ChEMBL ligand: CHEMBL42 (Clozapine, Clozapine (caraco), Clozapine (clozaril), Clozapine (fazaclo), Clozapine (ivax), Clozapine (mylan), Clozapine resolution mixture, Clozapine (teva), Clozapine (udl), Clozapine (versacloz), Clozaril, Fazaclo, Fazaclo odt, HF 1854, HF-1854, Leponex, NSC-757429, Versacloz, Zaponex)
aldehyde oxidase 1/Aldehyde oxidase in Human [ChEMBL: CHEMBL3257] [GtoPdb: 3186] [UniProtKB: Q06278] 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 Human [ChEMBL: CHEMBL232] [GtoPdb: 23] [UniProtKB: P35368] 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] α2A-adrenoceptor/Alpha-2a adrenergic receptor in Rat [ChEMBL: CHEMBL327] [GtoPdb: 25] [UniProtKB: P22909] 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!
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!
Calmodulin in Human [ChEMBL: CHEMBL6093] [UniProtKB: P0DP23] Calmodulin in Bovine [ChEMBL: CHEMBL6092] [UniProtKB: P62157] 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] Dopamine D1 receptor in Bovine [ChEMBL: CHEMBL2967] [UniProtKB: Q95136] 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 Mouse [ChEMBL: CHEMBL3427] [GtoPdb: 215] [UniProtKB: P61168] 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!
GABAA receptor π subunit/GABAA receptor β1 subunit/GABAA receptor δ subunit/GABAA receptor γ2 subunit/GABAA receptor α5 subunit/GABAA receptor α3 subunit/GABAA receptor γ1 subunit/GABAA receptor α2 subunit/GABAA receptor α4 subunit/GABAA receptor γ3 subunit/GABAA receptor α6 subunit/GABAA receptor α1 subunit/GABAA receptor β3 subunit/GABAA receptor β2 subunit/GABAA receptor ε subunit/GABA-A receptor; anion channel in Rat [ChEMBL: CHEMBL1907607] [GtoPdb: 419, 410, 416, 414, 408, 406, 413, 405, 407, 415, 409, 404, 412, 411, 417] [UniProtKB: O09028, P15431, P18506, P18508, P19969, P20236, P23574, P23576, P28471, P28473, P30191, P62813, P63079, P63138, Q91ZM7, Q9ES14] 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!
H3 receptor/Histamine H3 receptor in Human [ChEMBL: CHEMBL264] [GtoPdb: 264] [UniProtKB: Q9Y5N1] H3 receptor in Rat [GtoPdb: 264] [UniProtKB: Q9QYN8] There should be some charts here, you may need to enable JavaScript!
H4 receptor/Histamine H4 receptor in Human [ChEMBL: CHEMBL3759] [GtoPdb: 265] [UniProtKB: Q9H3N8] H4 receptor in Mouse [GtoPdb: 265] [UniProtKB: Q91ZY2] H4 receptor in Rat [GtoPdb: 265] [UniProtKB: Q91ZY1] There should be some charts here, you may need to enable JavaScript!
Histone H1.0 in Human [ChEMBL: CHEMBL3707465] [UniProtKB: P07305] 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 Human [ChEMBL: CHEMBL211] [GtoPdb: 14] [UniProtKB: P08172] 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!
M3 receptor/Muscarinic acetylcholine receptor M3 in Human [ChEMBL: CHEMBL245] [GtoPdb: 15] [UniProtKB: P20309] There should be some charts here, you may need to enable JavaScript!
M4 receptor/Muscarinic acetylcholine receptor M4 in Human [ChEMBL: CHEMBL1821] [GtoPdb: 16] [UniProtKB: P08173] 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!
NET/Norepinephrine transporter in Human [ChEMBL: CHEMBL222] [GtoPdb: 926] [UniProtKB: P23975] Norepinephrine transporter in Rat [ChEMBL: CHEMBL304] [UniProtKB: Q9WTR4] 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!
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 Mouse [ChEMBL: CHEMBL3737] [GtoPdb: 1] [UniProtKB: Q64264] 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 Human [ChEMBL: CHEMBL1898] [GtoPdb: 2] [UniProtKB: P28222] 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-HT1D receptor/Serotonin 1d (5-HT1d) receptor in Human [ChEMBL: CHEMBL1983] [GtoPdb: 3] [UniProtKB: P28221] There should be some charts here, you may need to enable JavaScript!
5-ht1e receptor/Serotonin 1e (5-HT1e) receptor in Human [ChEMBL: CHEMBL2182] [GtoPdb: 4] [UniProtKB: P28566] 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 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] 5-HT2B receptor/Serotonin 2b (5-HT2b) receptor in Rat [ChEMBL: CHEMBL323] [GtoPdb: 7] [UniProtKB: P30994] 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-HT3E/5-HT3B/5-HT3A/5-HT3D/5-HT3C/Serotonin 3 (5-HT3) receptor in Human [ChEMBL: CHEMBL2094132] [GtoPdb: 377, 374, 373, 376, 375] [UniProtKB: A5X5Y0, O95264, P46098, Q70Z44, Q8WXA8] 5-HT3A/5-HT3B/Serotonin 3 (5-HT3) receptor in Rat [ChEMBL: CHEMBL2094116] [GtoPdb: 373, 374] [UniProtKB: P35563, Q9JJ16] There should be some charts here, you may need to enable JavaScript!
5-HT3A/Serotonin 3a (5-HT3a) receptor in Human [ChEMBL: CHEMBL1899] [GtoPdb: 373] [UniProtKB: P46098] 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-HT5A receptor/Serotonin 5a (5-HT5a) receptor in Human [ChEMBL: CHEMBL3426] [GtoPdb: 10] [UniProtKB: P47898] 5-HT5A receptor in Mouse [GtoPdb: 10] [UniProtKB: P30966] 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] 5-HT6 receptor in Rat [GtoPdb: 11] [UniProtKB: P31388] 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 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!
5-HT1F receptor in Human [GtoPdb: 5] [UniProtKB: P30939] 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!

DB	Assay description	Assay Type	Standard value	Standard parameter	Original value	Original units	Original parameter	Reference
aldehyde oxidase 1/Aldehyde oxidase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3257] [GtoPdb: 3186] [UniProtKB: Q06278]
ChEMBL	Inhibition of aldehyde oxidase in human liver cytosolic fraction using methyl-nicotinamide substrate incubated for 120 mins by HPLC analysis	B	4.36	pIC50	43300	nM	IC50	WO-2018198842-A1. Therapeutic agent for nonalcoholic fatty liver disease (null)
α1A-adrenoceptor/Alpha-1a adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL229] [GtoPdb: 22] [UniProtKB: P35348]
ChEMBL	Inhibition of specific [3H]prazosin binding (0.2 nM) to rat brain membranes alpha-1 adrenergic receptor	B	7.43	pKd	37.15	nM	Kd	J Med Chem (1984) 27: 495-503 [PMID:6142954]
ChEMBL	Inhibition of adrenergic alpha1A receptor (unknown origin)	B	7.72	pKi	19	nM	Ki	J Med Chem (2014) 57: 2670-2682 [PMID:24559051]
ChEMBL	Binding Assay: Binding assay using 5-HT2A, Dopamine D2, SERT, αA1, 5-HT2C and H1 Receptors.	B	7.72	pKi	19	nM	Ki	US-8598119-B2. Methods and compositions for sleep disorders and other disorders (2013)
ChEMBL	Binding affinity to adrenergic alpha1A receptor (unknown origin) by PDSP assay	B	8	pKi	10	nM	Ki	Medchemcomm (2012) 3: 580-583
GtoPdb	-	-	8.3	pKi	-	-	-	Jpn J Pharmacol (2001) 86: 189-95 [PMID:11459121]; Pharmacol Res Perspect (2020) 8: e00602 [PMID:32608144]
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	6.8	pIC50	160	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 measured at the Alpha-1A adrenergic receptor by the inhibition of [3H]prazosin binding to rat cortex using unlabeled WB-4101 for nonspecific binding.	B	7.66	pKi	22	nM	Ki	J Med Chem (1998) 41: 5402-5409 [PMID:9876110]
ChEMBL	DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)	B	7.82	pKi	15	nM	Ki	DrugMatrix in vitro pharmacology data
ChEMBL	DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)	B	7.42	pIC50	38	nM	IC50	DrugMatrix in vitro pharmacology data
α1B-adrenoceptor/Alpha-1b adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL232] [GtoPdb: 23] [UniProtKB: P35368]
ChEMBL	Binding affinity to adrenergic alpha1B receptor (unknown origin) by PDSP assay	B	8	pKi	10	nM	Ki	Medchemcomm (2012) 3: 580-583
GtoPdb	-	-	8.2	pKi	-	-	-	Jpn J Pharmacol (2001) 86: 189-95 [PMID:11459121]; Pharmacol Res Perspect (2020) 8: e00602 [PMID:32608144]
α1B-adrenoceptor/Alpha-1b adrenergic receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL315] [GtoPdb: 23] [UniProtKB: P15823]
ChEMBL	Displacement of [3H]-prazosin from alpha1B adrenergic receptor in Wistar rat liver membrane after 45 mins by liquid scintillation counting	B	7.54	pKi	29	nM	Ki	Eur J Med Chem (2013) 62: 214-221 [PMID:23353740]
ChEMBL	Displacement of [3H]-prozosin from alpha1B adrenoreceptor in rat liver membranes after 45 mins by liquid scintillation counting	B	7.6	pKi	25	nM	Ki	Eur J Med Chem (2013) 66: 122-134 [PMID:23792350]
ChEMBL	Inhibition of rat adrenergic alpha1B receptor	B	7.92	pKi	12	nM	Ki	J Med Chem (2014) 57: 2670-2682 [PMID:24559051]
ChEMBL	DRUGMATRIX: Alpha-1B adrenergic receptor radioligand binding (ligand: prazosin)	B	8.44	pKi	3.59	nM	Ki	DrugMatrix in vitro pharmacology data
ChEMBL	DRUGMATRIX: Alpha-1B adrenergic receptor radioligand binding (ligand: prazosin)	B	8.19	pIC50	6.49	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]
GtoPdb	-	-	7.7	pKi	-	-	-	Jpn J Pharmacol (2001) 86: 189-95 [PMID:11459121]
ChEMBL	DRUGMATRIX: Alpha-1D adrenergic receptor radioligand binding (ligand: prazosin)	B	7.77	pKi	17	nM	Ki	DrugMatrix in vitro pharmacology data
ChEMBL	DRUGMATRIX: Alpha-1D adrenergic receptor radioligand binding (ligand: prazosin)	B	7.46	pIC50	35	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	Binding affinity to adrenergic alpha2A receptor (unknown origin) by PDSP assay	B	6	pKi	1000	nM	Ki	Medchemcomm (2012) 3: 580-583
ChEMBL	Displacement of [3H]-MK-912 from human cloned adrenergic alpha2A receptor expressed in insect Sf9 membranes after 60 mins by liquid scintillation counting	B	6.73	pKi	185	nM	Ki	J Med Chem (2012) 55: 1572-1582 [PMID:22268448]
ChEMBL	DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)	B	7.47	pKi	34	nM	Ki	DrugMatrix in vitro pharmacology data
ChEMBL	Inhibition of [3H]rauwolscine binding to Alpha-2A adrenergic receptor	B	7.62	pKi	24	nM	Ki	J Med Chem (2005) 48: 1709-1712 [PMID:15771415]
ChEMBL	DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)	B	7.05	pIC50	90	nM	IC50	DrugMatrix in vitro pharmacology data
α2A-adrenoceptor/Alpha-2a adrenergic receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL327] [GtoPdb: 25] [UniProtKB: P22909]
ChEMBL	Displacement of [3H]-RX821002 from alpha2A adrenergic receptor in Wistar rat cortical membrane after 45 mins by liquid scintillation counting	B	7	pKi	100	nM	Ki	Eur J Med Chem (2013) 62: 214-221 [PMID:23353740]
ChEMBL	Binding affinity measured at the Alpha-2 adrenergic receptor by the inhibition of [3H]clonidine binding to rat cortex using unlabeled NAbitartrate for nonspecific binding.	B	7.72	pKi	19	nM	Ki	J Med Chem (1998) 41: 5402-5409 [PMID:9876110]
α2B-adrenoceptor/Alpha-2b adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1942] [GtoPdb: 26] [UniProtKB: P18089]
ChEMBL	Binding affinity to adrenergic alpha2B receptor (unknown origin) by PDSP assay	B	7	pKi	100	nM	Ki	Medchemcomm (2012) 3: 580-583
ChEMBL	DRUGMATRIX: Alpha-2B adrenergic receptor radioligand binding (ligand: Rauwolscine)	B	7.96	pKi	11	nM	Ki	DrugMatrix in vitro pharmacology data
ChEMBL	DRUGMATRIX: Alpha-2B adrenergic receptor radioligand binding (ligand: Rauwolscine)	B	7.64	pIC50	23	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	Binding affinity to adrenergic alpha2C receptor (unknown origin) by PDSP assay	B	7	pKi	100	nM	Ki	Medchemcomm (2012) 3: 580-583
ChEMBL	Inhibition of [3H]rauwolscine binding to Alpha-2C adrenergic receptor	B	8.54	pKi	2.9	nM	Ki	J Med Chem (2005) 48: 1709-1712 [PMID:15771415]
ChEMBL	DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)	B	8.94	pKi	1.14	nM	Ki	DrugMatrix in vitro pharmacology data
ChEMBL	DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)	B	8.1	pIC50	7.88	nM	IC50	DrugMatrix in vitro pharmacology data
β1-adrenoceptor/Beta-1 adrenergic receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3252] [GtoPdb: 28] [UniProtKB: P18090]
ChEMBL	Binding affinity measured at the Beta-1 adrenergic receptor by the inhibition of [3H]DHA binding to rat cortex using unlabeled isoprenalin for nonspecific binding.	B	4.59	pKi	26000	nM	Ki	J Med Chem (1998) 41: 5402-5409 [PMID:9876110]
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]
Calmodulin in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6093] [UniProtKB: P0DP23]
ChEMBL	Binding affinity to CaM (unknown origin) by equilibrium dialysis method	B	4.7	pIC50	20000	nM	IC50	Eur J Med Chem (2016) 116: 36-45 [PMID:27043269]
Calmodulin in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6092] [UniProtKB: P62157]
ChEMBL	Binding affinity to bovine brain CaM by FTPFACE analysis	B	4.21	pKd	61000	nM	Kd	Eur J Med Chem (2016) 116: 36-45 [PMID:27043269]
D1 receptor/Dopamine D1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2056] [GtoPdb: 214] [UniProtKB: P21728]
ChEMBL	Binding affinity to dopamine D1 receptor (unknown origin) by PDSP assay	B	6	pKi	1000	nM	Ki	Medchemcomm (2012) 3: 580-583
ChEMBL	Binding affinity towards human Dopamine receptor D1	B	6.27	pKi	540	nM	Ki	J Med Chem (2004) 47: 1303-1314 [PMID:14998318]
ChEMBL	Binding affinity to human cloned dopamine D1 receptor	B	6.54	pKi	290	nM	Ki	Bioorg Med Chem (2008) 16: 7291-7301 [PMID:18595716]
ChEMBL	Displacement of [3H]SCH-23390 from human cloned D1 dopamine receptor expressed in HEKT cells incubated for 90 mins by scintillation counting based radioligand binding assay	B	6.72	pKi	189	nM	Ki	Medchemcomm (2015) 6: 1679-1686
ChEMBL	Compound was tested for the Binding affinity against Human cloned Dopamine receptor D1 by Radio ligand ([3H]SCH-23390) binding assay	B	6.74	pKi	180	nM	Ki	J Med Chem (1996) 39: 2764-2772 [PMID:8709107]
ChEMBL	Displacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cells	B	6.88	pKi	132	nM	Ki	Bioorg Med Chem Lett (2006) 16: 4543-4547 [PMID:16809034]
ChEMBL	Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells	B	6.88	pKi	132	nM	Ki	Bioorg Med Chem Lett (2006) 16: 4548-4553 [PMID:16806922]
GtoPdb	-	-	6.9	pKi	-	-	-	Nature (1991) 350: 614-9 [PMID:1826762]
ChEMBL	Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK cells	B	7.05	pKi	89	nM	Ki	Bioorg Med Chem Lett (2009) 19: 538-542 [PMID:19091563]
ChEMBL	Binding affinity against dopamine receptor D1	B	7.28	pKi	53	nM	Ki	J Med Chem (2001) 44: 477-501 [PMID:11170639]
ChEMBL	DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)	B	7.28	pKi	53	nM	Ki	DrugMatrix in vitro pharmacology data
ChEMBL	Antagonist activity at human D1 receptor expressed in CHO cells assessed as inhibition of dopamine-induced calcium accumulation	F	7.36	pKi	44	nM	Ki	Bioorg Med Chem Lett (2021) 40: 127911-127911 [PMID:33691168]
ChEMBL	Binding affinity to human dopamine D1 receptor	B	7.36	pKi	44	nM	Ki	Bioorg Med Chem Lett (2020) 30: 127563-127563 [PMID:32976928]
ChEMBL	Binding affinity against Dopamine D1 receptor	B	7.5	pKi	31.62	nM	Ki	Bioorg Med Chem Lett (2004) 14: 4263-4266 [PMID:15261283]
ChEMBL	Displacement of [3H]SCH23390 from human dopamine D1 receptor	B	7.67	pKi	21.38	nM	Ki	Bioorg Med Chem Lett (2009) 19: 6059-6062 [PMID:19796944]
ChEMBL	Binding affinity to dopamine D1 receptor (unknown origin)	B	8.12	pKi	7.5	nM	Ki	Med Chem Res (2013) 22: 520-530
ChEMBL	DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)	B	6.97	pIC50	107	nM	IC50	DrugMatrix in vitro pharmacology data
Dopamine D1 receptor in Pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5067] [UniProtKB: P50130]
ChEMBL	Displacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membrane	B	6.38	pKi	420	nM	Ki	J Med Chem (2006) 49: 3938-3947 [PMID:16789750]
Dopamine D1 receptor in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2967] [UniProtKB: Q95136]
ChEMBL	Binding affinity against bovine dopamine receptor D1 using radioligand [3H]-SCH- 23390	B	6.38	pKi	420	nM	Ki	J Med Chem (2001) 44: 2691-2694 [PMID:11495580]
ChEMBL	Displacement of [3H]SCH-23390 from Dopamine receptor D1 of bovine striatal membranes	B	6.38	pKi	420	nM	Ki	J Med Chem (2000) 43: 4563-4569 [PMID:11087581]
ChEMBL	Displacement of [3H]SCH-23390 from bovine striatal membrane Dopamine receptor D1	B	6.38	pKi	420	nM	Ki	Bioorg Med Chem Lett (1999) 9: 3143-3146 [PMID:10560741]
ChEMBL	In vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membrane	B	6.38	pKi	420	nM	Ki	Bioorg Med Chem Lett (2000) 10: 2041-2044 [PMID:10987445]
ChEMBL	Ability to displace [3H]SCH-23,390 radioligand from bovine Dopamine receptor D1	B	6.38	pKi	420	nM	Ki	Bioorg Med Chem Lett (2002) 12: 1937-1940 [PMID:12113813]
ChEMBL	Binding affinity was evaluated for the displacement of [3H]-SCH- 23390 against bovine Dopamine receptor D1	B	6.38	pKi	420	nM	Ki	Bioorg Med Chem Lett (1999) 9: 97-102 [PMID:9990464]
ChEMBL	In vitro binding affinity at human cloned dopamine receptor D1 stably expressed in CHO cells by [3H]-SCH- 23390 displacement.	B	6.38	pKi	420	nM	Ki	Bioorg Med Chem Lett (2002) 12: 633-636 [PMID:11844688]
