of [3H]-(+)-pentazocine from guinea pig brain sigma-1 receptor after 180 mins by scintillation counting analysis	B	8.41	pKi	3.9	nM	Ki	Medchemcomm (2012) 3: 673-679
ChEMBL	Displacement of [3H](+)-pentazocine from sigma 1 receptor in guinea pig brain membrane by scintillation analysis	B	8.41	pKi	3.9	nM	Ki	J Med Chem (2009) 52: 2126-2137 [PMID:19243173]
ChEMBL	Displacement of [3H](+)-pentazocine from sigma 1 receptor in guinea pig brain membrane	B	8.41	pKi	3.9	nM	Ki	J Med Chem (2008) 51: 6531-6537 [PMID:18816044]
ChEMBL	Displacement of [3H](+)-pentazocine from opioid sigma1 receptor in guinea pig brain homogenate	B	8.41	pKi	3.9	nM	Ki	Bioorg Med Chem (2009) 17: 777-793 [PMID:19081725]
ChEMBL	Displacement of [3H](+)-pentazocine from sigma1 opioid receptor in guinea pig brain by solid scintillation counting	B	8.41	pKi	3.9	nM	Ki	Bioorg Med Chem (2009) 17: 1445-1455 [PMID:19196515]
ChEMBL	Displacement of [3H](+)-pentazocine from sigma 1 receptor in guinea pig brain membrane by solid scintillation analysis	B	8.41	pKi	3.9	nM	Ki	Bioorg Med Chem (2009) 17: 3630-3641 [PMID:19394833]
ChEMBL	Displacement of [3H](+)-pentazocine from sigma 1 receptor in guinea pig brain membrane after 180 mins by scintillation counting	B	8.41	pKi	3.9	nM	Ki	J Med Chem (2009) 52: 6062-6072 [PMID:19791807]
ChEMBL	Displacement of [3H](+)-pentazocine from sigma 1 receptor in guinea pig brain after 180 mins by scintillation counting	B	8.41	pKi	3.9	nM	Ki	Eur J Med Chem (2009) 44: 4306-4314 [PMID:19709783]
ChEMBL	Displacement of [3H](+)-pentazocine from sigma1 receptor in guinea pig brain membrane	B	8.41	pKi	3.9	nM	Ki	J Med Chem (2010) 53: 4212-4222 [PMID:20441176]
ChEMBL	Displacement of (+)-[3H]pentazocine from guinea pig brain sigma 1 receptor after 180 mins by scintillation counting	B	8.41	pKi	3.9	nM	Ki	J Med Chem (2011) 54: 6704-6713 [PMID:21859078]
ChEMBL	Displacement of [3H]-(+)-pentazocine from sigma1 receptor in guinea pig brain membrane after 180 mins by solid scintillation counting	B	8.41	pKi	3.9	nM	Ki	Eur J Med Chem (2012) 53: 327-336 [PMID:22578786]
ChEMBL	Displacement of [3H]-(+)pentazocine from guinea pig brain sigma 1-type opioid receptor after 120 mins by scintillation counting analysis	B	8.41	pKi	3.9	nM	Ki	J Med Chem (2012) 55: 5350-5360 [PMID:22515405]
ChEMBL	Displacement of [3H]-(+)-pentazocine from sigma 1 receptor in guinea pig brain membranes after 120 mins by scintillation counting	B	8.41	pKi	3.9	nM	Ki	J Med Chem (2012) 55: 8047-8065 [PMID:22913577]
ChEMBL	Displacement of [3H]-(+)-pentazocine from sigma-1 receptor in guinea pig brain membranes after 120 mins by microbeta scintillation counting method	B	8.41	pKi	3.9	nM	Ki	Bioorg Med Chem (2017) 25: 3384-3395 [PMID:28501431]
ChEMBL	Displacement of [3H]-(+)-pentazocine from sigma1 receptor in guinea pig brain cortex membrane incubated for 120 mins measured for 5 mins by scintillation counting method	B	8.41	pKi	3.9	nM	Ki	Bioorg Med Chem (2017) 25: 2472-2481 [PMID:28320613]
ChEMBL	Displacement of [3H](+)-pentazocine from Sigma1 receptor in Dunkin Hartley guinea pig brain membrane after 120 mins by liquid scintillation counting analysis	B	8.44	pKi	3.6	nM	Ki	Bioorg Med Chem Lett (2016) 26: 2676-2679 [PMID:27090556]
ChEMBL	Displacement of [3H]-PTZ from sigma1 receptor in guinea pig brain membranes after 150 mins in presence of 1 mM DPH by liquid scintillation counting method	B	8.46	pKi	3.5	nM	Ki	Eur J Med Chem (2017) 125: 603-610 [PMID:27721146]
ChEMBL	Displacement of [3H](+)-pentazocine from sigma 1 receptor in guinea pig brain membranes after 120 mins by microbeta scintillation counting method	B	8.49	pKi	3.27	nM	Ki	Eur J Med Chem (2021) 209: 112906-112906 [PMID:33049607]
ChEMBL	Displacement of [3H](+)pentazocine from sigma1 receptor in Dunkin Hartley guinea pig brain membrane after 120 mins by liquid scintillation counting analysis	B	8.55	pKi	2.8	nM	Ki	Eur J Med Chem (2013) 64: 488-497 [PMID:23680866]
ChEMBL	Displacement of [3H]-(+)-pentazocine from sigma1 receptor in guinea pig brain membrane incubated for 150 mins by liquid scintillation counting method	B	8.57	pKi	2.7	nM	Ki	Bioorg Med Chem (2016) 24: 3149-3156 [PMID:27262426]
ChEMBL	Displacement of [3H]-PTZ from sigma1 receptor in guinea pig brain membranes after 150 mins in presence of 250 uM DPH by liquid scintillation counting method	B	8.57	pKi	2.7	nM	Ki	Eur J Med Chem (2017) 125: 603-610 [PMID:27721146]
ChEMBL	Displacement of [3H]-pentazocine from sigma1 receptor in guinea pig brain membranes by scintillation counting	B	8.57	pKi	2.7	nM	Ki	J Med Chem (2016) 59: 9960-9966 [PMID:27739690]
