haloperidol [Ligand Id: 86] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL54 (Dolpin, Dozic, Fortunan, Haldol, Haldol solutab, Haloperidol, Haloperidol decanoate impurity, haloperidol-, Kentace, Keselen, MCN-JR-1625, NSC-170973, NSC-615296, R-1625, Serenace)
  • 3-beta-hydroxysteroid-delta(8),delta(7)-isomerase in Human [ChEMBL: CHEMBL4931] [UniProtKB: Q15125]
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  • 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]
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  • α1B-adrenoceptor/Alpha-1b adrenergic receptor in Rat [ChEMBL: CHEMBL315] [GtoPdb: 23] [UniProtKB: P15823]
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  • α1D-adrenoceptor/Alpha-1d adrenergic receptor in Human [ChEMBL: CHEMBL223] [GtoPdb: 24] [UniProtKB: P25100]
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  • α2A-adrenoceptor/Alpha-2a adrenergic receptor in Human [ChEMBL: CHEMBL1867] [GtoPdb: 25] [UniProtKB: P08913]
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  • α2B-adrenoceptor/Alpha-2b adrenergic receptor in Human [ChEMBL: CHEMBL1942] [GtoPdb: 26] [UniProtKB: P18089]
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  • α2C-adrenoceptor/Alpha-2c adrenergic receptor in Human [ChEMBL: CHEMBL1916] [GtoPdb: 27] [UniProtKB: P18825]
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  • β1-adrenoceptor/Beta-1 adrenergic receptor in Rat [ChEMBL: CHEMBL3252] [GtoPdb: 28] [UniProtKB: P18090]
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  • β2-adrenoceptor/Beta-2 adrenergic receptor in Rat [ChEMBL: CHEMBL3754] [GtoPdb: 29] [UniProtKB: P10608]
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  • C-8 sterol isomerase in Saccharomyces cerevisiae S288c [ChEMBL: CHEMBL3224] [UniProtKB: P32352]
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  • Dopamine D2 receptor in Chlorocebus aethiops [ChEMBL: CHEMBL5456] [UniProtKB: P52702]
  • D2 receptor/Dopamine D2 receptor in Human [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416]
  • Dopamine D2 receptor in Bovine [ChEMBL: CHEMBL3998] [UniProtKB: P20288]
  • D2 receptor/Dopamine D2 receptor in Rat [ChEMBL: CHEMBL339] [GtoPdb: 215] [UniProtKB: P61169]
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  • 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]
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  • 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]
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  • D5 receptor/Dopamine D5 receptor in Human [ChEMBL: CHEMBL1850] [GtoPdb: 218] [UniProtKB: P21918]
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  • 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]
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  • H2 receptor/Histamine H2 receptor in Human [ChEMBL: CHEMBL1941] [GtoPdb: 263] [UniProtKB: P25021]
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  • HLA class I histocompatibility antigen A-3 in Human [ChEMBL: CHEMBL2632] [UniProtKB: P04439]
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  • Human immunodeficiency virus type 1 protease in Human immunodeficiency virus 1 [ChEMBL: CHEMBL243] [UniProtKB: Q72874]
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  • Human rhinovirus A protease in Human rhinovirus sp. [ChEMBL: CHEMBL2857] [UniProtKB: Q4U254]
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  • μ receptor/Mu opioid receptor in Human [ChEMBL: CHEMBL233] [GtoPdb: 319] [UniProtKB: P35372]
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  • 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]
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  • M2 receptor/Muscarinic acetylcholine receptor M2 in Rat [ChEMBL: CHEMBL309] [GtoPdb: 14] [UniProtKB: P10980]
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  • M5 receptor/Muscarinic acetylcholine receptor M5 in Human [ChEMBL: CHEMBL2035] [GtoPdb: 17] [UniProtKB: P08912]
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  • NET/Norepinephrine transporter in Human [ChEMBL: CHEMBL222] [GtoPdb: 926] [UniProtKB: P23975]
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  • K2P2.1/Potassium channel subfamily K member 2 in Human [ChEMBL: CHEMBL2321615] [GtoPdb: 514] [UniProtKB: O95069]
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  • 5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Human [ChEMBL: CHEMBL214] [GtoPdb: 1] [UniProtKB: P08908]
  • 5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Rat [ChEMBL: CHEMBL273] [GtoPdb: 1] [UniProtKB: P19327]
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  • 5-HT1B receptor/Serotonin 1b (5-HT1b) receptor in Rat [ChEMBL: CHEMBL3459] [GtoPdb: 2] [UniProtKB: P28564]
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  • 5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Human [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223]
  • Serotonin 2a (5-HT2a) receptor in Pig [ChEMBL: CHEMBL2490] [UniProtKB: P50129]
  • Serotonin 2a (5-HT2a) receptor in Bovine [ChEMBL: CHEMBL3446] [UniProtKB: Q75Z89]
  • 5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Rat [ChEMBL: CHEMBL322] [GtoPdb: 6] [UniProtKB: P14842]
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  • 5-HT2B receptor/Serotonin 2b (5-HT2b) receptor in Human [ChEMBL: CHEMBL1833] [GtoPdb: 7] [UniProtKB: P41595]
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  • 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]
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  • 5-HT3A/Serotonin 3a (5-HT3a) receptor in Mouse [ChEMBL: CHEMBL4972] [GtoPdb: 373] [UniProtKB: P23979]
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  • 5-HT6 receptor/Serotonin 6 (5-HT6) receptor in Human [ChEMBL: CHEMBL3371] [GtoPdb: 11] [UniProtKB: P50406]
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  • 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]
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  • 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]
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  • Vesicular acetylcholine transporter in Rat [ChEMBL: CHEMBL2125] [GtoPdb: 1013] [UniProtKB: Q62666]
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  • 5-HT1D receptor in Human [GtoPdb: 3] [UniProtKB: P28221]
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  • Kir3.2 in Mouse [GtoPdb: 435] [UniProtKB: P48542]
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  • Kv10.1 in Human [GtoPdb: 570] [UniProtKB: O95259]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
3-beta-hydroxysteroid-delta(8),delta(7)-isomerase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4931] [UniProtKB: Q15125]
ChEMBL Affinity for human EMP expressed in ERG2 deficient strain of Saccharomyces cerevisiae using [3H]ifenprodil or (+)-[3H]pentazocine as radioligand B 6.72 pKi 190 nM Ki J Med Chem (2005) 48: 4754-4764 [PMID:16033255]
α1A-adrenoceptor/Alpha-1a adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL229] [GtoPdb: 22] [UniProtKB: P35348]
ChEMBL Binding Assay: Binding assay using 5-HT2A, Dopamine D2, SERT, αA1, 5-HT2C and H1 Receptors. B 7.96 pKi 11 nM Ki US-8598119-B2. Methods and compositions for sleep disorders and other disorders (2013)
Alpha-1a adrenergic receptor in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4892] [UniProtKB: P18130]
ChEMBL Affinity towards Alpha-1A adrenergic receptor in membranes from bovine frontal cortex using [3H]prazosin B 7.7 pIC50 20 nM IC50 J Med Chem (1998) 41: 2010-2018 [PMID:9622542]
α1A-adrenoceptor/Alpha-1a adrenergic receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL319] [GtoPdb: 22] [UniProtKB: P43140]
ChEMBL Binding affinity towards Alpha-1A adrenergic receptor in rat denuded thoracic aorta B 7.76 pKd 17.38 nM Kd Bioorg Med Chem Lett (2003) 13: 175-178 [PMID:12482418]
ChEMBL DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin) B 7.55 pKi 28 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin) B 7.17 pIC50 68 nM IC50 DrugMatrix in vitro pharmacology data
α1B-adrenoceptor/Alpha-1b adrenergic receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL315] [GtoPdb: 23] [UniProtKB: P15823]
ChEMBL DRUGMATRIX: Alpha-1B adrenergic receptor radioligand binding (ligand: prazosin) B 8.31 pKi 4.95 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Alpha-1B adrenergic receptor radioligand binding (ligand: prazosin) B 8.05 pIC50 8.94 nM IC50 DrugMatrix in vitro pharmacology data
α1D-adrenoceptor/Alpha-1d adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL223] [GtoPdb: 24] [UniProtKB: P25100]
ChEMBL DRUGMATRIX: Alpha-1D adrenergic receptor radioligand binding (ligand: prazosin) B 7.39 pKi 41 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Alpha-1D adrenergic receptor radioligand binding (ligand: prazosin) B 7.08 pIC50 84 nM IC50 DrugMatrix in vitro pharmacology data
α2A-adrenoceptor/Alpha-2a adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1867] [GtoPdb: 25] [UniProtKB: P08913]
ChEMBL DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912) B 5.73 pKi 1865 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912) B 5.3 pIC50 4973 nM IC50 DrugMatrix in vitro pharmacology data
α2B-adrenoceptor/Alpha-2b adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1942] [GtoPdb: 26] [UniProtKB: P18089]
ChEMBL DRUGMATRIX: Alpha-2B adrenergic receptor radioligand binding (ligand: Rauwolscine) B 6.21 pKi 618 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Alpha-2B adrenergic receptor radioligand binding (ligand: Rauwolscine) B 5.87 pIC50 1354 nM IC50 DrugMatrix in vitro pharmacology data
α2C-adrenoceptor/Alpha-2c adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1916] [GtoPdb: 27] [UniProtKB: P18825]
ChEMBL DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912) B 6.57 pKi 268 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912) B 5.73 pIC50 1845 nM IC50 DrugMatrix in vitro pharmacology data
AP-2 complex subunit sigma in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1697667] [UniProtKB: P62744]
ChEMBL Displacement of [3H]-DTG from rat sigma2 receptor by liquid scintillation counting B 7.62 pKi 24.2 nM Ki J Med Chem (2011) 54: 1555-1564 [PMID:21348515]
β1-adrenoceptor/Beta-1 adrenergic receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3252] [GtoPdb: 28] [UniProtKB: P18090]
ChEMBL Binding affinity against beta-1 adrenergic receptor in rat brain using [3H]DHA B 5 pIC50 >10000 nM IC50 J Med Chem (1986) 29: 1628-1637 [PMID:2875184]
β2-adrenoceptor/Beta-2 adrenergic receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3754] [GtoPdb: 29] [UniProtKB: P10608]
ChEMBL Binding affinity against beta-2 adrenergic receptor in rat brain using [3H]DHA B 5 pIC50 >10000 nM IC50 J Med Chem (1986) 29: 1628-1637 [PMID:2875184]
C-8 sterol isomerase in Saccharomyces cerevisiae S288c (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3224] [UniProtKB: P32352]
ChEMBL Affinity for ERG2 of Saccharomyces cerevisiae using [3H]ifenprodil or (+)-[3H]pentazocine radioligand B 9.3 pKi 0.5 nM Ki J Med Chem (2005) 48: 4754-4764 [PMID:16033255]
D1 receptor/Dopamine D1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2056] [GtoPdb: 214] [UniProtKB: P21728]
ChEMBL Binding affinity towards human Dopamine receptor D1 B 6.57 pKi 270 nM Ki J Med Chem (2004) 47: 1303-1314 [PMID:14998318]
ChEMBL Displacement of [3H]SCH23390 from human dopamine D1 receptor by liquid scintillation counting B 6.92 pKi 120 nM Ki Bioorg Med Chem Lett (2014) 24: 4294-4297 [PMID:25070422]
ChEMBL Binding affinity to human cloned dopamine D1 receptor B 6.92 pKi 120 nM Ki Bioorg Med Chem (2008) 16: 7291-7301 [PMID:18595716]
ChEMBL Inhibition of human dopamine D1 receptor B 6.97 pKi 107 nM Ki J Med Chem (2011) 54: 2529-2591 [PMID:21413808]
ChEMBL Binding affinity for human recombinant dopamine receptor D1 B 7.09 pKi 82 nM Ki J Med Chem (2004) 47: 4155-4158 [PMID:15293986]
ChEMBL DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390) B 7.26 pKi 55 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL Compound was tested for the binding affinity against human cloned Dopamine receptor D1 by radioligand ([3H]SCH-23390) binding assay B 7.31 pKi 49 nM Ki J Med Chem (1996) 39: 2764-2772 [PMID:8709107]
ChEMBL Displacement of [3H]SCH233930 from human D1 receptor expressed in HEK cells B 7.6 pKi 25 nM Ki Bioorg Med Chem Lett (2011) 21: 3622-3626 [PMID:21555222]
GtoPdb - - 8.2 pKi - - - Nature (1991) 350: 614-9 [PMID:1826762];
J Psychopharmacol (Oxford) (2009) 23: 65-73 [PMID:18308814]
ChEMBL Displacement of [3H]SCH23390 from human dopamine D1 receptor B 8.21 pKi 6.17 nM Ki Bioorg Med Chem Lett (2009) 19: 6059-6062 [PMID:19796944]
ChEMBL DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390) B 6.96 pIC50 110 nM IC50 DrugMatrix in vitro pharmacology data
Dopamine D1 receptor in Pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5067] [UniProtKB: P50130]
ChEMBL Displacement of [3H]SCH23390 from dopamine D1 receptor in pig striatal membranes B 7.01 pKi 98 nM Ki J Med Chem (2010) 53: 7219-7228 [PMID:20839776]
ChEMBL Displacement of [3H]SCH23390 from D1 receptor from porcine cerebral cortex homogenates B 7.03 pKi 93 nM Ki J Med Chem (2011) 54: 4896-4903 [PMID:21599022]
ChEMBL Displacement of [3H]SCH 23390 from pig dopamine D1 receptor in striatal membrane B 7.03 pKi 93 nM Ki J Med Chem (2011) 54: 7911-7919 [PMID:21999579]
ChEMBL Displacement of [3H]SCH23390 from porcine striatal membranes D1 receptor by competitive binding assay B 8.02 pKi 9.5 nM Ki Bioorg Med Chem Lett (2014) 24: 3753-3756 [PMID:25047579]
D1 receptor/Dopamine D1 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL265] [GtoPdb: 214] [UniProtKB: P18901]
ChEMBL Tested for binding affinity towards rat striatal dopamine receptor D1 using [3H]-SCH- 23390 as radioligand B 6.33 pKi 467 nM Ki J Med Chem (1994) 37: 3523-3533 [PMID:7932581]
ChEMBL Inhibition of [3H]SCH-23390 binding to rat Dopamine receptor D1 B 6.44 pKi 359 nM Ki J Med Chem (2005) 48: 1709-1712 [PMID:15771415]
ChEMBL Binding affinity to dopamine D1 receptor in rat striatum by liquid scintillation counting method B 6.5 pKi 318 nM Ki J Med Chem (2018) 61: 372-384 [PMID:29220177]
ChEMBL Displacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometry B 6.5 pKi 318 nM Ki J Med Chem (2009) 52: 151-169 [PMID:19072656]
ChEMBL Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate B 6.5 pKi 318 nM Ki J Med Chem (2002) 45: 344-359 [PMID:11784139]
ChEMBL Inhibition of [3H]-SCH- 23390 binding to rat dopamine D1 receptor B 6.5 pKi 318 nM Ki J Med Chem (2005) 48: 1705-1708 [PMID:15771414]
ChEMBL In vitro binding affinity towards Dopamine receptor D1 in rat tissue homogenate using [3H]-SCH- 23390 as radioligand B 6.5 pKi 318 nM Ki J Med Chem (2004) 47: 143-157 [PMID:14695828]
ChEMBL Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate B 6.5 pKi 316.23 nM Ki J Med Chem (2002) 45: 344-359 [PMID:11784139]
ChEMBL In vitro affinity against Dopamine receptor D1 B 6.7 pKi 199.53 nM Ki J Med Chem (2000) 43: 4678-4693 [PMID:11101359]
ChEMBL In vitro ability to displace [3H]SCH-23390 binding from Dopamine 1 (D1) receptor in rat striatal membrane. B 6.8 pKi 158.49 nM Ki J Med Chem (1999) 42: 2774-2797 [PMID:10425088]
ChEMBL Binding affinity measured at the Dopamine receptor D1 by the inhibition of [3H]SCH-23390 binding to rat striatum using unlabeled apomorphine for nonspecific binding. B 6.84 pKi 145 nM Ki J Med Chem (1998) 41: 5402-5409 [PMID:9876110]
ChEMBL Inhibition constant for in vitro inhibition of [3H]-SCH- 23390 binding to striatal membranes Dopamine receptor D1 B 7.01 pKi 97.72 nM Ki Bioorg Med Chem Lett (1995) 5: 579-584
ChEMBL Compound was evaluated for its affinity (pKi) to inhibit [3H]SCH-23390 binding to the Dopamine receptor D1 B 7.01 pKi 97.72 nM Ki J Med Chem (1991) 34: 2242-2247 [PMID:1676759]
ChEMBL Inhibition of [3H]-SCH- 23390 binding to dopamine receptor D1 rat striatal membrane B 7.01 pKi 97.72 nM Ki J Med Chem (1994) 37: 2564-2573 [PMID:7914540]