ChEMBL	Ability to displace D1 selective radioligand [3H]-SCH- 23390 in bovine striatal membrane preparations was determined	B	6.38	pKi	420	nM	Ki	Bioorg Med Chem Lett (1999) 9: 1969-1972 [PMID:10450964]
ChEMBL	Displacement of [3H]SCH23390 from bovine dopamine D1 receptor	B	6.38	pKi	420	nM	Ki	Bioorg Med Chem (2009) 17: 4448-4458 [PMID:19481941]
D1 receptor/Dopamine D1 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL265] [GtoPdb: 214] [UniProtKB: P18901]
ChEMBL	Inhibition of [3H]SCH-23390 binding to rat Dopamine receptor D1	B	6.27	pKi	539	nM	Ki	J Med Chem (2005) 48: 1709-1712 [PMID:15771415]
ChEMBL	Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate	B	6.45	pKi	354.81	nM	Ki	J Med Chem (2002) 45: 344-359 [PMID:11784139]
ChEMBL	Binding affinity which represents concentration giving half-maximal inhibition of [3H]SCH-23390 (Dopamine receptor D1) binding to rat tissue homogenate	B	6.45	pKi	353	nM	Ki	J Med Chem (1998) 41: 3763-3772 [PMID:9748351]
ChEMBL	Displacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometry	B	6.45	pKi	353	nM	Ki	J Med Chem (2009) 52: 151-169 [PMID:19072656]
ChEMBL	In vitro binding affinity towards Dopamine receptor D1 in rat tissue homogenate using [3H]-SCH- 23390 as radioligand	B	6.45	pKi	353	nM	Ki	J Med Chem (2004) 47: 143-157 [PMID:14695828]
ChEMBL	Inhibition of [3H]-SCH- 23390 binding to rat dopamine D1 receptor	B	6.45	pKi	353	nM	Ki	J Med Chem (2005) 48: 1705-1708 [PMID:15771414]
ChEMBL	Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate	B	6.46	pKi	350	nM	Ki	J Med Chem (2002) 45: 344-359 [PMID:11784139]
ChEMBL	pKi value for Dopamine receptor D1 binding site	B	6.5	pKi	316.23	nM	Ki	J Med Chem (1998) 41: 3763-3772 [PMID:9748351]
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	6.63	pKi	235	nM	Ki	J Med Chem (1998) 41: 5402-5409 [PMID:9876110]
ChEMBL	Displacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometry	B	6.68	pKi	210	nM	Ki	J Med Chem (2010) 53: 4803-4807 [PMID:20481570]
ChEMBL	Binding affinity of [3H]SCH-23,390 towards Dopamine receptor D1 in cloned mammalian receptor expressed in cultured cells or from rat whole brain.	B	6.77	pKi	170	nM	Ki	J Med Chem (1996) 39: 2435-2437 [PMID:8691438]
ChEMBL	In vitro ability to displace [3H]SCH-23390 binding from Dopamine 1 (D1) receptor in rat striatal membrane.	B	6.77	pKi	169.82	nM	Ki	J Med Chem (1999) 42: 2774-2797 [PMID:10425088]
ChEMBL	In vitro affinity against Dopamine receptor D1	B	6.77	pKi	169.82	nM	Ki	J Med Chem (2000) 43: 4678-4693 [PMID:11101359]
ChEMBL	In vitro binding affinity against Dopamine receptor D1 in rat striatal tissue	B	6.94	pKi	115	nM	Ki	J Med Chem (1993) 36: 2107-2114 [PMID:8101877]
ChEMBL	Binding affinity against dopamine receptor D1	B	6.94	pKi	114.82	nM	Ki	J Med Chem (1994) 37: 519-525 [PMID:7907148]
ChEMBL	Affinity was evaluated as inhibition constant for dopamine receptor D1 using [3H]-SCH- 23390 as radioligand	B	7.37	pKi	43	nM	Ki	J Med Chem (1994) 37: 2686-2696 [PMID:8064797]
ChEMBL	Binding activity against Dopamine receptor D1 in rat brain, using [3H]SCH-23390 as the radioligand	B	6.72	pIC50	192	nM	IC50	J Med Chem (1989) 32: 2261-2268 [PMID:2571728]
ChEMBL	Binding affinity against Dopamine receptor D1 using [3H]-SCN 23390 in rat brain	B	6.72	pIC50	192	nM	IC50	J Med Chem (1990) 33: 809-814 [PMID:1967652]
ChEMBL	Binding affinity towards D1 CNS receptor of rat corpus striatum using [3H]SCH-23390 as radioligand	B	6.89	pIC50	130	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	6.89	pIC50	130	nM	IC50	J Med Chem (1997) 40: 4146-4153 [PMID:9406603]
ChEMBL	Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.	B	6.89	pIC50	130	nM	IC50	J Med Chem (1995) 38: 4380-4392 [PMID:7473566]
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	6.6	pKi	254	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	6.6	pKi	254	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	Binding affinity to dopamine D2 receptor (unknown origin) by PDSP assay	B	6	pKi	1000	nM	Ki	Medchemcomm (2012) 3: 580-583
ChEMBL	In vitro binding affinity towards Dopamine receptor D2L, using [3H]spiroperidol radioligand in Sf9 baculovirus expression.	B	6.06	pKi	876	nM	Ki	J Med Chem (2000) 43: 270-277 [PMID:10649982]
ChEMBL	Displacement of [3H]N-methylspiperone from human cloned D2 dopamine receptor expressed in human fibroblasts incubated for 90 mins by scintillation counting based radioligand binding assay	B	6.37	pKi	431	nM	Ki	Medchemcomm (2015) 6: 1679-1686
ChEMBL	Antagonist activity at human D2 receptor expressed in CHO cells assessed as inhibition of dopamine-induced calcium accumulation	F	6.41	pKi	389	nM	Ki	Bioorg Med Chem Lett (2021) 40: 127911-127911 [PMID:33691168]
ChEMBL	Binding affinity to human dopamine D2 receptor	B	6.41	pKi	389	nM	Ki	Bioorg Med Chem Lett (2020) 30: 127563-127563 [PMID:32976928]
ChEMBL	In vitro binding affinity at human cloned Dopamine receptor D2L expressed in Sf9 cell membranes	B	6.43	pKi	372	nM	Ki	J Med Chem (2002) 45: 5136-5149 [PMID:12408724]
ChEMBL	In vitro binding affinity towards Dopamine receptor D2 in human using [3H]-spiperone as radioligand	B	6.59	pKi	260	nM	Ki	J Med Chem (2004) 47: 143-157 [PMID:14695828]
ChEMBL	Binding affinity on human Dopamine receptor D2 expressed in CHO cells using radioligand [3H]-YM 09151	B	6.6	pKi	254	nM	Ki	J Med Chem (1997) 40: 1-3 [PMID:9016321]
ChEMBL	Potency was measured by the displacement of [3H]spiperone binding to human D2 dopaminergic receptor	B	6.6	pKi	250	nM	Ki	Bioorg Med Chem Lett (1997) 7: 1207-1212
ChEMBL	Displacement of [3H]spiperone from human cloned dopamine D2 receptor	B	6.65	pKi	223.87	nM	Ki	J Med Chem (2008) 51: 6085-6094 [PMID:18783204]
ChEMBL	Displacement of [3H]spiperone human cloned dopamine D2 receptor	B	6.65	pKi	223.87	nM	Ki	Bioorg Med Chem Lett (2007) 17: 4873-4877 [PMID:17588750]
ChEMBL	Displacement of [3H]spiperone from human D2 receptor	B	6.65	pKi	223.87	nM	Ki	Eur J Med Chem (2014) 71: 237-249 [PMID:24316025]
ChEMBL	Displacement of [3H]spiperone from human cloned dopamine D2 receptor	B	6.65	pKi	223.87	nM	Ki	Bioorg Med Chem Lett (2009) 19: 6059-6062 [PMID:19796944]
ChEMBL	Binding affinity towards dopamine receptor D2	B	6.65	pKi	223.87	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	6.65	pKi	223.87	nM	Ki	Medchemcomm (2011) 2: 1194-1200
ChEMBL	Affinity was evaluated as inhibition constant for dopamine D-2 receptor	B	6.66	pKi	220	nM	Ki	J Med Chem (1994) 37: 2686-2696 [PMID:8064797]
ChEMBL	Ability to inhibit the binding of [3H]spiperone to the Dopamine receptor D2L in COS7 cells	B	6.66	pKi	220	nM	Ki	J Med Chem (1995) 38: 708-714 [PMID:7861418]
ChEMBL	Binding affinity to dopamine D2 receptor (unknown origin)	B	6.68	pKi	210	nM	Ki	J Med Chem (2014) 57: 9578-9597 [PMID:25343529]
ChEMBL	Displacement of [3H]methylspiperone from human dopamine D2 receptor expressed in CHO cells	B	6.68	pKi	208	nM	Ki	Bioorg Med Chem Lett (2006) 16: 4543-4547 [PMID:16809034]
ChEMBL	Displacement of [3H]methylspiperone from dopamine D2 receptor expressed in CHO cells	B	6.68	pKi	208	nM	Ki	Bioorg Med Chem Lett (2006) 16: 4548-4553 [PMID:16806922]
ChEMBL	Binding affinity towards human D2 dopamine receptor.	B	6.72	pKi	190	nM	Ki	J Med Chem (2001) 44: 477-501 [PMID:11170639]
ChEMBL	Binding Assay: Binding assay using 5-HT2A, Dopamine D2, SERT, αA1, 5-HT2C and H1 Receptors.	B	6.72	pKi	190	nM	Ki	US-8598119-B2. Methods and compositions for sleep disorders and other disorders (2013)
ChEMBL	In vitro binding affinity against human D2 dopamine receptor in CHO cells by [3H]spiperone displacement.	B	6.81	pKi	155	nM	Ki	Bioorg Med Chem Lett (1998) 8: 725-730 [PMID:9871530]
ChEMBL	Binding affinity towards human Dopamine receptor D2	B	6.82	pKi	150	nM	Ki	J Med Chem (2004) 47: 1303-1314 [PMID:14998318]
ChEMBL	Inhibition of [3H]-spiperone binding to human Dopamine receptor D2	B	6.84	pKi	144	nM	Ki	J Med Chem (2005) 48: 1709-1712 [PMID:15771415]
ChEMBL	Binding affinity towards Dopamine receptor D2 was determined via standard competitive displacement assays using [3H]-YM 09151 as the competitive ligand	B	6.86	pKi	138	nM	Ki	Bioorg Med Chem Lett (2002) 12: 3111-3115 [PMID:12372513]
ChEMBL	Binding affinity towards human dopamine D2 receptor, using [3H]YM-09151 as a radioligand	B	6.86	pKi	138	nM	Ki	Bioorg Med Chem Lett (2002) 12: 3105-3109 [PMID:12372512]
ChEMBL	Cataleptogenic effect against cloned human Dopamine receptor D2 in male Sprague-Dawley rats in a bar test	B	6.87	pKi	134.9	nM	Ki	Bioorg Med Chem Lett (2003) 13: 3779-3782 [PMID:14552778]
ChEMBL	Displacement of [3H]spiperone from human Dopamine receptor D2	B	6.87	pKi	6.87	nM	pKi	J Med Chem (2004) 47: 497-508 [PMID:14736232]
ChEMBL	Inhibition of D2 receptor (unknown origin)	B	6.89	pKi	130	nM	Ki	Bioorg Med Chem (2016) 24: 3464-3471 [PMID:27312422]
ChEMBL	Binding affinity to human cloned dopamine D2 receptor	B	6.89	pKi	130	nM	Ki	Bioorg Med Chem (2008) 16: 7291-7301 [PMID:18595716]
ChEMBL	Binding affinity to human dopamine D2 receptor	B	6.89	pKi	130	nM	Ki	Bioorg Med Chem (2016) 24: 3994-4007 [PMID:27377863]
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	6.89	pKi	130	nM	Ki	Bioorg Med Chem Lett (2003) 13: 3779-3782 [PMID:14552778]
ChEMBL	DRUGMATRIX: Dopamine D2L radioligand binding (ligand: [3H] Spiperone)	B	6.89	pKi	129	nM	Ki	DrugMatrix in vitro pharmacology data
GtoPdb	-	-	6.9	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]; J Pharmacol Exp Ther (1994) 268: 495-502 [PMID:8301592]; J Psychopharmacol (Oxford) (2009) 23: 65-73 [PMID:18308814]
ChEMBL	Displacement of [3H]spiperone from human dopamine D2 receptor short form expressed in CHO cells	B	6.9	pKi	125.89	nM	Ki	J Med Chem (2007) 50: 5103-5108 [PMID:17880057]
ChEMBL	Binding affinity at human Dopamine receptor D2 by [3H]- YM 09151 displacement.	B	6.95	pKi	113	nM	Ki	Bioorg Med Chem Lett (2000) 10: 2119-2122 [PMID:10999484]
ChEMBL	Displacement of [3H]-YM 09151 from D2 receptor	B	6.95	pKi	113	nM	Ki	Bioorg Med Chem Lett (2003) 13: 701-704 [PMID:12639562]
ChEMBL	Displacement of [3H]-spiperone from human dopamine D2L receptor expressed in CHO FlpIn cell membrane measured after 60 mins by topcount scintillation counting	B	6.97	pKi	106	nM	Ki	J Med Chem (2012) 55: 1622-1634 [PMID:22243698]
ChEMBL	Displacement of [3H]-spiperone from human dopamine D2L receptor expressed in CHO FlpIn cell membrane measured after 60 mins by topcount scintillation counting	B	6.99	pKi	102.33	nM	Ki	J Med Chem (2012) 55: 1622-1634 [PMID:22243698]
ChEMBL	Binding affinity to dopamine D2 receptor (unknown origin) by radioligand binding assay	B	7	pKi	>100	nM	Ki	J Med Chem (2013) 56: 8955-8971 [PMID:23919353]
ChEMBL	Binding affinity against cloned human dopamine receptor D2 expressed in Chinese hamster ovary (CHO) K-1 cells by displacement of [3H]spiperone.	B	7.04	pKi	91	nM	Ki	J Med Chem (1997) 40: 4026-4029 [PMID:9406594]
ChEMBL	Ability to displace [3H]spiperone from human cloned Dopamine receptor D2 expressed in CHO K-1 cells in vitro.	B	7.04	pKi	91	nM	Ki	J Med Chem (1997) 40: 2688-2693 [PMID:9276014]
ChEMBL	Displacement of [3H]spiperone from wild-type human dopamine D2S receptor expressed in CHO-K1 cell membrane after 2 hrs by beta counting	B	7.05	pKi	89.13	nM	Ki	Eur J Med Chem (2014) 77: 91-95 [PMID:24631727]
ChEMBL	Displacement of [3H]spiperone from wild-type human dopamine D2S receptor expressed in CHO-K1 cell membrane after 2 hrs by beta counting	B	7.05	pKi	88.65	nM	Ki	Eur J Med Chem (2014) 77: 91-95 [PMID:24631727]
ChEMBL	Displacement of [3H]spiperone from human dopamine D2 receptor expressed in CHO cells	B	7.08	pKi	83	nM	Ki	Bioorg Med Chem Lett (2009) 19: 538-542 [PMID:19091563]
ChEMBL	Binding affinity against Dopamine receptor D2	B	7.11	pKi	77.62	nM	Ki	Bioorg Med Chem Lett (2004) 14: 4263-4266 [PMID:15261283]
ChEMBL	Displacement of [3H]spiperone from human Dopamine receptor D2 expressed in CHO cells	B	7.13	pKi	74	nM	Ki	Bioorg Med Chem Lett (1999) 9: 1285-1290 [PMID:10340615]
ChEMBL	Affinity to displace [3H]spiperone from cloned human Dopamine receptor D2 stably expressed in CHO cell lines	B	7.13	pKi	74	nM	Ki	J Med Chem (1999) 42: 2706-2715 [PMID:10411491]
ChEMBL	Displacement of [3H]spiperone from human Dopamine receptor D2 expressed in CHO cells	B	7.13	pKi	74	nM	Ki	J Med Chem (1996) 39: 1943-1945 [PMID:8642551]
ChEMBL	Binding affinity towards cloned human Dopamine receptor D2 stably expressed in CHO cells was evaluated using [3H]spiperone as radioligand	B	7.13	pKi	74	nM	Ki	J Med Chem (1996) 39: 1941-1942 [PMID:8642550]
ChEMBL	Ability to displace [3H]spiperone from human dopamine receptor D2 stably expressed in CHO cells.	B	7.13	pKi	74	nM	Ki	J Med Chem (1997) 40: 2374-2385 [PMID:9240352]
ChEMBL	Binding affinity to human dopamine D2L receptor expressed in HEK293 cells after 1 hr	B	7.14	pKi	72	nM	Ki	Eur J Med Chem (2012) 56: 348-360 [PMID:22926225]
ChEMBL	Competitive antagonist activity against human dopamine D2 receptor short isoform by R-SAT assay	B	7.14	pKi	72	nM	Ki	US-20040213816-A1. Selective serotonin 2A/2C receptor inverse agonists as therapeutics for neurodegenerative diseases (2004)
ChEMBL	Displacement of [3H]-raclopride from human D2LR expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method	B	7.15	pKi	71	nM	Ki	Eur J Med Chem (2018) 145: 790-804 [PMID:29407591]
ChEMBL	Binding affinity for dopamine receptor D2 determined using [3H]spiperone	B	7.16	pKi	69	nM	Ki	Bioorg Med Chem Lett (2001) 11: 2345-2349 [PMID:11527728]
ChEMBL	Displacement of [3H]spiperone from human dopamine D2S receptor S5.43T/S5.46A mutant expressed in CHO-K1 cell membrane after 2 hrs by beta counting	B	7.24	pKi	58.04	nM	Ki	Eur J Med Chem (2014) 77: 91-95 [PMID:24631727]
ChEMBL	Displacement of [3H]spiperone from human dopamine D2S receptor S5.43T/S5.46A mutant expressed in CHO-K1 cell membrane after 2 hrs by beta counting	B	7.24	pKi	57.54	nM	Ki	Eur J Med Chem (2014) 77: 91-95 [PMID:24631727]
ChEMBL	Displacement of [3H]spiperone from human Dopamine receptor D2L expressed in CHO cells	B	7.39	pKi	41	nM	Ki	J Med Chem (2000) 43: 4563-4569 [PMID:11087581]
ChEMBL	In vitro binding affinity at human cloned dopamine receptor D2 (long) stably expressed in CHO cells by [3H]-Spiperone displacement.	B	7.39	pKi	41	nM	Ki	Bioorg Med Chem Lett (2002) 12: 633-636 [PMID:11844688]
ChEMBL	Displacement of [3H]spiperone from human Dopamine receptor D2L expressed in CHO cells	B	7.39	pKi	41	nM	Ki	Bioorg Med Chem Lett (1999) 9: 3143-3146 [PMID:10560741]
ChEMBL	Ability to displace [3H]SCH-23390 radioligand from cloned human Dopamine receptor D2 in CHO cells	B	7.39	pKi	41	nM	Ki	Bioorg Med Chem Lett (2002) 12: 1937-1940 [PMID:12113813]
ChEMBL	Displacement of [3H]SCH23390 from human cloned dopamine D2 long receptor expressed in CHO cells	B	7.39	pKi	41	nM	Ki	Bioorg Med Chem (2009) 17: 4448-4458 [PMID:19481941]
ChEMBL	Displacement of [3H]spiperone from human dopamine receptor D2(long) in CHO cell membrane	B	7.39	pKi	41	nM	Ki	J Med Chem (2006) 49: 3938-3947 [PMID:16789750]
ChEMBL	Binding affinity against dopamine receptor D2L using radioligand [3H]-spiperone	B	7.39	pKi	41	nM	Ki	J Med Chem (2001) 44: 2691-2694 [PMID:11495580]
ChEMBL	In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D2L stably expressed in CHO cells	B	7.41	pKi	39	nM	Ki	Bioorg Med Chem Lett (2000) 10: 2041-2044 [PMID:10987445]
ChEMBL	Ability to displace [3H]spiperone from the cloned human Dopamine receptor D2L stably expressed in Chinese hamster ovary (CHO) cells was determined.	B	7.41	pKi	39	nM	Ki	Bioorg Med Chem Lett (1999) 9: 1969-1972 [PMID:10450964]
ChEMBL	In vitro binding affinity for Dopamine receptor D2	B	7.5	pKi	31.62	nM	Ki	Bioorg Med Chem Lett (2001) 11: 1313-1316 [PMID:11392544]
ChEMBL	In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D2 short form expressed in CHO cells	B	7.55	pKi	28	nM	Ki	Bioorg Med Chem Lett (2000) 10: 2041-2044 [PMID:10987445]
ChEMBL	Displacement of [3H]spiperone from human Dopamine receptor D2S expressed in CHO cells	B	7.55	pKi	28	nM	Ki	Bioorg Med Chem Lett (1999) 9: 3143-3146 [PMID:10560741]
ChEMBL	Ability to displace [3H]spiperone radioligand from cloned human Dopamine receptor D2 in CHO cells	B	7.55	pKi	28	nM	Ki	Bioorg Med Chem Lett (2002) 12: 1937-1940 [PMID:12113813]
ChEMBL	Competitive binding affinity against human Dopamine receptor D2S by displacing [3H]spiperone from CHO cells	B	7.55	pKi	28	nM	Ki	J Med Chem (2000) 43: 4563-4569 [PMID:11087581]