ChEMBL	Displacement of [3H]-(+)-pentazocine from Dunkin-Hartley guinea pig brain cortex Sigma 1 receptor incubated for 150 mins by liquid scintillation counting analysis	B	8.59	pKi	2.6	nM	Ki	Eur J Med Chem (2022) 230: 114091-114091 [PMID:35016113]
ChEMBL	Displacement of [3H]-(+)-pentazocine from sigma 1 receptor in Dunkin Hartley guinea pig membrane after 180 mins by liquid scintillation counting analysis	B	8.59	pKi	2.6	nM	Ki	Eur J Med Chem (2014) 79: 216-230 [PMID:24735647]
ChEMBL	Displacement of [3H]-(+)-pentazocine from sigma 1 receptor guinea pig brain membranes incubated for 150 mins by scintillation counting method	B	8.6	pKi	2.5	nM	Ki	Eur J Med Chem (2015) 90: 1-9 [PMID:25461306]
ChEMBL	Displacement of [3H]-PTZ from sigma1 receptor in guinea pig brain membranes after 150 mins in presence of DPH solvent by liquid scintillation counting method	B	8.6	pKi	2.5	nM	Ki	Eur J Med Chem (2017) 125: 603-610 [PMID:27721146]
ChEMBL	Displacement of [3H]-(+)-pentazocine from sigma1 receptor in guinea pig brain membranes incubated for 1 hr by liquid scintillation counting method	B	8.6	pKi	2.5	nM	Ki	ACS Med Chem Lett (2020) 11: 889-894 [PMID:32435401]
ChEMBL	Displacement of [3H]-(+)-pentazocine from sigma 1 receptor in guinea pig brain membranes after 150 mins by liquid scintillation counting method	B	8.6	pKi	2.5	nM	Ki	J Med Chem (2017) 60: 9531-9544 [PMID:29172528]
ChEMBL	Displacement of [3H]-(+)-pentazocine from sigma 1 receptor in guinea pig brain membranes after 150 mins	B	8.66	pKi	2.2	nM	Ki	J Med Chem (2011) 54: 3669-3673 [PMID:21476493]
ChEMBL	Displacement of [3H](+)-pentazocine from sigma 1 receptor in guinea pig brain membrane by liquid scintillation analyzer	B	8.66	pKi	2.2	nM	Ki	Eur J Med Chem (2009) 44: 519-525 [PMID:18499305]
ChEMBL	Displacement of [3H](+)-pentazocine from sigma 1 receptor in guinea pig brain membranes after 150 mins by microbeta scintillation counting method	B	8.66	pKi	2.2	nM	Ki	J Med Chem (2021) 64: 13622-13632 [PMID:34477381]
ChEMBL	Displacement of [3H]-(+)-pentazocine from sigma1 receptor in guinea pig brain membrane after 150 mins by liquid scintillation counting method	B	8.66	pKi	2.2	nM	Ki	J Med Chem (2018) 61: 372-384 [PMID:29220177]
ChEMBL	Displacement of [3H](+)-pentazocine from sigma 1 receptor in guinea pig brain membrane	B	8.66	pKi	2.2	nM	Ki	Eur J Med Chem (2007) 42: 1247-1262 [PMID:17420073]
ChEMBL	Displacement of [3H]-(+)-pentazocine from sigma 1 receptor in guinea pig brain membrane after 150 mins by liquid scintillation counting	B	8.66	pKi	2.2	nM	Ki	Eur J Med Chem (2011) 46: 433-438 [PMID:21055848]
ChEMBL	Displacement of [3H](+)-pentazocine from sigma 1 receptor in guinea pig brain membrane	B	8.72	pKi	1.9	nM	Ki	J Med Chem (2007) 50: 6144-6153 [PMID:17967001]
ChEMBL	Displacement of [3H]-(+)-pentazocine from sigma 1 receptor in guinea pig brain membranes after 2 hrs by scintillation counting	B	8.72	pKi	1.9	nM	Ki	Bioorg Med Chem (2016) 24: 4045-4055 [PMID:27396684]
ChEMBL	Displacement of [3H](+)-pentazocine from sigma 1 opioid receptor in guinea pig brain membrane	B	8.72	pKi	1.9	nM	Ki	Bioorg Med Chem (2008) 16: 2992-3001 [PMID:18221879]
ChEMBL	Displacement of [3H]-(+)-pentazocine from sigma1 receptor in guinea pig brain membranes incubated for 150 mins by scintillation counting method	B	8.8	pKi	1.6	nM	Ki	Eur J Med Chem (2019) 174: 226-235 [PMID:31042618]
ChEMBL	Displacement of [3H]-pentazocine from guinea pig sigma1 receptor by liquid scintillation counting	B	8.82	pKi	1.5	nM	Ki	J Med Chem (2011) 54: 1555-1564 [PMID:21348515]
ChEMBL	Displacement of [3H](+)-pentazocine from sigma 1 receptor in guinea pig brain homogenates after 1 hr by liquid scintillation counting	B	8.84	pKi	1.45	nM	Ki	Bioorg Med Chem (2010) 18: 5291-5300 [PMID:20542439]
ChEMBL	Displacement of [3H](+)-pentazocine from sigma 1-type opioid receptor in guinea pig brain homogenates	B	8.84	pKi	1.45	nM	Ki	Bioorg Med Chem (2009) 17: 1222-1231 [PMID:19119012]
ChEMBL	Displacement of [3H]-(+)-pentazocine from sigma-1 receptor in guinea pig brain membranes incubated for 1 hr in presence of 250 uM phenytoin liquid scintillation counting method	B	8.85	pKi	1.4	nM	Ki	J Med Chem (2021) 64: 890-904 [PMID:33372782]
ChEMBL	Displacement of [3H]-(+)-pentazocine from guinea pig brain sigma1 receptor after 150 mins by scintillation counting analysis	B	8.89	pKi	1.3	nM	Ki	Bioorg Med Chem (2014) 22: 393-397 [PMID:24290063]
ChEMBL	Displacement of [3H]-(+)-pentazocine from sigma-1 receptor in guinea pig brain membranes incubated for 1 hr by liquid scintillation counting method	B	8.89	pKi	1.3	nM	Ki	J Med Chem (2021) 64: 890-904 [PMID:33372782]
ChEMBL	Displacement of [3H]-(+)-pentazocine from Sigma1-receptor in guinea pig brain membrane	B	9.08	pKi	0.83	nM	Ki	Bioorg Med Chem (2011) 19: 1852-1859 [PMID:21376604]