ChEMBL In vitro binding affinity against Dopamine receptor D1 in rat striatal tissue B 7.12 pKi 76 nM Ki J Med Chem (1993) 36: 2107-2114 [PMID:8101877]
ChEMBL Binding affinity against dopamine receptor D1 B 7.12 pKi 75.86 nM Ki J Med Chem (1994) 37: 519-525 [PMID:7907148]
ChEMBL Binding Affinity was determined against Dopamine receptor D1 in rat striatal membranes using [3H]- SCH 23390 radioligand. B 7.15 pKi 70.79 nM Ki J Med Chem (2000) 43: 599-608 [PMID:10691686]
ChEMBL Displacement of [3H]SCH-23390 from dopamine D1 receptor in rat brain B 7.24 pKi 58.08 nM Ki Bioorg Med Chem (2007) 15: 7361-7367 [PMID:17869521]
ChEMBL Binding affinity was measured against dopamine receptor D1 in rat using [3H]SCH-23390 as radioligand B 7.33 pKi 47 nM Ki J Med Chem (1994) 37: 1964-1970 [PMID:8027978]
ChEMBL Ability to displace [3H]-SCH- 23390 (0.2 nM) from corpus striatum of rat Dopamine receptor D1 B 7.54 pKi 29 nM Ki J Med Chem (2003) 46: 265-283 [PMID:12519065]
ChEMBL Binding affinity towards Dopamine receptor D1 B 7.62 pKi 24 nM Ki J Med Chem (1987) 30: 1433-1454 [PMID:3039136]
ChEMBL Affinity for Dopamine receptor D1 B 7.7 pKi 20 nM Ki Bioorg Med Chem Lett (1998) 8: 983-988 [PMID:9871525]
ChEMBL Inhibitory concentration against rat striatal dopamine (D1) sensitive adenylate cyclase activity F 6.26 pIC50 550 nM IC50 J Med Chem (1987) 30: 1906-1910 [PMID:2888899]
ChEMBL Binding affinity towards Dopamine receptor D1 in rat membranes using [3H]SCH-23390 as radioligand B 6.47 pIC50 337 nM IC50 J Med Chem (1991) 34: 3360-3365 [PMID:1662725]
ChEMBL Binding affinity towards D1 CNS receptor of rat corpus striatum using [3H]SCH-23390 as radioligand B 7.44 pIC50 36 nM IC50 J Med Chem (1999) 42: 2235-2244 [PMID:10377229]
ChEMBL Inhibitory binding of [3H]SCH-23390 to Dopamine receptor D1 in membranes from rat corpus striatum B 7.44 pIC50 36 nM IC50 J Med Chem (1997) 40: 4146-4153 [PMID:9406603]
Dopamine D2 receptor in Chlorocebus aethiops (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5456] [UniProtKB: P52702]
ChEMBL Displacement of [3H]-YM 09151 from african green monkey Dopamine receptor D2 B 8.3 pKi 5 nM Ki J Med Chem (1995) 38: 4950-4952 [PMID:8523409]
ChEMBL Displacement of [3H]YM-09151 from recombinant African green monkey Dopamine receptor D2 B 8.32 pKi 4.8 nM Ki J Med Chem (1995) 38: 2251-2255 [PMID:7783157]
D2 receptor/Dopamine D2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416]
ChEMBL Displacement of PPHT-red from SNAP-tagged human D2LR expressed in CHOK1 cell membranes by TR-FRET assay B 9.31 pKd 0.49 nM Kd J Med Chem (2019) 62: 9488-9520 [PMID:31580666]
ChEMBL Displacement of [3H]spiroperidol from human cloned dopaminergic D2 receptor expressed in rat C6 cells B 5.19 pKi 6400 nM Ki J Med Chem (2008) 51: 7602-7613 [PMID:19053888]
ChEMBL Tested for affinity against cloned mammalian dopamine autoreceptor (DA) D2 receptors expressed in CHO-K1 cells using [3H]spiperone as radioligand B 6.66 pKi >217 nM Ki J Med Chem (1994) 37: 2735-2753 [PMID:8064801]
ChEMBL Displacement of the radioligand [3H]spiperone from the cloned human Dopamine receptor D2 long expressed in CHO cells B 7.74 pKi 18 nM Ki Bioorg Med Chem Lett (2002) 12: 1327-1330 [PMID:11992769]
ChEMBL Displacement of [3H]N-methylspiperone from human dopamine D2 receptor by PDSP assay B 8.02 pKi 9.6 nM Ki Bioorg Med Chem (2016) 24: 2060-2071 [PMID:27032890]
ChEMBL In vitro binding affinity at human cloned Dopamine receptor D2L expressed in Sf9 cell membranes B 8.07 pKi 8.5 nM Ki J Med Chem (2002) 45: 5136-5149 [PMID:12408724]
ChEMBL Antagonism of dopamine-stimulated [35S]GTP-gamma-S binding against human Dopamine receptor D2 in CHO cells F 8.15 pKi 7 nM Ki J Med Chem (2000) 43: 3923-3932 [PMID:11052797]
ChEMBL Displacement of [3H]-N-methylspiperone from D2 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method B 8.2 pKi 6.33 nM Ki J Med Chem (2021) 64: 17239-17258 [PMID:34797051]
ChEMBL Displacement of [3H]-N-methylspiperone from D2 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method B 8.2 pKi 6.31 nM Ki J Med Chem (2021) 64: 17239-17258 [PMID:34797051]
ChEMBL Displacement of [3H]spiperone from human D2S receptor expressed in CHO-K1 cells by radioligand competitive binding analysis B 8.21 pKi 6.22 nM Ki J Nat Prod (2020) 83: 127-133 [PMID:31933369]
ChEMBL Displacement of [3H]spiperone from human D2S receptor expressed in CHO-K1 cells by radioligand competitive binding analysis B 8.21 pKi 6.17 nM Ki J Nat Prod (2020) 83: 127-133 [PMID:31933369]
ChEMBL Displacement of [3H]methylspiperonee from recombinant human D2 receptor expressed in HEK293 cells cell membranes after 60 mins by liquid scintillation counting method B 8.23 pKi 5.9 nM Ki Bioorg Med Chem Lett (2018) 28: 2039-2049 [PMID:29730027]
ChEMBL In vitro binding affinity towards Dopamine receptor D2L, using [3H]spiroperidol radioligand in Sf9 baculovirus expression. B 8.25 pKi 5.6 nM Ki J Med Chem (2000) 43: 270-277 [PMID:10649982]
ChEMBL Displacement of [3H]-N-Methylspiperone from human dopamine D2 receptor expressed in stable fibroblast cells incubated for 90 mins by microbeta counting method B 8.25 pKi 5.58 nM Ki Bioorg Med Chem (2020) 28: 115578-115578 [PMID:32631561]
ChEMBL Displacement of [3H]N-methylspiperone from dopamine D2 receptor (unknown origin) B 8.25 pKi 5.58 nM Ki Bioorg Med Chem Lett (2020) 30: 127305-127305 [PMID:32631525]
ChEMBL Displacement of [3H]YM-09151-2 from human dopamine D2S receptor in membrane suspensions by liquid scintillation counter B 8.29 pKi 5.09 nM Ki Bioorg Med Chem (2008) 16: 8875-8881 [PMID:18793859]
ChEMBL Displacement of [3H]spiperone from human dopamine D2 receptor short form expressed in CHO cells B 8.3 pKi 5.01 nM Ki J Med Chem (2007) 50: 5103-5108 [PMID:17880057]
ChEMBL Binding affinity on human Dopamine receptor D2 expressed in CHO cells using radioligand [3H]-YM 09151 B 8.32 pKi 4.8 nM Ki J Med Chem (1997) 40: 1-3 [PMID:9016321]
ChEMBL Displacement of [3H]-raclopride from human D2 receptor expressed in HEK cells incubated for 1 hr by Cheng-Prusoff analysis based microbeta scintillation counting method B 8.35 pKi 4.5 nM Ki Eur J Med Chem (2019) 180: 383-397 [PMID:31325785]
ChEMBL Displacement of [3H]-raclopride from recombinant human D2 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting analysis B 8.35 pKi 4.5 nM Ki Eur J Med Chem (2019) 166: 144-158 [PMID:30703658]
ChEMBL Displacement of [3H]spiroperidol from human cloned dopamine D2L receptor by liquid scintillation counting B 8.38 pKi 4.2 nM Ki Bioorg Med Chem (2009) 17: 758-766 [PMID:19081257]
ChEMBL Displacement of [3H]spiroperidol from human cloned dopamine D2L receptor expressed in rat C6 cells B 8.38 pKi 4.2 nM Ki J Med Chem (2008) 51: 5813-5822 [PMID:18800769]
ChEMBL Displacement of [3H]N-methylspiperone from human recombinant D2 receptor expressed in CHO-K1 cell membrane after 60 mins by liquid scintillation counting analysis B 8.4 pKi 4 nM Ki J Med Chem (2014) 57: 4543-4557 [PMID:24805037]
ChEMBL Displacement of [3H]N-methylspiperone from human recombinant dopamine D2 receptor expressed in CHOK1 cells incubated for 60 mins by scintillation counting method B 8.4 pKi 4 nM Ki Eur J Med Chem (2015) 92: 221-235 [PMID:25557493]
ChEMBL In vitro binding affinity towards Dopamine receptor D2 in human using [3H]-spiperone as radioligand B 8.43 pKi 3.7 nM Ki J Med Chem (2004) 47: 143-157 [PMID:14695828]
ChEMBL Potency was measured by the displacement of [3H]spiperone binding to human D2 dopaminergic receptor B 8.44 pKi 3.6 nM Ki Bioorg Med Chem Lett (1997) 7: 1207-1212
ChEMBL Displacement of [3H]-N-methylspiperone from human dopamine D2 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysis B 8.45 pKi 3.55 nM Ki J Med Chem (2021) 64: 7778-7808 [PMID:34011153]
ChEMBL Displacement of [3H]N-Methylspiperone from dopamine D2 receptor (unknown origin) B 8.45 pKi 3.55 nM Ki Bioorg Med Chem Lett (2014) 24: 576-579 [PMID:24365159]
ChEMBL Displacement of [3H]N-Methylspiperone from dopamine D2 receptor (unknown origin) B 8.46 pKi 3.5 nM Ki Bioorg Med Chem Lett (2014) 24: 576-579 [PMID:24365159]
ChEMBL Displacement of [3H]spiperone from human cloned dopamine receptor D2 long expressed in CHO cells B 8.48 pKi 3.3 nM Ki Eur J Med Chem (2007) 42: 1044-1048 [PMID:17316913]
ChEMBL Displacement of [3H]Spiperone from human D2S receptor expressed in CHOK1 cell membranes measured after 120 mins B 8.49 pKi 3.25 nM Ki Eur J Med Chem (2019) 180: 673-689 [PMID:31357129]
ChEMBL Displacement of [3H]spiperone form human dopamine D2 receptor by liquid scintillation counting B 8.52 pKi 3 nM Ki Bioorg Med Chem Lett (2010) 20: 2983-2986 [PMID:20347298]
ChEMBL Displacement of [3H]raclopride from human D2L receptor expressed in CHO cells after 60 mins by scintillation proximity assay B 8.52 pKi 3 nM Ki Bioorg Med Chem Lett (2012) 22: 5134-5140 [PMID:22677319]
ChEMBL In vitro binding affinity at human cloned dopamine receptor D2 (long) stably expressed in CHO cells by [3H]spiperone displacement. B 8.52 pKi 3 nM Ki Bioorg Med Chem Lett (2003) 13: 405-408 [PMID:12565939]
ChEMBL Displacement of [3H]spiperone from D2 receptor B 8.52 pKi 3 nM Ki Bioorg Med Chem Lett (2009) 19: 5552-5555 [PMID:19720528]
ChEMBL Inhibition of human dopamine D2 receptor B 8.55 pKi 2.84 nM Ki J Med Chem (2011) 54: 2529-2591 [PMID:21413808]
ChEMBL Displacement of [3H]spiroperidol from human cloned dopamine D2L receptor B 8.59 pKi 2.6 nM Ki J Med Chem (2007) 50: 5043-5047 [PMID:17850060]
ChEMBL Inhibition of [3H]-spiperone binding to human Dopamine receptor D2 B 8.6 pKi 2.5 nM Ki J Med Chem (2005) 48: 1709-1712 [PMID:15771415]
ChEMBL Binding affinity for human recombinant dopamine D2 receptor B 8.66 pKi 2.2 nM Ki J Med Chem (2004) 47: 4155-4158 [PMID:15293986]
ChEMBL DRUGMATRIX: Dopamine D2L radioligand binding (ligand: [3H] Spiperone) B 8.66 pKi 2.2 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL Displacement of [3H]spiroperidol from human recombinant Dopamine D2 long receptor B 8.7 pKi 2 nM Ki J Med Chem (2007) 50: 4214-4221 [PMID:17649988]
ChEMBL In vitro inhibitory constant against [3H]spiperone binding to human dopamine D2 receptor expressed in CHO cells B 8.7 pKi 2 nM Ki J Med Chem (2005) 48: 6855-6869 [PMID:16250644]
ChEMBL Displacement of [3H]-raclopride from human D2LR expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method B 8.7 pKi 2 nM Ki Eur J Med Chem (2018) 145: 790-804 [PMID:29407591]
ChEMBL Binding affinity to human D2 receptor B 8.71 pKi 1.97 nM Ki Bioorg Med Chem Lett (2020) 30: 127053-127053 [PMID:32107165]
ChEMBL Displacement of [3H]spiperone from human dopamine D2 receptor at low affinity state expressed in HEK293 cells B 8.72 pKi 1.9 nM Ki J Med Chem (2010) 53: 2510-2520 [PMID:20155917]
ChEMBL Displacement of [3H]-methylspiperone from human D2 receptor transfected in CHO-K1 cells measured after 60 mins by scintillation counting method B 8.73 pKi 1.86 nM Ki J Med Chem (2021) 64: 12603-12629 [PMID:34436892]
ChEMBL Displacement of [3H]-methylspiperone from recombinant human D2 receptor expressed in CHOK1 cell membranes measured after 60 mins by microbeta counting method B 8.73 pKi 1.86 nM Ki Eur J Med Chem (2020) 191: 112149-112149 [PMID:32105980]
ChEMBL Ability to displace [3H]spiperone from human cloned Dopamine receptor D2 expressed in CHO K-1 cells in vitro. B 8.8 pKi 1.6 nM Ki J Med Chem (1997) 40: 2688-2693 [PMID:9276014]
ChEMBL Binding affinity against cloned human dopamine receptor D2 expressed in Chinese hamster ovary (CHO) K-1 cells by displacement of [3H]spiperone. B 8.8 pKi 1.6 nM Ki J Med Chem (1997) 40: 4026-4029 [PMID:9406594]
GtoPdb - - 8.8 pKi - - - J Pharmacol Exp Ther (1994) 268: 417-26 [PMID:8301582];
Eur J Pharmacol (1994) 266: 79-85 [PMID:7907989];
Eur J Pharmacol (1992) 225: 331-7 [PMID:1354163];
Eur J Pharmacol (1995) 290: 29-36 [PMID:7664822];
Pharmacol Biochem Behav (1994) 49: 567-71 [PMID:7862709]
ChEMBL Displacement of [3H]spiperone from human DRD2 Long receptor expressed in chinese hamster CHO cells by radioligand binding assay B 8.82 pKi 1.5 nM Ki J Med Chem (2011) 54: 7911-7919 [PMID:21999579]
ChEMBL Binding affinity for Dopamine receptor D2 by displacement of [3H]-spiperone B 8.82 pKi 1.5 nM Ki Bioorg Med Chem Lett (2000) 10: 509-512 [PMID:10743959]
ChEMBL Displacement of [3H]SCH23390 from human D2long receptor expressed in CHO cells B 8.82 pKi 1.5 nM Ki J Med Chem (2011) 54: 4896-4903 [PMID:21599022]
ChEMBL Binding affinity for dopamine receptor D2 determined using [3H]spiperone B 8.85 pKi 1.4 nM Ki Bioorg Med Chem Lett (2001) 11: 2345-2349 [PMID:11527728]
ChEMBL Displacement of [3H]-methylspiperone from human D2 receptor expressed in CHO-K1 cells after 60 mins by scintillation counting B 8.85 pKi 1.4 nM Ki J Med Chem (2017) 60: 7483-7501 [PMID:28763213]
ChEMBL Ability to displace [3H]spiperone from human dopamine receptor D2 stably expressed in CHO cells. B 8.85 pKi 1.4 nM Ki J Med Chem (1997) 40: 2374-2385 [PMID:9240352]
ChEMBL Displacement of [3H]spiperone from human Dopamine receptor D2 expressed in CHO cells B 8.85 pKi 1.4 nM Ki J Med Chem (1996) 39: 1943-1945 [PMID:8642551]
ChEMBL Binding affinity towards human Dopamine receptor D2 B 8.85 pKi 1.4 nM Ki J Med Chem (2004) 47: 1303-1314 [PMID:14998318]
ChEMBL Binding affinity towards cloned human Dopamine receptor D2 stably expressed in CHO cells was evaluated using [3H]spiperone as radioligand B 8.85 pKi 1.4 nM Ki J Med Chem (1996) 39: 1941-1942 [PMID:8642550]
ChEMBL Displacement of [3H]methylspiperone from human D2L receptor expressed in HEK cell membrane after 90 mins by scintillation counting analysis B 8.85 pKi 1.4 nM Ki J Med Chem (2014) 57: 3450-3463 [PMID:24666157]
ChEMBL Binding affinity to human cloned dopamine D2 receptor B 8.85 pKi 1.4 nM Ki Bioorg Med Chem (2008) 16: 7291-7301 [PMID:18595716]
ChEMBL Binding affinity for human dopamine receptor D2 long B 8.89 pKi 1.3 nM Ki J Med Chem (2005) 48: 694-709 [PMID:15689154]
ChEMBL Binding affinity to dopamine D2 B 8.95 pKi 1.12 nM Ki J Med Chem (2007) 50: 489-500 [PMID:17266201]
ChEMBL Displacement of [3H]spiperone from human D2short receptor expressed in CHO cells B 8.96 pKi 1.1 nM Ki J Med Chem (2011) 54: 4896-4903 [PMID:21599022]
ChEMBL Displacement of [3H]N-methylspiperone from human dopamine D2 receptor by liquid scintillation counting B 8.96 pKi 1.1 nM Ki Bioorg Med Chem (2009) 17: 1716-1723 [PMID:19155177]
ChEMBL Displacement of [125I]ABN from human dopamine D2 long receptor expressed in HEK293 cells after 60 mins by gamma counting B 8.96 pKi 1.1 nM Ki Bioorg Med Chem (2010) 18: 5291-5300 [PMID:20542439]
ChEMBL Displacement of [3H]Spiperone from human dopamine D2 long receptor expressed in CHO cells B 8.96 pKi 1.1 nM Ki J Med Chem (2010) 53: 7219-7228 [PMID:20839776]
ChEMBL Displacement of [3H]spiperone from human DRD2 short receptor expressed in chinese hamster CHO cells by radioligand binding assay B 8.96 pKi 1.1 nM Ki J Med Chem (2011) 54: 7911-7919 [PMID:21999579]
ChEMBL Displacement of [3H]N-methylspiperone from human D2 receptor expressed in HEK cells B 9 pKi 1 nM Ki Bioorg Med Chem Lett (2011) 21: 3622-3626 [PMID:21555222]
ChEMBL Binding affinity towards Dopamine type 2 receptor was determined by displacement assays using [3H]-YM 09151 as the competitive ligand B 9 pKi 1 nM Ki Bioorg Med Chem Lett (2002) 12: 3111-3115 [PMID:12372513]
ChEMBL Displacement of [3H]spiperone from human dopamine D2 receptor at high affinity state expressed in HEK293 cells B 9 pKi 1 nM Ki J Med Chem (2010) 53: 2510-2520 [PMID:20155917]
ChEMBL Binding affinity towards mouse LtK- cells transfected with human D2 receptor using [3H]spiperone B 9 pKi 1 nM Ki Bioorg Med Chem Lett (1995) 5: 219-222
ChEMBL Displacement of [3H]spiperone from human dopamine D2L receptor expressed in CHO cells B 9.02 pKi 0.96 nM Ki ACS Med Chem Lett (2015) 6: 882-887 [PMID:26288260]