ChEMBL	In vitro binding affinity at human cloned dopamine receptor D2 (short) stably expressed in CHO cells by [3H]spiperone displacement.	B	7.55	pKi	28	nM	Ki	Bioorg Med Chem Lett (2002) 12: 633-636 [PMID:11844688]
ChEMBL	Ability to displace [3H]spiperone from the cloned human Dopamine receptor D2S stably expressed in Chinese hamster ovary (CHO) cells was determined.	B	7.55	pKi	28	nM	Ki	Bioorg Med Chem Lett (1999) 9: 1969-1972 [PMID:10450964]
ChEMBL	Displacement of [3H]spiroperidol from human cloned dopamine D2 short receptor expressed in CHO cells	B	7.55	pKi	28	nM	Ki	Bioorg Med Chem (2009) 17: 4448-4458 [PMID:19481941]
ChEMBL	Displacement of [3H]spiperone from human dopamine receptor D2(short) in CHO cell membrane	B	7.55	pKi	28	nM	Ki	J Med Chem (2006) 49: 3938-3947 [PMID:16789750]
ChEMBL	Binding affinity against dopamine receptor D2S using radioligand [3H]spiperone	B	7.55	pKi	28	nM	Ki	J Med Chem (2001) 44: 2691-2694 [PMID:11495580]
ChEMBL	Binding affinity to dopamine D2 receptor (unknown origin)	B	8.15	pKi	7.11	nM	Ki	Med Chem Res (2013) 22: 520-530
ChEMBL	DRUGMATRIX: Dopamine D2L radioligand binding (ligand: [3H] Spiperone)	B	6.41	pIC50	387	nM	IC50	DrugMatrix in vitro pharmacology data
ChEMBL	Binding affinity towards human Dopamine receptor D2	B	6.59	pIC50	260	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	6.64	pIC50	230	nM	IC50	J Med Chem (1998) 41: 4903-4909 [PMID:9822559]
ChEMBL	Inhibition of human dopamine D2L receptor expressed in intact CHO FlpIn cells assessed as inhibition of receptor-mediated mediated ERK1/2 phosphorylation by Alpha-Screen plate-based assay	B	6.69	pIC50	206	nM	IC50	J Med Chem (2012) 55: 1622-1634 [PMID:22243698]
ChEMBL	Inhibition of human dopamine D2L receptor expressed in intact CHO FlpIn cells assessed as inhibition of receptor-mediated mediated ERK1/2 phosphorylation by Alpha-Screen plate-based assay	B	6.69	pIC50	204.17	nM	IC50	J Med Chem (2012) 55: 1622-1634 [PMID:22243698]
ChEMBL	Antagonist activity at D2L receptor (unknown origin) expressed in human HTLA cells assessed as inhibition of dopamine-stimulated beta-arrestin2 recruitment measured after 20 to 22 hrs by brightglo-luciferase reporter gene assay	B	6.85	pIC50	140	nM	IC50	J Med Chem (2019) 62: 4755-4771 [PMID:30964661]
ChEMBL	Binding affinity to dopamine receptor D2 cloned from human, using [3H]- YM09151 as competitive ligand	B	6.95	pIC50	113	nM	IC50	J Med Chem (2000) 43: 3923-3932 [PMID:11052797]
ChEMBL	Inhibitory concentration against dopamine receptor D2	B	8.05	pIC50	9	nM	IC50	J Med Chem (2005) 48: 6523-6543 [PMID:16220969]
Dopamine D2 receptor in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3998] [UniProtKB: P20288]
ChEMBL	Binding affinity was evaluated for the displacement of [3H]spiperone against bovine Dopamine receptor D2	B	6.16	pKi	690	nM	Ki	Bioorg Med Chem Lett (1999) 9: 97-102 [PMID:9990464]
ChEMBL	Competition in vitro with the dopamine receptor D2 antagonist [3H]spiperone, for binding sites on calf caudate membranes.	B	6.35	pIC50	450	nM	IC50	J Med Chem (1993) 36: 912-918 [PMID:8096548]
ChEMBL	Inhibitory activity against dDopamine receptor D2 in calf caudate tissue, using [3H]spiperone as the radioligand	B	6.6	pIC50	250	nM	IC50	J Med Chem (1989) 32: 2375-2381 [PMID:2571731]
ChEMBL	Affinity towards Dopamine receptor D2 in membranes from bovine striatum using [3H]raclopride	B	6.85	pIC50	140	nM	IC50	J Med Chem (1998) 41: 2010-2018 [PMID:9622542]
D2 receptor/Dopamine D2 receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3427] [GtoPdb: 215] [UniProtKB: P61168]
ChEMBL	Inhibition of mouse Dopamine receptor D2	B	6.54	pIC50	290	nM	IC50	J Med Chem (1996) 39: 4692-4703 [PMID:8941382]
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	6.1	pKi	790	nM	Ki	J Med Chem (1992) 35: 2712-2715 [PMID:1353116]
GtoPdb	-	-	6.2	pKi	-	-	-	Nature (1990) 347: 146-51 [PMID:1975644]
ChEMBL	Binding affinity to the dopamine receptor D2L in rat brain membranes	B	6.44	pKi	359	nM	Ki	J Med Chem (1999) 42: 3342-3355 [PMID:10464021]
ChEMBL	Displacement of [3H]spiperone from dopamine D2 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometry	B	6.5	pKi	319	nM	Ki	J Med Chem (2010) 53: 4803-4807 [PMID:20481570]
ChEMBL	Compound was measured for the inhibition of [3H]spiperone binding to striatal membrane Dopamine receptor D2	B	6.58	pKi	263.03	nM	Ki	Bioorg Med Chem Lett (1998) 8: 3571-3576 [PMID:9934473]
ChEMBL	In vitro ability to displace [3H]spiperone binding from dopamine receptor D2 in rat striatal membrane.	B	6.58	pKi	263.03	nM	Ki	J Med Chem (1999) 42: 2774-2797 [PMID:10425088]
ChEMBL	Affinity against Dopamine receptor D2	B	6.58	pKi	263.03	nM	Ki	J Med Chem (2000) 43: 4678-4693 [PMID:11101359]
ChEMBL	Binding affinity to rat Dopamine receptor D2 expressed in CHO cells was determined using [125 I ] iodosulpride as radioligand	B	6.59	pKi	260	nM	Ki	J Med Chem (1996) 39: 2764-2772 [PMID:8709107]
ChEMBL	pKi value for Dopamine receptor D2 binding site	B	6.6	pKi	251.19	nM	Ki	J Med Chem (1998) 41: 3763-3772 [PMID:9748351]
ChEMBL	Half-maximal inhibition of [3H]spiperone binding to Dopamine receptor D2 in rat striatal homogenate	B	6.6	pKi	251.19	nM	Ki	J Med Chem (2002) 45: 344-359 [PMID:11784139]
ChEMBL	In vitro binding affinity towards Dopamine receptor D2 in rat tissue homogenate using [3H]-spiperone as radioligand	B	6.6	pKi	250	nM	Ki	J Med Chem (2004) 47: 143-157 [PMID:14695828]
ChEMBL	Half-maximal inhibition of [3H]spiperone binding to Dopamine receptor D2 in rat striatal homogenate	B	6.6	pKi	250	nM	Ki	J Med Chem (2002) 45: 344-359 [PMID:11784139]
ChEMBL	Binding affinity which represents concentration giving half-maximal inhibition of [3H]spiperone (Dopamine receptor D2) binding to rat tissue homogenate	B	6.6	pKi	250	nM	Ki	J Med Chem (1998) 41: 3763-3772 [PMID:9748351]
ChEMBL	Inhibition of [3H]spiperone binding to rat dopamine D2 receptor	B	6.6	pKi	250	nM	Ki	J Med Chem (2005) 48: 1705-1708 [PMID:15771414]
ChEMBL	Displacement of [3H]spiperone from dopamine D2 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometry	B	6.68	pKi	210	nM	Ki	J Med Chem (2009) 52: 151-169 [PMID:19072656]
ChEMBL	Displacement of [3H]-N-methylspiperone from rat recombinant dopamine D2 short receptor expressed in CHO cells	B	6.72	pKi	190	nM	Ki	J Med Chem (2014) 57: 2670-2682 [PMID:24559051]
ChEMBL	In vitro binding affinity towards dopamine receptor D2 in rat striatal membranes by [3H]sulpiride displacement.	B	6.77	pKi	168	nM	Ki	J Med Chem (1993) 36: 3073-3076 [PMID:7901415]
ChEMBL	Displacement of [3H]spiperone from dopaminergic D2 receptor in rat striatum homogenates after 60 mins by liquid scintillation counting	B	6.81	pKi	155	nM	Ki	Bioorg Med Chem Lett (2015) 25: 5299-5305 [PMID:26483200]
ChEMBL	Binding affinity at dopamine D2 receptor in rat striatal membranes	B	6.84	pKi	144.54	nM	Ki	Bioorg Med Chem Lett (2007) 17: 5749-5753 [PMID:17870534]
ChEMBL	Displacement of [3H]-YM-09151-2 from D2 receptor in rat brain striatal membranes after 60 mins by liquid scintillation counting	B	6.85	pKi	140	nM	Ki	Eur J Med Chem (2013) 66: 122-134 [PMID:23792350]
ChEMBL	Binding affinity of [3H]spiperone towards cloned mammalian Dopamine receptor D2 expressed in cultured cells or from rat whole brain	B	6.86	pKi	138	nM	Ki	J Med Chem (1996) 39: 2435-2437 [PMID:8691438]
ChEMBL	Displacement of [3H]spiperone from dopamine D2 receptor in Sprague-Dawley rat striatum homogenate after 30 mins by liquid scintillation counting	B	6.88	pKi	130.7	nM	Ki	Eur J Med Chem (2014) 74: 427-439 [PMID:24487191]
ChEMBL	Displacement of [3H]spiperone from dopamine D2 receptor in rat striatum	B	6.88	pKi	130.7	nM	Ki	Medchemcomm (2015) 6: 831-838
ChEMBL	Displacement of [3H]spiperone from dopamine D2 receptor in rat striatum tissue after 20 mins by scintillation counting	B	6.89	pKi	130	nM	Ki	Eur J Med Chem (2011) 46: 4474-4488 [PMID:21816515]
ChEMBL	Displacement of [3H]-YM-09151-2 from D2 dopamine receptor in Wistar rat brain striatal membrane after 60 mins by liquid scintillation counting	B	6.89	pKi	130	nM	Ki	Eur J Med Chem (2013) 62: 214-221 [PMID:23353740]
ChEMBL	Displacement of [3H]spiperone from dopamine D2 receptor in rat striatum after 15 mins by liquid scintillation counting analysis	B	6.89	pKi	128.7	nM	Ki	J Med Chem (2013) 56: 4671-4690 [PMID:23675993]
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 113 to 362	B	6.93	pKi	118	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	6.93	pKi	117	nM	Ki	Bioorg Med Chem Lett (1997) 7: 1327-1330
ChEMBL	Tested in vitro for its ability to inhibit [3H]spiperone binding to Dopamine receptor D2 in rat striatal membrane	B	7	pKi	100	nM	Ki	Bioorg Med Chem Lett (1997) 7: 913-918
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	7.03	pKi	93	nM	Ki	J Med Chem (1998) 41: 5402-5409 [PMID:9876110]
ChEMBL	Displacement of [3H]NPA from rat brain Dopamine receptor D2	B	7.08	pKi	83.18	nM	Ki	J Med Chem (1996) 39: 143-148 [PMID:8568801]
ChEMBL	Displacement of [3H]NPA from rat brain Dopamine receptor D2	B	7.08	pKi	83	nM	Ki	J Med Chem (1996) 39: 143-148 [PMID:8568801]
ChEMBL	Binding affinity of [3H]YM-09151 towards cloned mammalian Dopamine receptor D2 expressed in cultured cells or from rat whole brain	B	7.09	pKi	82	nM	Ki	J Med Chem (1996) 39: 2435-2437 [PMID:8691438]
ChEMBL	Binding affinity towards dopamine D2 receptors in rat brain synaptosomal preparations	B	7.09	pKi	82	nM	Ki	J Med Chem (1994) 37: 1060-1062 [PMID:7909336]
ChEMBL	Binding affinity against Dopamine receptor D2 from rat striatum	B	7.09	pKi	82	nM	Ki	J Med Chem (1998) 41: 1997-2009 [PMID:9622541]
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	7.19	pKi	64.2	nM	Ki	Med Chem Res (2004) 13: 25-33
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	7.2	pKi	63.1	nM	Ki	Med Chem Res (2004) 13: 25-33
ChEMBL	Binding affinity of [3H]U-86170 towards Dopamine receptor D2 in cloned mammalian receptor expressed in cultured cells or from rat whole brain	B	7.26	pKi	55	nM	Ki	J Med Chem (1996) 39: 2435-2437 [PMID:8691438]
ChEMBL	Binding affinity towards dopamine receptor D2 by displacing [3H]spiperone radioligand in rat striatum	B	7.27	pKi	53.6	nM	Ki	J Med Chem (1992) 35: 552-558 [PMID:1346653]
ChEMBL	Binding affinity was determined against Dopamine receptor D2 using [3H]spiperone	B	7.27	pKi	53.6	nM	Ki	J Med Chem (1995) 38: 4211-4222 [PMID:7473548]
ChEMBL	Binding affinity was determined against Dopamine receptor D2 using [3H]spiperone	B	7.27	pKi	53.6	nM	Ki	J Med Chem (1995) 38: 4198-4210 [PMID:7473547]
ChEMBL	Binding affinity against dopamine D2 receptor	B	7.34	pKi	45.71	nM	Ki	J Med Chem (1994) 37: 519-525 [PMID:7907148]
ChEMBL	In vitro binding affinity against Dopamine D2 receptor in rat striatal tissue.	B	7.35	pKi	45	nM	Ki	J Med Chem (1993) 36: 2107-2114 [PMID:8101877]
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	7.47	pKi	34	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	7.47	pKi	34	nM	Ki	J Med Chem (1987) 30: 1100-1105 [PMID:2884314]
ChEMBL	Binding activity against dopamine D2 receptor in rat brain, using [3H]spiperone as the radioligand	B	5.56	pIC50	2770	nM	IC50	J Med Chem (1989) 32: 2261-2268 [PMID:2571728]
ChEMBL	Binding affinity for Dopamine receptor D2 using [3H]spiperone in rat brain	B	5.56	pIC50	2770	nM	IC50	J Med Chem (1990) 33: 809-814 [PMID:1967652]
ChEMBL	In vitro binding affinity for Dopamine D2 receptor of rat using [3H]YM-09151 as radioligand	B	5.68	pIC50	2108	nM	IC50	J Med Chem (2002) 45: 4655-4668 [PMID:12361392]
ChEMBL	In vitro affinity towards D2 receptor using [3H]spiroperidol as radioligand in striatum	B	5.79	pIC50	1610	nM	IC50	J Med Chem (1994) 37: 2308-2314 [PMID:7914536]
ChEMBL	Binding affinity towards Dopamine receptor D2 was determined in rat striatal homogenate using [3H]- spiperone as radioligand	B	5.79	pIC50	1610	nM	IC50	J Med Chem (1996) 39: 4044-4057 [PMID:8831770]
ChEMBL	Compound was measured for affinity at dopamine receptor D2 labeled with [3H]spiroperidol radioligand in striatum tissue	B	6	pIC50	1000	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	6.08	pIC50	830	nM	IC50	J Med Chem (1995) 38: 1119-1131 [PMID:7707315]
ChEMBL	In vitro inhibitory concentration against radioligand [3H]spiperone binding to rat striatal dopamine receptor D2	B	6.36	pIC50	440	nM	IC50	J Med Chem (1992) 35: 4516-4525 [PMID:1361578]
ChEMBL	Compound was tested in vitro for its affinity towards rat striatal Dopamine receptor D2 labeled with [3H]- spiperone	B	6.36	pIC50	440	nM	IC50	J Med Chem (1986) 29: 359-369 [PMID:2869146]
ChEMBL	Ability to bind at dopamine receptor D2 of rat corpus striatum by displacing [3H]spiperone	B	6.36	pIC50	440	nM	IC50	J Med Chem (1989) 32: 1147-1156 [PMID:2542551]
ChEMBL	Compound was tested for the inhibition of [3H]spiperone binding to dopamine receptor D2	B	6.39	pIC50	410	nM	IC50	J Med Chem (1992) 35: 1092-1101 [PMID:1348090]
ChEMBL	Ability to inhibit [3H]spiperone binding to Dopamine receptor D2 in rat corpus striatum	B	6.4	pIC50	400	nM	IC50	J Med Chem (1988) 31: 618-624 [PMID:2894466]
ChEMBL	Binding affinity against dopamine receptor D2	B	6.48	pIC50	330	nM	IC50	J Med Chem (1995) 38: 4380-4392 [PMID:7473566]
ChEMBL	Binding affinity towards Dopamine receptor D2 of rat corpus striatum using [3H]spiperone as radioligand	B	6.48	pIC50	330	nM	IC50	J Med Chem (1999) 42: 2235-2244 [PMID:10377229]
ChEMBL	Inhibitory binding of [3H]spiperone to Dopamine receptor D2 in membranes from rat corpus striatum	B	6.48	pIC50	330	nM	IC50	J Med Chem (1997) 40: 4146-4153 [PMID:9406603]
ChEMBL	In vitro binding affinity was measured by displacement of [3H]- raclopride from D2 receptor isolated from the striata of male Dawley rats	B	6.54	pIC50	290	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	6.54	pIC50	290	nM	IC50	J Med Chem (1996) 39: 149-157 [PMID:8568802]
ChEMBL	Inhibition of [3H]spiperone binding to Dopamine receptor D2 from striatum of the rat brain	B	6.6	pIC50	250	nM	IC50	J Med Chem (1989) 32: 2573-2582 [PMID:2573732]
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	6.76	pIC50	172	nM	IC50	J Med Chem (1991) 34: 1860-1866 [PMID:1676427]
ChEMBL	Inhibition of spiropiperidone binding at dopamine receptor D2 of rat.	B	6.88	pIC50	132	nM	IC50	J Med Chem (2001) 44: 372-389 [PMID:11462978]
ChEMBL	Inhibition of [3H]methylspiperone binding to rat striatal membrane Dopamine receptor D2	B	6.89	pIC50	130	nM	IC50	J Med Chem (1998) 41: 5402-5409 [PMID:9876110]
ChEMBL	In vitro binding affinity against Dopamine receptor D2 by displacement of [3H]haloperidol from rat striatal membranes.	B	7.42	pIC50	38	nM	IC50	J Med Chem (1987) 30: 1807-1812 [PMID:2888897]
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	6.33	pKi	466	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	Binding affinity to dopamine D3 receptor (unknown origin) by PDSP assay	B	6	pKi	1000	nM	Ki	Medchemcomm (2012) 3: 580-583
ChEMBL	Binding affinity against dopamine receptor D3 using radioligand [3H]spiperone	B	6.02	pKi	960	nM	Ki	J Med Chem (2001) 44: 2691-2694 [PMID:11495580]
ChEMBL	Competitive binding affinity against human Dopamine receptor D3 by displacing [3H]spiperone from CHO cells	B	6.02	pKi	960	nM	Ki	J Med Chem (2000) 43: 4563-4569 [PMID:11087581]
ChEMBL	Displacement of [3H]spiperone from human Dopamine receptor D3 expressed in CHO cells	B	6.02	pKi	960	nM	Ki	Bioorg Med Chem Lett (1999) 9: 3143-3146 [PMID:10560741]
ChEMBL	In vitro displacement of [3H]spiperone from the cloned human dopamine receptor D3 stably expressed in CHO cells	B	6.02	pKi	960	nM	Ki	Bioorg Med Chem Lett (2000) 10: 2041-2044 [PMID:10987445]
ChEMBL	Binding affinity evaluated for the displacement of [3H]-spiperone against human dopamine receptor D3	B	6.02	pKi	960	nM	Ki	Bioorg Med Chem Lett (1999) 9: 97-102 [PMID:9990464]
ChEMBL	In vitro binding affinity at human cloned dopamine receptor D3 stably expressed in CHO cells by [3H]spiperone displacement.	B	6.02	pKi	960	nM	Ki	Bioorg Med Chem Lett (2002) 12: 633-636 [PMID:11844688]
ChEMBL	Displacement of [3H]spiroperidol from human cloned dopamine D3 receptor expressed in CHO cells	B	6.02	pKi	960	nM	Ki	Bioorg Med Chem (2009) 17: 4448-4458 [PMID:19481941]
ChEMBL	Displacement of [3H]spiperone from human dopamine receptor D3 in CHO cell membrane	B	6.02	pKi	960	nM	Ki	J Med Chem (2006) 49: 3938-3947 [PMID:16789750]
ChEMBL	Ability to displace [3H]spiperone radioligand from cloned human Dopamine receptor D3 in CHO cells	B	6.02	pKi	960	nM	Ki	Bioorg Med Chem Lett (2002) 12: 1937-1940 [PMID:12113813]