ChEMBL	Displacement of [3H](+)-PTZ from sigma1 receptor in Hartley guinea pig brain	B	9.08	pKi	0.83	nM	Ki	Bioorg Med Chem (2008) 16: 755-761 [PMID:18029187]
σ2/Sigma intracellular receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105907] [GtoPdb: 2553] [UniProtKB: Q5BJF2]
ChEMBL	Binding affinity to sigma-2 receptor (unknown origin)	B	6.66	pKi	221	nM	Ki	J Med Chem (2020) 63: 15187-15217 [PMID:33111525]
ChEMBL	Displacement of [3H]-DTG from sigma-2 receptor in human Jurkat cell membrane incubated for 1 hr by liquid scintillation counting method	B	7.08	pKi	83	nM	Ki	J Med Chem (2021) 64: 890-904 [PMID:33372782]
ChEMBL	Binding affinity to human sigma 2 receptor	B	7.74	pKi	18	nM	Ki	Bioorg Med Chem (2022) 73: 117032-117032 [PMID:36202063]
ChEMBL	Displacement of [3H]-DTG from sigma2 receptor (unknown origin) incubated for 120 mins by scintillation counting method	B	7.75	pKi	17.6	nM	Ki	Eur J Med Chem (2019) 174: 226-235 [PMID:31042618]
ChEMBL	Displacement of [3H]-di-o-tolylguanidine from sigma2 receptor (unknown origin) incubated for 1 hr in presence of (+)SKF10047 by liquid scintillation counting method	B	7.8	pKi	16	nM	Ki	ACS Med Chem Lett (2020) 11: 889-894 [PMID:32435401]
ChEMBL	Displacement of [3H]-DTG from sigma 2 receptor (unknown origin) after 120 mins by liquid scintillation counting method	B	7.8	pKi	16	nM	Ki	J Med Chem (2017) 60: 9531-9544 [PMID:29172528]
ChEMBL	Binding affinity to sigma 2 receptor (unknown origin) assessed as inhibition constant by radioligand binding assay	B	7.8	pKi	16	nM	Ki	Bioorg Med Chem Lett (2022) 72: 128860-128860 [PMID:35724925]
σ2/Sigma intracellular receptor 2 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105864] [GtoPdb: 2553] [UniProtKB: Q5U3Y7]
ChEMBL	Displacement of [3H]DTG from sigma-2 receptor in Sprague-Dawley rat liver membrane incubated for 90 mins in presence of by liquid scintillation counter analysis (+)-pentazocine by liquid scintillation counter analysis	B	6.94	pKi	114.3	nM	Ki	RSC Med Chem (2022) 13: 986-997 [PMID:36092143]
ChEMBL	Displacement of [3H]-DTG from sigma2 receptor in rat brain membranes after 120 mins in presence of (+)-pentazocine by radioligand binding assay	B	7.09	pKi	80.6	nM	Ki	Eur J Med Chem (2019) 165: 250-257 [PMID:30685525]
ChEMBL	Displacement of [3H]-DTG from sigma2 receptor in rat liver membranes after 120 mins by liquid scintillation counting	B	7.11	pKi	78	nM	Ki	Bioorg Med Chem (2017) 25: 4778-4799 [PMID:28764962]
ChEMBL	Displacement of [3H]-DTG from sigma 2 receptor in rat liver membranes after 120 mins by scintillation counting analysis	B	7.11	pKi	78	nM	Ki	Bioorg Med Chem (2018) 26: 501-508 [PMID:29254894]
ChEMBL	Displacement of [3H]DTG from sigma2 receptor in Sprague-Dawley rat liver membranes after 120 mins by scintillation counting analysis	B	7.11	pKi	78	nM	Ki	Medchemcomm (2016) 7: 2368-2380
ChEMBL	Displacement of [3H]-di-o-tolylguanidine from sigma-2 receptor in rat liver membranes incubated for 120 mins measured for 5 mins by scintillation counting method	B	7.11	pKi	78	nM	Ki	Eur J Med Chem (2018) 144: 672-681 [PMID:29289890]
ChEMBL	Displacement of [3H]-di-o-tolylguanidine from sigma2 receptor in rat liver membranes in the presence of sigma1 receptor ligand (+)-pentazocine incubated for 120 mins by scintillation counting method	B	7.11	pKi	78	nM	Ki	Eur J Med Chem (2019) 180: 268-282 [PMID:31319263]
ChEMBL	Displacement of [3H]di-o-tolylguanidine from sigma2 receptor in rat liver membranes measured after 120 mins by solid scintillation counting method	B	7.11	pKi	78	nM	Ki	Bioorg Med Chem (2019) 27: 115146-115146 [PMID:31648876]
ChEMBL	Displacement of [3H]-Di-o-tolylguanidine from sigma-2 receptor in rat liver membranes after 120 mins by scintillation counting method	B	7.11	pKi	78	nM	Ki	Bioorg Med Chem (2019) 27: 3559-3567 [PMID:31255496]
ChEMBL	Displacement of [3H]DTG from sigma2 receptor in rat liver membranes after 120 mins by scintillation counting method	B	7.11	pKi	78	nM	Ki	J Med Chem (2019) 62: 893-907 [PMID:30543421]
ChEMBL	Displacement of [3H]-di-o-tolylguanidine from sigma2 receptor in rat liver membranes incubated for 120 mins by scintillation counting method	B	7.11	pKi	78	nM	Ki	Eur J Med Chem (2019) 177: 47-62 [PMID:31129453]
ChEMBL	Displacement of [3H]-di-o-tolylguanidine from sigma2 receptor in rat liver membranes incubated for 120 mins in the presence of sigma1 receptor ligand (+)-pentazocine by scintillation counting method	B	7.11	pKi	78	nM	Ki	Bioorg Med Chem (2020) 28: 115245-115245 [PMID:31843460]