ChEMBL Cataleptogenic effect against cloned human Dopamine receptor D2 in male Sprague-Dawley rats in a bar test B 9.05 pKi 0.89 nM Ki Bioorg Med Chem Lett (2003) 13: 3779-3782 [PMID:14552778]
ChEMBL Displacement of [3H]spiperone from human Dopamine receptor D2 B 9.05 pKi 9.05 nM pKi J Med Chem (2004) 47: 497-508 [PMID:14736232]
ChEMBL Displacement of [3H]N-methylspiperone from human dopamine D2 receptor by liquid scintillation counting B 9.05 pKi 0.89 nM Ki Bioorg Med Chem Lett (2014) 24: 4294-4297 [PMID:25070422]
ChEMBL In vitro ability to inhibit the binding of [3H]spiperone to cloned human Dopamine receptor D2 using apomorphine induced climbing test in male Swiss mice B 9.05 pKi 0.89 nM Ki Bioorg Med Chem Lett (2003) 13: 3779-3782 [PMID:14552778]
ChEMBL Displacement of [3H]Spiperone from human dopamine D2 short receptor expressed in CHO cells B 9.06 pKi 0.87 nM Ki J Med Chem (2010) 53: 7219-7228 [PMID:20839776]
ChEMBL Displacement of [3H]spiperone from human D2short receptor stably expressed in CHO cell membranes by competitive binding assay B 9.07 pKi 0.85 nM Ki Bioorg Med Chem Lett (2014) 24: 3753-3756 [PMID:25047579]
ChEMBL Displacement of [3H]spiperone from human D2 receptor transfected in HEK cells B 9.07 pKi 0.85 nM Ki J Med Chem (2014) 57: 4368-4381 [PMID:24779610]
ChEMBL In vitro binding affinity against human D2 dopamine receptor in CHO cells by [3H]spiperone displacement. B 9.08 pKi 0.84 nM Ki Bioorg Med Chem Lett (1998) 8: 725-730 [PMID:9871530]
ChEMBL Displacement of [3H]spiperone from human D2long receptor stably expressed in CHO cell membranes by competitive binding assay B 9.09 pKi 0.81 nM Ki Bioorg Med Chem Lett (2014) 24: 3753-3756 [PMID:25047579]
ChEMBL In vitro binding affinity for Dopamine receptor D2 B 9.1 pKi 0.79 nM Ki Bioorg Med Chem Lett (2001) 11: 1313-1316 [PMID:11392544]
ChEMBL Binding Assay: Binding assay using 5-HT2A, Dopamine D2, SERT, αA1, 5-HT2C and H1 Receptors. B 9.15 pKi 0.7 nM Ki US-8598119-B2. Methods and compositions for sleep disorders and other disorders (2013)
ChEMBL Inhibition of [3H]raclopride binding to Dopamine receptor D2 B 9.18 pKi 0.66 nM Ki J Med Chem (1996) 39: 4421-4429 [PMID:8893836]
ChEMBL Displacement of [3H]spiperone from human cloned dopamine D2 receptor B 9.22 pKi 0.6 nM Ki J Med Chem (2008) 51: 6085-6094 [PMID:18783204]
ChEMBL Displacement of [3H]spiperone from human cloned D2 receptor by in vitro binding assay B 9.22 pKi 0.6 nM Ki Medchemcomm (2011) 2: 1194-1200
ChEMBL Binding affinity towards dopamine receptor D2 B 9.22 pKi 0.6 nM Ki Bioorg Med Chem Lett (2004) 14: 585-589 [PMID:14741248]
ChEMBL Displacement of [3H]spiperone from human D2 receptor B 9.22 pKi 0.6 nM Ki Eur J Med Chem (2014) 71: 237-249 [PMID:24316025]
ChEMBL Displacement of [3H]spiperone human cloned dopamine D2 receptor B 9.22 pKi 0.6 nM Ki Bioorg Med Chem Lett (2007) 17: 4873-4877 [PMID:17588750]
ChEMBL Displacement of [3H]spiperone from human cloned dopamine D2 receptor B 9.22 pKi 0.6 nM Ki Bioorg Med Chem Lett (2009) 19: 6059-6062 [PMID:19796944]
ChEMBL Tested for binding affinity towards human D2L receptor using [3H]spiperone as radioligand B 9.3 pKi 0.5 nM Ki J Med Chem (1994) 37: 3523-3533 [PMID:7932581]
ChEMBL Displacement of PPHT-red from SNAP-tagged human D2LR expressed in CHOK1 cell membranes by TR-FRET assay B 9.33 pKi 0.47 nM Ki J Med Chem (2019) 62: 9488-9520 [PMID:31580666]
ChEMBL Displacement of [3H]spiperone from CHO-K1 cell membranes expressing human dopamine receptor D2 B 9.36 pKi 0.44 nM Ki J Med Chem (1993) 36: 3929-3936 [PMID:7902870]
ChEMBL Displacement of [3H]raclopride from human dopamine D2A receptors expressed in LtK cells B 9.36 pKi 0.44 nM Ki Bioorg Med Chem Lett (1999) 9: 2167-2172 [PMID:10465538]
ChEMBL Displacement of [3H]spiperone from human D2long receptor expressed in CHO cell membranes by radioligand binding assay B 9.38 pKi 0.42 nM Ki Bioorg Med Chem (2017) 25: 5084-5094 [PMID:28666858]
ChEMBL Displacement of [3H]N-methylspiperone from human D2L receptor expressed in HEK293T cells co-expressing CRE-Luc incubated for 60 mins by microbeta scintillation counting method B 9.58 pKi 0.26 nM Ki Eur J Med Chem (2021) 214: 113190-113190 [PMID:33548637]
ChEMBL Displacement of [3H]spiperone from human D2short receptor expressed in CHO cell membranes by radioligand binding assay B 9.6 pKi 0.25 nM Ki Bioorg Med Chem (2017) 25: 5084-5094 [PMID:28666858]
ChEMBL Displacement of [3H]quinpirole from Dopamine receptor D2 B 9.8 pKi 0.16 nM Ki J Med Chem (1996) 39: 4421-4429 [PMID:8893836]
ChEMBL Displacement of [3H]quinpirole from human dopamine D2A receptors expressed in LtK cells B 9.8 pKi 0.16 nM Ki Bioorg Med Chem Lett (1999) 9: 2167-2172 [PMID:10465538]
ChEMBL Binding affinity towards human Dopamine receptor D2 using [3H]spiroperidol as radioligand B 9.92 pKi 0.12 nM Ki J Med Chem (2002) 45: 5727-5735 [PMID:12477356]
ChEMBL Antagonist activity at dopamine D2 receptor (unknown origin) B 9.92 pKi 0.12 nM Ki J Med Chem (2020) 63: 15187-15217 [PMID:33111525]
ChEMBL Antagonist activity at dopamine D2 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of [35S]GTPgammaS binding by scintillation proximity assay F 6.26 pIC50 550 nM IC50 Bioorg Med Chem (2013) 21: 856-868 [PMID:23332346]
ChEMBL Antagonist activity at D2 receptor (unknown origin) after 40 mins by [35S]GTP-gammaS binding assay in presence of quinpirole F 6.39 pIC50 410 nM IC50 Bioorg Med Chem (2014) 22: 5838-5846 [PMID:25308766]
ChEMBL DRUGMATRIX: Dopamine D2L radioligand binding (ligand: [3H] Spiperone) B 8.18 pIC50 6.59 nM IC50 DrugMatrix in vitro pharmacology data
ChEMBL Binding affinity towards human Dopamine receptor D2 B 8.31 pIC50 4.9 nM IC50 J Med Chem (1999) 42: 2235-2244 [PMID:10377229]
ChEMBL In vitro binding affinity at human cloned Dopamine receptor D2 by [3H]spiroperidol displacement. B 8.39 pIC50 4.1 nM IC50 J Med Chem (1998) 41: 4903-4909 [PMID:9822559]
ChEMBL Binding affinity to dopamine receptor D2 cloned from human, using [3H]- YM09151 as competitive ligand B 8.4 pIC50 4 nM IC50 J Med Chem (2000) 43: 3923-3932 [PMID:11052797]
ChEMBL Antagonist activity at human dopamine D2 short receptor transiently expressed in HEK293 cells assessed as inhibition of beta-arrestin recruitment after 6 hrs by chemiluminescence assay B 9.15 pIC50 0.71 nM IC50 J Med Chem (2014) 57: 4861-4875 [PMID:24831693]
ChEMBL Antagonist activity at human dopamine D2 short receptor transiently expressed in HEK293 cells assessed as inhibition of beta-arrestin recruitment after 6 hrs by chemiluminescence assay B 9.15 pIC50 0.7 nM IC50 J Med Chem (2014) 57: 4861-4875 [PMID:24831693]
ChEMBL Antagonist activity against human D2LR expressed in CHOK1 cells assessed as inhibition of pergolide-induced beta-arrestin translocation by beta-galactosidase based beta-arrestin recruitment assay B 9.8 pIC50 0.16 nM IC50 J Med Chem (2014) 57: 7042-7060 [PMID:25126833]
Dopamine D2 receptor in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3998] [UniProtKB: P20288]
ChEMBL Binding affinity towards dopamine receptor D2 was determined by displacement of [3H]spiroperidol from bovine nucleus caudate membranes. B 7.7 pKi 20 nM Ki J Med Chem (1987) 30: 814-819 [PMID:2883318]
ChEMBL Binding towards Dopamine receptor D2 expressed in CHO-K1 cells using [3H]U-86170 B 9.15 pKi 0.7 nM Ki J Med Chem (1993) 36: 3188-3196 [PMID:8230107]
ChEMBL Evaluated for binding towards Dopamine receptor D2 using [3H]-spiperone as radioligand, in cloned mammalian receptors expressed in CHO-K1 cells B 9.52 pKi 0.3 nM Ki J Med Chem (1993) 36: 3188-3196 [PMID:8230107]
ChEMBL Competition in vitro with the dopamine receptor D2 antagonist [3H]spiperone, for binding sites on calf caudate membranes. B 7.52 pIC50 30 nM IC50 J Med Chem (1993) 36: 912-918 [PMID:8096548]
ChEMBL Affinity towards Dopamine receptor D2 in membranes from bovine striatum using [3H]raclopride B 8.92 pIC50 1.2 nM IC50 J Med Chem (1998) 41: 2010-2018 [PMID:9622542]
D2 receptor/Dopamine D2 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL339] [GtoPdb: 215] [UniProtKB: P61169]
ChEMBL Compound was evaluated for in vitro binding affinity towards Dopamine receptor D2 in rat striatum using [3H]- spiperone as radioligand B 8 pKi 10 nM Ki J Med Chem (1992) 35: 2712-2715 [PMID:1353116]
ChEMBL Binding affinity measured at the Dopamine receptor D2 by the inhibition of [3H]methylspiperone binding to rat striatum using unlabeled haloperidol for nonspecific binding. B 8.01 pKi 9.8 nM Ki J Med Chem (1998) 41: 5402-5409 [PMID:9876110]
ChEMBL Binding affinity for dopamine receptor D2 long expressed in Sf9 cells using [125I]IABN radioligand B 8.12 pKi 7.6 nM Ki J Med Chem (2001) 44: 1815-1826 [PMID:11356115]
ChEMBL Tested in vitro for its ability to inhibit [3H]spiperone binding to Dopamine receptor D2 in rat striatal membrane B 8.3 pKi 5.01 nM Ki Bioorg Med Chem Lett (1997) 7: 913-918
ChEMBL Inhibition of [3H]-spiperone 23390 binding to dopamine receptor D2 rat striatal membrane B 8.3 pKi 5.01 nM Ki J Med Chem (1994) 37: 2564-2573 [PMID:7914540]
ChEMBL Inhibition constant for in vitro inhibition of [3H]spiperone binding to striatal membranes Dopamine receptor D2 B 8.3 pKi 5.01 nM Ki Bioorg Med Chem Lett (1995) 5: 579-584
ChEMBL Compound was evaluated for its affinity (pKi) to inhibit [3H]spiperone binding to the Dopamine receptor D2 B 8.3 pKi 5.01 nM Ki J Med Chem (1991) 34: 2242-2247 [PMID:1676759]
GtoPdb - - 8.3 pKi - - - Nature (1990) 347: 146-51 [PMID:1975644]
ChEMBL Compound was tested for its binding affinity towards Dopamine receptor D2 using [3H]spiperone from rat striatum B 8.32 pKi 4.8 nM Ki J Med Chem (1998) 41: 1557-1560 [PMID:9572880]
ChEMBL In vitro binding affinity towards Dopamine receptor D2 in rat tissue homogenate using [3H]-spiperone as radioligand B 8.32 pKi 4.8 nM Ki J Med Chem (2004) 47: 143-157 [PMID:14695828]
ChEMBL Inhibition of [3H]spiperone binding to rat dopamine D2 receptor B 8.32 pKi 4.8 nM Ki J Med Chem (2005) 48: 1705-1708 [PMID:15771414]
ChEMBL Half-maximal inhibition of [3H]spiperone binding to Dopamine receptor D2 in rat striatal homogenate B 8.32 pKi 4.8 nM Ki J Med Chem (2002) 45: 344-359 [PMID:11784139]
ChEMBL Half-maximal inhibition of [3H]spiperone binding to Dopamine receptor D2 in rat striatal homogenate B 8.32 pKi 4.79 nM Ki J Med Chem (2002) 45: 344-359 [PMID:11784139]
ChEMBL Displacement of [3H]YM-09151-2 from rat striatum D2 receptor B 8.36 pKi 4.37 nM Ki J Med Chem (2007) 50: 865-876 [PMID:17300168]
ChEMBL In vitro Dopamine receptor D2 affinity by using [3H]-Spiperone as the radioligand in rat limbic system at 1 uM concentration of compound B 8.4 pKi 4 nM Ki J Med Chem (1987) 30: 1818-1823 [PMID:2888898]
ChEMBL In vitro binding affinity for dopamine receptor D2 of rat nucleus accumbens labeled with [3H]spiperone B 8.4 pKi 4 nM Ki J Med Chem (1987) 30: 1100-1105 [PMID:2884314]
ChEMBL In vitro ability to displace [3H]spiperone binding from dopamine receptor D2 in rat striatal membrane. B 8.48 pKi 3.31 nM Ki J Med Chem (1999) 42: 2774-2797 [PMID:10425088]
ChEMBL Compound was measured for the inhibition of [3H]spiperone binding to striatal membrane Dopamine receptor D2 B 8.48 pKi 3.31 nM Ki Bioorg Med Chem Lett (1998) 8: 3571-3576 [PMID:9934473]
ChEMBL Affinity against Dopamine receptor D2 B 8.48 pKi 3.31 nM Ki J Med Chem (2000) 43: 4678-4693 [PMID:11101359]
ChEMBL Binding affinity towards Dopamine receptor D2 in rat frontal striatum using [3H]spiperone B 8.53 pKi 2.95 nM Ki Bioorg Med Chem Lett (2003) 13: 175-178 [PMID:12482418]
ChEMBL Inhibitory constant against dopamine D2 receptor using 0.2 nM [3H]-spiperone B 8.57 pKi 2.69 nM Ki J Med Chem (2005) 48: 266-273 [PMID:15634021]
ChEMBL Displacement of [3H]spiperone from dopamine D2 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometry B 8.59 pKi 2.6 nM Ki J Med Chem (2009) 52: 151-169 [PMID:19072656]
ChEMBL Displacement of [3H]-spiperone from DRD2 in rat striatum by scintillation counting B 8.6 pKi 2.5 nM Ki J Med Chem (2016) 59: 9960-9966 [PMID:27739690]
ChEMBL Displacement of [3H]-spiperone from dopamine D2 receptor in rat striatum by scintillation counting method B 8.64 pKi 2.3 nM Ki Eur J Med Chem (2015) 90: 1-9 [PMID:25461306]
ChEMBL Binding affinity to the dopamine receptor D2L in rat brain membranes B 8.66 pKi 2.2 nM Ki J Med Chem (1999) 42: 3342-3355 [PMID:10464021]
ChEMBL Binding Affinity was determined against Dopamine receptor D2 in rat striatal membranes using [3H]- spiperone radioligand. B 8.67 pKi 2.14 nM Ki J Med Chem (2000) 43: 599-608 [PMID:10691686]
ChEMBL Displacement of [3H]-spiperone from dopamine D2 receptor in rat strriatum after 15 mins by liquid scintillation counting method B 8.68 pKi 2.1 nM Ki J Med Chem (2018) 61: 372-384 [PMID:29220177]
ChEMBL Displacement radioligand form dopamine D2 receptor in rat striatum by liquid scintillation counting B 8.68 pKi 2.1 nM Ki Eur J Med Chem (2011) 46: 433-438 [PMID:21055848]
ChEMBL Inhibition of [3H]spiroperidol binding to Dopamine receptor D2 of rat striatal membranes B 8.71 pKi 1.95 nM Ki J Med Chem (1998) 41: 1574-1580 [PMID:9572883]
ChEMBL Displacement of [3H]spiperone (0.5 nM) from rat corpus striatum dopamine D2 receptor B 8.72 pKi 1.9 nM Ki J Med Chem (2003) 46: 265-283 [PMID:12519065]
ChEMBL Tested for binding affinity towards rat striatal D2 receptor using [3H]spiperone as radioligand B 8.73 pKi 1.86 nM Ki J Med Chem (1994) 37: 3523-3533 [PMID:7932581]
ChEMBL In vitro Dopamine receptor D2 affinity by using [3H]spiperone as the radioligand in rat limbic system at 1 uM concentration of compound; value may range from 0.7 to 3.5 B 8.74 pKi 1.8 nM Ki J Med Chem (1987) 30: 1818-1823 [PMID:2888898]
ChEMBL Displacement of [3H]spiperone from Dopamine receptor D2 of rat corpora striata synaptic membranes B 8.77 pKi 1.7 nM Ki Bioorg Med Chem Lett (1997) 7: 1327-1330
ChEMBL Displacement of [3H]nemonapride from Rattus norvegicus (rat) chimeric dopamine D2 trunk/D2 tail receptor transfected in african green monkey COS7 cells after 1 hr by beta scintillation counting B 8.79 pKi 1.63 nM Ki Med Chem Res (2004) 13: 25-33
ChEMBL Ability to displace [3H]spiperone from D2 dopamine receptor isolated from the striata of male Wistar rats B 8.82 pKi 1.5 nM Ki Bioorg Med Chem Lett (1995) 5: 1245-1250
ChEMBL Displacement of [3H]-Spiperone from Dopamine receptor D2 in rat striatum B 8.85 pKi 1.4 nM Ki J Med Chem (1988) 31: 1934-1940 [PMID:2902226]
ChEMBL Ability to inhibit the [3H]spiperone binding to striatum Dopamine receptor D2 was determined in rat B 8.85 pKi 1.4 nM Ki J Med Chem (1987) 30: 2099-2104 [PMID:2889830]
ChEMBL Affinity against the dopamine receptor D2 using [3H]spiperinone. B 8.85 pKi 1.4 nM Ki J Med Chem (1995) 38: 4211-4222 [PMID:7473548]
ChEMBL Binding affinity to rat Dopamine receptor D2 expressed in CHO cells was determined using [125 I ] iodosulpride as radioligand B 8.96 pKi 1.1 nM Ki J Med Chem (1996) 39: 2764-2772 [PMID:8709107]
ChEMBL Binding affinity was measured against dopamine (D2) receptor in rat using [3H]spiperone as radioligand B 8.96 pKi 1.1 nM Ki J Med Chem (1994) 37: 1964-1970 [PMID:8027978]
ChEMBL Displacement of [3H]nemonapride from Rattus norvegicus (rat) wild type dopamine D2 receptor transfected in african green monkey COS7 cells after 1 hr by beta scintillation counting B 9 pKi 1.01 nM Ki Med Chem Res (2004) 13: 25-33
ChEMBL In vitro binding affinity against Dopamine D2 receptor in rat striatal tissue. B 9.06 pKi 0.88 nM Ki J Med Chem (1993) 36: 2107-2114 [PMID:8101877]
ChEMBL Binding affinity against dopamine D2 receptor B 9.06 pKi 0.87 nM Ki J Med Chem (1994) 37: 519-525 [PMID:7907148]
ChEMBL Binding affinity towards dopamine receptor D2 in rat striatal membranes B 9.1 pKi 0.8 nM Ki J Med Chem (2001) 44: 4431-4442 [PMID:11728188]
ChEMBL Binding affinity towards Dopamine receptor D2 B 9.12 pKi 0.75 nM Ki J Med Chem (1987) 30: 1433-1454 [PMID:3039136]
ChEMBL Displacement of [3H]NPA from rat brain Dopamine receptor D2 B 9.15 pKi 0.71 nM Ki J Med Chem (1996) 39: 143-148 [PMID:8568801]