ChEMBL	Ability to displace [3H]spiperone from the cloned human D3 dopamine receptor stably expressed in Chinese hamster ovary (CHO) cells was determined.	B	6.02	pKi	960	nM	Ki	Bioorg Med Chem Lett (1999) 9: 1969-1972 [PMID:10450964]
ChEMBL	Displacement of [3H]spiperone from human dopamine D3 receptor	B	6.04	pKi	912.01	nM	Ki	Bioorg Med Chem Lett (2009) 19: 6059-6062 [PMID:19796944]
ChEMBL	Displacement of [3H]N-methylspiperone from human cloned D3 dopamine receptor expressed in HEKT cells incubated for 90 mins by scintillation counting based radioligand binding assay	B	6.19	pKi	646	nM	Ki	Medchemcomm (2015) 6: 1679-1686
ChEMBL	Binding affinity measured at the Dopamine receptor D3 by the inhibition of [3H]YM-09151-2 binding to human recombinant CCL 1.3 cells using unlabeled 7-OH-DPAT for nonspecific binding.	B	6.29	pKi	513	nM	Ki	J Med Chem (1998) 41: 5402-5409 [PMID:9876110]
GtoPdb	-	-	6.3	pKi	-	-	-	J Pharmacol Exp Ther (1994) 268: 417-26 [PMID:8301582]; Eur J Pharmacol (1992) 225: 331-7 [PMID:1354163]
ChEMBL	Binding affinity on human Dopamine receptor D3 expressed in CHO cells using radioligand [3H]-YM 09151	B	6.34	pKi	454	nM	Ki	J Med Chem (1997) 40: 1-3 [PMID:9016321]
ChEMBL	Binding affinity to dopamine D3 receptor	B	6.43	pKi	372.3	nM	Ki	J Nat Prod (2010) 73: 1015-1021 [PMID:20408551]
ChEMBL	Binding affinity towards human Dopamine receptor D3	B	6.44	pKi	360	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	6.5	pKi	319	nM	Ki	J Med Chem (2005) 48: 1705-1708 [PMID:15771414]
ChEMBL	Binding affinity to dopamine D3 receptor (unknown origin)	B	6.5	pKi	319	nM	Ki	J Med Chem (2014) 57: 9578-9597 [PMID:25343529]
ChEMBL	Displacement of [3H]7OH-DPAT from dopamine D3 receptor expressed in Sf9 cells by scintillation spectrometry	B	6.5	pKi	319	nM	Ki	J Med Chem (2009) 52: 151-169 [PMID:19072656]
ChEMBL	Displacement of [3H]spiperone from human dopamine D3 receptor expressed in CHO cells	B	6.53	pKi	295	nM	Ki	Bioorg Med Chem Lett (2009) 19: 538-542 [PMID:19091563]
ChEMBL	Binding affinity towards human dopamine receptor D3	B	6.55	pKi	280	nM	Ki	J Med Chem (2001) 44: 477-501 [PMID:11170639]
ChEMBL	Inhibition of [125I]iodosulpiride binding to human Dopamine receptor D3	B	6.62	pKi	242	nM	Ki	J Med Chem (2005) 48: 1709-1712 [PMID:15771415]
ChEMBL	Binding affinity to human cloned dopamine D3 receptor	B	6.62	pKi	240	nM	Ki	Bioorg Med Chem (2008) 16: 7291-7301 [PMID:18595716]
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	6.62	pKi	240	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	6.62	pKi	6.62	nM	pKi	J Med Chem (2004) 47: 497-508 [PMID:14736232]
ChEMBL	Cataleptogenic effect against cloned human Dopamine receptor D3 in male Sprague-Dawley rats in a bar test	B	6.62	pKi	239.88	nM	Ki	Bioorg Med Chem Lett (2003) 13: 3779-3782 [PMID:14552778]
ChEMBL	Binding affinity against cloned human dopamine receptor D3 expressed in Chinese hamster ovary (CHO) K-1 cells by displacement of [3H]spiperone.	B	6.65	pKi	222	nM	Ki	J Med Chem (1997) 40: 4026-4029 [PMID:9406594]
ChEMBL	Ability to displace [3H]spiperone from human cloned Dopamine receptor D3 expressed in CHO K-1 cells in vitro.	B	6.65	pKi	222	nM	Ki	J Med Chem (1997) 40: 2688-2693 [PMID:9276014]
ChEMBL	compound was tested for its affinity to displace [3H]spiperone cloned human Dopamine receptor D3 stably expressed in HEK393 cell lines	B	6.7	pKi	200	nM	Ki	J Med Chem (1999) 42: 2706-2715 [PMID:10411491]
ChEMBL	Displacement of [3H]spiperone from human Dopamine receptor D3 expressed in CHO cells	B	6.7	pKi	200	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	6.7	pKi	200	nM	Ki	J Med Chem (1997) 40: 2374-2385 [PMID:9240352]
ChEMBL	Binding affinity towards cloned human Dopamine receptor D3 stably expressed in CHO cells was evaluated using [3H]spiperone as radioligand	B	6.7	pKi	200	nM	Ki	J Med Chem (1996) 39: 1941-1942 [PMID:8642550]
ChEMBL	Displacement of [3H]spiperone from human Dopamine receptor D3 expressed in HEK293 cells	B	6.7	pKi	200	nM	Ki	Bioorg Med Chem Lett (1999) 9: 1285-1290 [PMID:10340615]
ChEMBL	Displacement of [3H]spiperone from human dopamine D3 receptor expressed in CHO cells	B	7	pKi	100	nM	Ki	J Med Chem (2007) 50: 5103-5108 [PMID:17880057]
ChEMBL	DRUGMATRIX: Dopamine D3 radioligand binding (ligand: [3H] Spiperone)	B	7.06	pKi	88	nM	Ki	DrugMatrix in vitro pharmacology data
ChEMBL	Displacement of [125I]iodosulpiride from human Dopamine receptor D3 expressed in CHO cells	B	7.06	pKi	88	nM	Ki	J Med Chem (2003) 46: 4377-4392 [PMID:14521403]
ChEMBL	Binding affinity towards human Dopamine receptor D3	B	6.35	pIC50	450	nM	IC50	J Med Chem (1999) 42: 2235-2244 [PMID:10377229]
ChEMBL	DRUGMATRIX: Dopamine D3 radioligand binding (ligand: [3H] Spiperone)	B	6.59	pIC50	258	nM	IC50	DrugMatrix in vitro pharmacology data
D3 receptor/Dopamine D3 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3138] [GtoPdb: 216] [UniProtKB: P19020]
GtoPdb	-	-	5.7	pKi	-	-	-	Nature (1990) 347: 146-51 [PMID:1975644]
ChEMBL	Binding affinity towards baculovirus expressed rat dopamine D3 receptors	B	6.3	pKi	500	nM	Ki	J Med Chem (1994) 37: 1060-1062 [PMID:7909336]
ChEMBL	Displacement of [3H]7-OH-DPAT from dopamine D3 receptor in rat olfactory tubercle	B	6.47	pKi	340.1	nM	Ki	Medchemcomm (2015) 6: 831-838
ChEMBL	Half-maximal inhibition of [3H]-7-OH-DPAT binding to Dopamine receptor D3 in rat tissue homogenate	B	6.49	pKi	320	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	6.5	pKi	319	nM	Ki	J Med Chem (2004) 47: 143-157 [PMID:14695828]
ChEMBL	Half-maximal inhibition of [3H]7-OH-DPAT binding to Dopamine receptor D3 in rat tissue homogenate	B	6.5	pKi	316.23	nM	Ki	J Med Chem (2002) 45: 344-359 [PMID:11784139]
ChEMBL	Binding affinity to rat Dopamine receptor D3 expressed in CHO cells was determined using [125 I] iodosulpride as radioligand	B	6.55	pKi	280	nM	Ki	J Med Chem (1996) 39: 2435-2437 [PMID:8691438]
ChEMBL	Displacement of [3H]7-OH-DPA from dopamine D3 receptor in Sprague-Dawley rat olfactory tubercle homogenate after 60 mins by liquid scintillation counting	B	6.58	pKi	260.1	nM	Ki	Eur J Med Chem (2014) 74: 427-439 [PMID:24487191]
ChEMBL	Displacement of [3H]7-OH-DPAT from dopamine D3 receptor in rat olfactory tubercle after 60 mins by liquid scintillation counting analysis	B	6.62	pKi	239.8	nM	Ki	J Med Chem (2013) 56: 4671-4690 [PMID:23675993]
ChEMBL	Binding affinity to rat Dopamine receptor D3 expressed in CHO cells was determined using [125 I] iodosulpride as radioligand	B	6.64	pKi	230	nM	Ki	J Med Chem (1996) 39: 2764-2772 [PMID:8709107]
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	6.73	pKi	188	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	6.79	pKi	161	nM	Ki	Med Chem Res (2004) 13: 25-33
D4 receptor/Dopamine D4 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL219] [GtoPdb: 217] [UniProtKB: P21917]
ChEMBL	Binding affinity towards Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as the competitive ligand	B	5.05	pKi	9000	nM	Ki	Bioorg Med Chem Lett (2002) 12: 3111-3115 [PMID:12372513]
ChEMBL	Binding affinity to dopamine D4 receptor (unknown origin) by PDSP assay	B	7	pKi	100	nM	Ki	Medchemcomm (2012) 3: 580-583
ChEMBL	Potency was measured by the displacement of [3H]-spiperone binding to human D4 dopaminergic receptor	B	7.14	pKi	72	nM	Ki	Bioorg Med Chem Lett (1997) 7: 1207-1212
ChEMBL	Displacement of [3H]-YM 09151 from human Dopamine receptor D4	B	7.15	pKi	71	nM	Ki	J Med Chem (1995) 38: 4950-4952 [PMID:8523409]
ChEMBL	Binding affinity on human Dopamine receptor D4 expressed in CHO cells using radioligand [3H]-YM 09151	B	7.15	pKi	70	nM	Ki	J Med Chem (1997) 40: 1-3 [PMID:9016321]
ChEMBL	Displacement of [3H]-YM-09151-2 from human D4 receptor after 120 mins by liquid scintillation counting	B	7.22	pKi	60	nM	Ki	Eur J Med Chem (2013) 66: 122-134 [PMID:23792350]
ChEMBL	Displacement of [3H]-YM-09151-2 from human D4 dopamine receptor after 120 mins by liquid scintillation counting	B	7.22	pKi	60	nM	Ki	Eur J Med Chem (2013) 62: 214-221 [PMID:23353740]
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	7.27	pKi	54	nM	Ki	Bioorg Med Chem Lett (2003) 13: 3779-3782 [PMID:14552778]
ChEMBL	Binding affinity to human cloned dopamine D4 receptor	B	7.27	pKi	54	nM	Ki	Bioorg Med Chem (2008) 16: 7291-7301 [PMID:18595716]
ChEMBL	Displacement of [3H]spiperone from human Dopamine receptor D4	B	7.27	pKi	7.27	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	7.27	pKi	53.7	nM	Ki	Bioorg Med Chem Lett (2003) 13: 3779-3782 [PMID:14552778]
ChEMBL	In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.	B	7.33	pKi	47	nM	Ki	Bioorg Med Chem Lett (1998) 8: 725-730 [PMID:9871530]
ChEMBL	Displacement of radiolabeled clozapine from human dopamine D4.4 receptor	B	7.36	pKi	44	nM	Ki	J Med Chem (2008) 51: 7094-7098 [PMID:18983139]
ChEMBL	Binding affinity towards human dopamine-4.2 receptor	B	7.4	pKi	40	nM	Ki	J Med Chem (2004) 47: 1303-1314 [PMID:14998318]
ChEMBL	Binding affinity towards human dopamine receptor D4	B	7.4	pKi	40	nM	Ki	J Med Chem (2001) 44: 477-501 [PMID:11170639]
ChEMBL	Inhibition of human dopamine D4 receptor	B	7.4	pKi	40	nM	Ki	J Med Chem (2014) 57: 2670-2682 [PMID:24559051]
ChEMBL	Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells	B	7.4	pKi	39.81	nM	Ki	J Med Chem (2007) 50: 5103-5108 [PMID:17880057]
ChEMBL	Binding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligand	B	7.41	pKi	39	nM	Ki	J Med Chem (1996) 39: 2764-2772 [PMID:8709107]
ChEMBL	Displacement of [3H]N-methylspiperone from human D4 dopamine receptor incubated for 90 mins by scintillation counting based radioligand binding assay	B	7.41	pKi	39	nM	Ki	Medchemcomm (2015) 6: 1679-1686
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	7.44	pKi	36	nM	Ki	J Med Chem (1998) 41: 5402-5409 [PMID:9876110]
GtoPdb	-	-	7.5	pKi	-	-	-	Eur J Pharmacol (1993) 236: 483-6 [PMID:8102973]
ChEMBL	In vitro ability to inhibit [3H]6b binding to human Dopamine receptor D4.4	B	7.52	pKi	30.4	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	7.52	pKi	30	nM	Ki	J Med Chem (2000) 43: 270-277 [PMID:10649982]
ChEMBL	Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand	B	7.52	pKi	30	nM	Ki	J Med Chem (2002) 45: 5727-5735 [PMID:12477356]
ChEMBL	Displacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cells	B	7.52	pKi	30	nM	Ki	J Med Chem (2003) 46: 265-283 [PMID:12519065]
ChEMBL	In vitro ability to inhibit [3H]spiperone binding to human Dopamine receptor D4.4	B	7.55	pKi	28.4	nM	Ki	Bioorg Med Chem Lett (2004) 14: 5095-5098 [PMID:15380206]
ChEMBL	Ability to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cells	B	7.68	pKi	21	nM	Ki	J Med Chem (1995) 38: 708-714 [PMID:7861418]
ChEMBL	Affinity was evaluated as inhibition constant for dopamine D-4 receptor	B	7.68	pKi	21	nM	Ki	J Med Chem (1994) 37: 2686-2696 [PMID:8064797]
ChEMBL	Displacement of [3H]-YM09151-2 from human cloned dopamine D4 receptor expressed in insect Sf9 cells after 60 mins by liquid scintillation counting	B	7.74	pKi	18	nM	Ki	J Med Chem (2012) 55: 1572-1582 [PMID:22268448]
ChEMBL	In vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranes	B	7.74	pKi	18	nM	Ki	J Med Chem (2002) 45: 5136-5149 [PMID:12408724]
ChEMBL	Displacement of [3H]-YM 09151 from D4 receptor	B	7.77	pKi	17	nM	Ki	Bioorg Med Chem Lett (2003) 13: 701-704 [PMID:12639562]
ChEMBL	Binding affinity at human Dopamine receptor D4 by [3H]- YM 09151 displacement.	B	7.77	pKi	17	nM	Ki	Bioorg Med Chem Lett (2000) 10: 2119-2122 [PMID:10999484]
ChEMBL	Displacement of [3H]methylspiperone from human recombinant D4 receptor expressed in CHO cells	B	7.77	pKi	17	nM	Ki	J Med Chem (2014) 57: 4543-4557 [PMID:24805037]
ChEMBL	Displacement of [3H]methylspiperone from human dopamine D4 receptor expressed in CHO cells	B	7.77	pKi	17	nM	Ki	Eur J Med Chem (2015) 92: 221-235 [PMID:25557493]
ChEMBL	Ability to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitro	B	7.8	pKi	16	nM	Ki	J Med Chem (1997) 40: 2688-2693 [PMID:9276014]
ChEMBL	Binding affinity evaluated for the displacement of [3H]spiperone against human dopamine receptor D4	B	7.8	pKi	16	nM	Ki	Bioorg Med Chem Lett (1999) 9: 97-102 [PMID:9990464]
ChEMBL	Ability to displace [3H]spiperone radioligand from cloned human Dopamine receptor D4 in CHO cells	B	7.8	pKi	16	nM	Ki	Bioorg Med Chem Lett (2002) 12: 1937-1940 [PMID:12113813]
ChEMBL	Displacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membrane	B	7.8	pKi	16	nM	Ki	J Med Chem (2006) 49: 3938-3947 [PMID:16789750]
ChEMBL	In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells	B	7.8	pKi	16	nM	Ki	Bioorg Med Chem Lett (2000) 10: 2041-2044 [PMID:10987445]
ChEMBL	Displacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cells	B	7.8	pKi	16	nM	Ki	Bioorg Med Chem (2009) 17: 4448-4458 [PMID:19481941]
ChEMBL	Displacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cells	B	7.8	pKi	16	nM	Ki	Bioorg Med Chem Lett (1999) 9: 3143-3146 [PMID:10560741]
ChEMBL	Competitive binding affinity against human Dopamine receptor D4 by displacing [3H]spiperone from CHO cells	B	7.8	pKi	16	nM	Ki	J Med Chem (2000) 43: 4563-4569 [PMID:11087581]
ChEMBL	Binding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperone	B	7.8	pKi	16	nM	Ki	J Med Chem (1997) 40: 4026-4029 [PMID:9406594]
ChEMBL	Binding affinity against human dopamine receptor D4.4 using radioligand [3H]spiperone	B	7.8	pKi	16	nM	Ki	J Med Chem (2001) 44: 2691-2694 [PMID:11495580]
ChEMBL	Binding affinity of compound towards human cloned Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperone as radioligand	B	7.8	pKi	16	nM	Ki	Bioorg Med Chem Lett (1999) 9: 1969-1972 [PMID:10450964]
ChEMBL	In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.	B	7.8	pKi	16	nM	Ki	Bioorg Med Chem Lett (2002) 12: 633-636 [PMID:11844688]
ChEMBL	In vitro binding affinity for Dopamine receptor D4	B	7.8	pKi	15.85	nM	Ki	Bioorg Med Chem Lett (2001) 11: 1313-1316 [PMID:11392544]
ChEMBL	Ability to displace [3H]spiperone from dopamine receptor D4.4 expressed in CHO-K1 cells	B	7.8	pKi	7.8	D4	Log Ki	J Med Chem (2001) 44: 1151-1157 [PMID:11312915]
ChEMBL	Binding affinity to human dopamine D4.4 receptor by radioligand displacement assay	B	7.82	pKi	15	nM	Ki	Eur J Med Chem (2013) 63: 85-94 [PMID:23466604]
ChEMBL	Displacement of [3H]YM-09151-2 from human Dopamine receptor D4.2 expressed in baculovirus Sf9 cells	B	7.89	pKi	13	nM	Ki	Bioorg Med Chem Lett (1997) 7: 1327-1330
ChEMBL	Binding affinity towards cloned human Dopamine receptor D4 stably expressed in CHO cells was evaluated using [3H]spiperone as radioligand	B	8	pKi	10	nM	Ki	J Med Chem (1996) 39: 1941-1942 [PMID:8642550]
ChEMBL	Displacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cells	B	8	pKi	10	nM	Ki	J Med Chem (1996) 39: 1943-1945 [PMID:8642551]
ChEMBL	Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.	B	8	pKi	10	nM	Ki	J Med Chem (1997) 40: 2374-2385 [PMID:9240352]
ChEMBL	Binding affinity towards human Dopamine receptor D4.2 in CHO cells	B	8	pKi	10	nM	Ki	J Med Chem (1996) 39: 4044-4057 [PMID:8831770]
ChEMBL	Inhibition of human dopamine D4 receptor	B	8	pKi	10	nM	Ki	J Med Chem (2017) 60: 7233-7243 [PMID:28489950]
ChEMBL	compound was tested for its affinity to displace [3H]spiperone cloned human Dopamine receptor D4 stably expressed in HEK393 cell lines	B	8	pKi	10	nM	Ki	J Med Chem (1999) 42: 2706-2715 [PMID:10411491]
ChEMBL	Displacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cells	B	8	pKi	10	nM	Ki	Bioorg Med Chem Lett (1999) 9: 1285-1290 [PMID:10340615]
ChEMBL	Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand	B	8.05	pKi	9	nM	Ki	Bioorg Med Chem Lett (2002) 12: 3105-3109 [PMID:12372512]
ChEMBL	Antagonist activity at human recombinant at D4 receptor assessed as inhibition of dopamine-induced cAMP accumulation	F	6.77	pIC50	168	nM	IC50	J Med Chem (2014) 57: 4543-4557 [PMID:24805037]
ChEMBL	Percent inhibition against Dopamine receptor D4 at 1 uM	B	6.81	pIC50	156	nM	IC50	J Med Chem (2005) 48: 6887-6896 [PMID:16250647]
ChEMBL	Inhibitory concentration against dopamine receptor D4	B	6.86	pIC50	138	nM	IC50	J Med Chem (2005) 48: 6523-6543 [PMID:16220969]
ChEMBL	Inhibition of human dopamine D4.4 receptor	B	6.92	pIC50	120	nM	IC50	Bioorg Med Chem (2010) 18: 7675-7699 [PMID:20875743]
ChEMBL	Displacement of radiolabeled clozapine from human dopamine D4.4 receptor	B	6.96	pIC50	110	nM	IC50	J Med Chem (2008) 51: 7094-7098 [PMID:18983139]
ChEMBL	Inhibitory concentration against human Dopamine receptor D4.2 in CHO cells	B	7.24	pIC50	58	nM	IC50	J Med Chem (1996) 39: 4044-4057 [PMID:8831770]