ChEMBL	Displacement of [3H]-Di-o-tolylguanidine from sigma-2 receptor in rat liver membranes after 120 mins by scintillation counting method	B	7.11	pKi	78	nM	Ki	ACS Med Chem Lett (2020) 11: 651-656 [PMID:32435366]
ChEMBL	Displacement of [3H]DTG from sigma 2 receptor in rat liver membranes incubated for 120 mins by scintillation counting method	B	7.11	pKi	78	nM	Ki	Eur J Med Chem (2020) 190: 112138-112138 [PMID:32070917]
ChEMBL	Displacement of [3H]DTG from sigma-2 receptor in rat liver membranes after 120 mins by microbeta scintillation counting method	B	7.11	pKi	78	nM	Ki	Bioorg Med Chem (2017) 25: 3384-3395 [PMID:28501431]
ChEMBL	Displacement of [3H]-di-o-tolylguanidine from sigma2 receptor in rat liver membrane incubated for 120 mins measured for 5 mins by scintillation counting method	B	7.11	pKi	78	nM	Ki	Bioorg Med Chem (2017) 25: 2472-2481 [PMID:28320613]
ChEMBL	Displacement of [3H]-di-o-tolylguanidine from sigma2 receptor in rat liver membrane incubated for 120 mins by liquid scintillation counting method relative to control	B	7.11	pKi	78	nM	Ki	Eur J Med Chem (2021) 210: 112950-112950 [PMID:33148494]
ChEMBL	Displacement of [3H]-di-o-tolylguanidine from sigma2 receptor in rat liver membrane by solid scintillation counting method	B	7.11	pKi	78	nM	Ki	Eur J Med Chem (2021) 219: 113443-113443 [PMID:33901806]
ChEMBL	Displacement of [3H]DTG from sigma 2 receptor in rat liver membranes measured after 120 mins by scintillation counting method	B	7.11	pKi	78	nM	Ki	J Med Chem (2022) 65: 12292-12318 [PMID:36084304]
ChEMBL	Displacement of [3H]-DTG from sigma 2 receptor in rat liver membrane measured after 120 mins by microbeta counting analysis	B	7.11	pKi	78	nM	Ki	Eur J Med Chem (2022) 237: 114359-114359 [PMID:35468513]
ChEMBL	Displacement of [3H]-di-o-tolylguanidine from sigma2 receptor in rat liver membrane measured by competitive radioligand receptor binding assay	B	7.11	pKi	78	nM	Ki	Eur J Med Chem (2022) 230: 114079-114079 [PMID:35033825]
ChEMBL	Displacement of [3H]di-O-tolylguanidine from sigma 2 receptor in rat liver membrane by competitive radioligand receptor binding assay	B	7.11	pKi	78	nM	Ki	Eur J Med Chem (2022) 230: 114113-114113 [PMID:35065412]
ChEMBL	Displacement of [H3]DTG from rat liver homogenates sigma 2 receptor assessed as inhibition constant by radioligand binding assay	B	7.11	pKi	77	nM	Ki	RSC Med Chem (2023) 14: 1734-1742 [PMID:37731701]
ChEMBL	Displacement of [3H]-DTG from Sprague-Dawley rat liver Sigma 2 receptor incubated for 120 mins in presence of [3H]-(+)-pentazocine by liquid scintillation counting analysis	B	7.11	pKi	77	nM	Ki	Eur J Med Chem (2022) 230: 114091-114091 [PMID:35016113]
ChEMBL	Displacement of [3H]-(+)-DTG from rat liver homogenate S2R incubated for 120 mins by liquid scintillation counting method	B	7.11	pKi	77	nM	Ki	J Med Chem (2023) 66: 11447-11463 [PMID:37535861]
ChEMBL	Displacement of [3H]DTG from sigma2 receptor in rat liver membranes after 60 mins by liquid scintillation counting method	B	7.36	pKi	43.9	nM	Ki	J Med Chem (2018) 61: 6937-6943 [PMID:29969030]
ChEMBL	Displacement of [125I]-RHM-4 from sigma 2 receptor in rat liver membranes after 120 mins by microbeta scintillation counting method	B	7.45	pKi	35.22	nM	Ki	Eur J Med Chem (2021) 209: 112906-112906 [PMID:33049607]
ChEMBL	Displacement of (+)-[3H]DTG from sigma 2 receptor in SPRD rat liver membrane incubated for 2 hrs by liquid scintillation counting method	B	7.69	pKi	20.5	nM	Ki	RSC Med Chem (2021) 12: 1000-1004 [PMID:34223165]
sigma non-opioid intracellular receptor 1/Sigma opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL287] [GtoPdb: 2552] [UniProtKB: Q99720]
ChEMBL	Displacement of [3H](+)-Pentazocine from sigma 1 receptor in human RPMI8226 cell membranes	B	7.4	pKi	40	nM	Ki	J Med Chem (2016) 59: 5505-5519 [PMID:27156565]
ChEMBL	Displacement of [3H]-(+)-pentazocine from sigma-1 receptor in human RPMI8226 cell membranes after 120 mins by scintillation counting analysis	B	7.4	pKi	40	nM	Ki	J Med Chem (2014) 57: 2884-2894 [PMID:24617836]
ChEMBL	Inhibitory constant against sigma receptor type 2 using 3 nM [3H]ditolylguanidine	B	7.8	pKi	16	nM	Ki	J Med Chem (2005) 48: 266-273 [PMID:15634021]
ChEMBL	Displacement of [3H](+)-pentazocine from human sigma 1 receptor in human Jurkat cell membranes incubated for 2 hrs by liquid scintillation counting	B	7.92	pKi	11.9	nM	Ki	Eur J Med Chem (2015) 89: 198-206 [PMID:25462240]
ChEMBL	Displacement of [3H](+)Pentazocine from sigma 1 receptor in human Jurkat cells after 120 mins by liquid scintillation counting analysis	B	7.92	pKi	11.9	nM	Ki	Eur J Med Chem (2015) 92: 575-582 [PMID:25602932]