ChEMBL Displacement of [3H]NPA from rat brain Dopamine receptor D2 B 9.15 pKi 0.71 nM Ki J Med Chem (1996) 39: 143-148 [PMID:8568801]
ChEMBL Evaluated for binding towards Dopamine receptor D2 using [3H]N-0437 as radioligand from rat striatal membrane B 9.15 pKi 0.7 nM Ki J Med Chem (1993) 36: 3188-3196 [PMID:8230107]
ChEMBL In vitro by displacement of [3H]raclopride from Dopamine receptor D2 on rat striatal membrane B 9.2 pKi 0.63 nM Ki J Med Chem (1997) 40: 586-593 [PMID:9046349]
ChEMBL Binding affinity was evaluated against Dopamine receptor D2 on rat striatum using [3H]spiperone as radioligand; ND = Not determined B 9.23 pKi 0.59 nM Ki J Med Chem (1998) 41: 2765-2778 [PMID:9667967]
ChEMBL Displacement of [3H]spiperone from dopamine D2 receptor in rat brain B 9.3 pKi 0.5 nM Ki Bioorg Med Chem (2007) 15: 7361-7367 [PMID:17869521]
ChEMBL In vitro binding affinity towards dopamine receptor D2 in rat striatal membranes by [3H]sulpiride displacement. B 9.33 pKi 0.47 nM Ki J Med Chem (1993) 36: 3073-3076 [PMID:7901415]
ChEMBL Binding affinity against dopamine receptor D2 from rat corpus striatum by using radioligand [3H]sulpiride B 9.33 pKi 0.47 nM Ki J Med Chem (1993) 36: 1488-1495 [PMID:8496917]
ChEMBL Binding affinity towards dopamine D2 receptors in rat brain synaptosomal preparations B 9.43 pKi 0.37 nM Ki J Med Chem (1994) 37: 1060-1062 [PMID:7909336]
ChEMBL Compound was evaluated for its binding affinity with Dopamine receptor D2 using membranes prepared from rat striatum B 9.43 pKi 0.37 nM Ki J Med Chem (1998) 41: 1997-2009 [PMID:9622541]
ChEMBL Inhibition of [3H]spiperone binding to rat striatal membrane Dopamine receptor D2 B 9.48 pKi 0.33 nM Ki J Med Chem (1990) 33: 1155-1163 [PMID:1969484]
ChEMBL Affinity for Dopamine receptor D2 B 9.7 pKi 0.2 nM Ki Bioorg Med Chem Lett (1998) 8: 983-988 [PMID:9871525]
ChEMBL Binding affinity towards dopamine receptor D2 by displacing [3H]spiperone radioligand in rat striatum B 9.7 pKi 0.2 nM Ki J Med Chem (1992) 35: 552-558 [PMID:1346653]
ChEMBL Binding towards Dopamine receptor D2 using [3H]spiperone from rat striatal membrane B 9.7 pKi 0.2 nM Ki J Med Chem (1993) 36: 3188-3196 [PMID:8230107]
ChEMBL Binding affinity was determined against Dopamine receptor D2 using [3H]spiperone B 9.7 pKi 0.2 nM Ki J Med Chem (1995) 38: 4198-4210 [PMID:7473547]
ChEMBL In vitro binding affinity was measured by displacement of [3H]- raclopride from D2 receptor isolated from the striata of male Dawley rats B 7.4 pIC50 40 nM IC50 J Med Chem (1994) 37: 2552-2563 [PMID:7914539]
ChEMBL Inhibition of [3H]raclopride binding at Dopamine receptor D2 from rat striata. B 7.4 pIC50 40 nM IC50 J Med Chem (1996) 39: 149-157 [PMID:8568802]
ChEMBL Binding affinity towards Dopamine receptor D2 was determined in rat striatal homogenate using [3H]- spiperone as radioligand B 7.48 pIC50 33 nM IC50 J Med Chem (1996) 39: 4044-4057 [PMID:8831770]
ChEMBL In vitro affinity towards D2 receptor using [3H]spiroperidol as radioligand in striatum B 7.49 pIC50 32.7 nM IC50 J Med Chem (1994) 37: 2308-2314 [PMID:7914536]
ChEMBL Compound was measured for affinity at dopamine receptor D2 labeled with [3H]spiroperidol radioligand in striatum tissue B 7.7 pIC50 20 nM IC50 J Med Chem (1991) 34: 1068-1072 [PMID:1672156]
ChEMBL Affinity for dopamine receptor D2 binding sites by its ability to displace [3H]spiperone from rat striatum. B 7.74 pIC50 18 nM IC50 J Med Chem (1995) 38: 1119-1131 [PMID:7707315]
ChEMBL In vitro binding affinity for Dopamine D2 receptor of rat using [3H]YM-09151 as radioligand B 7.76 pIC50 17.5 nM IC50 J Med Chem (2002) 45: 4655-4668 [PMID:12361392]
ChEMBL Inhibition of [3H]methylspiperone binding to rat striatal membrane Dopamine receptor D2 B 7.86 pIC50 13.7 nM IC50 J Med Chem (1998) 41: 5402-5409 [PMID:9876110]
ChEMBL In vitro binding affinity at Dopamine receptor D2 in rat by displacing [3H]- spiperone from rat striatal membrane B 7.92 pIC50 12 nM IC50 J Med Chem (1985) 28: 1263-1269 [PMID:4040977]
ChEMBL In vitro ability to inhibit the binding of [3H]spiperone to dopamine receptor D2 in rat striatal membranes. B 7.92 pIC50 12 nM IC50 J Med Chem (1990) 33: 1155-1163 [PMID:1969484]
ChEMBL Inhibitory binding of [3H]spiperone to Dopamine receptor D2 in membranes from rat corpus striatum B 8.12 pIC50 7.5 nM IC50 J Med Chem (1997) 40: 4146-4153 [PMID:9406603]
ChEMBL Compound was tested for the inhibition of [3H]spiperone binding to dopamine receptor D2 B 8.12 pIC50 7.5 nM IC50 J Med Chem (1992) 35: 1092-1101 [PMID:1348090]
ChEMBL Binding affinity towards Dopamine receptor D2 binding site using [3H]spiroperidol. B 8.12 pIC50 7.5 nM IC50 J Med Chem (1995) 38: 1998-2008 [PMID:7783131]
ChEMBL Binding affinity towards Dopamine receptor D2 of rat corpus striatum using [3H]spiperone as radioligand B 8.12 pIC50 7.5 nM IC50 J Med Chem (1999) 42: 2235-2244 [PMID:10377229]
ChEMBL Compound was tested in vitro for its affinity towards rat striatal Dopamine receptor D2 labeled with [3H]- spiperone B 8.15 pIC50 7 nM IC50 J Med Chem (1986) 29: 359-369 [PMID:2869146]
ChEMBL In vitro inhibitory concentration against radioligand [3H]spiperone binding to rat striatal dopamine receptor D2 B 8.15 pIC50 7 nM IC50 J Med Chem (1992) 35: 4516-4525 [PMID:1361578]
ChEMBL Inhibition of [3H](S)-sulpiride binding in striatal homogenates of rat brain B 8.22 pIC50 6 nM IC50 J Med Chem (1988) 31: 2027-2033 [PMID:3172140]
ChEMBL Compound was tested for its binding affinity towards Dopamine receptor D2 by using [3H]domperidone as radioligand B 8.26 pIC50 5.5 nM IC50 J Med Chem (1991) 34: 3360-3365 [PMID:1662725]
ChEMBL Affinity towards Dopamine receptor D2 was evaluated in rat striatal membrane using [3H]spiperone as radioligand B 8.32 pIC50 4.8 nM IC50 J Med Chem (1996) 39: 4928-4934 [PMID:8960552]
ChEMBL Binding affinity to rat Dopamine receptor D2 expressed in CHO cells was determined using [125 I ] iodosulpride as radioligand B 8.32 pIC50 4.8 nM IC50 J Med Chem (1996) 39: 3195-3202 [PMID:8759642]
ChEMBL Neuroleptic activity in terms of [3H]spiroperidol binding in rat striatal membrane to Dopamine receptor D2 B 8.37 pIC50 4.24 nM IC50 J Med Chem (1991) 34: 194-197 [PMID:1671414]
ChEMBL Ability to inhibit the specific binding of [3H]- spiroperidol to Dopamine receptor D2 in rat striatal membrane preparation by 50% B 8.37 pIC50 4.24 nM IC50 J Med Chem (1987) 30: 1906-1910 [PMID:2888899]
ChEMBL Compound was evaluated In vitro for its activity by binding to Dopamine receptor D2 in the rat brain using [3H]NPA as radioligand. B 8.51 pIC50 3.1 nM IC50 J Med Chem (1991) 34: 1860-1866 [PMID:1676427]
ChEMBL Displacement of [3H]spiroperidol from D2 dopamine receptor B 8.6 pIC50 2.5 nM IC50 J Med Chem (1994) 37: 1320-1325 [PMID:8176710]
ChEMBL Inhibition of 0.1 nM of [125I]- (S)-N-(1-Ethyl-pyrrolidin-2-ylmethyl)-5-iodo-2-methoxy-benzamide binding in striatal homogenates of rat brain B 8.92 pIC50 1.2 nM IC50 J Med Chem (1988) 31: 2027-2033 [PMID:3172140]
ChEMBL In vivo binding affinity against dopamine (D2) receptor in rat caudate-putamen tissue using [3H]nemonapride as radioligand B 10.12 pIC50 0.07 nM IC50 Bioorg Med Chem Lett (2003) 13: 4015-4017 [PMID:14592497]
Dopamine D3 receptor in Chlorocebus aethiops (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2304406] [UniProtKB: P52703]
ChEMBL Displacement of [3H]-YM 09151 from african monkey Dopamine receptor D3 B 8.52 pKi 3 nM Ki J Med Chem (1995) 38: 4950-4952 [PMID:8523409]
D3 receptor/Dopamine D3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL234] [GtoPdb: 216] [UniProtKB: P35462]
ChEMBL Intrinsic activity against dopamine receptor D3 by Eu-GTP binding assay F 6.5 pKd 316.23 nM Kd J Med Chem (2005) 48: 7919-7922 [PMID:16335915]
ChEMBL Binding affinity of compound towards Dopamine receptor D3 using [3H]spiperone (1.2 nM) ligand in cortex was determined B 6.94 pKi 115 nM Ki J Med Chem (1997) 40: 952-960 [PMID:9083484]
ChEMBL Displacement of [3H]N-methylspiperone from human D3 receptor expressed in HEK cells B 7.54 pKi 29 nM Ki Bioorg Med Chem Lett (2011) 21: 3622-3626 [PMID:21555222]
ChEMBL Displacement of the radioligand [3H]YM-09151-2 from cloned human Dopamine receptor D3 expressed in CHO cells B 7.6 pKi 25 nM Ki Bioorg Med Chem Lett (2002) 12: 1327-1330 [PMID:11992769]
ChEMBL Displacement of [3H]-SCH23390 from D3 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method B 7.64 pKi 22.91 nM Ki J Med Chem (2021) 64: 17239-17258 [PMID:34797051]
ChEMBL Displacement of [3H]-SCH23390 from D3 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method B 7.64 pKi 22.7 nM Ki J Med Chem (2021) 64: 17239-17258 [PMID:34797051]
ChEMBL Binding affinity towards human Dopamine receptor D3 B 7.68 pKi 21 nM Ki J Med Chem (2004) 47: 1303-1314 [PMID:14998318]
ChEMBL Inhibition of [3H]7-OH-DPAT binding to Dopamine D3 receptor expressed in Sf9 cells B 7.74 pKi 18 nM Ki J Med Chem (2005) 48: 1705-1708 [PMID:15771414]
ChEMBL Displacement of [3H]Spiperone from D3 receptor (unknown origin) transfected in HEK293T cells after 50 mins by liquid scintillation counting analysis B 7.79 pKi 16.04 nM Ki Bioorg Med Chem (2014) 22: 5838-5846 [PMID:25308766]
ChEMBL Displacement of [3H]spiroperidol from human cloned dopamine D3 receptor B 7.8 pKi 16 nM Ki J Med Chem (2007) 50: 5043-5047 [PMID:17850060]
ChEMBL Displacement of [3H]spiroperidol from cloned human dopamine receptor D3 in CHO cell membrane B 7.8 pKi 16 nM Ki J Med Chem (2005) 48: 7919-7922 [PMID:16335915]
ChEMBL Displacement of [125I]ABN from human dopamine D3 receptor expressed in HEK293 cells after 60 mins by gamma counting B 7.9 pKi 12.7 nM Ki Bioorg Med Chem (2010) 18: 5291-5300 [PMID:20542439]
ChEMBL Displacement of [3H]spiperone from human dopamine D3 receptor B 7.94 pKi 11.48 nM Ki Bioorg Med Chem Lett (2009) 19: 6059-6062 [PMID:19796944]
ChEMBL Inhibition of human dopamine D3 receptor B 7.98 pKi 10.4 nM Ki J Med Chem (2011) 54: 2529-2591 [PMID:21413808]
ChEMBL Binding affinity for human dopamine receptor D3 B 8 pKi 10 nM Ki J Med Chem (2005) 48: 694-709 [PMID:15689154]
ChEMBL Displacement of [3H]spiperone from human dopamine D3 expressed in CHO cell membrane B 8.08 pKi 8.32 nM Ki J Med Chem (2007) 50: 489-500 [PMID:17266201]
ChEMBL Binding affinity towards Chinese hamster ovary cells transfected with human D3 receptor using [3H]spiperone B 8.1 pKi 7.94 nM Ki Bioorg Med Chem Lett (1995) 5: 219-222
ChEMBL Binding affinity for human recombinant dopamine receptor D3 B 8.11 pKi 7.8 nM Ki J Med Chem (2004) 47: 4155-4158 [PMID:15293986]
ChEMBL Displacement of [3H]Spiperone from human dopamine D3 receptor expressed in CHO cells B 8.12 pKi 7.5 nM Ki J Med Chem (2010) 53: 7219-7228 [PMID:20839776]
ChEMBL DRUGMATRIX: Dopamine D3 radioligand binding (ligand: [3H] Spiperone) B 8.16 pKi 6.84 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL Displacement of [3H]spiperone from human dopamine D3 receptor expressed in CHO cells B 8.17 pKi 6.8 nM Ki ACS Med Chem Lett (2015) 6: 882-887 [PMID:26288260]
ChEMBL Displacement of [3H]YM-09151-2 from human cloned dopamine D3 receptor expressed in CHO cells B 8.19 pKi 6.4 nM Ki Eur J Med Chem (2007) 42: 1044-1048 [PMID:17316913]
ChEMBL Binding towards Dopamine receptor D3 expressed in CHO-K1 cells using [3H]spiperone B 8.19 pKi 6.4 nM Ki J Med Chem (1993) 36: 3188-3196 [PMID:8230107]
ChEMBL Displacement of [3H]spiperone from human D3 receptor expressed in CHO cells B 8.2 pKi 6.3 nM Ki J Med Chem (2011) 54: 4896-4903 [PMID:21599022]
ChEMBL Displacement of [3H]spiperone from human dopamine D3 receptor expressed in chinese hamster CHO cells by radioligand binding assay B 8.2 pKi 6.3 nM Ki J Med Chem (2011) 54: 7911-7919 [PMID:21999579]
ChEMBL Displacement of [3H]spiperone from human D3 receptor expressed in CHO-K1 cells by radioligand competitive binding analysis B 8.24 pKi 5.75 nM Ki J Nat Prod (2020) 83: 127-133 [PMID:31933369]
ChEMBL Displacement of [3H]N-methylspiperone from human dopamine D3 receptor by liquid scintillation counting B 8.26 pKi 5.5 nM Ki Bioorg Med Chem (2009) 17: 1716-1723 [PMID:19155177]
ChEMBL Displacement of [3H]spiperone from human D3 receptor expressed in CHO-K1 cells by radioligand competitive binding analysis B 8.29 pKi 5.16 nM Ki J Nat Prod (2020) 83: 127-133 [PMID:31933369]
ChEMBL Displacement of [3H]N-methylspiperone from human dopamine D3 receptor by liquid scintillation counting B 8.34 pKi 4.6 nM Ki Bioorg Med Chem (2012) 20: 1291-1297 [PMID:22245230]
ChEMBL In vitro ability to inhibit the binding of [3H]7-OH-DPAT to cloned human Dopamine receptor D3 using apomorphine induced climbing test in male Swiss mice B 8.34 pKi 4.6 nM Ki Bioorg Med Chem Lett (2003) 13: 3779-3782 [PMID:14552778]
ChEMBL Cataleptogenic effect against cloned human Dopamine receptor D3 in male Sprague-Dawley rats in a bar test B 8.34 pKi 4.57 nM Ki Bioorg Med Chem Lett (2003) 13: 3779-3782 [PMID:14552778]
ChEMBL Displacement of [3H]7-OH-DPAT from human Dopamine receptor D3 B 8.34 pKi 8.34 nM pKi J Med Chem (2004) 47: 497-508 [PMID:14736232]
ChEMBL Displacement of [3H]-N-methylspiperone from human dopamine D3 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysis B 8.36 pKi 4.4 nM Ki J Med Chem (2021) 64: 7778-7808 [PMID:34011153]
ChEMBL Inhibition of [125I]iodosulpiride binding to human Dopamine receptor D3 B 8.36 pKi 4.4 nM Ki J Med Chem (2005) 48: 1709-1712 [PMID:15771415]
ChEMBL Displacement of [3H]raclopride from Dopamine receptor D3 B 8.56 pKi 2.74 nM Ki J Med Chem (1996) 39: 4421-4429 [PMID:8893836]
ChEMBL Ability to displace [3H]spiperone (0.3 nM) from CHO cells of human Dopamine receptor D3 B 8.57 pKi 2.7 nM Ki J Med Chem (2003) 46: 265-283 [PMID:12519065]
ChEMBL Displacement of [3H]spiperone from human D3 receptor stably expressed in CHO cell membranes by competitive binding assay B 8.59 pKi 2.6 nM Ki Bioorg Med Chem Lett (2014) 24: 3753-3756 [PMID:25047579]
GtoPdb - - 8.6 pKi - - - J Pharmacol Exp Ther (1994) 268: 417-26 [PMID:8301582];
Eur J Pharmacol (1992) 225: 331-7 [PMID:1354163];
Pharmacol Biochem Behav (1994) 49: 567-71 [PMID:7862709];
J Psychopharmacol (Oxford) (2009) 23: 65-73 [PMID:18308814]
ChEMBL Displacement of [3H]N-methylspiperone from human dopamine D3 receptor by liquid scintillation counting B 8.6 pKi 2.5 nM Ki Bioorg Med Chem Lett (2014) 24: 4294-4297 [PMID:25070422]
ChEMBL Binding affinity to human cloned dopamine D3 receptor B 8.6 pKi 2.5 nM Ki Bioorg Med Chem (2008) 16: 7291-7301 [PMID:18595716]
ChEMBL Displacement of [3H]spiperone from human D3 receptor expressed in CHO cell membranes by radioligand binding assay B 8.64 pKi 2.3 nM Ki Bioorg Med Chem (2017) 25: 5084-5094 [PMID:28666858]
ChEMBL Binding affinity against cloned human dopamine receptor D3 expressed in Chinese hamster ovary (CHO) K-1 cells by displacement of [3H]spiperone. B 8.66 pKi 2.2 nM Ki J Med Chem (1997) 40: 4026-4029 [PMID:9406594]
ChEMBL Ability to displace [3H]spiperone from human cloned Dopamine receptor D3 expressed in CHO K-1 cells in vitro. B 8.66 pKi 2.2 nM Ki J Med Chem (1997) 40: 2688-2693 [PMID:9276014]
ChEMBL Displacement of [125I]iodosulpiride from human Dopamine receptor D3 expressed in CHO cells B 8.66 pKi 2.2 nM Ki J Med Chem (2003) 46: 4377-4392 [PMID:14521403]
ChEMBL Displacement of [3H]spiperone from human Dopamine receptor D3 expressed in CHO cells B 8.7 pKi 2 nM Ki J Med Chem (1996) 39: 1943-1945 [PMID:8642551]
ChEMBL Ability to displace [3H]spiperone from human dopamine receptor D3 (hD3) receptor stably expressed in HEK293 cells. B 8.7 pKi 2 nM Ki J Med Chem (1997) 40: 2374-2385 [PMID:9240352]
ChEMBL Binding affinity towards cloned human Dopamine receptor D3 stably expressed in CHO cells was evaluated using [3H]spiperone as radioligand B 8.7 pKi 2 nM Ki J Med Chem (1996) 39: 1941-1942 [PMID:8642550]
ChEMBL Displacement of [3H]methylspiperone from human D3 receptor expressed in HEK293 cell membrane after 90 mins by scintillation counting analysis B 8.7 pKi 2 nM Ki J Med Chem (2014) 57: 3450-3463 [PMID:24666157]