ChEMBL	Binding affinity towards human D4.2 receptor	B	7.28	pIC50	52	nM	IC50	J Med Chem (1999) 42: 2235-2244 [PMID:10377229]
ChEMBL	Displacement of [3H]methylspiperone from human recombinant Dopamine D4.4 receptor expressed in CHO cells	B	7.39	pIC50	41	nM	IC50	Bioorg Med Chem (2016) 24: 1793-1810 [PMID:26988801]
ChEMBL	Binding affinity to human dopamine D4.4 receptor by radioligand displacement assay	B	7.4	pIC50	40	nM	IC50	Eur J Med Chem (2013) 63: 85-94 [PMID:23466604]
ChEMBL	Binding affinity to human dopamine D4.4 receptor by radioligand displacement assay	B	7.49	pIC50	32	nM	IC50	Bioorg Med Chem (2013) 21: 2764-2771 [PMID:23582449]
ChEMBL	In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.	B	7.64	pIC50	23	nM	IC50	J Med Chem (1998) 41: 4903-4909 [PMID:9822559]
ChEMBL	Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand	B	7.77	pIC50	17	nM	IC50	J Med Chem (2000) 43: 3923-3932 [PMID:11052797]
D4 receptor/Dopamine D4 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3361] [GtoPdb: 217] [UniProtKB: P30729]
ChEMBL	Binding affinity of [3H]spiperone towards Dopamine receptor D4 expressed in cultured cells or from rat whole brain.	B	7.49	pKi	32	nM	Ki	J Med Chem (1996) 39: 2435-2437 [PMID:8691438]
ChEMBL	Binding affinity of [3H]YM-09151 towards cloned mammalian Dopamine receptor D4 expressed in cultured cells or from rat whole brain	B	7.54	pKi	29	nM	Ki	J Med Chem (1996) 39: 2435-2437 [PMID:8691438]
ChEMBL	Binding affinity of [3H]-spiperone towards cloned mammalian Dopamine receptor D4 expressed in cultured cells or from rat whole brain	B	8.05	pKi	9	nM	Ki	J Med Chem (1996) 39: 2435-2437 [PMID:8691438]
D5 receptor/Dopamine D5 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1850] [GtoPdb: 218] [UniProtKB: P21918]
ChEMBL	Binding affinity to dopamine D5 receptor (unknown origin) by PDSP assay	B	6	pKi	1000	nM	Ki	Medchemcomm (2012) 3: 580-583
ChEMBL	Compound was tested for the Binding affinity against Human cloned Dopamine receptor D5 by Radio ligand ([3H]SCH-23390) binding assay	B	6.11	pKi	780	nM	Ki	J Med Chem (1996) 39: 2764-2772 [PMID:8709107]
GtoPdb	-	-	6.6	pKi	-	-	-	Nature (1991) 350: 614-9 [PMID:1826762]
ChEMBL	Displacement of [3H]SCH-23390 from human cloned D5 dopamine receptor expressed in HEKT cells incubated for 90 mins by scintillation counting based radioligand binding assay	B	6.63	pKi	235	nM	Ki	Medchemcomm (2015) 6: 1679-1686
ChEMBL	Displacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK cells	B	6.7	pKi	198	nM	Ki	Bioorg Med Chem Lett (2009) 19: 538-542 [PMID:19091563]
GABAA receptor π subunit/GABAA receptor β1 subunit/GABAA receptor δ subunit/GABAA receptor γ2 subunit/GABAA receptor α5 subunit/GABAA receptor α3 subunit/GABAA receptor γ1 subunit/GABAA receptor α2 subunit/GABAA receptor α4 subunit/GABAA receptor γ3 subunit/GABAA receptor α6 subunit/GABAA receptor α1 subunit/GABAA receptor β3 subunit/GABAA receptor β2 subunit/GABAA receptor ε subunit/GABA-A receptor; anion channel in Rat (target type: PROTEIN COMPLEX GROUP) [ChEMBL: CHEMBL1907607] [GtoPdb: 419, 410, 416, 414, 408, 406, 413, 405, 407, 415, 409, 404, 412, 411, 417] [UniProtKB: O09028, P15431, P18506, P18508, P19969, P20236, P23574, P23576, P28471, P28473, P30191, P62813, P63079, P63138, Q91ZM7, Q9ES14]
ChEMBL	Inhibition of [3H]muscimol binding to Gamma-aminobutyric acid (GABA-A) receptor	B	6	pIC50	>1000	nM	IC50	J Med Chem (1986) 29: 359-369 [PMID:2869146]
Kv11.1/HERG in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809]
ChEMBL	Binding affinity to human ERG expressed in HEK293 cells by whole cell patch clamp method	B	4.77	pKi	17000	nM	Ki	J Med Chem (2009) 52: 151-169 [PMID:19072656]
ChEMBL	Binding affinity to human ERG expressed in HEK293 cells	B	4.77	pKi	17000	nM	Ki	J Med Chem (2010) 53: 4803-4807 [PMID:20481570]
ChEMBL	DRUGMATRIX: Potassium Channel HERG radioligand binding (ligand: [3H] Astemizole)	B	5.06	pKi	8660.6	nM	Ki	DrugMatrix in vitro pharmacology data
ChEMBL	Binding affinity at hERG expressed in HEK293 cells by fluorescence polarization assay	B	5.39	pKi	4060	nM	Ki	J Med Chem (2007) 50: 2931-2941 [PMID:17536794]
ChEMBL	Displacement of [3H]dofetilide from hERG expressed in HEK293 cells by SPA	B	5.51	pKi	3080	nM	Ki	J Med Chem (2007) 50: 2931-2941 [PMID:17536794]
ChEMBL	DRUGMATRIX: Potassium Channel HERG radioligand binding (ligand: [3H] Astemizole)	B	4.98	pIC50	10571	nM	IC50	DrugMatrix in vitro pharmacology data
ChEMBL	Inhibition of partially open human voltage-gated potassium channel subunit Kv11.1 (ERG K+ channel)	F	5.24	pIC50	5754.4	nM	IC50	Bioorg Med Chem Lett (2005) 15: 1737-1741 [PMID:15745831]
ChEMBL	Inhibition of human ERG	B	5.4	pIC50	3981.07	nM	IC50	Eur J Med Chem (2011) 46: 618-630 [PMID:21185626]
ChEMBL	Inhibition of human ERG	B	5.49	pIC50	3200	nM	IC50	Bioorg Med Chem Lett (2020) 30: 127563-127563 [PMID:32976928]
ChEMBL	Inhibition of human ERG	B	6.05	pIC50	901	nM	IC50	Medchemcomm (2015) 6: 831-838
ChEMBL	Inhibition of human ERG expressed in HEK293 cells by electrophysiology assay	B	6.19	pIC50	650	nM	IC50	J Med Chem (2013) 56: 4671-4690 [PMID:23675993]
ChEMBL	Inhibition of human ERG expressed in CHO cells by whole cell patch clamp technique	B	6.49	pIC50	323.59	nM	IC50	Bioorg Med Chem (2008) 16: 6252-6260 [PMID:18448342]
ChEMBL	Inhibition of human Potassium channel HERG expressed in mammalian cells	B	6.49	pIC50	323.59	nM	IC50	Bioorg Med Chem Lett (2003) 13: 2773-2775 [PMID:12873512]
ChEMBL	Inhibitory concentration against potassium channel HERG	B	6.49	pIC50	323.59	nM	IC50	Bioorg Med Chem Lett (2005) 15: 2886-2890 [PMID:15911273]
ChEMBL	Inhibition of human ERG channel	B	6.49	pIC50	320	nM	IC50	J Med Chem (2009) 52: 4266-4276 [PMID:19534531]
ChEMBL	Inhibition of human ERG channel	B	6.49	pIC50	320	nM	IC50	J Med Chem (2009) 52: 4266-4276 [PMID:19534531]
ChEMBL	K+ channel blocking activity in human embryonic kidney cells expressing HERG Kv11.1	F	6.72	pIC50	191	nM	IC50	J Med Chem (2002) 45: 3844-3853 [PMID:12190308]
ChEMBL	Inhibition of human ERG in MCF7 cells	B	6.72	pIC50	190.55	nM	IC50	Eur J Med Chem (2009) 44: 1926-1932 [PMID:19110341]
H1 receptor/Histamine H1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL231] [GtoPdb: 262] [UniProtKB: P35367]
ChEMBL	Binding affinity to human histamine H1 receptor	B	8.51	pKd	3.1	nM	Kd	J Med Chem (2011) 54: 26-53 [PMID:21062081]
ChEMBL	Binding affinity against histamine H1 receptor	B	7.77	pKi	17	nM	Ki	J Med Chem (2001) 44: 477-501 [PMID:11170639]
ChEMBL	Binding affinity to H1 histamine receptor (unknown origin) by PDSP assay	B	8	pKi	10	nM	Ki	Medchemcomm (2012) 3: 580-583
ChEMBL	Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO cells	B	8.62	pKi	2.38	nM	Ki	Bioorg Med Chem Lett (2009) 19: 538-542 [PMID:19091563]
ChEMBL	Binding affinity towards human histamine H1 receptor	B	8.68	pKi	2.1	nM	Ki	J Med Chem (2004) 47: 1303-1314 [PMID:14998318]
ChEMBL	Binding affinity to human cloned histamine H1 receptor	B	8.74	pKi	1.8	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	8.74	pKi	1.8	nM	Ki	Bioorg Med Chem (2012) 20: 1291-1297 [PMID:22245230]
ChEMBL	Inhibition of [3H]pyrilamine binding to human Histamine H1 receptor	B	8.96	pKi	1.1	nM	Ki	J Med Chem (2005) 48: 1709-1712 [PMID:15771415]
ChEMBL	Inhibition of histamine H1 receptor (unknown origin)	B	9	pKi	1	nM	Ki	J Med Chem (2014) 57: 2670-2682 [PMID:24559051]
ChEMBL	DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)	B	9.24	pKi	0.57	nM	Ki	DrugMatrix in vitro pharmacology data
GtoPdb	-	-	9.6	pKi	-	-	-	Psychopharmacology (Berl.) (1996) 124: 57-73 [PMID:8935801]; Neuropsychopharmacology (2003) 28: 519-26 [PMID:12629531]; J Pharmacol Exp Ther (2002) 302: 328-36 [PMID:12065734]
ChEMBL	DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)	B	8.31	pIC50	4.91	nM	IC50	DrugMatrix in vitro pharmacology data
ChEMBL	Inverse agonist activity at human histamine H1 receptor by R-SAT assay	B	9.4	pEC50	0.4	nM	EC50	US-20040213816-A1. Selective serotonin 2A/2C receptor inverse agonists as therapeutics for neurodegenerative diseases (2004)
H1 receptor/Histamine H1 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4701] [GtoPdb: 262] [UniProtKB: P31390]
ChEMBL	Half-maximal inhibition of [3H]pyrilamine binding to Histamine H1 receptor in rat frontal cortex homogenate	B	7.85	pKi	14	nM	Ki	J Med Chem (2002) 45: 344-359 [PMID:11784139]
ChEMBL	Compound was tested for the binding affinity against rat cortical H1 receptor by radioligand [3H]-pyrilamine binding assay.	B	8.3	pKi	5	nM	Ki	J Med Chem (1996) 39: 2764-2772 [PMID:8709107]
ChEMBL	In vitro binding affinity towards Histamine H1 receptor of rat frontal cortex homogenate by using radioligand [3H]pyrilamine	B	8.54	pKi	2.9	nM	Ki	J Med Chem (2004) 47: 143-157 [PMID:14695828]
ChEMBL	Binding affinity towards histamine H1 receptor from rat brain membranes using [3H]mepyramine as radioligand	B	7.64	pIC50	23	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	7.64	pIC50	23	nM	IC50	J Med Chem (1997) 40: 4146-4153 [PMID:9406603]
ChEMBL	Displacement of [3H]mepyramine from H1R in rat brain	B	8.05	pIC50	9	nM	IC50	Proc Natl Acad Sci U S A (2007) 104: 3456-3459 [PMID:17360666]
Histamine H1 receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3943] [UniProtKB: P31389]
ChEMBL	Displacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum homogenates after 60 mins by liquid scintillation counting	B	7.91	pKi	12.2	nM	Ki	Bioorg Med Chem Lett (2015) 25: 5299-5305 [PMID:26483200]
ChEMBL	Displacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum	B	8.09	pKi	8.1	nM	Ki	Medchemcomm (2015) 6: 831-838
ChEMBL	Displacement of [3H]pyrilamine from histaminergic H1 receptor guinea pig cerebellum	B	8.1	pKi	7.94	nM	Ki	J Med Chem (2007) 50: 5103-5108 [PMID:17880057]
ChEMBL	Displacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum homogenate after 60 mins by liquid scintillation counting	B	8.17	pKi	6.8	nM	Ki	Eur J Med Chem (2014) 74: 427-439 [PMID:24487191]
ChEMBL	Displacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum after 60 mins by liquid scintillation counting analysis	B	8.42	pKi	3.8	nM	Ki	J Med Chem (2013) 56: 4671-4690 [PMID:23675993]
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	5.45	pKi	3550	nM	Ki	DrugMatrix in vitro pharmacology data
ChEMBL	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	B	5.44	pIC50	3610	nM	IC50	DrugMatrix in vitro pharmacology data
H3 receptor/Histamine H3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL264] [GtoPdb: 264] [UniProtKB: Q9Y5N1]
ChEMBL	Displacement of [125I]iodoproxyfan from human histamine H3 receptor expressed in CHO/HEK293 cells	B	6	pKi	>1000	nM	Ki	Bioorg Med Chem Lett (2009) 19: 538-542 [PMID:19091563]
ChEMBL	Antagonist potency against human H3 receptor in GTPgamma-S-Assay	F	6.2	pKi	631	nM	Ki	J Med Chem (2005) 48: 306-311 [PMID:15634025]
H3 receptor in Rat [GtoPdb: 264] [UniProtKB: Q9QYN8]
GtoPdb	-	-	5.8	pKi	-	-	-	J Pharmacol Exp Ther (2000) 293: 771-8 [PMID:10869375]
H4 receptor/Histamine H4 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3759] [GtoPdb: 265] [UniProtKB: Q9H3N8]
ChEMBL	Displacement of [3H]histamine from human histamine H4 receptor transfected in SK-N-MC cells at 1 uM	B	7.15	pKd	70.2	nM	Kd	J Med Chem (2006) 49: 4512-4516 [PMID:16854056]
ChEMBL	Displacement of [3H]histamine from human histamine H4 receptor transfected in SK-N-MC cells at 300 nM	B	7.68	pKd	20.9	nM	Kd	J Med Chem (2006) 49: 4512-4516 [PMID:16854056]
ChEMBL	Displacement of [3H]Histamine from human histamine H4 receptor transfected in SK-N-MC cells at 100 nM	B	7.84	pKd	14.5	nM	Kd	J Med Chem (2006) 49: 4512-4516 [PMID:16854056]
ChEMBL	Displacement of [3H]histamine from human histamine H4 receptor transfected in SK-N-MC cells	B	7.92	pKd	11.9	nM	Kd	J Med Chem (2006) 49: 4512-4516 [PMID:16854056]
ChEMBL	Displacement of [3H]histamine from wild type human histamine H4 receptor transfected in HEK293T cells after 1 hr by liquid scintillation counting analysis	B	6.3	pKi	501.19	nM	Ki	Medchemcomm (2013) 4: 193-204
ChEMBL	Displacement of [3H]histamine from human H4 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting	B	6.7	pKi	199.53	nM	Ki	J Med Chem (2011) 54: 8136-8147 [PMID:22003888]
GtoPdb	-	-	6.7	pKi	-	-	-	Mol Pharmacol (2001) 59: 420-6 [PMID:11179434]; J Pharmacol Exp Ther (2001) 299: 121-30 [PMID:11561071]; Mol Pharmacol (2001) 59: 434-41 [PMID:11179436]; J Pharmacol Exp Ther (2005) 314: 1310-21 [PMID:15947036]
ChEMBL	Displacement of [3H]histamine from human histamine H4 receptor transfected in SK-N-MC cells	B	6.75	pKi	177.83	nM	Ki	J Med Chem (2006) 49: 4512-4516 [PMID:16854056]
H4 receptor in Mouse [GtoPdb: 265] [UniProtKB: Q91ZY2]
GtoPdb	-	-	5.5	pKi	-	-	-	J Pharmacol Exp Ther (2001) 299: 121-30 [PMID:11561071]
H4 receptor in Rat [GtoPdb: 265] [UniProtKB: Q91ZY1]
GtoPdb	-	-	5.7	pKi	-	-	-	J Pharmacol Exp Ther (2001) 299: 121-30 [PMID:11561071]
Histone H1.0 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3707465] [UniProtKB: P07305]
ChEMBL	Binding Assay: Binding assay using 5-HT2A, Dopamine D2, SERT, αA1, 5-HT2C and H1 Receptors.	B	9	pKi	1	nM	Ki	US-8598119-B2. Methods and compositions for sleep disorders and other disorders (2013)
M1 receptor/Muscarinic acetylcholine receptor M1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL216] [GtoPdb: 13] [UniProtKB: P11229]
ChEMBL	Binding affinity to M1 receptor (unknown origin) by PDSP assay	B	7	pKi	100	nM	Ki	Medchemcomm (2012) 3: 580-583
ChEMBL	Displacement of [3H]pirenzepine from human M1 receptor expressed in CHO cells	B	8.2	pKi	6.31	nM	Ki	J Med Chem (2007) 50: 5103-5108 [PMID:17880057]
ChEMBL	DRUGMATRIX: Muscarinic M1 radioligand binding (ligand: [3H] N-Methylscopolamine)	B	8.61	pKi	2.47	nM	Ki	DrugMatrix in vitro pharmacology data
ChEMBL	Binding affinity to human cloned muscarinic M1 receptor	B	8.74	pKi	1.8	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	8.74	pKi	1.8	nM	Ki	Bioorg Med Chem (2012) 20: 1291-1297 [PMID:22245230]
ChEMBL	Binding affinity towards human M1 muscarinic receptor.	B	9.01	pKi	0.98	nM	Ki	J Med Chem (2001) 44: 477-501 [PMID:11170639]
GtoPdb	-	-	7.9	pIC50	-	-	-	Proc Natl Acad Sci USA (2003) 100: 13674-9 [PMID:14595031]
ChEMBL	DRUGMATRIX: Muscarinic M1 radioligand binding (ligand: [3H] N-Methylscopolamine)	B	8	pIC50	10	nM	IC50	DrugMatrix in vitro pharmacology data
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	8.03	pIC50	9.4	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	8.03	pIC50	9.4	nM	IC50	J Med Chem (1997) 40: 4146-4153 [PMID:9406603]
ChEMBL	Agonist activity at muscarinic M1 receptor (unknown origin) expressed in CHO cells	F	5	pEC50	>10000	nM	EC50	Bioorg Med Chem Lett (2021) 40: 127911-127911 [PMID:33691168]
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	7.26	pKi	55	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	7.27	pKi	54	nM	Ki	J Med Chem (2004) 47: 143-157 [PMID:14695828]
ChEMBL	Compound was tested for the binding affinity against rat cortical Muscarinic acetylcholine receptor M1 by radioligand [3H]pirenzepine binding assay.	B	8.68	pKi	2.1	nM	Ki	J Med Chem (1996) 39: 2764-2772 [PMID:8709107]
GtoPdb	-	-	7.7	pIC50	-	-	-	Mol Pharmacol (2006) 70: 1974-83 [PMID:16959945]
M2 receptor/Muscarinic acetylcholine receptor M2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL211] [GtoPdb: 14] [UniProtKB: P08172]
ChEMBL	DRUGMATRIX: Muscarinic M2 radioligand binding (ligand: [3H] N-Methylscopolamine)	B	6.77	pKi	169	nM	Ki	DrugMatrix in vitro pharmacology data
ChEMBL	Binding affinity to M2 receptor (unknown origin) by PDSP assay	B	7	pKi	100	nM	Ki	Medchemcomm (2012) 3: 580-583
ChEMBL	DRUGMATRIX: Muscarinic M2 radioligand binding (ligand: [3H] N-Methylscopolamine)	B	6.32	pIC50	476	nM	IC50	DrugMatrix in vitro pharmacology data
ChEMBL	Agonist activity at muscarinic M2 receptor (unknown origin) expressed in CHO cells	F	5	pEC50	>10000	nM	EC50	Bioorg Med Chem Lett (2021) 40: 127911-127911 [PMID:33691168]
M2 receptor/Muscarinic acetylcholine receptor M2 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL309] [GtoPdb: 14] [UniProtKB: P10980]
ChEMBL	Compound was tested for the binding affinity against rat heart Muscarinic acetylcholine receptor M2 by Radio ligand [3H]quinuclidinyl binding assay.	B	7.34	pKi	46	nM	Ki	J Med Chem (1996) 39: 2764-2772 [PMID:8709107]
M3 receptor/Muscarinic acetylcholine receptor M3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL245] [GtoPdb: 15] [UniProtKB: P20309]