ChEMBL	The compound was tested for its binding affinity towards Sigma opioid receptor in guinea pig brain membranes	B	7.98	pKi	10.4	nM	Ki	J Med Chem (1991) 34: 3360-3365 [PMID:1662725]
ChEMBL	Displacement of [3H]Haloperidol from sigma 1 receptor in human jurkat cells after 4 hrs	B	8.06	pKi	8.8	nM	Ki	Bioorg Med Chem Lett (2013) 23: 1834-1838 [PMID:23403082]
ChEMBL	Displacement of [3H](+)-pentazocine from sigma1 receptor in human Jurkat cell membrane	B	8.11	pKi	7.76	nM	Ki	J Med Chem (2010) 53: 1261-1269 [PMID:20067271]
ChEMBL	Displacement of [3H]-(+)-pentazocine from recombinant human sigma1 receptor expressed in HEK293 cell membranes after 120 mins by microbeta scintillation counting method	B	8.15	pKi	7	nM	Ki	Bioorg Med Chem (2019) 27: 1824-1835 [PMID:30904383]
ChEMBL	Binding affinity to sigma-1 receptor (unknown origin)	B	8.19	pKi	6.4	nM	Ki	J Med Chem (2020) 63: 15187-15217 [PMID:33111525]
ChEMBL	Binding affinity to sigma-1 receptor (unknown origin) by radioligand displacement assay	B	8.2	pKi	6.3	nM	Ki	Bioorg Med Chem Lett (2016) 26: 889-893 [PMID:26750254]
ChEMBL	Binding affinity for Sigma opioid receptor type 2 in guinea pig brain homogenate with 4 nM [3H]-(+)-DTG	B	8.22	pKi	6	nM	Ki	Bioorg Med Chem Lett (1994) 4: 2185-2188
ChEMBL	Displacement of (+)-[3H]pentazocine from human sigma1 receptor expressed in HEK293 cell membranes after 60 mins by liquid scintillation counting method	B	8.23	pKi	5.9	nM	Ki	J Med Chem (2018) 61: 6937-6943 [PMID:29969030]
ChEMBL	DRUGMATRIX: Sigma1 radioligand binding (ligand: [3H] Haloperidol)	B	8.25	pKi	5.67	nM	Ki	DrugMatrix in vitro pharmacology data
ChEMBL	Inhibition of [3H]DTG binding to Sigma opioid receptor	B	8.3	pKi	5	nM	Ki	J Med Chem (1991) 34: 1855-1859 [PMID:1648139]
ChEMBL	Binding affinity against sigma receptor of MCF cells	B	8.34	pKi	4.6	nM	Ki	J Med Chem (1994) 37: 1737-1739 [PMID:8021913]
ChEMBL	Inhibitory activity against sigma receptor isolated from guinea pig brain cortex membrane using [3H]DTG as radioligand	B	8.38	pKi	4.2	nM	Ki	J Med Chem (1996) 39: 176-182 [PMID:8568804]
ChEMBL	Binding affinity was evaluated against sigma-1 binding site in guinea pig, using [3H]- -(+)- Pentazocine	B	8.43	pKi	3.7	nM	Ki	J Med Chem (1993) 36: 566-571 [PMID:8496936]
ChEMBL	Compound was evaluated for its in vitro competition binding studies using sigma-ligand (0.05-10000 nM) - [3H](+)-pentazocine (sigma1 receptor) in guinea pig brain membranes	B	8.43	pKi	3.7	nM	Ki	J Med Chem (1998) 41: 2445-2450 [PMID:9651150]
ChEMBL	Ability to displace [3H](+)-pentazocine at sigma receptor in guinea pig brain membrane was determined	B	8.43	pKi	3.7	nM	Ki	J Med Chem (1993) 36: 2311-2320 [PMID:8360875]
ChEMBL	Binding affinity towards sigma 1 receptor was determined in guinea pig brain membrane using [3H](+)-pentazocine as radioligand	B	8.43	pKi	3.7	nM	Ki	J Med Chem (1994) 37: 314-321 [PMID:8295220]
ChEMBL	Binding affinity for sigma receptor using [3H](+)-pentazocine in guinea pig brain homogenates	B	8.43	pKi	3.7	nM	Ki	J Med Chem (1992) 35: 4334-4343 [PMID:1447735]
ChEMBL	Displacement of [3H]pentazocine from human sigma 1 receptor expressed in HEK293 cell membrane incubated for 2 hrs by liquid scintillation counting method	B	8.45	pKi	3.53	nM	Ki	RSC Med Chem (2021) 12: 1000-1004 [PMID:34223165]
ChEMBL	Compound was tested for its binding affinity towards sigma 1 receptor using [3H](+)-pentazocine from guinea pig brain	B	8.49	pKi	3.2	nM	Ki	J Med Chem (1998) 41: 1557-1560 [PMID:9572880]
ChEMBL	Binding affinity for sigma 1 opioid receptor, measured on guinea pig brain membranes using [3H]- (+)-pentazocine as radioligand	B	8.6	pKi	2.53	nM	Ki	J Med Chem (2001) 44: 4404-4415 [PMID:11728186]
ChEMBL	Compound tested for binding affinity towards sigma 1 receptor in quinea pig brain membranes using [3H](+)-pentazocine as the radioligand.	B	8.6	pKi	2.53	nM	Ki	J Med Chem (1998) 41: 2361-2370 [PMID:9632369]
ChEMBL	Binding affinity to human sigma 1 receptor	B	8.6	pKi	2.5	nM	Ki	Bioorg Med Chem (2022) 73: 117032-117032 [PMID:36202063]
ChEMBL	Binding affinity to sigma 1 receptor (unknown origin) assessed as inhibition constant by radioligand binding assay	B	8.6	pKi	2.5	nM	Ki	Bioorg Med Chem Lett (2022) 72: 128860-128860 [PMID:35724925]
ChEMBL	Displacement of [3H]-Pentazocine from sigma 1 receptor (unknown origin) expressed in HEK293T cell membranes	B	8.61	pKi	2.46	nM	Ki	Bioorg Med Chem (2019) 27: 2629-2636 [PMID:30987780]
ChEMBL	Displacement of [3H]-Pentazocine from sigma 1 receptor (unknown origin) expressed in HEK293T cell membranes	B	8.61	pKi	2.46	nM	Ki	Bioorg Med Chem (2019) 27: 2629-2636 [PMID:30987780]
ChEMBL	Displacement of [3H]-pentazocine from sigma-1 receptor in human Jurkat cell membrane incubated for 2 hr by liquid scintillation counting method	B	8.64	pKi	2.3	nM	Ki	J Med Chem (2021) 64: 890-904 [PMID:33372782]