ChEMBL Displacement of [3H]spiperone from human dopamine D3 receptor expressed in CHO cells B 8.8 pKi 1.58 nM Ki J Med Chem (2007) 50: 5103-5108 [PMID:17880057]
ChEMBL Displacement of [3H]N-methylspiperone from human D3 receptor expressed in HEK293T cells co-expressing CRE-Luc incubated for 60 mins by microbeta scintillation counting method B 8.95 pKi 1.12 nM Ki Eur J Med Chem (2021) 214: 113190-113190 [PMID:33548637]
ChEMBL Displacement of [3H]-spiperone from CHO-K1 cell membranes expressing human dopamine 3 receptors B 9.02 pKi 0.96 nM Ki J Med Chem (1993) 36: 3929-3936 [PMID:7902870]
ChEMBL Displacement of [3H]7OH-DPAT from dopamine D3 receptor expressed in Sf9 cells by scintillation spectrometry B 9.05 pKi 0.9 nM Ki J Med Chem (2009) 52: 151-169 [PMID:19072656]
ChEMBL Tested for binding affinity towards human D3 receptor using [3H]spiperone as radioligand B 9.16 pKi 0.69 nM Ki J Med Chem (1994) 37: 3523-3533 [PMID:7932581]
ChEMBL DRUGMATRIX: Dopamine D3 radioligand binding (ligand: [3H] Spiperone) B 7.7 pIC50 20 nM IC50 DrugMatrix in vitro pharmacology data
ChEMBL Binding affinity towards human Dopamine receptor D3 B 8 pIC50 10 nM IC50 J Med Chem (1999) 42: 2235-2244 [PMID:10377229]
ChEMBL Antagonist activity at human dopamine D3 opioid receptor expressed in HEK293T cells assessed as GalphaoA activation preincubated with compound in D-PBS for 3 hrs followed by coelenterazine addition for 5 mins once again compound addition for 10 mins by BRET assay F 8.46 pIC50 3.47 nM IC50 J Med Chem (2021) 64: 7778-7808 [PMID:34011153]
ChEMBL Antagonist activity against D3R in human U2OS cells assessed as inhibition of (+)-PD128907-induced beta-arrestin translocation by beta-galactosidase based beta-arrestin recruitment assay B 10.22 pIC50 0.06 nM IC50 J Med Chem (2014) 57: 7042-7060 [PMID:25126833]
D3 receptor/Dopamine D3 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3138] [GtoPdb: 216] [UniProtKB: P19020]
GtoPdb - - 7 pKi - - - Nature (1990) 347: 146-51 [PMID:1975644]
ChEMBL Binding affinity for dopamine receptor D3 expressed in Sf9 cells using [125I]IABN the radioligand. B 7.33 pKi 47 nM Ki J Med Chem (2001) 44: 1815-1826 [PMID:11356115]
ChEMBL Binding affinity towards Dopamine receptor D3 of rat using [3H]spiroperidol as radioligand B 7.55 pKi 28 nM Ki J Med Chem (2002) 45: 5727-5735 [PMID:12477356]
ChEMBL Displacement of [3H]PD 128907 from rat ventral striatal membrane dopamine D3-like receptor B 7.62 pKi 24 nM Ki Bioorg Med Chem Lett (2006) 16: 443-446 [PMID:16290142]
ChEMBL Half-maximal inhibition of [3H]7-OH-DPAT binding to Dopamine receptor D3 in rat tissue homogenate B 7.74 pKi 18.2 nM Ki J Med Chem (2002) 45: 344-359 [PMID:11784139]
ChEMBL Half-maximal inhibition of [3H]-7-OH-DPAT binding to Dopamine receptor D3 in rat tissue homogenate B 7.74 pKi 18 nM Ki J Med Chem (2002) 45: 344-359 [PMID:11784139]
ChEMBL In vitro binding affinity towards Dopamine receptor D3 in Sf9 cell membranes using [3H]7-OH-DPAT as radioligand B 7.74 pKi 18 nM Ki J Med Chem (2004) 47: 143-157 [PMID:14695828]
ChEMBL Tested for binding affinity against dopamine receptor D3 expressed in Sf9 cells. B 7.84 pKi 14.3 nM Ki J Med Chem (1993) 36: 1499-1500 [PMID:8098771]
ChEMBL Displacement of [3H]-7-OH-DPAT from dopamine D3 receptor in rat olfactory tubercle by scintillation counting method B 8.06 pKi 8.8 nM Ki Eur J Med Chem (2015) 90: 1-9 [PMID:25461306]
ChEMBL Binding affinity to rat Dopamine receptor D3 expressed in CHO cells was determined using [125 I] iodosulpride as radioligand B 8.19 pKi 6.4 nM Ki J Med Chem (1996) 39: 2764-2772 [PMID:8709107]
ChEMBL Displacement of [3H]-7-OH-DPAT from DRD3 in rat olfactory tubercle by scintillation counting B 8.21 pKi 6.1 nM Ki J Med Chem (2016) 59: 9960-9966 [PMID:27739690]
ChEMBL Displacement radioligand form dopamine D3 receptor in rat olfactory tubercle by liquid scintillation counting B 8.24 pKi 5.8 nM Ki Eur J Med Chem (2011) 46: 433-438 [PMID:21055848]
ChEMBL Displacement of [3H]nemonapride from Rattus norvegicus (rat) chimeric dopamine D3 trunk/D3 tail receptor transfected in african green monkey COS7 cells after 1 hr by beta scintillation counting B 8.25 pKi 5.57 nM Ki Med Chem Res (2004) 13: 25-33
ChEMBL Displacement of [3H]nemonapride from Rattus norvegicus (rat) wild type dopamine D3 receptor transfected in african green monkey COS7 cells after 1 hr by beta scintillation counting B 8.3 pKi 5.04 nM Ki Med Chem Res (2004) 13: 25-33
ChEMBL Binding affinity towards baculovirus expressed rat dopamine D3 receptors B 8.52 pKi 3 nM Ki J Med Chem (1994) 37: 1060-1062 [PMID:7909336]
D4 receptor/Dopamine D4 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL219] [GtoPdb: 217] [UniProtKB: P21917]
ChEMBL DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone) B 6.7 pKi 198 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL Displacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cells B 6.99 pKi 103 nM Ki Eur J Med Chem (2007) 42: 1044-1048 [PMID:17316913]
ChEMBL Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells B 7.38 pKi 42 nM Ki Bioorg Med Chem Lett (2002) 12: 1327-1330 [PMID:11992769]
ChEMBL Displacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method B 7.58 pKi 26.3 nM Ki J Med Chem (2021) 64: 17239-17258 [PMID:34797051]
ChEMBL Displacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method B 7.58 pKi 26.3 nM Ki J Med Chem (2021) 64: 17239-17258 [PMID:34797051]
ChEMBL Displacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation counting B 7.9 pKi 12.7 nM Ki Bioorg Med Chem (2009) 17: 1716-1723 [PMID:19155177]
ChEMBL Binding affinity towards human dopamine-4.2 receptor B 7.96 pKi 11 nM Ki J Med Chem (2004) 47: 1303-1314 [PMID:14998318]
ChEMBL Displacement of [3H]spiperone from human Dopamine receptor D4 B 7.98 pKi 7.98 nM pKi J Med Chem (2004) 47: 497-508 [PMID:14736232]
ChEMBL Cataleptogenic effect against cloned human dopamine receptor D4 in male Sprague-Dawley rats in a bar test B 7.98 pKi 10.47 nM Ki Bioorg Med Chem Lett (2003) 13: 3779-3782 [PMID:14552778]
ChEMBL In vitro ability to inhibit the binding of [3H]spiperone to cloned human dopamine receptor D4 using apomorphine induced climbing test in male Swiss mice B 8 pKi 10 nM Ki Bioorg Med Chem Lett (2003) 13: 3779-3782 [PMID:14552778]
ChEMBL Inhibition of human dopamine D4 receptor B 8.1 pKi 7.94 nM Ki J Med Chem (2011) 54: 2529-2591 [PMID:21413808]
ChEMBL Binding affinity for human recombinant dopamine receptor D4.2 B 8.14 pKi 7.3 nM Ki J Med Chem (2004) 47: 4155-4158 [PMID:15293986]
ChEMBL Binding affinity on human Dopamine receptor D4 expressed in CHO cells using radioligand [3H]-YM 09151 B 8.14 pKi 7.3 nM Ki J Med Chem (1997) 40: 1-3 [PMID:9016321]
ChEMBL Binding affinity for Dopamine receptor D4 B 8.14 pKi 7.3 nM Ki J Med Chem (2005) 48: 694-709 [PMID:15689154]
ChEMBL Displacement of [3H]-YM 09151 from human Dopamine receptor D4 B 8.15 pKi 7 nM Ki J Med Chem (1995) 38: 4950-4952 [PMID:8523409]
ChEMBL Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells B 8.2 pKi 6.31 nM Ki J Med Chem (2007) 50: 5103-5108 [PMID:17880057]
ChEMBL Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in chinese hamster CHO cells by radioligand binding assay B 8.2 pKi 6.3 nM Ki J Med Chem (2011) 54: 7911-7919 [PMID:21999579]
ChEMBL Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells B 8.2 pKi 6.3 nM Ki J Med Chem (2011) 54: 4896-4903 [PMID:21599022]
ChEMBL Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane B 8.22 pKi 6.03 nM Ki J Med Chem (2007) 50: 489-500 [PMID:17266201]
ChEMBL Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells B 8.22 pKi 6 nM Ki J Med Chem (2010) 53: 7219-7228 [PMID:20839776]
ChEMBL Displacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assay B 8.23 pKi 5.9 nM Ki Bioorg Med Chem Lett (2014) 24: 3753-3756 [PMID:25047579]
ChEMBL Binding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligand B 8.3 pKi 5 nM Ki Bioorg Med Chem Lett (2002) 12: 3111-3115 [PMID:12372513]
ChEMBL Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK cells B 8.3 pKi 5 nM Ki Bioorg Med Chem Lett (2011) 21: 3622-3626 [PMID:21555222]
ChEMBL Binding affinity measured at the Dopamine receptor D4 by the inhibition of [3H]spiperone binding to human recombinant CHO cells using unlabeled haloperidol for nonspecific binding. B 8.37 pKi 4.3 nM Ki J Med Chem (1998) 41: 5402-5409 [PMID:9876110]
ChEMBL Potency was measured by the displacement of [3H]-spiperone binding to human D4 dopaminergic receptor B 8.42 pKi 3.8 nM Ki Bioorg Med Chem Lett (1997) 7: 1207-1212
ChEMBL Displacement of [3H]YM-09151-2 from human Dopamine receptor D4.2 expressed in baculovirus Sf9 cells B 8.44 pKi 3.6 nM Ki Bioorg Med Chem Lett (1997) 7: 1327-1330
ChEMBL Binding affinity to human cloned dopamine D4 receptor B 8.48 pKi 3.3 nM Ki Bioorg Med Chem (2008) 16: 7291-7301 [PMID:18595716]
ChEMBL In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement. B 8.48 pKi 3.3 nM Ki Bioorg Med Chem Lett (1998) 8: 725-730 [PMID:9871530]
ChEMBL Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells. B 8.64 pKi 2.3 nM Ki J Med Chem (1997) 40: 2374-2385 [PMID:9240352]
ChEMBL Inhibition of human dopamine D4 receptor B 8.64 pKi 2.3 nM Ki J Med Chem (2017) 60: 7233-7243 [PMID:28489950]
ChEMBL Displacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cells B 8.64 pKi 2.3 nM Ki J Med Chem (1996) 39: 1943-1945 [PMID:8642551]
ChEMBL Binding affinity towards cloned human Dopamine receptor D4 stably expressed in CHO cells was evaluated using [3H]spiperone as radioligand B 8.64 pKi 2.3 nM Ki J Med Chem (1996) 39: 1941-1942 [PMID:8642550]
ChEMBL In vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranes B 8.66 pKi 2.2 nM Ki J Med Chem (2002) 45: 5136-5149 [PMID:12408724]
ChEMBL Binding towards dopamine receptor D4 expressed in CHO-K1 cells using [3H]spiperone B 8.66 pKi 2.2 nM Ki J Med Chem (1993) 36: 3188-3196 [PMID:8230107]
ChEMBL Ability to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitro B 8.66 pKi 2.2 nM Ki J Med Chem (1997) 40: 2688-2693 [PMID:9276014]
ChEMBL Binding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperone B 8.66 pKi 2.2 nM Ki J Med Chem (1997) 40: 4026-4029 [PMID:9406594]
ChEMBL Binding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligand B 8.68 pKi 2.1 nM Ki J Med Chem (1996) 39: 2764-2772 [PMID:8709107]
ChEMBL Antagonism of dopamine-stimulated [35S]GTP-gamma-S binding against human Dopamine receptor D4 in CHO cells F 8.7 pKi 2 nM Ki J Med Chem (2000) 43: 3923-3932 [PMID:11052797]
ChEMBL In vitro ability to inhibit [3H]6b binding to human Dopamine receptor D4.4 B 8.72 pKi 1.9 nM Ki Bioorg Med Chem Lett (2004) 14: 5095-5098 [PMID:15380206]
ChEMBL In vitro binding affinity for Dopamine receptor D4 B 8.8 pKi 1.58 nM Ki Bioorg Med Chem Lett (2001) 11: 1313-1316 [PMID:11392544]
GtoPdb - - 8.8 pKi - - - Eur J Pharmacol (1993) 236: 483-6 [PMID:8102973];
Pharmacol Biochem Behav (1994) 49: 567-71 [PMID:7862709];
J Psychopharmacol (Oxford) (2009) 23: 65-73 [PMID:18308814]
ChEMBL Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysis B 8.84 pKi 1.43 nM Ki J Med Chem (2021) 64: 7778-7808 [PMID:34011153]
ChEMBL In vitro ability to inhibit [3H]spiperone binding to human Dopamine receptor D4.4 B 8.85 pKi 1.4 nM Ki Bioorg Med Chem Lett (2004) 14: 5095-5098 [PMID:15380206]
ChEMBL In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement. B 9 pKi 1 nM Ki J Med Chem (2000) 43: 270-277 [PMID:10649982]
ChEMBL Binding affinity towards human Dopamine receptor D4.2 in CHO cells B 9 pKi 1 nM Ki J Med Chem (1996) 39: 4044-4057 [PMID:8831770]
ChEMBL Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand B 9.13 pKi 0.74 nM Ki J Med Chem (2002) 45: 5727-5735 [PMID:12477356]
ChEMBL DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone) B 6.25 pIC50 563 nM IC50 DrugMatrix in vitro pharmacology data
ChEMBL Binding affinity towards human D4.2 receptor B 8.19 pIC50 6.5 nM IC50 J Med Chem (1999) 42: 2235-2244 [PMID:10377229]
ChEMBL Inhibitory concentration against human Dopamine receptor D4.2 in CHO cells B 8.22 pIC50 6 nM IC50 J Med Chem (1996) 39: 4044-4057 [PMID:8831770]
ChEMBL Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand B 8.3 pIC50 5 nM IC50 J Med Chem (2000) 43: 3923-3932 [PMID:11052797]
ChEMBL In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement. B 8.89 pIC50 1.3 nM IC50 J Med Chem (1998) 41: 4903-4909 [PMID:9822559]
ChEMBL Agonist activity was calculated in calcium flux assay using HEK293 cells co-transfected with human Dopamine receptor D4.4 and Galphaqo5 F 5 pEC50 >10000 nM EC50 Bioorg Med Chem Lett (2004) 14: 5095-5098 [PMID:15380206]
ChEMBL Agonistic activity against human Dopamine receptor D4.2 using [35S]GTP-gamma-S binding assay F 7.77 pEC50 17 nM EC50 Bioorg Med Chem Lett (2003) 13: 2921-2924 [PMID:14611858]
D4 receptor/Dopamine D4 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3361] [GtoPdb: 217] [UniProtKB: P30729]
ChEMBL Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting B 8 pKi 10 nM Ki Bioorg Med Chem Lett (2014) 24: 4294-4297 [PMID:25070422]
D5 receptor/Dopamine D5 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1850] [GtoPdb: 218] [UniProtKB: P21918]
GtoPdb - - 6.3 pKi - - - Nature (1991) 350: 614-9 [PMID:1826762]
ChEMBL Compound was tested for the Binding affinity against Human cloned Dopamine receptor D5 by Radio ligand ([3H]SCH-23390) binding assay B 6.59 pKi 260 nM Ki J Med Chem (1996) 39: 2764-2772 [PMID:8709107]
ChEMBL Binding affinity for human recombinant dopamine receptor D5 B 7.24 pKi 58 nM Ki J Med Chem (2004) 47: 4155-4158 [PMID:15293986]
ChEMBL Displacement of [3H]SCH233930 from human D5 receptor expressed in HEK cells B 7.32 pKi 48 nM Ki Bioorg Med Chem Lett (2011) 21: 3622-3626 [PMID:21555222]
ChEMBL Inhibition of human dopamine D5 receptor B 7.42 pKi 38 nM Ki J Med Chem (2011) 54: 2529-2591 [PMID:21413808]
DAT/Dopamine transporter in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL338] [GtoPdb: 927] [UniProtKB: P23977]
ChEMBL Inhibitory constant towards reuptake of [125I]-12 from dopamine transporter in rat striatal membranes B 6 pKi >1000 nM Ki J Med Chem (1994) 37: 1535-1542 [PMID:8182712]
GluN1/GluN2A/GluN2B/GluN2C/GluN2D/GluN3B/GluN3A/Glutamate NMDA receptor in Rat (target type: PROTEIN COMPLEX GROUP) [ChEMBL: CHEMBL1907608] [GtoPdb: 455456457458459461460] [UniProtKB: P35439Q00959Q00960Q00961Q62645Q8VHN2Q9R1M7]
ChEMBL Binding affinity was measured against phencyclidine (PCP) receptor in rat using [3H]TCP as radioligand B 5 pKi >10000 nM Ki J Med Chem (1994) 37: 1964-1970 [PMID:8027978]
Kv11.1/HERG in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809]
ChEMBL Displacement of [3H]Astemizole from hERG expressed in HEK293 cells at 10 uM B 6.29 pKi 512 nM Ki Bioorg Med Chem Lett (2006) 16: 5303-5308 [PMID:16908150]
ChEMBL Binding affinity to human ERG expressed in HEK293 cells by whole cell patch clamp method B 6.92 pKi 120 nM Ki J Med Chem (2009) 52: 151-169 [PMID:19072656]
ChEMBL Inhibitory concentration against IKr potassium channel B 5.85 pIC50 1400 nM IC50 Bioorg Med Chem Lett (2004) 14: 4771-4777 [PMID:15324906]
ChEMBL Inhibition of human ERG expressed in HEK293 cells measured after 30 mins by FluxOR dye based FLIPR TETRA assay B 5.94 pIC50 1160 nM IC50 J Med Chem (2020) 63: 5734-5751 [PMID:32392053]
ChEMBL Inhibition of human ERG expressed in CHO cells after 30 mins by Rb+ flux assay B 5.96 pIC50 1100 nM IC50 Bioorg Med Chem Lett (2012) 22: 5134-5140 [PMID:22677319]
ChEMBL Inhibition of human ERG expressed in HEK293 cells coexpressing Kir2.3 after 30 mins by FluxOR based FLIPR assay B 6.64 pIC50 230 nM IC50 J Nat Prod (2012) 75: 1210-1214 [PMID:22694270]
ChEMBL Inhibition of K+ channel activity in CHO cells expressing HERG Kv11.1 B 7.49 pIC50 32 nM IC50 Bioorg Med Chem Lett (2003) 13: 1829-1835 [PMID:12729675]