ChEMBL	Binding affinity to M3 receptor (unknown origin) by PDSP assay	B	7	pKi	100	nM	Ki	Medchemcomm (2012) 3: 580-583
ChEMBL	DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)	B	7.77	pKi	17	nM	Ki	DrugMatrix in vitro pharmacology data
ChEMBL	DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)	B	7.11	pIC50	78	nM	IC50	DrugMatrix in vitro pharmacology data
ChEMBL	Agonist activity at muscarinic M3 receptor (unknown origin) expressed in CHO cells	F	5	pEC50	>10000	nM	EC50	Bioorg Med Chem Lett (2021) 40: 127911-127911 [PMID:33691168]
M4 receptor/Muscarinic acetylcholine receptor M4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1821] [GtoPdb: 16] [UniProtKB: P08173]
ChEMBL	Binding affinity to M4 receptor (unknown origin) by PDSP assay	B	7	pKi	100	nM	Ki	Medchemcomm (2012) 3: 580-583
ChEMBL	Displacement of [3H]4-DAMP from human M4 receptor expressed in CHO cells	B	7.9	pKi	12.59	nM	Ki	J Med Chem (2007) 50: 5103-5108 [PMID:17880057]
ChEMBL	DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)	B	8.2	pKi	6.3	nM	Ki	DrugMatrix in vitro pharmacology data
ChEMBL	DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)	B	7.35	pIC50	45	nM	IC50	DrugMatrix in vitro pharmacology data
ChEMBL	Agonist activity at muscarinic M4 receptor (unknown origin) expressed in CHO cells	F	5	pEC50	>10000	nM	EC50	Bioorg Med Chem Lett (2021) 40: 127911-127911 [PMID:33691168]
M5 receptor/Muscarinic acetylcholine receptor M5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2035] [GtoPdb: 17] [UniProtKB: P08912]
ChEMBL	Binding affinity to M5 receptor (unknown origin) by PDSP assay	B	7	pKi	100	nM	Ki	Medchemcomm (2012) 3: 580-583
ChEMBL	DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)	B	8.02	pKi	9.53	nM	Ki	DrugMatrix in vitro pharmacology data
ChEMBL	DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)	B	7.89	pIC50	13	nM	IC50	DrugMatrix in vitro pharmacology data
NET/Norepinephrine transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL222] [GtoPdb: 926] [UniProtKB: P23975]
ChEMBL	DRUGMATRIX: Norepinephrine Transporter radioligand binding (ligand: [125I] RTI-55)	B	5.84	pKi	1458	nM	Ki	DrugMatrix in vitro pharmacology data
ChEMBL	DRUGMATRIX: Norepinephrine Transporter radioligand binding (ligand: [125I] RTI-55)	B	5.83	pIC50	1470	nM	IC50	DrugMatrix in vitro pharmacology data
Norepinephrine transporter in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL304] [UniProtKB: Q9WTR4]
ChEMBL	Inhibition of [3H]nisoxetine binding to rat Norepinephrine transporter	B	6.16	pKi	697	nM	Ki	J Med Chem (2005) 48: 1709-1712 [PMID:15771415]
Plasmodium falciparum (target type: ORGANISM) [ChEMBL: CHEMBL364]
ChEMBL	Antiplasmodial activity against Plasmodium falciparum HB3 after 72 hrs by SYBR green assay	F	4.9	pIC50	12589.25	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	pIC50	10000	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	5.1	pIC50	7943.28	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	5.1	pIC50	7943.28	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	5.4	pIC50	3981.07	nM	IC50	Nat Chem Biol (2009) 5: 765-771 [PMID:19734910]
5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL214] [GtoPdb: 1] [UniProtKB: P08908]
ChEMBL	Binding affinity to serotonin 5-HT1A receptor (unknown origin) by PDSP assay	B	6	pKi	1000	nM	Ki	Medchemcomm (2012) 3: 580-583
ChEMBL	Binding affinity towards human 5-hydroxytryptamine 1 receptor	B	6.15	pKi	710	nM	Ki	J Med Chem (2001) 44: 477-501 [PMID:11170639]
ChEMBL	Binding affinity against 5-Hydroxytryptamine 1A receptor	B	6.38	pKi	416.87	nM	Ki	Bioorg Med Chem Lett (2004) 14: 4263-4266 [PMID:15261283]
ChEMBL	Binding affinity for 5-hydroxytryptamine 1A receptor determined using [3H]8-OH-DPAT as radioligand	B	6.57	pKi	270	nM	Ki	Bioorg Med Chem Lett (2001) 11: 2345-2349 [PMID:11527728]
ChEMBL	Binding affinity to 5HT1A receptor (unknown origin)	B	6.8	pKi	160	nM	Ki	J Med Chem (2014) 57: 9578-9597 [PMID:25343529]
ChEMBL	Displacement of [3H]-8-OH-DPAT from human 5-HT1A receptor expressed in HEK293 cells after 1 hr	B	6.84	pKi	143	nM	Ki	Eur J Med Chem (2012) 56: 348-360 [PMID:22926225]
ChEMBL	Displacement of [3H]-8-OH-DPAT from human 5-HT1AR expressed in HEK293 cell membranes after 1 hr by microbeta counting method	B	6.84	pKi	143	nM	Ki	Eur J Med Chem (2018) 145: 790-804 [PMID:29407591]
ChEMBL	Displacement of [3H]8-OH-DPAT from human 5HT1A receptor expressed in HEK293 cells after 1 hr	B	6.84	pKi	143	nM	Ki	Bioorg Med Chem Lett (2013) 23: 4419-4423 [PMID:23787101]
ChEMBL	Binding affinity to human cloned 5HT1A receptor	B	6.85	pKi	140	nM	Ki	Bioorg Med Chem (2008) 16: 7291-7301 [PMID:18595716]
ChEMBL	Inhibition of human 5HT1A receptor	B	6.85	pKi	140	nM	Ki	J Med Chem (2014) 57: 2670-2682 [PMID:24559051]
GtoPdb	-	-	6.9	pKi	-	-	-	Eur J Pharmacol (1998) 355: 245-56 [PMID:9760039]; Psychopharmacology (Berl.) (1996) 124: 57-73 [PMID:8935801]; J Pharmacol Exp Ther (1998) 286: 1341-55 [PMID:9732398]
ChEMBL	Displacement of [3H]8-OH-DPAT from human recombinant 5HT1A receptor expressed in CHO cells after 60 mins by liquid scintillation counting	B	7	pKi	101	nM	Ki	J Med Chem (2012) 55: 1572-1582 [PMID:22268448]
ChEMBL	Displacement of [3H]8-OH-DPAT from human 5HT1A receptor expressed in CHO cells	B	7	pKi	100	nM	Ki	J Med Chem (2007) 50: 5103-5108 [PMID:17880057]
ChEMBL	Binding affinity to human 5HT1A receptor	B	8.05	pKi	8.9	nM	Ki	Bioorg Med Chem (2016) 24: 3994-4007 [PMID:27377863]
ChEMBL	Binding affinity to 5-HT1A receptor (unknown origin)	B	8.2	pKi	6.38	nM	Ki	Med Chem Res (2013) 22: 520-530
ChEMBL	Affinity towards 5-hydroxytryptamine 1A receptor in membranes from bovine hippocampus using [3H]OH-DPAT	B	6.82	pIC50	150	nM	IC50	J Med Chem (1998) 41: 2010-2018 [PMID:9622542]
5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3737] [GtoPdb: 1] [UniProtKB: Q64264]
ChEMBL	Inhibitory activity against serotonin 5-hydroxytryptamine 1A receptor from mice.	B	5.7	pIC50	2000	nM	IC50	J Med Chem (1996) 39: 4692-4703 [PMID:8941382]
5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL273] [GtoPdb: 1] [UniProtKB: P19327]
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	6.19	pKi	640	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	6.35	pKi	443	nM	Ki	J Med Chem (2000) 43: 270-277 [PMID:10649982]
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	6.38	pKi	415	nM	Ki	J Med Chem (1999) 42: 3342-3355 [PMID:10464021]
ChEMBL	Displacement of [3H]-8-OH-DPAT from 5HT1A receptor in Wistar rat hippocampus homogenate	B	6.42	pKi	380	nM	Ki	Bioorg Med Chem (2010) 18: 1925-1935 [PMID:20153652]
ChEMBL	DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1A radioligand binding (ligand: [3H] 8-OH-DPAT)	B	6.55	pKi	281	nM	Ki	DrugMatrix in vitro pharmacology data
ChEMBL	Displacement of [3H]-OH-8-DPAT from 5HT1A receptor in Wistar rat hippocampal membrane after 15 mins by liquid scintillation counting	B	6.59	pKi	260	nM	Ki	Eur J Med Chem (2013) 62: 214-221 [PMID:23353740]
ChEMBL	Displacement of [3H]-8-OH-DPAT from 5HT1A receptor in rat brain hippocampal membranes after 15 mins by liquid scintillation counting	B	6.59	pKi	260	nM	Ki	Eur J Med Chem (2013) 66: 122-134 [PMID:23792350]
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	6.61	pKi	247	nM	Ki	J Med Chem (1998) 41: 5402-5409 [PMID:9876110]
ChEMBL	Displacement of [3H]8-OH-DPAT from 5HT1A receptor in rat brain cortex	B	6.73	pKi	185.6	nM	Ki	Medchemcomm (2015) 6: 831-838
ChEMBL	Displacement of [3H]8-OH-DPAT from 5HT1A receptor in Sprague-Dawley rat brain cortex homogenate after 30 mins by liquid scintillation counting	B	6.73	pKi	185.6	nM	Ki	Eur J Med Chem (2014) 74: 427-439 [PMID:24487191]
ChEMBL	Displacement of [3H]8-OH-DPAT from 5-HT1A receptor in rat cerebral cortex homogenates after 60 mins by liquid scintillation counting	B	6.79	pKi	161	nM	Ki	Bioorg Med Chem Lett (2015) 25: 5299-5305 [PMID:26483200]
ChEMBL	Displacement of [3H]8OH-DPAT from 5HT1A receptor in CRL:CD(SD)BR-COBS rat hippocampus by scintillation spectrometry	B	6.8	pKi	160	nM	Ki	J Med Chem (2009) 52: 151-169 [PMID:19072656]
ChEMBL	Displacement of [3H]8OH-DPAT from 5HT1A receptor in rat CRL:CD(SD)BR-COBS hippocampus by scintillation spectrometry	B	6.8	pKi	160	nM	Ki	J Med Chem (2010) 53: 4803-4807 [PMID:20481570]
ChEMBL	Binding affinity of [3H]-8-OH-DPAT towards 5-hydroxytryptamine 1A receptor in cloned mammalian receptor expressed in cultured cells or from rat whole brain.	B	6.82	pKi	150	nM	Ki	J Med Chem (1996) 39: 2435-2437 [PMID:8691438]
ChEMBL	Displacement of [3H]8-OH-DPAT from 5HT1A receptor in rat cerebral cortex after 30 mins by liquid scintillation counting analysis	B	6.85	pKi	141.6	nM	Ki	J Med Chem (2013) 56: 4671-4690 [PMID:23675993]
ChEMBL	Displacement of [3H]8OH-DPAT from 5HT1A in rat brain cerebral cortex after 15 mins by scintillation counting	B	6.85	pKi	140	nM	Ki	Eur J Med Chem (2011) 46: 4474-4488 [PMID:21816515]
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	6.89	pKi	130	nM	Ki	J Med Chem (1996) 39: 2764-2772 [PMID:8709107]
ChEMBL	Binding affinity towards 5-hydroxytryptamine 1A receptor of rat brain synaptosomal preparations	B	6.95	pKi	111	nM	Ki	J Med Chem (1994) 37: 1060-1062 [PMID:7909336]
ChEMBL	Compound was evaluated for its binding affinity against 5-hydroxytryptamine 1A receptor from rat cerebral cortex	B	6.95	pKi	111	nM	Ki	J Med Chem (1998) 41: 1997-2009 [PMID:9622541]
ChEMBL	Binding affinity at 5HT1A receptor in rat striatal membranes	B	7.02	pKi	95.5	nM	Ki	Bioorg Med Chem Lett (2007) 17: 5749-5753 [PMID:17870534]
ChEMBL	Binding affinity was determined against 5-hydroxytryptamine 1A receptor using [3H]WB-4101	B	7.41	pKi	39	nM	Ki	J Med Chem (1995) 38: 4198-4210 [PMID:7473547]
ChEMBL	The compound was tested for its binding affinity towards 5-hydroxytryptamine 1A receptor by displacing [3H]WB-4101 radioligand in rat hippocampus	B	7.41	pKi	39	nM	Ki	J Med Chem (1992) 35: 552-558 [PMID:1346653]
ChEMBL	Affinity against the 5-hydroxytryptamine receptor 1A using [3H]WB-4101.	B	7.41	pKi	38.5	nM	Ki	J Med Chem (1995) 38: 4211-4222 [PMID:7473548]
ChEMBL	In vitro binding affinity was measured on serotonergic 5-hydroxytryptamine 1A receptor by displacement of [3H]- tetralin	B	5.7	pIC50	2000	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	5.7	pIC50	2000	nM	IC50	J Med Chem (1996) 39: 149-157 [PMID:8568802]
ChEMBL	In vitro affinity towards 5-hydroxytryptamine 1A receptor using [3H]8-OH-DPAT as radioligand in hippocampus	B	5.99	pIC50	1015.5	nM	IC50	J Med Chem (1994) 37: 2308-2314 [PMID:7914536]
ChEMBL	Binding affinity towards serotonin 5-HT1A receptor was determined in rat hippocampus using [3H]8-OH-DPAT as ligand	B	6	pIC50	1010	nM	IC50	J Med Chem (1996) 39: 4044-4057 [PMID:8831770]
ChEMBL	Binding affinity to 5-hydroxytryptamine 1A receptor in the rat brain using [3H]8-hydroxy-2-(di-n-propylamine)tetralin as radioligand.	B	6.22	pIC50	600	nM	IC50	J Med Chem (1991) 34: 1860-1866 [PMID:1676427]
ChEMBL	Affinity for 5-hydroxytryptamine 1A receptor labeled with [3H]8-OH-DPAT radioligand in hippocampus tissue	B	6.24	pIC50	580	nM	IC50	J Med Chem (1991) 34: 1068-1072 [PMID:1672156]
ChEMBL	DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1A radioligand binding (ligand: [3H] 8-OH-DPAT)	B	6.31	pIC50	491	nM	IC50	DrugMatrix in vitro pharmacology data
ChEMBL	In vitro binding affinity for serotonin 5-hydroxytryptamine 1A receptor fof rat cerebral cortex using [3H]8-OH-DPAT as radioligand	B	6.57	pIC50	267.6	nM	IC50	J Med Chem (2002) 45: 4655-4668 [PMID:12361392]
5-HT1B receptor/Serotonin 1b (5-HT1b) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1898] [GtoPdb: 2] [UniProtKB: P28222]
ChEMBL	Binding affinity to serotonin 5-HT1B receptor (unknown origin) by PDSP assay	B	6	pKi	1000	nM	Ki	Medchemcomm (2012) 3: 580-583
GtoPdb	-	-	6.2	pKi	-	-	-	Psychopharmacology (Berl.) (1996) 124: 57-73 [PMID:8935801]
5-HT1B receptor/Serotonin 1b (5-HT1b) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3459] [GtoPdb: 2] [UniProtKB: P28564]
ChEMBL	DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)	B	6.02	pKi	959	nM	Ki	DrugMatrix in vitro pharmacology data
ChEMBL	Affinity towards 5-hydroxytryptamine 1B receptor in membranes from rat frontal cortex using [3H]5-HT	B	5.6	pIC50	2500	nM	IC50	J Med Chem (1998) 41: 2010-2018 [PMID:9622542]
ChEMBL	DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)	B	5.68	pIC50	2109	nM	IC50	DrugMatrix in vitro pharmacology data
5-HT1D receptor/Serotonin 1d (5-HT1d) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1983] [GtoPdb: 3] [UniProtKB: P28221]
ChEMBL	Binding affinity to serotonin 5-HT1D receptor (unknown origin) by PDSP assay	B	6	pKi	>1000	nM	Ki	Medchemcomm (2012) 3: 580-583
GtoPdb	-	-	6.4	pKi	-	-	-	Psychopharmacology (Berl.) (1996) 124: 57-73 [PMID:8935801]
5-ht1e receptor/Serotonin 1e (5-HT1e) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2182] [GtoPdb: 4] [UniProtKB: P28566]
ChEMBL	Binding affinity to serotonin 5-HT1E receptor (unknown origin) by PDSP assay	B	6	pKi	1000	nM	Ki	Medchemcomm (2012) 3: 580-583
GtoPdb	-	-	6.4	pKi	-	-	-	Psychopharmacology (Berl.) (1996) 124: 57-73 [PMID:8935801]
5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223]
ChEMBL	Binding affinity to human 5HT2A receptor	B	6.64	pKi	230	nM	Ki	Bioorg Med Chem (2016) 24: 3994-4007 [PMID:27377863]
ChEMBL	Displacement of [3H]ketanserin from human 5HT2A receptor expressed in tsA201 cell membranes after 1 hr by scintillation counting analysis	B	7.44	pKi	36.31	nM	Ki	J Med Chem (2013) 56: 1211-1227 [PMID:23301527]
ChEMBL	Displacement of [3H]ketanserin from human 5HT2A receptor expressed in tsA201 cell membranes after 1 hr by scintillation counting analysis	B	7.44	pKi	36	nM	Ki	J Med Chem (2013) 56: 1211-1227 [PMID:23301527]
ChEMBL	Displacement of [3H]ketanserin from human recombinant 5-HT2A receptor expressed in HEKT cell membranes by radioligand binding assay	B	7.74	pKi	18	nM	Ki	J Nat Prod (2015) 78: 722-729 [PMID:25695425]
ChEMBL	Displacement of [3H]ketanserin from human 5HT2A receptor expressed in HEKT cell membranes after 1.5 hrs by liquid scintillation counting method	B	7.79	pKi	16.1	nM	Ki	Medchemcomm (2018) 9: 1069-1075 [PMID:30108996]
ChEMBL	Displacement of [3H]ketanserin from human 5-HT2A receptor measured after 90 mins by microbeta scintillation counting method	B	7.82	pKi	15	nM	Ki	Bioorg Med Chem Lett (2016) 26: 3216-3219 [PMID:27261181]
ChEMBL	Displacement of [3H]ketanserin from human recombinant 5-HT2A receptor expressed in HEKT cell membrane after 90 mins by scintillation counting method	B	7.82	pKi	15	nM	Ki	Medchemcomm (2015) 6: 601-605
ChEMBL	Displacement of [3H]-ketanserin from human 5-HT2AR expressed in CHO-K1 cell membranes after 1.5 hrs by microbeta counting method	B	7.89	pKi	13	nM	Ki	Eur J Med Chem (2018) 145: 790-804 [PMID:29407591]
ChEMBL	Binding affinity to serotonin 5-HT2A receptor (unknown origin) by PDSP assay	B	8	pKi	10	nM	Ki	Medchemcomm (2012) 3: 580-583
ChEMBL	Binding affinity to 5HT2A receptor (unknown origin)	B	8	pKi	10	nM	Ki	J Med Chem (2014) 57: 9578-9597 [PMID:25343529]
ChEMBL	Binding Assay: Binding assay using 5-HT2A, Dopamine D2, SERT, αA1, 5-HT2C and H1 Receptors.	B	8.02	pKi	9.6	nM	Ki	US-8598119-B2. Methods and compositions for sleep disorders and other disorders (2013)
ChEMBL	Displacement of [125]DOI from human recombinant full length 5HT2A receptor expressed in HEK293E cells	B	8.02	pKi	9.6	nM	Ki	J Med Chem (2014) 57: 2670-2682 [PMID:24559051]
ChEMBL	Displacement of [3H]ketanserin from human 5-HT2A receptor	B	8.04	pKi	9.12	nM	Ki	Eur J Med Chem (2014) 71: 237-249 [PMID:24316025]
ChEMBL	Binding affinity towards serotonin 5-hydroxytryptamine 2A receptor	B	8.04	pKi	9.12	nM	Ki	Bioorg Med Chem Lett (2004) 14: 585-589 [PMID:14741248]
ChEMBL	Displacement of [3H]ketanserin human cloned serotonin 5HT2A receptor	B	8.04	pKi	9.12	nM	Ki	Bioorg Med Chem Lett (2007) 17: 4873-4877 [PMID:17588750]
ChEMBL	Displacement of [3H]ketanserin from human cloned 5HT2A receptor	B	8.04	pKi	9.12	nM	Ki	J Med Chem (2008) 51: 6085-6094 [PMID:18783204]
ChEMBL	Displacement of [3H]ketanserin from human cloned 5HT2A receptor	B	8.04	pKi	9.12	nM	Ki	Bioorg Med Chem Lett (2009) 19: 6059-6062 [PMID:19796944]
ChEMBL	Antagonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced intracellular calcium release measured for 90 secs by fluorescence assay	F	8.04	pKi	9.12	nM	Ki	J Med Chem (2013) 56: 1211-1227 [PMID:23301527]
ChEMBL	Displacement of [3H]ketanserin from human cloned 5-HT2A receptor by in vitro binding assay	B	8.04	pKi	9.12	nM	Ki	Medchemcomm (2011) 2: 1194-1200