ChEMBL	Ability to displace [3H](+)-pentazocine from Sigma opioid receptor type 1 of guinea pig brain	B	8.66	pKi	2.2	nM	Ki	J Med Chem (2002) 45: 4923-4930 [PMID:12383018]
ChEMBL	Inhibitory constant against sigma receptor type 1 using 3 nM [3H]pentazocine	B	8.66	pKi	2.2	nM	Ki	J Med Chem (2005) 48: 266-273 [PMID:15634021]
ChEMBL	Sigma opioid receptor type 1 affinity in guinea pig brain by employing [3H](+)-pentazocine as radioligand.	B	8.66	pKi	2.2	nM	Ki	J Med Chem (2002) 45: 438-448 [PMID:11784148]
ChEMBL	Displacement of [3H]-(+)-pentazocine from human sigma1 receptor transfected in HEK293 cells after 120 mins by liquid scintillation counting analysis	B	8.68	pKi	2.1	nM	Ki	J Med Chem (2013) 56: 3656-3665 [PMID:23560650]
ChEMBL	Displacement of [3H](+)pentazocine from human sigma 1 receptor transfected in HEK293 cell membranes after 120 mins by scintillation counter	B	8.68	pKi	2.1	nM	Ki	J Med Chem (2012) 55: 8211-8224 [PMID:22784008]
ChEMBL	Displacement of [3H]-(+)-pentazocine from human sigma1 receptor expressed in HEK293 cell membranes incubated for 120 mins by liquid scintillation counting method	B	8.7	pKi	2	nM	Ki	J Med Chem (2020) 63: 14979-14988 [PMID:33237785]
ChEMBL	Displacement of [3H]-(+)-pentazocine from human sigma-1 receptor expressed in HEK293 membranes incubated for 120 mins by liquid scintillation counting method	B	8.7	pKi	2	nM	Ki	J Med Chem (2020) 63: 2434-2454 [PMID:31743642]
ChEMBL	Inhibition of sigma 1 receptor	B	8.72	pKi	1.9	nM	Ki	J Med Chem (2011) 54: 2529-2591 [PMID:21413808]
ChEMBL	Inhibition of [3H]- pentazocine binding against alpha-1 from guinea pig brain	B	8.74	pKi	1.8	nM	Ki	J Med Chem (1999) 42: 5181-5187 [PMID:10602703]
ChEMBL	Displacement of [3H](+)Pentazocine from sigma 1 receptor (unknown origin)	B	8.78	pKi	1.66	nM	Ki	Bioorg Med Chem Lett (2014) 24: 576-579 [PMID:24365159]
ChEMBL	Displacement of [3H]-(+)-pentazocine from sigma-1 receptor in human Jurkat cell membranes after 2 hrs by liquid scintillation counting method	B	8.8	pKi	1.6	nM	Ki	Eur J Med Chem (2019) 162: 234-248 [PMID:30447434]
ChEMBL	Inhibition of [3H]pentazocine binding to sigma-1 sites in guinea pig brain membranes	B	8.8	pKi	1.6	nM	Ki	J Med Chem (1998) 41: 1574-1580 [PMID:9572883]
ChEMBL	Binding affinity for sigma-1 receptor measured on guinea pig brain membranes using [3H](+)-pentazocine as radioligand	B	8.82	pKi	1.5	nM	Ki	J Med Chem (2001) 44: 1815-1826 [PMID:11356115]
ChEMBL	Binding affinity measured at the sigma receptor by the inhibition of [3H]-3-PPP binding to guinea pig cerebellum using unlabeled 3-PPP for nonspecific binding.	B	8.82	pKi	1.5	nM	Ki	J Med Chem (1998) 41: 5402-5409 [PMID:9876110]
ChEMBL	Displacement of [3H](+)Pentazocine from sigma 1 receptor (unknown origin)	B	8.92	pKi	1.2	nM	Ki	Bioorg Med Chem Lett (2014) 24: 576-579 [PMID:24365159]
ChEMBL	Displacement of [3H](+)-pentazocine from human sigma1 receptor by PDSP assay	B	8.96	pKi	1.1	nM	Ki	Bioorg Med Chem (2016) 24: 2060-2071 [PMID:27032890]
ChEMBL	The compound was evaluated for affinity at sigma-1 site by inhibition of [3H](+)-pentazocine (PENT) binding in guinea pig brain.	B	9.22	pKi	0.6	nM	Ki	J Med Chem (1994) 37: 1964-1970 [PMID:8027978]
ChEMBL	Binding affinity for Sigma opioid receptor type 1 in guinea pig brain homogenate with 0.5 nM [3H](+)-PENT	B	9.22	pKi	0.6	nM	Ki	Bioorg Med Chem Lett (1994) 4: 2185-2188
ChEMBL	Inhibition of [3H]pentazocine binding to Sigma opioid receptor type 1	B	9.36	pKi	0.44	nM	Ki	Bioorg Med Chem Lett (1997) 7: 2303-2306
ChEMBL	Tested for [3H](+)-pentazocine binding to sigma-1 receptor in guinea pig brain membrane	B	9.48	pKi	0.33	nM	Ki	J Med Chem (1993) 36: 3929-3936 [PMID:7902870]
ChEMBL	Displacement of [3H]-(+)-pentazocine from sigma1 in human MDA-MB-468 cell membranes	B	9.68	pKi	0.21	nM	Ki	Bioorg Med Chem Lett (2017) 27: 2216-2220 [PMID:28385503]
ChEMBL	Affinity for sigma receptor type 1 of guinea pig using [3H]ifenprodil or (+)-[3H]pentazocine radioligand	B	9.7	pKi	0.2	nM	Ki	J Med Chem (2005) 48: 4754-4764 [PMID:16033255]
ChEMBL	Displacement of [3H](+)-pentazocine from sigma 1 opioid receptor in human Jurkat cells by scintillation counting	B	6.64	pIC50	230	nM	IC50	Eur J Med Chem (2010) 45: 256-263 [PMID:19875205]
ChEMBL	The compound was tested for affinity towards sigma-3 receptor	B	6.67	pIC50	213.8	nM	IC50	J Med Chem (1994) 37: 4109-4117 [PMID:7990111]
ChEMBL	Displacement of [3H]Haloperidol from sigma 1 receptor in human jurkat cells after 4 hrs	B	7.68	pIC50	21	nM	IC50	Bioorg Med Chem Lett (2013) 23: 1834-1838 [PMID:23403082]