ChEMBL Inhibition of human ERG expressed in CHO cells by whole cell patch clamp technique B 7.52 pIC50 30.2 nM IC50 Bioorg Med Chem (2008) 16: 6252-6260 [PMID:18448342]
ChEMBL Inhibition of human Potassium channel HERG expressed in mammalian cells B 7.52 pIC50 30.2 nM IC50 Bioorg Med Chem Lett (2003) 13: 2773-2775 [PMID:12873512]
ChEMBL Inhibitory concentration against potassium channel HERG B 7.52 pIC50 30.2 nM IC50 Bioorg Med Chem Lett (2005) 15: 2886-2890 [PMID:15911273]
ChEMBL Inhibition of human voltage-gated potassium channel subunit Kv11.1 (ERG K+ channel) in open state F 7.55 pIC50 28.18 nM IC50 Bioorg Med Chem Lett (2005) 15: 1737-1741 [PMID:15745831]
ChEMBL Inhibition of human ERG in MCF7 cells B 7.55 pIC50 28.18 nM IC50 Eur J Med Chem (2009) 44: 1926-1932 [PMID:19110341]
ChEMBL K+ channel blocking activity in human embryonic kidney cells expressing HERG Kv11.1 F 7.55 pIC50 28.1 nM IC50 J Med Chem (2002) 45: 3844-3853 [PMID:12190308]
ChEMBL Inhibition of hERG K channel F 7.57 pIC50 27 nM IC50 Cardiovasc Res (2011) 91: 53-61 [PMID:21300721]
ChEMBL Inhibition of human ERG B 7.57 pIC50 26.92 nM IC50 Eur J Med Chem (2011) 46: 618-630 [PMID:21185626]
ChEMBL Inhibition of human ERG channel B 7.57 pIC50 26.8 nM IC50 J Med Chem (2009) 52: 4266-4276 [PMID:19534531]
ChEMBL Inhibition of human ERG channel B 7.57 pIC50 26.8 nM IC50 J Med Chem (2009) 52: 4266-4276 [PMID:19534531]
ChEMBL Inhibition of human ERG B 8 pIC50 10 nM IC50 J Med Chem (2013) 56: 8955-8971 [PMID:23919353]
H1 receptor/Histamine H1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL231] [GtoPdb: 262] [UniProtKB: P35367]
GtoPdb - - 6.1 pKi - - - Psychopharmacology (Berl.) (1996) 124: 57-73 [PMID:8935801];
Neuropsychopharmacology (2003) 28: 519-26 [PMID:12629531]
ChEMBL Binding affinity towards human histamine H1 receptor B 6.14 pKi 730 nM Ki J Med Chem (2004) 47: 1303-1314 [PMID:14998318]
ChEMBL Binding affinity to human cloned histamine H1 receptor B 6.36 pKi 440 nM Ki Bioorg Med Chem (2008) 16: 7291-7301 [PMID:18595716]
ChEMBL Displacement of [3H]pyrilamine from human H1 receptor by liquid scintillation counting B 6.36 pKi 440 nM Ki Bioorg Med Chem (2012) 20: 1291-1297 [PMID:22245230]
ChEMBL Displacement of [3H]Pyrilamine from human histamine H1 receptor by liquid scintillation counting B 6.36 pKi 440 nM Ki Bioorg Med Chem Lett (2014) 24: 4294-4297 [PMID:25070422]
ChEMBL DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine) B 6.49 pKi 323 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine) B 5.56 pIC50 2781 nM IC50 DrugMatrix in vitro pharmacology data
H1 receptor/Histamine H1 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4701] [GtoPdb: 262] [UniProtKB: P31390]
ChEMBL Compound was tested for the binding affinity against rat cortical H1 receptor by Radio ligand [3H]pyrilamine binding assay. B 5.68 pKi 2100 nM Ki J Med Chem (1996) 39: 2764-2772 [PMID:8709107]
ChEMBL Half-maximal inhibition of [3H]pyrilamine binding to Histamine H1 receptor in rat frontal cortex homogenate B 6.42 pKi 384 nM Ki J Med Chem (2002) 45: 344-359 [PMID:11784139]
ChEMBL In vitro binding affinity towards Histamine H1 receptor of rat frontal cortex homogenate by using radioligand [3H]pyrilamine B 6.42 pKi 384 nM Ki J Med Chem (2004) 47: 143-157 [PMID:14695828]
ChEMBL Displacement of [3H]mepyramine from H1R in rat brain B 5.7 pIC50 >2000 nM IC50 Proc Natl Acad Sci U S A (2007) 104: 3456-3459 [PMID:17360666]
ChEMBL Binding affinity towards histamine H1 receptor from rat brain membranes using [3H]mepyramine as radioligand B 6 pIC50 >1000 nM IC50 J Med Chem (1999) 42: 2235-2244 [PMID:10377229]
ChEMBL Inhibitory binding of [3H]mepyramine to histamine H1 receptors in rat brain membranes B 6 pIC50 >1000 nM IC50 J Med Chem (1997) 40: 4146-4153 [PMID:9406603]
Histamine H1 receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3943] [UniProtKB: P31389]
ChEMBL Displacement of [3H]pyrilamine from histaminergic H1 receptor guinea pig cerebellum B 6.4 pKi 398.11 nM Ki J Med Chem (2007) 50: 5103-5108 [PMID:17880057]
H2 receptor/Histamine H2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1941] [GtoPdb: 263] [UniProtKB: P25021]
ChEMBL DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine) B 5.94 pKi 1147 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine) B 5.93 pIC50 1166 nM IC50 DrugMatrix in vitro pharmacology data
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 6.11 pKi 780 nM Ki US-8598119-B2. Methods and compositions for sleep disorders and other disorders (2013)
HLA class I histocompatibility antigen A-3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2632] [UniProtKB: P04439]
ChEMBL Binding affinity to human biotinylated HLA-A2 by surface plasmon resonance assay B 5 pKd <10000 nM Kd Bioorg Med Chem Lett (2018) 28: 2837-2841 [PMID:30077568]
Human immunodeficiency virus type 1 protease in Human immunodeficiency virus 1 (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL243] [UniProtKB: Q72874]
ChEMBL Binding affinity to HIV-1 protease B 4 pKi 100000 nM Ki J Med Chem (1994) 37: 1769-1778 [PMID:8021917]
ChEMBL Binding affinity for HIV-1 protease B 7 pKi 100 nM Ki J Med Chem (1991) 34: 2305-2314 [PMID:1875332]
Human rhinovirus A protease in Human rhinovirus sp. (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2857] [UniProtKB: Q4U254]
ChEMBL The compound was tested for its affinity against HIV-2 protease B 7 pKi 100 nM Ki J Med Chem (1991) 34: 2305-2314 [PMID:1875332]
μ receptor/Mu opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL233] [GtoPdb: 319] [UniProtKB: P35372]
ChEMBL Displacement of [3H]-DAMGO from human MOR expressed in CHOK1 cell membranes incubated for 60 mins by liquid scintillation counting method B 5 pKi >10000 nM Ki J Med Chem (2020) 63: 2434-2454 [PMID:31743642]
ChEMBL Displacement of [3H]DAMGO from human mu opioid receptor expressed in HEK293 cell membrane incubated for 60 mins by radioligand binding assay B 5.61 pKi 2470 nM Ki J Med Chem (2021) 64: 7778-7808 [PMID:34011153]
ChEMBL DRUGMATRIX: Opiate mu (OP3, MOP) radioligand binding (ligand: [3H] Diprenorphine) B 6 pKi 992 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Opiate mu (OP3, MOP) radioligand binding (ligand: [3H] Diprenorphine) B 5.61 pIC50 2443 nM IC50 DrugMatrix in vitro pharmacology data
ChEMBL Agonist activity at human MOR expressed in CHOK1 cells assessed as stimulation of cAMP accumulation incubated for 45 mins by HTRF assay F 5 pEC50 >10000 nM EC50 J Med Chem (2020) 63: 2434-2454 [PMID:31743642]
M1 receptor/Muscarinic acetylcholine receptor M1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL216] [GtoPdb: 13] [UniProtKB: P11229]
ChEMBL Binding affinity to human cloned muscarinic M1 receptor B 5.8 pKi 1600 nM Ki Bioorg Med Chem (2008) 16: 7291-7301 [PMID:18595716]
ChEMBL Displacement of [3H]QNB from human M1 receptor by liquid scintillation counting B 5.8 pKi 1600 nM Ki Bioorg Med Chem (2012) 20: 1291-1297 [PMID:22245230]
ChEMBL Inhibition of binding of 1.0 nM [3H]pirenzepine to cloned human Muscarinic acetylcholine receptor M1 expressed in membranes from CHO-K1 cells B 5.26 pIC50 5500 nM IC50 J Med Chem (1999) 42: 2235-2244 [PMID:10377229]
ChEMBL Inhibitory binding of [3H]pirenzepine to human Muscarinic acetylcholine receptor M1 in membranes from CHO-K1 cells B 5.26 pIC50 5500 nM IC50 J Med Chem (1997) 40: 4146-4153 [PMID:9406603]
M1 receptor/Muscarinic acetylcholine receptor M1 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL276] [GtoPdb: 13] [UniProtKB: P08482]
ChEMBL Half-maximal inhibition of [3H]QNB binding to Muscarinic acetylcholine receptor M1 in rat frontal cortex homogenate B 5 pKi >10000 nM Ki J Med Chem (2002) 45: 344-359 [PMID:11784139]
ChEMBL In vitro binding affinity towards M1 receptor of rat frontal cortex homogenate by using radioligand [3H]QNB B 5 pKi >10000 nM Ki J Med Chem (2004) 47: 143-157 [PMID:14695828]
ChEMBL Binding affinity was measured against muscarinic (M1) receptor in rat using [3H]pirenzepine as radioligand B 5.67 pKi 2140 nM Ki J Med Chem (1994) 37: 1964-1970 [PMID:8027978]
ChEMBL Compound was tested for the binding affinity against rat cortical Muscarinic acetylcholine receptor M1 by Radio ligand [3H]pirenzepine binding assay. B 5.74 pKi 1800 nM Ki J Med Chem (1996) 39: 2764-2772 [PMID:8709107]
M2 receptor/Muscarinic acetylcholine receptor M2 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL309] [GtoPdb: 14] [UniProtKB: P10980]
ChEMBL Binding affinity was measured against muscarinic (M2) receptor at 10 uM in rat using [3H]QN as radioligand B 5.21 pKi 6120 nM Ki J Med Chem (1994) 37: 1964-1970 [PMID:8027978]
ChEMBL Compound was tested for the binding affinity against rat heart Muscarinic acetylcholine receptor M2 by quinuclidinyl binding assay. B 5.6 pKi 2500 nM Ki J Med Chem (1996) 39: 2764-2772 [PMID:8709107]
ChEMBL Inhibition of [3H]N-methylscopolamine binding to Muscarinic acetylcholine receptor M2 of rat heart membranes B 6.62 pKi 238 nM Ki J Med Chem (1998) 41: 1574-1580 [PMID:9572883]
M5 receptor/Muscarinic acetylcholine receptor M5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2035] [GtoPdb: 17] [UniProtKB: P08912]
ChEMBL DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine) B 5.55 pKi 2795 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine) B 5.41 pIC50 3890 nM IC50 DrugMatrix in vitro pharmacology data
NET/Norepinephrine transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL222] [GtoPdb: 926] [UniProtKB: P23975]
ChEMBL Displacement of [3H]Nisoxetine from human Norepinephrine transporter by liquid scintillation counting B 5.26 pKi 5500 nM Ki Bioorg Med Chem Lett (2014) 24: 4294-4297 [PMID:25070422]
ChEMBL DRUGMATRIX: Norepinephrine Transporter radioligand binding (ligand: [125I] RTI-55) B 5.74 pKi 1820 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Norepinephrine Transporter radioligand binding (ligand: [125I] RTI-55) B 5.74 pIC50 1836 nM IC50 DrugMatrix in vitro pharmacology data
ABCB1/P-glycoprotein 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4302] [GtoPdb: 768] [UniProtKB: P08183]
ChEMBL High affinity constant at binding site of human P-Glycoprotein (P-gp) in two-affinity model B 6.7 pKi 200 nM Ki J Med Chem (2002) 45: 5671-5686 [PMID:12477351]
ChEMBL Concentration required for 50% inhibition at binding site of human P-Glycoprotein (P-gp) in one-affinity model B 5.28 pIC50 5300 nM IC50 J Med Chem (2002) 45: 5671-5686 [PMID:12477351]
Plasmodium falciparum (target type: ORGANISM) [ChEMBL: CHEMBL364]
ChEMBL Antiplasmodial activity against Plasmodium falciparum D10 after 72 hrs by SYBR green assay F 5 pIC50 10000 nM IC50 Nat Chem Biol (2009) 5: 765-771 [PMID:19734910]
ChEMBL Antiplasmodial activity against Plasmodium falciparum HB3 after 72 hrs by SYBR green assay F 5.1 pIC50 7943.28 nM IC50 Nat Chem Biol (2009) 5: 765-771 [PMID:19734910]
ChEMBL Antiplasmodial activity against Plasmodium falciparum 7G8 after 72 hrs by SYBR green assay F 5.3 pIC50 5011.87 nM IC50 Nat Chem Biol (2009) 5: 765-771 [PMID:19734910]
ChEMBL Antiplasmodial activity against Plasmodium falciparum Dd2 after 72 hrs by SYBR green assay F 5.3 pIC50 5011.87 nM IC50 Nat Chem Biol (2009) 5: 765-771 [PMID:19734910]
ChEMBL Antiplasmodial activity against Plasmodium falciparum 3D7 after 72 hrs by SYBR green assay F 5.5 pIC50 3162.28 nM IC50 Nat Chem Biol (2009) 5: 765-771 [PMID:19734910]
ChEMBL Antiplasmodial activity against Plasmodium falciparum GB4 after 72 hrs by SYBR green assay F 5.5 pIC50 3162.28 nM IC50 Nat Chem Biol (2009) 5: 765-771 [PMID:19734910]
ChEMBL Antiplasmodial activity against Plasmodium falciparum W2 after 72 hrs by SYBR green assay F 5.7 pIC50 1995.26 nM IC50 Nat Chem Biol (2009) 5: 765-771 [PMID:19734910]
K2P2.1/Potassium channel subfamily K member 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2321615] [GtoPdb: 514] [UniProtKB: O95069]
ChEMBL Inhibition of of human TREK1 expressed in whole COS cells assessed as reduction in channel currents B 5.26 pIC50 5500 nM IC50 J Med Chem (2016) 59: 5149-5157 [PMID:26588045]
Prion protein in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4869] [UniProtKB: P04156]
ChEMBL Half maximal inhibition of Prion protein PrPsc formation was assayed in ScN2a cells B 5 pEC50 >10000 nM EC50 J Med Chem (2003) 46: 3563-3564 [PMID:12904059]
5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL214] [GtoPdb: 1] [UniProtKB: P08908]
ChEMBL Binding affinity to human cloned 5HT1A receptor B 5.44 pKi 3600 nM Ki Bioorg Med Chem (2008) 16: 7291-7301 [PMID:18595716]
ChEMBL Displacement of [3H] 8-OH-DPAT from human 5-HT1A receptor by liquid scintillation counting B 5.44 pKi 3600 nM Ki Bioorg Med Chem Lett (2014) 24: 4294-4297 [PMID:25070422]
ChEMBL Binding affinity for 5-hydroxytryptamine 1A receptor determined using [3H]8-OH-DPAT as radioligand B 5.55 pKi 2800 nM Ki Bioorg Med Chem Lett (2001) 11: 2345-2349 [PMID:11527728]
ChEMBL Displacement of [3H]-8-OH-DPAT from human 5-HT1AR expressed in HEK293 cell membranes after 1 hr by microbeta counting method B 5.77 pKi 1703 nM Ki Eur J Med Chem (2018) 145: 790-804 [PMID:29407591]
GtoPdb - - 5.8 pKi - - - Eur J Pharmacol (1998) 355: 245-56 [PMID:9760039];
J Pharmacol Exp Ther (1997) 280: 1241-9 [PMID:9067310];
Psychopharmacology (Berl.) (1996) 124: 57-73 [PMID:8935801];
J Pharmacol Exp Ther (1998) 286: 1341-55 [PMID:9732398]
ChEMBL Affinity towards 5-hydroxytryptamine 1A receptor in membranes from bovine hippocampus using [3H]OH-DPAT B 5.82 pIC50 1500 nM IC50 J Med Chem (1998) 41: 2010-2018 [PMID:9622542]
5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL273] [GtoPdb: 1] [UniProtKB: P19327]
ChEMBL Binding affinity measured at the 5-hydroxytryptamine 1A receptor by the inhibition of [3H]8-OH-DPAT binding to rat cortex using unlabeled buspirone for nonspecific binding. B 5.08 pKi 8400 nM Ki J Med Chem (1998) 41: 5402-5409 [PMID:9876110]
ChEMBL Compound was evaluated for in vitro binding affinity towards 5-hydroxytryptamine 1A receptor in rat hippocampus using [3H]8-OH-DPAT as radioligand B 5.24 pKi 5750 nM Ki J Med Chem (1992) 35: 2712-2715 [PMID:1353116]
ChEMBL In vitro binding affinity towards 5-hydroxytryptamine receptor 1A receptor by using [3H]8-OH-DPAT in rat hippocampal membranes. B 5.62 pKi 2390 nM Ki J Med Chem (2000) 43: 270-277 [PMID:10649982]
ChEMBL Compound was tested for the Binding affinity against rat hippocampal 5-hydroxytryptamine 1A receptor by Radio ligand [3H]8-OH-DPAT binding assay. B 5.72 pKi 1900 nM Ki J Med Chem (1996) 39: 2764-2772 [PMID:8709107]
ChEMBL Displacement of [3H]8OH-DPAT from 5HT1A receptor in CRL:CD(SD)BR-COBS rat hippocampus by scintillation spectrometry B 5.74 pKi 1800 nM Ki J Med Chem (2009) 52: 151-169 [PMID:19072656]
ChEMBL Ability to displace [3H]-8-OH-DPAT from serotonergic 5-hydroxytryptamine 1A receptor B 5.74 pKi 1800 nM Ki Bioorg Med Chem Lett (1995) 5: 1245-1250
ChEMBL Displacement of [3H]OH-DPAT from rat cortex 5HT1A receptor B 5.77 pKi 1698.24 nM Ki J Med Chem (2007) 50: 865-876 [PMID:17300168]
ChEMBL Binding affinity towards 5-hydroxytryptamine 1A receptor of rat brain synaptosomal preparations B 6 pKi >1000 nM Ki J Med Chem (1994) 37: 1060-1062 [PMID:7909336]
ChEMBL Compound was evaluated for its binding affinity with 5-hydroxytryptamine 1A receptor using membranes prepared from rat cerebral cortex B 6 pKi >1000 nM Ki J Med Chem (1998) 41: 1997-2009 [PMID:9622541]
ChEMBL The compound was tested binding affinity against 5-hydroxytryptamine 1A receptor from rat brain using [3H]8-OH-DPAT as radioligand at 10e-6 M. B 6.3 pKi >500 nM Ki J Med Chem (1999) 42: 3342-3355 [PMID:10464021]
ChEMBL Binding affinity was determined against 5-hydroxytryptamine 1A receptor using [3H]WB-4101 B 6.4 pKi 401 nM Ki J Med Chem (1995) 38: 4198-4210 [PMID:7473547]
ChEMBL Affinity against the 5-hydroxytryptamine receptor 1A using [3H]WB-4101. B 6.4 pKi 401 nM Ki J Med Chem (1995) 38: 4211-4222 [PMID:7473548]