ChEMBL	Antagonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced intracellular calcium release measured for 90 secs by fluorescence assay	F	8.04	pKi	9.1	nM	Ki	J Med Chem (2013) 56: 1211-1227 [PMID:23301527]
ChEMBL	Binding affinity to human cloned 5HT2A receptor	B	8.05	pKi	8.9	nM	Ki	Bioorg Med Chem (2008) 16: 7291-7301 [PMID:18595716]
ChEMBL	Binding affinity to 5-HT2A receptor (unknown origin)	B	8.07	pKi	8.57	nM	Ki	Med Chem Res (2013) 22: 520-530
ChEMBL	In vitro binding affinity towards 5-hydroxytryptamine 2A receptor in human using [3H]ketanserin as radioligand	B	8.11	pKi	7.8	nM	Ki	J Med Chem (2004) 47: 143-157 [PMID:14695828]
ChEMBL	Displacement of [3H]Ketanserin from 5-HT2A receptor (unknown origin)	B	8.13	pKi	7.41	nM	Ki	Bioorg Med Chem Lett (2014) 24: 576-579 [PMID:24365159]
ChEMBL	Displacement of [3H]Ketanserin from 5-HT2A receptor (unknown origin)	B	8.14	pKi	7.3	nM	Ki	Bioorg Med Chem Lett (2014) 24: 576-579 [PMID:24365159]
ChEMBL	Inhibition of [125I]R91150 binding to human 5-hydroxytryptamine 2A receptor	B	8.2	pKi	6.3	nM	Ki	J Med Chem (2005) 48: 1709-1712 [PMID:15771415]
ChEMBL	Antagonist activity at 5HT2A receptor (unknown origin)	B	8.27	pKi	5.35	nM	Ki	Eur J Med Chem (2020) 193: 112214-112214 [PMID:32182489]
ChEMBL	Binding affinity to 5-HT2A receptor (unknown origin)	B	8.27	pKi	5.35	nM	Ki	Bioorg Med Chem Lett (2015) 25: 3970-3974 [PMID:26227779]
ChEMBL	Displacement of [3H]ketanserin from human 5HT2A receptor expressed in CHO cells	B	8.3	pKi	5.01	nM	Ki	J Med Chem (2007) 50: 5103-5108 [PMID:17880057]
ChEMBL	Binding affinity towards human 5-HT2A receptor in BEK cells	B	8.3	pKi	5	nM	Ki	J Med Chem (1996) 39: 4044-4057 [PMID:8831770]
ChEMBL	Displacement of [3H]ketanserin from human recombinant 5HT2A receptor expressed in CHO cells after 60 mins by liquid scintillation counting	B	8.32	pKi	4.84	nM	Ki	J Med Chem (2012) 55: 1572-1582 [PMID:22268448]
ChEMBL	Binding affinity for human 5-hydroxytryptamine 2A receptor	B	8.4	pKi	4	nM	Ki	J Med Chem (2001) 44: 477-501 [PMID:11170639]
ChEMBL	Binding affinity towards human serotonin 5-hydroxytryptamine 2A receptor	B	8.48	pKi	3.3	nM	Ki	J Med Chem (2004) 47: 1303-1314 [PMID:14998318]
ChEMBL	Binding affinity to human 5HT2A receptor	B	8.52	pKi	3.03	nM	Ki	Bioorg Med Chem Lett (2020) 30: 127053-127053 [PMID:32107165]
ChEMBL	Displacement of [3H]-Ketanserin from 5-HT2A receptor (unknown origin) incubated for 90 mins by microbeta counting method	B	8.52	pKi	3	nM	Ki	Bioorg Med Chem (2020) 28: 115578-115578 [PMID:32631561]
ChEMBL	Binding affinity against 5-Hydroxytryptamine 2A receptor	B	8.57	pKi	2.69	nM	Ki	Bioorg Med Chem Lett (2004) 14: 4263-4266 [PMID:15261283]
ChEMBL	Binding affinity to human 5HT2A receptor	B	8.85	pKi	1.4	nM	Ki	Bioorg Med Chem Lett (2020) 30: 127563-127563 [PMID:32976928]
ChEMBL	DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2A radioligand binding (ligand: [3H] Ketanserin)	B	8.92	pKi	1.2	nM	Ki	DrugMatrix in vitro pharmacology data
GtoPdb	-	-	9	pKi	-	-	-	Psychopharmacology (Berl.) (1996) 124: 57-73 [PMID:8935801]; J Pharmacol Exp Ther (1998) 286: 1341-55 [PMID:9732398]; Naunyn Schmiedebergs Arch Pharmacol (2004) 370: 114-23 [PMID:15322733]; Neuropsychopharmacology (2003) 28: 519-26 [PMID:12629531]; J Pharmacol Exp Ther (2004) 310: 943-51 [PMID:15102927]
ChEMBL	Inhibitory concentration against human 5-HT2A receptor in BEK cells	B	7.92	pIC50	12	nM	IC50	J Med Chem (1996) 39: 4044-4057 [PMID:8831770]
ChEMBL	DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2A radioligand binding (ligand: [3H] Ketanserin)	B	8.38	pIC50	4.2	nM	IC50	DrugMatrix in vitro pharmacology data
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	8.52	pIC50	3	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	Compound was tested for Antagonistic activity against denuded rat aorta	F	8.62	pKd	2.4	nM	Kd	Bioorg Med Chem Lett (1998) 8: 3571-3576 [PMID:9934473]
ChEMBL	Negative log concentration of antagonist on 5-hydroxytryptamine 2A receptor in rat thoracic aorta	F	9.16	pKd	0.69	nM	Kd	J Med Chem (2002) 45: 54-71 [PMID:11754579]
ChEMBL	In vitro affinity against serotonin 5-hydroxytryptamine 2A receptor	B	7.56	pKi	27.54	nM	Ki	J Med Chem (2000) 43: 4678-4693 [PMID:11101359]
ChEMBL	Displacement of [3H]-ketanserin from 5HT2A receptor in rat brain cortical membranes after 15 mins by liquid scintillation counting	B	7.68	pKi	21	nM	Ki	Eur J Med Chem (2013) 66: 122-134 [PMID:23792350]
ChEMBL	Displacement of [3H]-ketanserin from 5HT2A receptor in Wistar rat cortical membrane after 15 mins by liquid scintillation counting	B	7.7	pKi	20	nM	Ki	Eur J Med Chem (2013) 62: 214-221 [PMID:23353740]
ChEMBL	Compound was tested for the Binding affinity against rat frontal cortex 5-hydroxytryptamine 2A receptor by Radio ligand [3H]ketanserin binding assay.	B	7.77	pKi	17	nM	Ki	J Med Chem (1996) 39: 2764-2772 [PMID:8709107]
ChEMBL	Displacement of [3H]-ketanserin from rat brain 5-hydroxytryptamine 2A receptor	B	7.82	pKi	15.14	nM	Ki	J Med Chem (1996) 39: 143-148 [PMID:8568801]
ChEMBL	Displacement of [3H]ketanserine from 5-HT2A receptor in rat cerebral cortex homogenates after 60 mins by liquid scintillation counting	B	7.84	pKi	14.5	nM	Ki	Bioorg Med Chem Lett (2015) 25: 5299-5305 [PMID:26483200]
ChEMBL	Displacement of [3H]ketanserin from 5HT2A receptor in Wistar rat cortex homogenate	B	7.85	pKi	14	nM	Ki	Bioorg Med Chem (2010) 18: 1925-1935 [PMID:20153652]
ChEMBL	Binding affinity at 5HT2A receptor in rat striatal membranes	B	7.88	pKi	13.18	nM	Ki	Bioorg Med Chem Lett (2007) 17: 5749-5753 [PMID:17870534]
ChEMBL	Displacement of [3H]Ketanserin from 5HT2A receptor in Sprague-Dawley rat brain cortex homogenate after 30 mins by liquid scintillation counting	B	7.89	pKi	12.9	nM	Ki	Eur J Med Chem (2014) 74: 427-439 [PMID:24487191]
ChEMBL	Displacement of [3H]ketanserin from 5HT2A receptor in rat brain cortex	B	7.89	pKi	12.9	nM	Ki	Medchemcomm (2015) 6: 831-838
ChEMBL	Displacement of [3H]ketanserin from 5HT2A receptor in rat cerebral cortex after 15 mins by liquid scintillation counting analysis	B	7.94	pKi	11.6	nM	Ki	J Med Chem (2013) 56: 4671-4690 [PMID:23675993]
ChEMBL	In vitro binding affinity towards 5-hydroxytryptamine 2A receptor in rat tissue homogenate using [3H]ketanserin as radioligand	B	8	pKi	10	nM	Ki	J Med Chem (2004) 47: 143-157 [PMID:14695828]
ChEMBL	Displacement of [3H]ketanserin from 5HT2A receptor in CRL:CD(SD)BR-COBS rat cortex by scintillation spectrometry	B	8	pKi	10	nM	Ki	J Med Chem (2010) 53: 4803-4807 [PMID:20481570]
ChEMBL	Half-maximal inhibition of [3H]- Ketanserin binding to 5-hydroxytryptamine 2A receptor in rat cerebral cortex homogenate	B	8	pKi	10	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	8	pKi	10	nM	Ki	J Med Chem (2009) 52: 151-169 [PMID:19072656]
ChEMBL	Half-maximal inhibition of [3H]ketanserin binding to 5-hydroxytryptamine 2A receptor in rat cerebral cortex homogenate	B	8	pKi	10	nM	Ki	J Med Chem (2002) 45: 344-359 [PMID:11784139]
ChEMBL	Inhibition of [3H]ketanserin binding to rat 5-hydroxytryptamine 2A receptor	B	8	pKi	10	nM	Ki	J Med Chem (2005) 48: 1705-1708 [PMID:15771414]
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	8.03	pKi	9.4	nM	Ki	J Med Chem (1998) 41: 5402-5409 [PMID:9876110]
ChEMBL	Compound was evaluated for its binding affinity towards rat 5-hydroxytryptamine 2A receptor	B	8.05	pKi	9	nM	Ki	J Med Chem (2000) 43: 1011-1018 [PMID:10715164]
ChEMBL	Displacement of [3H]ketanserin from 5HT2A in rat brain cerebral cortex after 20 mins by scintillation counting	B	8.05	pKi	8.9	nM	Ki	Eur J Med Chem (2011) 46: 4474-4488 [PMID:21816515]
ChEMBL	Ability to inhibit the binding of iodine-125-labelled lysergic acid diethylamide([125I]-LSD) to the S-2A serotonin receptor.	B	8.1	pKi	8	nM	Ki	J Med Chem (1995) 38: 708-714 [PMID:7861418]
ChEMBL	Affinity was evaluated as inhibition constant for serotonin 5-hydroxytryptamine 2A receptor	B	8.1	pKi	8	nM	Ki	J Med Chem (1994) 37: 2686-2696 [PMID:8064797]
ChEMBL	Compound was measured for the inhibition of [3H]ketanserin binding to rat frontal cortex membrane (5-HT2A receptor)	B	8.12	pKi	7.59	nM	Ki	Bioorg Med Chem Lett (1998) 8: 3571-3576 [PMID:9934473]
ChEMBL	Inhibitory constant on 5-hydroxytryptamine 2A receptor of Rat frontal cortex	B	8.12	pKi	7.59	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	8.17	pKi	6.7	nM	Ki	J Med Chem (2002) 45: 5136-5149 [PMID:12408724]
ChEMBL	Displacement of [3H]ketanserin from 5HT2A receptor in rat cortical membrane	B	8.22	pKi	6.05	nM	Ki	Eur J Med Chem (2009) 44: 800-808 [PMID:18603331]
ChEMBL	Tested in vitro for its ability to inhibit [3H]ketanserin binding to 5-hydroxytryptamine 2A receptor in rat frontal cortex membranes	B	8.3	pKi	5.01	nM	Ki	Bioorg Med Chem Lett (1997) 7: 913-918
ChEMBL	In vitro ability to displace [3H]ketanserin binding from 5-hydroxytryptamine 2A receptor in rat striatal membrane.	B	8.3	pKi	5.01	nM	Ki	J Med Chem (1999) 42: 2774-2797 [PMID:10425088]
ChEMBL	Affinity at 5-hydroxytryptamine 2A receptor of the rat brain cortex was assessed on the basis of their ability to displace [3H]ketanserin	B	8.8	pKi	1.58	nM	Ki	J Med Chem (2000) 43: 1901-1909 [PMID:10821703]
GtoPdb	-	-	8.9	pKi	-	-	-	J Pharmacol Exp Ther (1998) 286: 85-90 [PMID:9655845]
ChEMBL	In vitro affinity towards 5-hydroxytryptamine 2A receptor using [3H]spiroperidol as radioligand in cortex	B	7.14	pIC50	72	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	7.39	pIC50	40.7	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	7.89	pIC50	13	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	7.92	pIC50	12	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	8.11	pIC50	7.8	nM	IC50	J Med Chem (1997) 40: 4146-4153 [PMID:9406603]
ChEMBL	Binding affinity for 5-hydroxytryptamine 2A receptor, activity is expressed as IC50 values.	B	8.11	pIC50	7.8	nM	IC50	J Med Chem (1995) 38: 4380-4392 [PMID:7473566]
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	8.14	pKi	7.18	nM	Ki	DrugMatrix in vitro pharmacology data
ChEMBL	Displacement of [3H]LSD from 5HT2B receptor expressed in CHO cells	B	8.5	pKi	3.16	nM	Ki	J Med Chem (2007) 50: 5103-5108 [PMID:17880057]
GtoPdb	-	-	8.8	pKi	-	-	-	J Pharmacol Exp Ther (1998) 286: 1341-55 [PMID:9732398]; Naunyn Schmiedebergs Arch Pharmacol (2004) 370: 114-23 [PMID:15322733]; 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	7.96	pIC50	11	nM	IC50	DrugMatrix in vitro pharmacology data
ChEMBL	Inverse agonist activity at human 5HT2B receptor by R-SAT assay	B	7.7	pEC50	20	nM	EC50	US-20040213816-A1. Selective serotonin 2A/2C receptor inverse agonists as therapeutics for neurodegenerative diseases (2004)
5-HT2B receptor/Serotonin 2b (5-HT2b) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL323] [GtoPdb: 7] [UniProtKB: P30994]
ChEMBL	Negative log concentration of antagonistic compound was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundus	F	6.77	pKd	169.82	nM	Kd	J Med Chem (2002) 45: 54-71 [PMID:11754579]
ChEMBL	Compound was evaluated for antagonism against serotonin (5-hydroxytryptamine 2B receptor ) receptor	F	6.9	pKd	125.89	nM	Kd	J Med Chem (2000) 43: 4678-4693 [PMID:11101359]
5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL225] [GtoPdb: 8] [UniProtKB: P28335]
ChEMBL	Binding affinity to serotonin 5-HT2C receptor (unknown origin) by PDSP assay	B	7	pKi	100	nM	Ki	Medchemcomm (2012) 3: 580-583
ChEMBL	Antagonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced intracellular calcium release measured for 90 secs by fluorescence assay	F	7.14	pKi	73	nM	Ki	J Med Chem (2013) 56: 1211-1227 [PMID:23301527]
ChEMBL	Antagonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced intracellular calcium release measured for 90 secs by fluorescence assay	F	7.14	pKi	72.44	nM	Ki	J Med Chem (2013) 56: 1211-1227 [PMID:23301527]
ChEMBL	Displacement of [3H]-mesulergine from human 5HT2C receptor after 60 mins by liquid scintillation counting	B	7.62	pKi	24	nM	Ki	Eur J Med Chem (2013) 62: 214-221 [PMID:23353740]
ChEMBL	Displacement of [3H]-mesulergine from human 5HT2C receptor after 60 mins by liquid scintillation counting	B	7.64	pKi	23	nM	Ki	Eur J Med Chem (2013) 66: 122-134 [PMID:23792350]
ChEMBL	Inhibition of [3H]mesulergine binding to human 5-hydroxytryptamine 2C receptor	B	7.68	pKi	21	nM	Ki	J Med Chem (2005) 48: 1709-1712 [PMID:15771415]
ChEMBL	Binding affinity to human cloned 5HT2C receptor	B	7.77	pKi	17	nM	Ki	Bioorg Med Chem (2008) 16: 7291-7301 [PMID:18595716]
ChEMBL	In vitro ability to displace [3H]mesulergine binding from 5-hydroxytryptamine 2C receptor from bovine choroid plexus.	B	7.8	pKi	15.85	nM	Ki	J Med Chem (1999) 42: 2774-2797 [PMID:10425088]
ChEMBL	Inhibitory constant was determined on 5-hydroxytryptamine 2C receptor of Bovine choroid plexus	B	7.8	pKi	15.85	nM	Ki	J Med Chem (2002) 45: 54-71 [PMID:11754579]
ChEMBL	Displacement of [3H]mesulergine from human 5HT2C receptor in human tsA201 cells	B	7.82	pKi	15	nM	Ki	Bioorg Med Chem Lett (2010) 20: 5431-5433 [PMID:20719507]
ChEMBL	Binding Assay: Binding assay using 5-HT2A, Dopamine D2, SERT, αA1, 5-HT2C and H1 Receptors.	B	7.89	pKi	13	nM	Ki	US-8598119-B2. Methods and compositions for sleep disorders and other disorders (2013)
ChEMBL	Displacement of [125]DOI from human recombinant full length 5HT2C receptor expressed in HEK293E cells	B	7.89	pKi	13	nM	Ki	J Med Chem (2014) 57: 2670-2682 [PMID:24559051]
ChEMBL	Binding affinity towards human serotonin 5-hydroxytryptamine 2C receptor	B	7.89	pKi	13	nM	Ki	J Med Chem (2004) 47: 1303-1314 [PMID:14998318]
ChEMBL	Displacement of [3H]mesulergine from human cloned 5HT2C receptor	B	7.98	pKi	10.47	nM	Ki	J Med Chem (2008) 51: 6085-6094 [PMID:18783204]
ChEMBL	Displacement of [3H]mesulergine human cloned serotonin 5HT2C receptor	B	7.98	pKi	10.47	nM	Ki	Bioorg Med Chem Lett (2007) 17: 4873-4877 [PMID:17588750]
ChEMBL	Displacement of [3H]mesulergine from human 5HT2C receptor	B	7.98	pKi	10.47	nM	Ki	Bioorg Med Chem Lett (2009) 19: 6059-6062 [PMID:19796944]
ChEMBL	Binding affinity towards serotonin 5-hydroxytryptamine 2C receptor	B	7.98	pKi	10.47	nM	Ki	Bioorg Med Chem Lett (2004) 14: 585-589 [PMID:14741248]
ChEMBL	Displacement of [3H]mesulergine from human 5HT2C receptor expressed in tsA201 cell membranes after 1 hr by scintillation counting analysis	B	8.03	pKi	9.33	nM	Ki	J Med Chem (2013) 56: 1211-1227 [PMID:23301527]
ChEMBL	Displacement of [3H]mesulergine from human 5HT2C receptor expressed in tsA201 cell membranes after 1 hr by scintillation counting analysis	B	8.03	pKi	9.3	nM	Ki	J Med Chem (2013) 56: 1211-1227 [PMID:23301527]
ChEMBL	Displacement of [3H]mesulergine from 5HT2C receptor expressed in CHO cells	B	8.1	pKi	7.94	nM	Ki	J Med Chem (2007) 50: 5103-5108 [PMID:17880057]
ChEMBL	In vitro affinity against serotonin (5-hydroxytryptamine 2C) receptor	B	8.3	pKi	5.01	nM	Ki	J Med Chem (2000) 43: 4678-4693 [PMID:11101359]
ChEMBL	Binding affinity towards human 5-hydroxytryptamine 2C receptor	B	8.3	pKi	5	nM	Ki	J Med Chem (2001) 44: 477-501 [PMID:11170639]
ChEMBL	Binding affinity to 5HT2C receptor (unknown origin)	B	8.32	pKi	4.8	nM	Ki	J Med Chem (2014) 57: 9578-9597 [PMID:25343529]
ChEMBL	DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2C radioligand binding (ligand: [3H] Mesulergine)	B	8.5	pKi	3.16	nM	Ki	DrugMatrix in vitro pharmacology data
ChEMBL	Binding affinity against 5-Hydroxytryptamine 2C receptor	B	8.54	pKi	2.88	nM	Ki	Bioorg Med Chem Lett (2004) 14: 4263-4266 [PMID:15261283]
ChEMBL	Binding affinity to 5-HT2C receptor (unknown origin)	B	8.54	pKi	2.88	nM	Ki	Med Chem Res (2013) 22: 520-530
GtoPdb	-	-	8.7	pKi	-	-	-	J Pharmacol Exp Ther (1998) 286: 1341-55 [PMID:9732398]; Naunyn Schmiedebergs Arch Pharmacol (2004) 370: 114-23 [PMID:15322733]; Neuropsychopharmacology (2003) 28: 519-26 [PMID:12629531]; J Pharmacol Exp Ther (2004) 310: 943-51 [PMID:15102927]; J Pharmacol Exp Ther (2000) 295: 226-32 [PMID:10991983]; J Neurochem (1999) 72: 2127-34 [PMID:10217294]
ChEMBL	Affinity towards 5-hydroxytryptamine 2C receptor in membranes from pig choroid plexus using [3H]N-methyl-mesulergine	B	8	pIC50	10	nM	IC50	J Med Chem (1998) 41: 2010-2018 [PMID:9622542]
ChEMBL	DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2C radioligand binding (ligand: [3H] Mesulergine)	B	8.22	pIC50	6.04	nM	IC50	DrugMatrix in vitro pharmacology data
ChEMBL	Inverse agonist activity at human 5HT2C receptor by R-SAT assay	B	6.6	pEC50	250	nM	EC50	US-20040213816-A1. Selective serotonin 2A/2C receptor inverse agonists as therapeutics for neurodegenerative diseases (2004)