ChEMBL	Inhibition of specific binding of [3H]3-PPP to sigma binding site in Guinea pig brain membranes	B	7.77	pIC50	17	nM	IC50	J Med Chem (1992) 35: 4683-4689 [PMID:1469697]
ChEMBL	DRUGMATRIX: Sigma1 radioligand binding (ligand: [3H] Haloperidol)	B	7.89	pIC50	13	nM	IC50	DrugMatrix in vitro pharmacology data
ChEMBL	Inhibition of specific binding of [125I]-PIPAG to sigma binding site in Guinea pig brain membranes	B	8.1	pIC50	8	nM	IC50	J Med Chem (1992) 35: 4683-4689 [PMID:1469697]
ChEMBL	In vitro binding affinity measured on sigma opioid receptor using [3H]DTG as radioligand	B	8.25	pIC50	5.64	nM	IC50	J Med Chem (1995) 38: 942-949 [PMID:7699710]
ChEMBL	Displacement of [3H]DTG from sigma opioid receptor of homogenized guinea pig whole brain	B	8.3	pIC50	5	nM	IC50	J Med Chem (1991) 34: 1867-1870 [PMID:1648140]
ChEMBL	Inhibition of specific binding of [3H]DTG to sigma binding site in Guinea pig brain membranes	B	8.3	pIC50	5	nM	IC50	J Med Chem (1992) 35: 4683-4689 [PMID:1469697]
ChEMBL	Inhibition of specific binding of [3H]NANM of sigma binding site in Guinea pig brain membranes	B	8.4	pIC50	4	nM	IC50	J Med Chem (1992) 35: 4683-4689 [PMID:1469697]
ChEMBL	Inhibitory activity against opioid receptor sigma 1 in guinea pig cerebral cortex using [3H](+)-pentazocine as radio ligand at pH 7.5 for 150 min at 22 degree C	B	8.68	pIC50	2.1	nM	IC50	Bioorg Med Chem Lett (2005) 15: 4828-4832 [PMID:16140009]
ChEMBL	Inhibitory concentration against opioid receptor sigma 1 of guinea pig cerebral cortex using [3H](+)-pentazocine upon incubation for 150 minutes at 22 degree C	B	8.68	pIC50	2.1	nM	IC50	Bioorg Med Chem Lett (2005) 15: 4833-4837 [PMID:16140011]
sigma non-opioid intracellular receptor 1/Sigma opioid receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3602] [GtoPdb: 2552] [UniProtKB: Q9R0C9]
ChEMBL	Binding affinity was measured on Sigma receptor type 2 with rat liver membranes and [3H]- DTG as ligand.	B	7.33	pKi	46.5	nM	Ki	J Med Chem (2000) 43: 3913-3922 [PMID:11052796]
ChEMBL	Binding affinity of compound towards sigma receptor using [3H]DTG (4 nM) ligand in hippocampus rat was determined	B	7.42	pKi	38	nM	Ki	J Med Chem (1997) 40: 952-960 [PMID:9083484]
ChEMBL	Ability to displace [3H]ditolylguanidine in the presence of 100 nM (+)-pentazocine from Sigma opioid receptor type 2 of rat liver	B	7.47	pKi	34.2	nM	Ki	J Med Chem (2002) 45: 4923-4930 [PMID:12383018]
ChEMBL	Sigma opioid receptor type 2 affinity in rat liver by employing [3H]ditolylguanidine as radioligand	B	7.47	pKi	34.2	nM	Ki	J Med Chem (2002) 45: 438-448 [PMID:11784148]
ChEMBL	Displacement of (+)-[3H]pentazocine from sigma-1 receptor in Sprague-Dawley rat cerebral membrane incubated for 90 mins by liquid scintillation counter analysis	B	7.86	pKi	13.9	nM	Ki	RSC Med Chem (2022) 13: 986-997 [PMID:36092143]
ChEMBL	Inhibitory activity against Opioid receptor sigma 1 isolated from whole rat membranes using [3H](+)-pentazocine as radioligand	B	8	pKi	10	nM	Ki	J Med Chem (1996) 39: 176-182 [PMID:8568804]
ChEMBL	Displacement of [3H]pentazocine from sigma 1 receptor in rat brain membrane after 2.5 hrs by microbeta scintillation counting analysis	B	8.15	pKi	7	nM	Ki	ACS Med Chem Lett (2012) 3: 1054-1058 [PMID:23641311]
ChEMBL	Displacement of [3H](+)-pentazocine from sigma 1 receptor in rat liver membrane	B	8.24	pKi	5.7	nM	Ki	Eur J Med Chem (2009) 44: 124-130 [PMID:18440098]
ChEMBL	Displacement of [3H](+)-pentazocine from sigma1 receptor in rat liver membrane by liquid scintillation counting	B	8.24	pKi	5.7	nM	Ki	J Med Chem (2009) 52: 5380-5393 [PMID:19673530]
ChEMBL	Displacement of [3H]-pentazocine from sigma 1 opioid receptor in rat liver homogenate by liquid scintillation counting	B	8.24	pKi	5.7	nM	Ki	ACS Med Chem Lett (2011) 2: 834-839 [PMID:24900272]
ChEMBL	Displacement of (+)-[3H]pentazocine from sigma1 receptor in rat brain membranes after 60 mins by liquid scintillation counting method	B	8.27	pKi	5.39	nM	Ki	J Med Chem (2018) 61: 6937-6943 [PMID:29969030]
ChEMBL	Displacement of (+)-[3H]pentazocine from rat brain sigma1 receptor by competitive binding assay	B	8.31	pKi	4.95	nM	Ki	J Med Chem (2013) 56: 3478-3491 [PMID:23566245]
ChEMBL	Displacement of (+)-[3H]pentazocine from sigma1 receptor in rat brain membranes	B	8.31	pKi	4.95	nM	Ki	Bioorg Med Chem (2013) 21: 215-222 [PMID:23199475]
ChEMBL	Displacement of (+)-[3H]pentazocine from sigma1 receptor in Sprague-Dawley rat cerebral membrane after 90 mins by liquid scintillation counting	B	8.46	pKi	3.5	nM	Ki	Bioorg Med Chem (2012) 20: 4936-4941 [PMID:22831799]
ChEMBL	Displacement of [3H](+)-pentazocine from Sigma1 receptor in rat brain homogenate	B	8.47	pKi	3.35	nM	Ki	J Med Chem (2012) 55: 8272-8282 [PMID:22853801]