ChEMBL The compound was tested for its binding affinity towards 5-hydroxytryptamine 1A receptor by displacing [3H]WB-4101 radioligand in rat hippocampus B 6.4 pKi 401 nM Ki J Med Chem (1992) 35: 552-558 [PMID:1346653]
ChEMBL Binding affinity towards serotonin 5-HT1A receptor was determined in rat hippocampus using [3H]8-OH-DPAT as ligand B 5.15 pIC50 7079 nM IC50 J Med Chem (1996) 39: 4044-4057 [PMID:8831770]
ChEMBL In vitro affinity towards 5-hydroxytryptamine 1A receptor using [3H]8-OH-DPAT as radioligand in hippocampus B 5.15 pIC50 7079 nM IC50 J Med Chem (1994) 37: 2308-2314 [PMID:7914536]
ChEMBL In vitro binding affinity was measured on serotonergic 5-hydroxytryptamine 1A receptor by displacement of [3H]- tetralin B 5.15 pIC50 7000 nM IC50 J Med Chem (1994) 37: 2552-2563 [PMID:7914539]
ChEMBL Inhibition of [3H]8-OH-DPAT binding at serotonin 5-hydroxytryptamine 1A receptor from rat hippocampus tissue. B 5.15 pIC50 7000 nM IC50 J Med Chem (1996) 39: 149-157 [PMID:8568802]
ChEMBL Compound was measured for affinity at 5-hydroxytryptamine 1A receptor labeled with [3H]8-OH-DPAT radioligand in hippocampus tissue B 5.21 pIC50 6210 nM IC50 J Med Chem (1991) 34: 1068-1072 [PMID:1672156]
ChEMBL Binding affinity towards 5-hydroxytryptamine 1A receptor binding site using [3H]8-OH-DPAT. B 5.49 pIC50 3200 nM IC50 J Med Chem (1995) 38: 1998-2008 [PMID:7783131]
ChEMBL In vitro binding affinity for serotonin 5-hydroxytryptamine 1A receptor fof rat cerebral cortex using [3H]8-OH-DPAT as radioligand B 5.7 pIC50 1993 nM IC50 J Med Chem (2002) 45: 4655-4668 [PMID:12361392]
ChEMBL Binding affinity to 5-hydroxytryptamine 1A receptor in the rat brain using [3H]8-hydroxy-2-(di-n-propylamine)tetralin as radioligand. B 6 pIC50 >1000 nM IC50 J Med Chem (1991) 34: 1860-1866 [PMID:1676427]
ChEMBL Inhibitory concentration against binding of 5-hydroxytryptamine 1A receptor from striata of male Wistar rats by displacement of [3H]8-OH-DPAT B 6 pIC50 >1000 nM IC50 Bioorg Med Chem Lett (2000) 10: 509-512 [PMID:10743959]
5-HT1B receptor/Serotonin 1b (5-HT1b) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3459] [GtoPdb: 2] [UniProtKB: P28564]
ChEMBL Affinity towards 5-hydroxytryptamine 1B receptor in membranes from rat frontal cortex using [3H]5-HT B 5 pIC50 >10000 nM IC50 J Med Chem (1998) 41: 2010-2018 [PMID:9622542]
5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223]
ChEMBL Inhibition of [125I]R91150 binding to human 5-hydroxytryptamine 2A receptor B 6.36 pKi 435 nM Ki J Med Chem (2005) 48: 1709-1712 [PMID:15771415]
ChEMBL Displacement of [3H]ketanserin from human cloned 5HT2A receptor B 6.78 pKi 165.96 nM Ki Bioorg Med Chem Lett (2009) 19: 6059-6062 [PMID:19796944]
ChEMBL Displacement of [3H]ketanserin from human cloned 5-HT2A receptor by in vitro binding assay B 6.78 pKi 165.96 nM Ki Medchemcomm (2011) 2: 1194-1200
ChEMBL Displacement of [3H]ketanserin from human cloned 5HT2A receptor B 6.78 pKi 165.96 nM Ki J Med Chem (2008) 51: 6085-6094 [PMID:18783204]
ChEMBL Binding affinity towards serotonin 5-hydroxytryptamine 2A receptor B 6.78 pKi 165.96 nM Ki Bioorg Med Chem Lett (2004) 14: 585-589 [PMID:14741248]
ChEMBL Displacement of [3H]ketanserin from human 5-HT2A receptor B 6.78 pKi 165.96 nM Ki Eur J Med Chem (2014) 71: 237-249 [PMID:24316025]
ChEMBL Displacement of [3H]ketanserin human cloned serotonin 5HT2A receptor B 6.78 pKi 165.96 nM Ki Bioorg Med Chem Lett (2007) 17: 4873-4877 [PMID:17588750]
ChEMBL In vitro binding affinity towards 5-hydroxytryptamine 2A receptor in human using [3H]ketanserin as radioligand B 6.89 pKi 130 nM Ki J Med Chem (2004) 47: 143-157 [PMID:14695828]
ChEMBL Displacement of [3H]Ketanserin from human 5-HT2A receptor by liquid scintillation counting B 6.92 pKi 120 nM Ki Bioorg Med Chem Lett (2014) 24: 4294-4297 [PMID:25070422]
ChEMBL Binding affinity to human cloned 5HT2A receptor B 6.92 pKi 120 nM Ki Bioorg Med Chem (2008) 16: 7291-7301 [PMID:18595716]
ChEMBL Binding affinity towards human 5-HT2A receptor in BEK cells B 6.97 pKi 108 nM Ki J Med Chem (1996) 39: 4044-4057 [PMID:8831770]
ChEMBL Displacement of [3H]ketanserin from human 5HT2A receptor expressed in CHO cells B 7 pKi 100 nM Ki J Med Chem (2007) 50: 5103-5108 [PMID:17880057]
ChEMBL Binding Assay: Binding assay using 5-HT2A, Dopamine D2, SERT, αA1, 5-HT2C and H1 Receptors. B 7 pKi 100 nM Ki US-8598119-B2. Methods and compositions for sleep disorders and other disorders (2013)
ChEMBL Displacement of [3H]-ketanserin from human 5-HT2AR expressed in CHO-K1 cell membranes after 1.5 hrs by microbeta counting method B 7.05 pKi 89 nM Ki Eur J Med Chem (2018) 145: 790-804 [PMID:29407591]
GtoPdb - - 7.3 pKi - - - Psychopharmacology (Berl.) (1996) 124: 57-73 [PMID:8935801];
J Pharmacol Exp Ther (1998) 286: 1341-55 [PMID:9732398];
Neuropsychopharmacology (2003) 28: 519-26 [PMID:12629531];
J Pharmacol Exp Ther (2004) 310: 943-51 [PMID:15102927];
J Psychopharmacol (Oxford) (2009) 23: 65-73 [PMID:18308814]
ChEMBL Binding affinity towards human serotonin 5-hydroxytryptamine 2A receptor B 7.6 pKi 25 nM Ki J Med Chem (2004) 47: 1303-1314 [PMID:14998318]
ChEMBL Displacement of [3H]-ketanserin from human human 5-HT2A receptor transfected in CHO-K1 cells measured after 60 mins by scintillation counting method B 7.64 pKi 22.91 nM Ki J Med Chem (2021) 64: 12603-12629 [PMID:34436892]
ChEMBL DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2A radioligand binding (ligand: [3H] Ketanserin) B 7.68 pKi 21 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL Inhibitory concentration against human 5-HT2A receptor in BEK cells B 6.54 pIC50 288 nM IC50 J Med Chem (1996) 39: 4044-4057 [PMID:8831770]
ChEMBL DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2A radioligand binding (ligand: [3H] Ketanserin) B 7.12 pIC50 75 nM IC50 DrugMatrix in vitro pharmacology data
Serotonin 2a (5-HT2a) receptor in Pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2490] [UniProtKB: P50129]
ChEMBL Displacement of [3H]Ketanserin from 5-HT2 receptor in pig cortex membranes B 7.52 pKi 30 nM Ki J Med Chem (2010) 53: 7219-7228 [PMID:20839776]
Serotonin 2a (5-HT2a) receptor in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3446] [UniProtKB: Q75Z89]
ChEMBL Affinity towards 5-hydroxytryptamine 2A receptor in membranes from bovine frontal cortex using [3H]ketanserin B 7.52 pIC50 30 nM IC50 J Med Chem (1998) 41: 2010-2018 [PMID:9622542]
5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL322] [GtoPdb: 6] [UniProtKB: P14842]
ChEMBL Half-maximal inhibition of [3H]- Ketanserin binding to 5-hydroxytryptamine 2A receptor in rat cerebral cortex homogenate B 6.78 pKi 165.96 nM Ki J Med Chem (2002) 45: 344-359 [PMID:11784139]
ChEMBL Inhibition of [3H]ketanserin binding to rat 5-hydroxytryptamine 2A receptor B 6.79 pKi 164 nM Ki J Med Chem (2005) 48: 1705-1708 [PMID:15771414]
ChEMBL Half-maximal inhibition of [3H]ketanserin binding to 5-hydroxytryptamine 2A receptor in rat cerebral cortex homogenate B 6.79 pKi 164 nM Ki J Med Chem (2002) 45: 344-359 [PMID:11784139]
ChEMBL Displacement of [3H]ketanserin from 5HT2A receptor in CRL:CD(SD)BR-COBS rat cortex by scintillation spectrometry B 6.79 pKi 164 nM Ki J Med Chem (2009) 52: 151-169 [PMID:19072656]
ChEMBL In vitro binding affinity towards 5-hydroxytryptamine 2A receptor in rat tissue homogenate using [3H]ketanserin as radioligand B 6.79 pKi 164 nM Ki J Med Chem (2004) 47: 143-157 [PMID:14695828]
ChEMBL Compound was tested for the Binding affinity against rat frontal cortex 5-hydroxytryptamine 2A receptor by Radio ligand [3H]ketanserin binding assay. B 7.06 pKi 87 nM Ki J Med Chem (1996) 39: 2764-2772 [PMID:8709107]
ChEMBL Displacement of [3H]ketanserin from rat cortex 5HT2A receptor B 7.08 pKi 83.18 nM Ki J Med Chem (2007) 50: 865-876 [PMID:17300168]
ChEMBL Binding affinity measured at the 5-hydroxytryptamine 2A receptor by the inhibition of [3H]ketanserin binding to rat cortex using unlabeled mianserin for nonspecific binding. B 7.12 pKi 75 nM Ki J Med Chem (1998) 41: 5402-5409 [PMID:9876110]
ChEMBL Binding affinity towards 5-hydroxytryptamine 2A receptor using [3H]ketanserin B 7.28 pKi 52.48 nM Ki Bioorg Med Chem Lett (2003) 13: 175-178 [PMID:12482418]
ChEMBL In vitro affinity against serotonin 5-hydroxytryptamine 2A receptor B 7.28 pKi 52.48 nM Ki J Med Chem (2000) 43: 4678-4693 [PMID:11101359]
ChEMBL Inhibitory constant on 5-hydroxytryptamine 2A receptor of Rat frontal cortex B 7.28 pKi 52.48 nM Ki J Med Chem (2002) 45: 54-71 [PMID:11754579]
ChEMBL In vitro binding affinity at serotonin 5-hydroxytryptamine 2A receptor in rat cortical membrane B 7.31 pKi 49 nM Ki J Med Chem (2002) 45: 5136-5149 [PMID:12408724]
ChEMBL In vitro ability to displace [3H]ketanserin from 5-hydroxytryptamine 2A receptor in rat brain. B 7.35 pKi 45 nM Ki J Med Chem (1996) 39: 143-148 [PMID:8568801]
ChEMBL Displacement of [3H]-ketanserin from rat brain 5-hydroxytryptamine 2A receptor B 7.35 pKi 44.67 nM Ki J Med Chem (1996) 39: 143-148 [PMID:8568801]
GtoPdb - - 7.4 pKi - - - J Pharmacol Exp Ther (1998) 286: 85-90 [PMID:9655845]
ChEMBL Displacement of [3H]ketanserin from 5HT2A receptor in rat brain B 7.46 pKi 34.67 nM Ki Bioorg Med Chem (2007) 15: 7361-7367 [PMID:17869521]
ChEMBL In vitro ability to displace [3H]ketanserin binding from 5-hydroxytryptamine 2A receptor in rat striatal membrane. B 7.7 pKi 19.95 nM Ki J Med Chem (1999) 42: 2774-2797 [PMID:10425088]
ChEMBL Compound was measured for the inhibition of [3H]ketanserin binding to rat frontal cortex membrane (5-HT2A receptor) B 7.7 pKi 19.95 nM Ki Bioorg Med Chem Lett (1998) 8: 3571-3576 [PMID:9934473]
ChEMBL Inhibition constant for in vitro inhibition of [3H]ketanserin binding to rat frontal cortex membranes 5-hydroxytryptamine 2A receptor B 7.7 pKi 19.95 nM Ki Bioorg Med Chem Lett (1995) 5: 579-584
ChEMBL Serotonergic activity of the compound. B 7.7 pKi 19.95 nM Ki J Med Chem (2000) 43: 3233-3243 [PMID:10966742]
ChEMBL Inhibition of [3H]ketanserin binding to 5-hydroxytryptamine 2A receptor rat frontal cortex membrane B 7.7 pKi 19.95 nM Ki J Med Chem (1994) 37: 2564-2573 [PMID:7914540]
ChEMBL Tested in vitro for its ability to inhibit [3H]ketanserin binding to 5-hydroxytryptamine 2A receptor in rat frontal cortex membranes B 7.7 pKi 19.95 nM Ki Bioorg Med Chem Lett (1997) 7: 913-918
ChEMBL In vitro affinity towards 5-hydroxytryptamine 2A receptor using [3H]spiroperidol as radioligand in cortex B 6.89 pIC50 129 nM IC50 J Med Chem (1994) 37: 2308-2314 [PMID:7914536]
ChEMBL In vitro binding affinity for serotonin 5-hydroxytryptamine 2A receptor of rat cerebral cortex using [3H]ketanserin as radioligand B 6.9 pIC50 125 nM IC50 J Med Chem (2002) 45: 4655-4668 [PMID:12361392]
ChEMBL Inhibition of [3H]ketanserin binding to rat frontal cortex membrane 5-hydroxytryptamine 2A receptor B 6.98 pIC50 104 nM IC50 J Med Chem (1998) 41: 5402-5409 [PMID:9876110]
ChEMBL Binding affinity towards 5-hydroxytryptamine 2A receptor from rat frontal cortex using [3H]ketanserin as radioligand B 7.26 pIC50 55 nM IC50 J Med Chem (1999) 42: 2235-2244 [PMID:10377229]
ChEMBL Inhibition of [3H]ketanserin binding to 5-hydroxytryptamine 2A receptor from rat brain B 7.26 pIC50 55 nM IC50 J Med Chem (1997) 40: 4146-4153 [PMID:9406603]
ChEMBL Binding affinity towards 5-hydroxytryptamine 2A receptor binding site using [3H]ketanserin. B 7.26 pIC50 55 nM IC50 J Med Chem (1995) 38: 1998-2008 [PMID:7783131]
5-HT2B receptor/Serotonin 2b (5-HT2b) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1833] [GtoPdb: 7] [UniProtKB: P41595]
ChEMBL DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide) B 5.88 pKi 1305 nM Ki DrugMatrix in vitro pharmacology data
GtoPdb - - 6.4 pKi - - - Naunyn Schmiedebergs Arch Pharmacol (1998) 357: 17-24 [PMID:9459568]
ChEMBL DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide) B 5.69 pIC50 2050 nM IC50 DrugMatrix in vitro pharmacology data
5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL225] [GtoPdb: 8] [UniProtKB: P28335]
ChEMBL Displacement of [3H]mesulergine from human cloned 5HT2C receptor B 5.14 pKi 7244.36 nM Ki J Med Chem (2008) 51: 6085-6094 [PMID:18783204]
ChEMBL Displacement of [3H]mesulergine from human 5HT2C receptor B 5.14 pKi 7244.36 nM Ki Bioorg Med Chem Lett (2009) 19: 6059-6062 [PMID:19796944]
ChEMBL Binding affinity towards serotonin 5-hydroxytryptamine 2C receptor B 5.14 pKi 7244.36 nM Ki Bioorg Med Chem Lett (2004) 14: 585-589 [PMID:14741248]
ChEMBL Displacement of [3H]mesulergine human cloned serotonin 5HT2C receptor B 5.14 pKi 7244.36 nM Ki Bioorg Med Chem Lett (2007) 17: 4873-4877 [PMID:17588750]
ChEMBL Binding affinity towards human serotonin 5-hydroxytryptamine 2C receptor B 5.3 pKi >5000 nM Ki J Med Chem (2004) 47: 1303-1314 [PMID:14998318]
ChEMBL Binding affinity to human cloned 5HT2C receptor B 5.33 pKi 4700 nM Ki Bioorg Med Chem (2008) 16: 7291-7301 [PMID:18595716]
ChEMBL Inhibitory constant was determined on 5-hydroxytryptamine 2C receptor of Bovine choroid plexus B 5.34 pKi 4570.88 nM Ki J Med Chem (2002) 45: 54-71 [PMID:11754579]
ChEMBL In vitro affinity against serotonin (5-hydroxytryptamine 2C) receptor B 5.34 pKi 4570.88 nM Ki J Med Chem (2000) 43: 4678-4693 [PMID:11101359]
ChEMBL Binding Assay: Binding assay using 5-HT2A, Dopamine D2, SERT, αA1, 5-HT2C and H1 Receptors. B 5.4 pKi 3949 nM Ki US-8598119-B2. Methods and compositions for sleep disorders and other disorders (2013)
ChEMBL In vitro ability to displace [3H]mesulergine binding from 5-hydroxytryptamine 2C receptor from bovine choroid plexus. B 5.6 pKi 2511.89 nM Ki J Med Chem (1999) 42: 2774-2797 [PMID:10425088]
ChEMBL DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2C radioligand binding (ligand: [3H] Mesulergine) B 5.76 pKi 1753 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL Affinity towards 5-hydroxytryptamine 2C receptor in membranes from pig choroid plexus using [3H]N-methyl-mesulergine B 5 pIC50 >10000 nM IC50 J Med Chem (1998) 41: 2010-2018 [PMID:9622542]
ChEMBL DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2C radioligand binding (ligand: [3H] Mesulergine) B 5.48 pIC50 3347 nM IC50 DrugMatrix in vitro pharmacology data
5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL324] [GtoPdb: 8] [UniProtKB: P08909]
ChEMBL Displacement of [3H]Mesulergine from rat 5-HT2C receptor by liquid scintillation counting B 5.33 pKi 4700 nM Ki Bioorg Med Chem Lett (2014) 24: 4294-4297 [PMID:25070422]
ChEMBL Binding affinity towards 5-HT2C receptor from rat using [3H]mesulergine as radioligand B 6 pIC50 >1000 nM IC50 J Med Chem (1999) 42: 2235-2244 [PMID:10377229]
ChEMBL Inhibition of [3H]mesulergine binding to 5-hydroxytryptamine 2C receptor in rat brain membranes B 6 pIC50 >1000 nM IC50 J Med Chem (1997) 40: 4146-4153 [PMID:9406603]
5-HT3A/Serotonin 3a (5-HT3a) receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4972] [GtoPdb: 373] [UniProtKB: P23979]
ChEMBL Compound was tested for the Binding affinity against N1e-115 neuroblastoma 5-hydroxytryptamine 3 receptor by Radio ligand [3H]GR-65630 binding assay. B 5 pKi >10000 nM Ki J Med Chem (1996) 39: 2764-2772 [PMID:8709107]
5-HT6 receptor/Serotonin 6 (5-HT6) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3371] [GtoPdb: 11] [UniProtKB: P50406]
ChEMBL Binding affinity to human cloned 5HT6 receptor B 5.22 pKi 6000 nM Ki Bioorg Med Chem (2008) 16: 7291-7301 [PMID:18595716]
ChEMBL Binding affinity towards human 5-hydroxytryptamine 6 receptor B 5.3 pKi >5000 nM Ki J Med Chem (2003) 46: 2795-2812 [PMID:12825922]
ChEMBL Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method B 5.97 pKi 1083 nM Ki Eur J Med Chem (2018) 145: 790-804 [PMID:29407591]
5-HT7 receptor/Serotonin 7 (5-HT7) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3155] [GtoPdb: 12] [UniProtKB: P34969]
ChEMBL Displacement of [3H]-5-carboxyamidotryptamine from human 5HT7 receptor by liquid scintillation counting method B 5.95 pKi 1122.02 nM Ki Bioorg Med Chem (2016) 24: 3671-3679 [PMID:27364609]