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 5-HT2C receptor in rat cerebral cortex homogenates after 60 mins by liquid scintillation counting	B	7.38	pKi	41.9	nM	Ki	Bioorg Med Chem Lett (2015) 25: 5299-5305 [PMID:26483200]
ChEMBL	Displacement of [3H]mesulergine from 5HT2C receptor in rat brain cortex	B	7.48	pKi	33.1	nM	Ki	Medchemcomm (2015) 6: 831-838
ChEMBL	Compound was evaluated for its binding affinity towards rat r5-hydroxytryptamine 2C receptor	B	7.64	pKi	23	nM	Ki	J Med Chem (2000) 43: 1011-1018 [PMID:10715164]
ChEMBL	Displacement of [3H]mesulergine from 5HT2C receptor in rat cerebral cortex after 15 mins by liquid scintillation counting analysis	B	7.79	pKi	16.2	nM	Ki	J Med Chem (2013) 56: 4671-4690 [PMID:23675993]
ChEMBL	Affinity was evaluated as inhibition constant for serotonin 5-hydroxytryptamine 2C receptor	B	8.1	pKi	8	nM	Ki	J Med Chem (1994) 37: 2686-2696 [PMID:8064797]
ChEMBL	Ability to inhibit the binding of iodine-125-labelled lysergic acid diethylamide([125I]-LSD) to the S-2C serotonin receptor.	B	8.1	pKi	8	nM	Ki	J Med Chem (1995) 38: 708-714 [PMID:7861418]
ChEMBL	Binding affinity towards 5-HT2C receptor from rat using [3H]mesulergine as radioligand	B	7.96	pIC50	11	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	7.96	pIC50	11	nM	IC50	J Med Chem (1997) 40: 4146-4153 [PMID:9406603]
5-HT3E/5-HT3B/5-HT3A/5-HT3D/5-HT3C/Serotonin 3 (5-HT3) receptor in Human (target type: PROTEIN COMPLEX GROUP) [ChEMBL: CHEMBL2094132] [GtoPdb: 377, 374, 373, 376, 375] [UniProtKB: A5X5Y0, O95264, P46098, Q70Z44, Q8WXA8]
ChEMBL	Displacement of [3H]BLR-43694 from human 5HT3 receptor expressed in HEK293 cells	B	6.4	pKi	398.11	nM	Ki	J Med Chem (2007) 50: 5103-5108 [PMID:17880057]
5-HT3A/5-HT3B/Serotonin 3 (5-HT3) receptor in Rat (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2094116] [GtoPdb: 373, 374] [UniProtKB: P35563, Q9JJ16]
ChEMBL	Affinity was evaluated as inhibition constant for serotonin 5-hydroxytryptamine 3 receptor	B	7.28	pKi	53	nM	Ki	J Med Chem (1994) 37: 2686-2696 [PMID:8064797]
5-HT3A/Serotonin 3a (5-HT3a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1899] [GtoPdb: 373] [UniProtKB: P46098]
ChEMBL	Binding affinity to serotonin 5-HT3 receptor (unknown origin) by PDSP assay	B	6	pKi	1000	nM	Ki	Medchemcomm (2012) 3: 580-583
ChEMBL	Binding affinity against 5-Hydroxytryptamine 3 receptor	B	6.73	pKi	186.21	nM	Ki	Bioorg Med Chem Lett (2004) 14: 4263-4266 [PMID:15261283]
ChEMBL	Binding affinity to 5-HT3 receptor (unknown origin)	B	6.73	pKi	186.21	nM	Ki	Med Chem Res (2013) 22: 520-530
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	7.49	pKi	32	nM	Ki	J Med Chem (1996) 39: 2764-2772 [PMID:8709107]
5-HT5A receptor/Serotonin 5a (5-HT5a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3426] [GtoPdb: 10] [UniProtKB: P47898]
ChEMBL	Binding affinity towards human 5-hydroxytryptamine 5A receptor was evaluated using [3H]-5-CT as radioligand	B	6	pKi	1000	nM	Ki	J Med Chem (2003) 46: 2795-2812 [PMID:12825922]
ChEMBL	Binding affinity to serotonin 5-HT5A receptor (unknown origin) by PDSP assay	B	6	pKi	>1000	nM	Ki	Medchemcomm (2012) 3: 580-583
GtoPdb	-	-	6.5	pKi	-	-	-	FEBS Lett (1994) 355: 242-6 [PMID:7988681]; Eur J Pharmacol (2001) 418: 157-67 [PMID:11343685]
5-HT5A receptor in Mouse [GtoPdb: 10] [UniProtKB: P30966]
GtoPdb	-	-	5.3	pKi	-	-	-	Eur J Pharmacol (2001) 418: 157-67 [PMID:11343685]
5-HT6 receptor/Serotonin 6 (5-HT6) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3371] [GtoPdb: 11] [UniProtKB: P50406]
ChEMBL	Binding affinity to serotonin 5-HT6 receptor (unknown origin) by PDSP assay	B	7	pKi	100	nM	Ki	Medchemcomm (2012) 3: 580-583
ChEMBL	Binding affinity for human 5-hydroxytryptamine 6 receptor	B	7.3	pKi	<50	nM	Ki	J Med Chem (2005) 48: 1781-1795 [PMID:15771424]
ChEMBL	Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation counting	B	7.77	pKi	17	nM	Ki	J Med Chem (2012) 55: 5704-5719 [PMID:22537153]
ChEMBL	Displacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cells	B	7.77	pKi	17	nM	Ki	Bioorg Med Chem Lett (2010) 20: 5431-5433 [PMID:20719507]
ChEMBL	Binding affinity to human cloned 5HT6 receptor	B	7.96	pKi	11	nM	Ki	Bioorg Med Chem (2008) 16: 7291-7301 [PMID:18595716]
ChEMBL	Antagonist activity at human recombinant 5-HT6 receptor assessed as inhibition of serotonin-induced cAMP accumulation	F	8	pKi	<10	nM	Ki	J Med Chem (2014) 57: 4543-4557 [PMID:24805037]
ChEMBL	Compound was evaluated for its binding affinity towards human 5-hydroxytryptamine 6 receptor	B	8	pKi	10	nM	Ki	J Med Chem (2000) 43: 1011-1018 [PMID:10715164]
ChEMBL	Binding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [3H]-LSD as radioligand	B	8.02	pKi	9.5	nM	Ki	J Med Chem (2003) 46: 2795-2812 [PMID:12825922]
GtoPdb	-	-	8.1	pKi	-	-	-	J Neurochem (1996) 66: 47-56 [PMID:8522988]; Mol Pharmacol (1998) 54: 577-583 [PMID:9730917]; Mol Pharmacol (1997) 52: 515-523 [PMID:9284367]; Psychopharmacology (Berl.) (2005) 179: 461-9 [PMID:15821958]
ChEMBL	Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells	B	8.1	pKi	7.94	nM	Ki	J Med Chem (2007) 50: 5103-5108 [PMID:17880057]
ChEMBL	Displacement of [3H]LSD from 5-HT6 receptor (unknown origin)	B	8.21	pKi	6.1	nM	Ki	Bioorg Med Chem Lett (2014) 24: 576-579 [PMID:24365159]
ChEMBL	Displacement of [3H]LSD from 5-HT6 receptor (unknown origin)	B	8.22	pKi	6.03	nM	Ki	Bioorg Med Chem Lett (2014) 24: 576-579 [PMID:24365159]
ChEMBL	DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)	B	8.3	pKi	5.05	nM	Ki	DrugMatrix in vitro pharmacology data
ChEMBL	Binding affinity against human 5-hydroxytryptamine 6 receptor stably transfected to HEK 293 human embryonic kidney cells using [3H]-lysergic acid diethylamide as radioligand	B	8.32	pKi	4.8	nM	Ki	Bioorg Med Chem Lett (2000) 10: 2295-2299 [PMID:11055342]
ChEMBL	Displacement of [3H]-LSD from human 5-HT6 receptor expresssed in stable HEK cell membrane incubated for 90 mins by microbeta counting method	B	8.4	pKi	4	nM	Ki	Bioorg Med Chem (2020) 28: 115578-115578 [PMID:32631561]
ChEMBL	Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr	B	8.4	pKi	4	nM	Ki	Eur J Med Chem (2012) 56: 348-360 [PMID:22926225]
ChEMBL	Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1 hr	B	8.4	pKi	4	nM	Ki	Bioorg Med Chem Lett (2013) 23: 4419-4423 [PMID:23787101]
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	8.4	pKi	4	nM	Ki	Eur J Med Chem (2018) 145: 790-804 [PMID:29407591]
ChEMBL	Binding affinity towards human 5-hydroxytryptamine 6 receptor	B	8.4	pKi	4	nM	Ki	J Med Chem (2003) 46: 2795-2812 [PMID:12825922]
ChEMBL	Antagonist activity at human 5HT6 receptor expressed in CHO-K1 cells assessed as inhibition of 5HT-induced calcium flux incubated for 60 mins at 37 degC followed by 15 mins incubation at room temperature and subsequent 5HT addition by calcium 4 dye based FLIPR assay	F	7.69	pIC50	20.3	nM	IC50	Eur J Med Chem (2020) 207: 112709-112709 [PMID:32877805]
ChEMBL	Antagonist activity at serotonin human 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced calcium flux after 15 mins by calcium 4-dye based FLIPR assay	F	7.7	pIC50	20	nM	IC50	J Med Chem (2018) 61: 10017-10039 [PMID:30383372]
ChEMBL	Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cells	B	7.77	pIC50	17	nM	IC50	Bioorg Med Chem (2014) 22: 1782-1790 [PMID:24495863]
ChEMBL	DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)	B	7.96	pIC50	11	nM	IC50	DrugMatrix in vitro pharmacology data
5-HT6 receptor in Rat [GtoPdb: 11] [UniProtKB: P31388]
GtoPdb	-	-	8.4	pKi	-	-	-	Mol Pharmacol (1993) 43: 320-7 [PMID:7680751]; J Pharmacol Exp Ther (1998) 286: 1341-55 [PMID:9732398]; Neuropharmacology (1997) 36: 713-20 [PMID:9225298]; Mol Pharmacol (1998) 54: 577-583 [PMID:9730917]; J Neurochem (1998) 71: 2169-77 [PMID:9798944]; J Pharmacol Exp Ther (1994) 268: 1403-10 [PMID:7908055]; Eur J Pharmacol (1996) 317: 417-23 [PMID:8997630]
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-CT from human 5-HT7R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method	B	5	pKi	>10000	nM	Ki	Eur J Med Chem (2018) 145: 790-804 [PMID:29407591]
ChEMBL	Binding affinity to serotonin 5-HT7 receptor (unknown origin) by PDSP assay	B	7	pKi	100	nM	Ki	Medchemcomm (2012) 3: 580-583
ChEMBL	Displacement of [3H]-5-CT from human 5HT7 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method	B	7.32	pKi	48.4	nM	Ki	Eur J Med Chem (2019) 179: 1-15 [PMID:31229883]
ChEMBL	Inhibition of [3H]5-HT binding to human 5-hydroxytryptamine 7 receptor	B	7.32	pKi	48	nM	Ki	J Med Chem (2005) 48: 1709-1712 [PMID:15771415]
ChEMBL	Displacement of [3H]-5-CT from human 5HT7 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method	B	7.32	pKi	47.86	nM	Ki	Eur J Med Chem (2019) 179: 1-15 [PMID:31229883]
ChEMBL	Displacement of [3H]-5-CT from human recombinant 5-HT7B receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting method	B	7.32	pKi	47.4	nM	Ki	Eur J Med Chem (2019) 170: 261-275 [PMID:30904783]
ChEMBL	Displacement of [3H]-CT from human 5-HT7 receptor expressed in HEK293 cells after 1 hr by microbeta plate reader analysis	B	7.34	pKi	45.5	nM	Ki	Eur J Med Chem (2020) 185: 111857-111857 [PMID:31734022]
ChEMBL	Displacement of [3H]-5-CT from 5-HT7b receptor (unknown origin)	B	7.34	pKi	45.5	nM	Ki	ACS Med Chem Lett (2017) 8: 390-394 [PMID:28435524]
ChEMBL	Displacement of [3H]5-HT from human 5-hydroxytryptamine 7 receptor	B	7.4	pKi	40	nM	Ki	J Med Chem (2003) 46: 2795-2812 [PMID:12825922]
ChEMBL	Displacement of [3H]5CT from 5HT7 receptor	B	7.4	pKi	39.81	nM	Ki	Bioorg Med Chem Lett (2010) 20: 2465-2468 [PMID:20346662]
ChEMBL	Displacement of [3H]LSD from human recombinant 5-HT7 receptor expressed in HEK cell membranes by radioligand binding assay	B	7.43	pKi	37	nM	Ki	J Nat Prod (2015) 78: 722-729 [PMID:25695425]
ChEMBL	Displacement of [3H]-5-CT from human recombinant 5-HT7 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysis	B	7.6	pKi	25	nM	Ki	Eur J Med Chem (2014) 78: 324-339 [PMID:24691057]
ChEMBL	Displacement of [3H]LSD from human 5HT7 receptor expressed in CHO cells	B	7.7	pKi	19.95	nM	Ki	J Med Chem (2007) 50: 5103-5108 [PMID:17880057]
ChEMBL	Displacement of [3H]-5-CT from human 5HT7 receptor expressed in HEK293 cells measured after 1 hr by microbeta counting method	B	7.74	pKi	18	nM	Ki	Eur J Med Chem (2020) 201: 112437-112437 [PMID:32673902]
ChEMBL	Displacement of [3H]-5-CT from human 5-HT7b receptor expressed in HEK293 cells after 1 hr	B	7.74	pKi	18	nM	Ki	Eur J Med Chem (2012) 56: 348-360 [PMID:22926225]
ChEMBL	Displacement of [3H]5-CT from human 5HT7b receptor expressed in HEK293 cells after 1 hr	B	7.74	pKi	18	nM	Ki	Bioorg Med Chem Lett (2013) 23: 4419-4423 [PMID:23787101]
ChEMBL	Displacement of [3H]]-5-CT from human cloned 5-HT7R expressed in HEK293 cells	B	7.74	pKi	18	nM	Ki	Bioorg Med Chem (2015) 23: 212-221 [PMID:25435254]
ChEMBL	Displacement of [3H]-5-CT from human 5-HT7 receptor expressed in HEK293 cells	B	7.74	pKi	18	nM	Ki	Eur J Med Chem (2016) 112: 258-269 [PMID:26900658]
ChEMBL	Displacement of [3H]-5-CT from human 5HT7BR expressed in HEK293 cell membranes after 1 hr by Microbeta scintillation counting method	B	7.74	pKi	18	nM	Ki	Eur J Med Chem (2018) 147: 102-114 [PMID:29425815]
ChEMBL	Displacement of [3H]-5-carboxamidotryptamine from human 5-HT7B receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting method	B	7.74	pKi	18	nM	Ki	Medchemcomm (2018) 9: 1033-1044 [PMID:30108992]
ChEMBL	Displacement of [3H]-5-CT from human 5-HT7R expressed in human HEK293 cells assessed as inhibitory constant incubated for 1 hr by radioligand binding assay	B	7.74	pKi	18	nM	Ki	Eur J Med Chem (2019) 178: 740-751 [PMID:31229876]
ChEMBL	Displacement of [3H]-5-CT from human 5HT7 receptor expressed in HEK cells incubated for 1 hr by Cheng-Prusoff analysis based microbeta scintillation counting method	B	7.74	pKi	18	nM	Ki	Eur J Med Chem (2019) 180: 383-397 [PMID:31325785]
ChEMBL	Displacement of [3H]-5-CT from recombinant human 5HT7 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting analysis	B	7.74	pKi	18	nM	Ki	Eur J Med Chem (2019) 166: 144-158 [PMID:30703658]
GtoPdb	-	-	7.8	pKi	-	-	-	Psychopharmacology (Berl.) (2005) 179: 461-9 [PMID:15821958]; Naunyn Schmiedebergs Arch Pharmacol (2001) 363: 620-32 [PMID:11414657]; Br J Pharmacol (1998) 124: 1300-6 [PMID:9720804]
ChEMBL	Non-selective inhibitory activity was determined against 5-hydroxytryptamine 7 receptor	B	7.9	pKi	12.59	nM	Ki	J Med Chem (2003) 46: 5638-5650 [PMID:14667218]
ChEMBL	Displacement of [3H]-LSD from human 5-HT7A receptor expresssed in stable HEK cell membrane incubated for 90 mins by microbeta counting method	B	7.94	pKi	11.4	nM	Ki	Bioorg Med Chem (2020) 28: 115578-115578 [PMID:32631561]
ChEMBL	Compound was evaluated for its binding affinity towards human 5-hydroxytryptamine 7 receptor	B	8.05	pKi	9	nM	Ki	J Med Chem (2000) 43: 1011-1018 [PMID:10715164]
ChEMBL	Displacement of [3H]LSD from 5-HT7 receptor (unknown origin)	B	8.23	pKi	5.89	nM	Ki	Bioorg Med Chem Lett (2014) 24: 576-579 [PMID:24365159]
ChEMBL	Displacement of [3H]LSD from 5-HT7 receptor (unknown origin)	B	8.26	pKi	5.5	nM	Ki	Bioorg Med Chem Lett (2014) 24: 576-579 [PMID:24365159]
5-HT7 receptor in Mouse [GtoPdb: 12] [UniProtKB: P32304]
GtoPdb	-	-	7.4	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	Displacement of [3H]-5-CT from 5-HT7 receptor in rat hypothalamus homogenates after 120 mins by liquid scintillation counting	B	7.2	pKi	62.6	nM	Ki	Bioorg Med Chem Lett (2015) 25: 5299-5305 [PMID:26483200]
ChEMBL	Binding affinity towards 5-hydroxytryptamine 7 receptor	B	7.9	pKi	12.59	nM	Ki	Bioorg Med Chem Lett (2000) 10: 1097-1100 [PMID:10843226]
GtoPdb	-	-	8.2	pKi	-	-	-	Eur J Pharmacol (1996) 317: 417-23 [PMID:8997630]; J Pharmacol Exp Ther (1994) 268: 1403-10 [PMID:7908055]; J Biol Chem (1993) 268: 18200-4 [PMID:8394362]; Proc Natl Acad Sci USA (1993) 90: 8547-51 [PMID:8397408]
ChEMBL	Binding affinity towards rat 5-hydroxytryptamine 7 receptor	B	8.2	pKi	6.3	nM	Ki	J Med Chem (2003) 46: 2795-2812 [PMID:12825922]
SERT/Serotonin transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL228] [GtoPdb: 928] [UniProtKB: P31645]
ChEMBL	Binding affinity to human SERT	B	5.41	pKi	3900	nM	Ki	Bioorg Med Chem (2008) 16: 7291-7301 [PMID:18595716]
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	6.54	pKi	290	nM	Ki	DrugMatrix in vitro pharmacology data
ChEMBL	Inhibition of 5-HT uptake at SERT (unknown origin)	B	5	pIC50	>10000	nM	IC50	Med Chem Res (2013) 22: 520-530
ChEMBL	DRUGMATRIX: Transporter, Serotonin (5-Hydroxytryptamine) (SERT) radioligand binding (ligand: [3H] Paroxetine)	B	6.26	pIC50	546	nM	IC50	DrugMatrix in vitro pharmacology data
SERT/Serotonin transporter in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL313] [GtoPdb: 928] [UniProtKB: P31652]
ChEMBL	Inhibitory concentration against reuptake of 5-HT from rat synaptosomes	F	5	pIC50	>10000	nM	IC50	Bioorg Med Chem Lett (2004) 14: 4263-4266 [PMID:15261283]
sigma non-opioid intracellular receptor 1/Sigma opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL287] [GtoPdb: 2552] [UniProtKB: Q99720]
ChEMBL	Compound was tested for its binding affinity towards sigma 1 receptor using [3H](+)-pentazocine from guinea pig brain	B	5.07	pKi	8500	nM	Ki	J Med Chem (1998) 41: 1557-1560 [PMID:9572880]
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	5.07	pKi	8500	nM	Ki	J Med Chem (1998) 41: 5402-5409 [PMID:9876110]
sigma non-opioid intracellular receptor 1/Sigma opioid receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3602] [GtoPdb: 2552] [UniProtKB: Q9R0C9]
ChEMBL	Compound was tested in vitro for its ability to displace radioligand (+)-[3H]-3-PPP from rat cortical sigma receptor	B	6	pIC50	>1000	nM	IC50	J Med Chem (1992) 35: 4516-4525 [PMID:1361578]
Transporter in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6184] [UniProtKB: Q63380]
ChEMBL	Binding affinity to rat NET	B	6.41	pKi	390	nM	Ki	Bioorg Med Chem (2008) 16: 7291-7301 [PMID:18595716]
5-HT1F receptor in Human [GtoPdb: 5] [UniProtKB: P30939]
GtoPdb	-	-	6.9	pKi	-	-	-	Psychopharmacology (Berl.) (1996) 124: 57-73 [PMID:8935801]
Kir3.2 in Mouse [GtoPdb: 435] [UniProtKB: P48542]
GtoPdb	-	-	3.8	pEC50	-	-	-	Br J Pharmacol (2000) 129: 1716-22 [PMID:10780978]

ChEMBL data shown on this page come from version 33:

Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
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]