ChEMBL	Displacement of (-)-[3H]pentazocine from sigma 1 receptor in rat brain membrane after 120 mins	B	8.47	pKi	3.35	nM	Ki	Eur J Med Chem (2011) 46: 5154-5161 [PMID:21899931]
ChEMBL	Displacement of [3H](+)-pentazocine from opioid sigma1 receptor in rat brain homogenate	B	8.47	pKi	3.35	nM	Ki	J Med Chem (2008) 51: 1482-1486 [PMID:18278854]
ChEMBL	Displacement of [3H](+)-pentazocine from sigma1 receptor in rat brain membranes after 120 mins by radioligand binding assay	B	8.47	pKi	3.35	nM	Ki	Eur J Med Chem (2019) 165: 250-257 [PMID:30685525]
ChEMBL	Displacement of [3H](+)-pentazocine from Sigma1 receptor in rat liver homogenate	B	8.48	pKi	3.3	nM	Ki	J Med Chem (2012) 55: 8272-8282 [PMID:22853801]
ChEMBL	Binding affinity was measured on Sigma receptor type 1 with guinea pig membranes and [3H]- pentazocine as ligand.	B	8.53	pKi	2.95	nM	Ki	J Med Chem (2000) 43: 3913-3922 [PMID:11052796]
ChEMBL	Displacement of [3H]-(+)-pentazocine from rat liver homogenate S1R incubated for 120 mins by liquid scintillation counting method	B	8.59	pKi	2.6	nM	Ki	J Med Chem (2023) 66: 11447-11463 [PMID:37535861]
ChEMBL	Displacement of [3H](+)-pentazocine from rat liver homogenates sigma 1 receptor assessed as inhibition constant by radioligand binding assay	B	8.59	pKi	2.6	nM	Ki	RSC Med Chem (2023) 14: 1734-1742 [PMID:37731701]
ChEMBL	Displacement of [3H](+)-pentazocine from sigma 1 receptor in rat brain membrane after 2.5 hrs by scintillation counting	B	8.77	pKi	1.7	nM	Ki	Bioorg Med Chem (2012) 20: 6856-6861 [PMID:23084435]
ChEMBL	Displacement of [3H](+)-pentazocine from sigma 1 receptor in rat brain homogenate	B	9.05	pKi	0.9	nM	Ki	Bioorg Med Chem Lett (2011) 21: 3622-3626 [PMID:21555222]
ChEMBL	Binding affinity towards Sigma receptor type 2 in whole rat brain homogenates except cerebellum using radioligand ([3H]DTG) binding assay.	B	7.77	pIC50	17	nM	IC50	J Med Chem (1995) 38: 2009-2017 [PMID:7783132]
ChEMBL	Binding effinity for sigma receptor using 2 nM of [3H]-DTG as radioligand, in membranes from brain minus cerebellum	B	7.77	pIC50	17	nM	IC50	J Med Chem (1993) 36: 3188-3196 [PMID:8230107]
ChEMBL	Inhibitory activity against Sigma opioid receptor	B	8.52	pIC50	3	nM	IC50	J Med Chem (1991) 34: 1855-1859 [PMID:1648139]
ChEMBL	Compound was tested in vitro for its ability to displace radioligand (+)-[3H]-3-PPP from rat cortical sigma receptor	B	8.85	pIC50	1.4	nM	IC50	J Med Chem (1992) 35: 4516-4525 [PMID:1361578]
ChEMBL	Compound was evaluated for the binding affinity towards Sigma receptor type 1 using radioligand ([3H]-(+)- Pentazocine) binding assay.	B	9.19	pIC50	0.65	nM	IC50	J Med Chem (1995) 38: 2009-2017 [PMID:7783132]
ChEMBL	Binding affinity towards sigma receptor binding site 1 using [3H](+)-pentazocine	B	9.19	pIC50	0.65	nM	IC50	J Med Chem (1995) 38: 1998-2008 [PMID:7783131]
Transporter in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6184] [UniProtKB: Q63380]
ChEMBL	Binding affinity to rat NET	B	5.26	pKi	5500	nM	Ki	Bioorg Med Chem (2008) 16: 7291-7301 [PMID:18595716]
Urokinase plasminogen activator surface receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4883] [UniProtKB: Q03405]
ChEMBL	Binding affinity to uPAR H47C/N259C (unknown origin) mutant assessed as equilibrium dissociation constant by surface plasmon resonance (SPR) analysis relative to control	B	4.39	pKd	41200	nM	Kd	J Med Chem (2023) 66: 5415-5426 [PMID:36854648]
Vesicular acetylcholine transporter in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2125] [GtoPdb: 1013] [UniProtKB: Q62666]
ChEMBL	Displacement of (-)-[3H]vesamicol from rat VAChT expressed in rat PC12 cell membranes after 60 mins by liquid scintillation counting method	B	6.41	pKi	391	nM	Ki	J Med Chem (2018) 61: 6937-6943 [PMID:29969030]
Zinc finger protein 664 in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105757] [UniProtKB: Q60493]
ChEMBL	Displacement of [3H]-(+)-pentazocine from sigma1-type opioid receptor in guinea pig cortex membranes after 120 mins by solid scintillation counting	B	8.18	pKi	6.6	nM	Ki	J Med Chem (2017) 60: 2526-2551 [PMID:28218838]
5-HT1D receptor in Human [GtoPdb: 3] [UniProtKB: P28221]
GtoPdb	-	-	6.6	pKi	-	-	-	Psychopharmacology (Berl.) (1996) 124: 57-73 [PMID:8935801]
Kir3.2 in Mouse [GtoPdb: 435] [UniProtKB: P48542]
GtoPdb	-	-	4.1	pEC50	-	-	-	Br J Pharmacol (2000) 129: 1716-22 [PMID:10780978]
Kv10.1 in Human [GtoPdb: 570] [UniProtKB: O95259]
GtoPdb	-	-	6.2	pIC50	-	-	-	Br J Pharmacol (2003) 138: 161-71 [PMID:12522086]

ChEMBL data shown on this page come from version 35:

Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]