ChEMBL Displacement of [3H]-5-carboxyamidotryptamine from human 5HT7 receptor by liquid scintillation counting method B 5.96 pKi 1100 nM Ki Bioorg Med Chem (2016) 24: 3671-3679 [PMID:27364609]
ChEMBL Displacement of [3H]-5-CT from human 5-HT7R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method B 6.39 pKi 408 nM Ki Eur J Med Chem (2018) 145: 790-804 [PMID:29407591]
ChEMBL Displacement of [3H]LSD from human 5HT7 receptor expressed in CHO cells B 6.5 pKi 316.23 nM Ki J Med Chem (2007) 50: 5103-5108 [PMID:17880057]
GtoPdb - - 6.6 pKi - - - Br J Pharmacol (1997) 122: 126-32 [PMID:9298538]
5-HT7 receptor in Mouse [GtoPdb: 12] [UniProtKB: P32304]
GtoPdb - - 6.3 pKi - - - Mol Pharmacol (1993) 44: 229-36 [PMID:8394987]
5-HT7 receptor/Serotonin 7 (5-HT7) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3223] [GtoPdb: 12] [UniProtKB: P32305]
ChEMBL Binding affinity towards rat 5-hydroxytryptamine 7 receptor B 6.58 pKi 263 nM Ki J Med Chem (2003) 46: 2795-2812 [PMID:12825922]
GtoPdb - - 6.6 pKi - - - Eur J Pharmacol (1996) 317: 417-23 [PMID:8997630];
J Pharmacol Exp Ther (1994) 268: 1403-10 [PMID:7908055];
Proc Natl Acad Sci USA (1993) 90: 8547-51 [PMID:8397408]
SERT/Serotonin transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL228] [GtoPdb: 928] [UniProtKB: P31645]
ChEMBL Binding affinity to human SERT B 5.74 pKi 1800 nM Ki Bioorg Med Chem (2008) 16: 7291-7301 [PMID:18595716]
ChEMBL Displacement of [3H]Citalopram from human Serotonin transporter by liquid scintillation counting B 5.74 pKi 1800 nM Ki Bioorg Med Chem Lett (2014) 24: 4294-4297 [PMID:25070422]
ChEMBL DRUGMATRIX: Transporter, Serotonin (5-Hydroxytryptamine) (SERT) radioligand binding (ligand: [3H] Paroxetine) B 5.74 pKi 1799 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL Binding Assay: Binding assay using 5-HT2A, Dopamine D2, SERT, αA1, 5-HT2C and H1 Receptors. B 6 pKi >1000 nM Ki US-8598119-B2. Methods and compositions for sleep disorders and other disorders (2013)
ChEMBL DRUGMATRIX: Transporter, Serotonin (5-Hydroxytryptamine) (SERT) radioligand binding (ligand: [3H] Paroxetine) B 5.47 pIC50 3386 nM IC50 DrugMatrix in vitro pharmacology data
SERT/Serotonin transporter in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL313] [GtoPdb: 928] [UniProtKB: P31652]
ChEMBL In vitro binding affinity for serotonin reuptake sites in rat frontal cortex membranes by [3H]paroxetine displacement. B 6 pKi >1000 nM Ki Bioorg Med Chem Lett (2003) 13: 405-408 [PMID:12565939]
Sigma-1 receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4153] [UniProtKB: Q60492]
ChEMBL Displacement of [3H](+)pentazocine from sigma-1 receptor in Cavia porcellus (guinea pig) brain membranes B 8.04 pKi 9.2 nM Ki Med Chem Res (2005) 14: 158-168
ChEMBL Displacement of [3H]-(+)-pentazocine from sigma1 receptor in guinea pig brain membranes after 120 mins by scintillation counting method B 8.18 pKi 6.6 nM Ki J Med Chem (2019) 62: 893-907 [PMID:30543421]
ChEMBL Displacement of [3H]-(+)-Pentazocine from sigma1 receptor in guinea pig brain cortex membranes after 120 mins by scintillation counting analysis B 8.18 pKi 6.6 nM Ki Medchemcomm (2016) 7: 2368-2380
ChEMBL Displacement of [3H]-(+)-pentazocine from sigma1 receptor in guinea pig brain cortex membranes after 120 mins by scintillation counting method B 8.18 pKi 6.6 nM Ki Eur J Med Chem (2016) 121: 712-726 [PMID:27366902]
ChEMBL Displacement of [3H](+)-Pentazocine from sigma 1 receptor in guinea pig brain membranes after 120 mins by scintillation counting analysis B 8.18 pKi 6.6 nM Ki J Med Chem (2016) 59: 5505-5519 [PMID:27156565]
ChEMBL Displacement of [3H]-(+)-pentazocine from guinea pig Sigma1-receptor after 120 mins by liquid scintillation counting method B 8.18 pKi 6.6 nM Ki Medchemcomm (2016) 7: 317-326
ChEMBL Displacement of (+)-[3H]pentazocine from guinea pig brain cortex sigma1 receptor by scintillation analyzer B 8.18 pKi 6.6 nM Ki Eur J Med Chem (2015) 90: 797-808 [PMID:25528334]
ChEMBL Displacement of [3H]-(+)-pentazocine from sigma-1 receptor in guinea pig brain cortex membranes B 8.18 pKi 6.6 nM Ki J Med Chem (2014) 57: 6845-6860 [PMID:25062506]
ChEMBL Displacement of [3H]-(+)-pentazocine from sigma-1 receptor in guinea pig brain cortex membranes after 120 mins by scintillation counting analysis B 8.18 pKi 6.6 nM Ki J Med Chem (2014) 57: 2884-2894 [PMID:24617836]
ChEMBL Displacement of [3H]-(+)pentazocine from sigma-1 receptor in guinea pig brain membranes after 120 mins by scintillation counting method B 8.2 pKi 6.3 nM Ki ACS Med Chem Lett (2020) 11: 651-656 [PMID:32435366]
ChEMBL Displacement of [3H](+)-pentazocine from sigma1 receptor guinea pig brain after 180 mins scintillation counting B 8.2 pKi 6.3 nM Ki Bioorg Med Chem (2010) 18: 8005-8015 [PMID:20965739]
ChEMBL Displacement of [3H]-(+)-pentazocine from sigma1 receptor in guinea pig brain membrane by scintillation counting B 8.2 pKi 6.3 nM Ki Bioorg Med Chem (2011) 19: 393-405 [PMID:21126878]
ChEMBL Displacement of [3H](+)-pentazocine from sigma 1 receptor in guinea pig brain by scintillation analyzer B 8.2 pKi 6.3 nM Ki Bioorg Med Chem (2011) 19: 3141-3151 [PMID:21531141]
ChEMBL Displacement of [3H]-(+)-pentazocine from sigma 1 receptor in guinea pig brain homogenates after 180 mins by solid scintillation counting B 8.2 pKi 6.3 nM Ki Bioorg Med Chem (2012) 20: 257-269 [PMID:22136765]
ChEMBL Displacement of [3H](+)-Pentazocine from sigma 1 receptor in guinea pig brain membranes after 120 mins by scintillation counting analysis B 8.2 pKi 6.3 nM Ki Bioorg Med Chem (2013) 21: 1844-1856 [PMID:23462714]
ChEMBL Displacement of (+)-pentazocine from sigma-1 receptor in guinea pig brain cortex membrane after 120 mins by scintillation counting B 8.2 pKi 6.3 nM Ki Eur J Med Chem (2013) 69: 490-497 [PMID:24095744]
ChEMBL Displacement of (+)-pentazocine from sigma1 receptor in guinea pig brain cortex membrane by scintillation counting analysis B 8.2 pKi 6.3 nM Ki Eur J Med Chem (2014) 83: 526-533 [PMID:24996139]
ChEMBL Displacement of [3H](+)-pentazocine from sigma1 receptor in guinea pig brain membranes after 180 mins by scintillation counting method B 8.2 pKi 6.3 nM Ki Bioorg Med Chem (2014) 22: 6638-6646 [PMID:25458498]
ChEMBL Displacement of [3H]-(+)-pentazocine from sigma 1 receptor in guinea pig brain cortex membranes B 8.2 pKi 6.3 nM Ki Bioorg Med Chem (2014) 22: 4277-4284 [PMID:24913984]
ChEMBL Displacement of [3H]-(+)-Pentazocine from sigma1 receptor in guniea pig brain cortex membranes by scintillation counting analysis B 8.2 pKi 6.3 nM Ki Bioorg Med Chem Lett (2015) 25: 5748-5751 [PMID:26531150]
ChEMBL Displacement of [3H](+)-pentazocine from sigma 1 receptor in guinea pig brain membranes after 150 mins by liquid scintillation spectrometry B 8.2 pKi 6.3 nM Ki Medchemcomm (2016) 7: 327-331
ChEMBL Displacement of [3H]-(+)-Pentazocine from sigma1 receptor in guinea pig brain homogenate incubated for 120 mins by solid scintillation counting analysis B 8.2 pKi 6.3 nM Ki Eur J Med Chem (2016) 116: 136-146 [PMID:27061977]
ChEMBL Displacement of [3H]-pentazocine from sigma1 receptor in guinea pig brain membranes after 120 mins by liquid scintillation counting B 8.2 pKi 6.3 nM Ki Bioorg Med Chem (2017) 25: 4778-4799 [PMID:28764962]
ChEMBL Displacement of [3H](+)-Pentazocine from sigma 1 receptor in guinea pig brain membranes after 120 mins by scintillation counting analysis B 8.2 pKi 6.3 nM Ki Bioorg Med Chem (2017) 25: 5365-5372 [PMID:28797770]
ChEMBL Displacement of [3H]-(+)-Pentazocine from sigma 1 receptor in guinea pig brain cortex membranes after 120 mins by scintillation counting analysis B 8.2 pKi 6.3 nM Ki Bioorg Med Chem (2018) 26: 501-508 [PMID:29254894]
ChEMBL Displacement of [3H]-(+)-pentazocine from sigma-1 receptor in guinea pig brain cortex membranes incubated for 120 mins measured for 5 mins by scintillation counting method B 8.2 pKi 6.3 nM Ki Eur J Med Chem (2018) 144: 672-681 [PMID:29289890]
ChEMBL Displacement of [3H](+)-Pentazocine from sigma 1 receptor in guinea pig brain membranes after 120 mins by scintillation counting analysis B 8.2 pKi 6.3 nM Ki Medchemcomm (2017) 8: 975-981 [PMID:30108812]
ChEMBL Displacement of [3H]-(+)-pentazocine from sigma1 receptor in guinea pig brain cortex membranes incubated for 120 mins by solid scintillation counting method B 8.2 pKi 6.3 nM Ki Eur J Med Chem (2019) 180: 268-282 [PMID:31319263]
ChEMBL Displacement of [3H]-(+)-pentazocine from sigma1 receptor in guinea pig brain cortex membranes incubated for 120 mins by solid scintillation counting method B 8.2 pKi 6.3 nM Ki Bioorg Med Chem (2019) 27: 115146-115146 [PMID:31648876]
ChEMBL Displacement of [3H]-(+)pentazocine from sigma-1 receptor in guinea pig brain membranes after 120 mins by scintillation counting method B 8.2 pKi 6.3 nM Ki Bioorg Med Chem (2019) 27: 3559-3567 [PMID:31255496]
ChEMBL Displacement of [3H]-(+)-pentazocine from sigma1 receptor in guinea pig brain cortex membranes incubated for 120 mins by scintillation counting method B 8.2 pKi 6.3 nM Ki Eur J Med Chem (2019) 177: 47-62 [PMID:31129453]
ChEMBL Displacement of [3H]-(+)-pentazocine from sigma1 receptor in guinea pig brain membranes incubated for 120 mins by scintillation counting method B 8.2 pKi 6.3 nM Ki Bioorg Med Chem (2020) 28: 115245-115245 [PMID:31843460]
ChEMBL Displacement of [3H]-(+)-pentazocine from Sigma1 receptor in guinea pig cortex membranes incubated for 120 mins by scintillation counting method B 8.2 pKi 6.3 nM Ki Eur J Med Chem (2020) 190: 112138-112138 [PMID:32070917]
ChEMBL Displacement of [3H]-pentazocine from sigma1 receptor in guinea pig brain membrane incubated for 120 mins by liquid scintillation counting method B 8.2 pKi 6.3 nM Ki Eur J Med Chem (2021) 210: 112950-112950 [PMID:33148494]
ChEMBL Displacement of [3H]-(+)-pentazocine from sigma1 receptor in guinea pig brain membrane measured after 120 mins by solid scintillation counting method B 8.2 pKi 6.3 nM Ki Eur J Med Chem (2021) 219: 113443-113443 [PMID:33901806]
ChEMBL Displacement of [3H]-(+)-pentazocine from sigma-1 receptor in guinea pig brain homogenates B 8.22 pKi 6 nM Ki J Med Chem (2012) 55: 8953-8957 [PMID:23013229]
ChEMBL Displacement of [3H]pentazocine from guinea pig sigma1 receptor measured after 90 mins by microbeta scintillation counting method B 8.4 pKi 4 nM Ki Bioorg Med Chem Lett (2016) 26: 5689-5694 [PMID:27839919]
ChEMBL Displacement of [3H]-(+)-pentazocine from sigma1 receptor in guinea pig brain cortex membrane incubated for 120 mins measured for 5 mins by scintillation counting method B 8.41 pKi 3.9 nM Ki Bioorg Med Chem (2017) 25: 2472-2481 [PMID:28320613]
ChEMBL Displacement of [3H]-(+)-pentazocine from guinea pig brain sigma-1 receptor after 180 mins by scintillation counting analysis B 8.41 pKi 3.9 nM Ki Medchemcomm (2012) 3: 673-679
ChEMBL Displacement of [3H](+)-pentazocine from opioid sigma1 receptor in guinea pig brain homogenate B 8.41 pKi 3.9 nM Ki Bioorg Med Chem (2009) 17: 777-793 [PMID:19081725]
ChEMBL Displacement of [3H](+)-pentazocine from sigma 1 receptor in guinea pig brain after 180 mins by scintillation counting B 8.41 pKi 3.9 nM Ki Eur J Med Chem (2009) 44: 4306-4314 [PMID:19709783]
ChEMBL Displacement of (+)-[3H]pentazocine from guinea pig brain sigma 1 receptor after 180 mins by scintillation counting B 8.41 pKi 3.9 nM Ki J Med Chem (2011) 54: 6704-6713 [PMID:21859078]
ChEMBL Displacement of [3H](+)-pentazocine from sigma 1 receptor in guinea pig brain membrane by scintillation analysis B 8.41 pKi 3.9 nM Ki J Med Chem (2009) 52: 2126-2137 [PMID:19243173]
ChEMBL Displacement of [3H]-(+)-pentazocine from sigma 1 receptor in guinea pig brain membranes after 120 mins by scintillation counting B 8.41 pKi 3.9 nM Ki J Med Chem (2012) 55: 8047-8065 [PMID:22913577]
ChEMBL Displacement of [3H]-(+)pentazocine from guinea pig brain sigma 1-type opioid receptor after 120 mins by scintillation counting analysis B 8.41 pKi 3.9 nM Ki J Med Chem (2012) 55: 5350-5360 [PMID:22515405]
ChEMBL Displacement of [3H]-(+)-pentazocine from sigma1 receptor in guinea pig brain membrane after 180 mins by solid scintillation counting B 8.41 pKi 3.9 nM Ki Eur J Med Chem (2012) 53: 327-336 [PMID:22578786]
ChEMBL Displacement of [3H]-(+)-pentazocine from sigma-1 receptor in guinea pig brain membranes after 120 mins by microbeta scintillation counting method B 8.41 pKi 3.9 nM Ki Bioorg Med Chem (2017) 25: 3384-3395 [PMID:28501431]
ChEMBL Displacement of [3H](+)-pentazocine from sigma 1 receptor in guinea pig brain membrane by solid scintillation analysis B 8.41 pKi 3.9 nM Ki Bioorg Med Chem (2009) 17: 3630-3641 [PMID:19394833]
ChEMBL Displacement of [3H](+)-pentazocine from sigma 1 receptor in guinea pig brain membrane after 180 mins by scintillation counting B 8.41 pKi 3.9 nM Ki J Med Chem (2009) 52: 6062-6072 [PMID:19791807]
ChEMBL Displacement of [3H](+)-pentazocine from sigma1 receptor in guinea pig brain membrane B 8.41 pKi 3.9 nM Ki J Med Chem (2010) 53: 4212-4222 [PMID:20441176]
ChEMBL Displacement of [3H](+)-pentazocine from sigma 1 receptor in guinea pig brain membrane B 8.41 pKi 3.9 nM Ki J Med Chem (2008) 51: 6531-6537 [PMID:18816044]
ChEMBL Displacement of [3H](+)-pentazocine from sigma1 opioid receptor in guinea pig brain by solid scintillation counting B 8.41 pKi 3.9 nM Ki Bioorg Med Chem (2009) 17: 1445-1455 [PMID:19196515]
ChEMBL Displacement of [3H](+)-pentazocine from Sigma1 receptor in Dunkin Hartley guinea pig brain membrane after 120 mins by liquid scintillation counting analysis B 8.44 pKi 3.6 nM Ki Bioorg Med Chem Lett (2016) 26: 2676-2679 [PMID:27090556]
ChEMBL Displacement of [3H]-PTZ from sigma1 receptor in guinea pig brain membranes after 150 mins in presence of 1 mM DPH by liquid scintillation counting method B 8.46 pKi 3.5 nM Ki Eur J Med Chem (2017) 125: 603-610 [PMID:27721146]
ChEMBL Displacement of [3H](+)-pentazocine from sigma 1 receptor in guinea pig brain membranes after 120 mins by microbeta scintillation counting method B 8.49 pKi 3.27 nM Ki Eur J Med Chem (2021) 209: 112906-112906 [PMID:33049607]
ChEMBL Displacement of [3H](+)pentazocine from sigma1 receptor in Dunkin Hartley guinea pig brain membrane after 120 mins by liquid scintillation counting analysis B 8.55 pKi 2.8 nM Ki Eur J Med Chem (2013) 64: 488-497 [PMID:23680866]
ChEMBL Displacement of [3H]-(+)-pentazocine from sigma1 receptor in guinea pig brain membrane incubated for 150 mins by liquid scintillation counting method B 8.57 pKi 2.7 nM Ki Bioorg Med Chem (2016) 24: 3149-3156 [PMID:27262426]
ChEMBL Displacement of [3H]-PTZ from sigma1 receptor in guinea pig brain membranes after 150 mins in presence of 250 uM DPH by liquid scintillation counting method B 8.57 pKi 2.7 nM Ki Eur J Med Chem (2017) 125: 603-610 [PMID:27721146]
ChEMBL Displacement of [3H]-pentazocine from sigma1 receptor in guinea pig brain membranes by scintillation counting B 8.57 pKi 2.7 nM Ki J Med Chem (2016) 59: 9960-9966 [PMID:27739690]
ChEMBL Displacement of [3H]-(+)-pentazocine from sigma 1 receptor in Dunkin Hartley guinea pig membrane after 180 mins by liquid scintillation counting analysis B 8.59 pKi 2.6 nM Ki Eur J Med Chem (2014) 79: 216-230 [PMID:24735647]
ChEMBL Displacement of [3H]-PTZ from sigma1 receptor in guinea pig brain membranes after 150 mins in presence of DPH solvent by liquid scintillation counting method B 8.6 pKi 2.5 nM Ki Eur J Med Chem (2017) 125: 603-610 [PMID:27721146]
ChEMBL Displacement of [3H]-(+)-pentazocine from sigma 1 receptor guinea pig brain membranes incubated for 150 mins by scintillation counting method B 8.6 pKi 2.5 nM Ki Eur J Med Chem (2015) 90: 1-9 [PMID:25461306]
ChEMBL Displacement of [3H]-(+)-pentazocine from sigma 1 receptor in guinea pig brain membranes after 150 mins by liquid scintillation counting method B 8.6 pKi 2.5 nM Ki J Med Chem (2017) 60: 9531-9544 [PMID:29172528]
ChEMBL Displacement of [3H]-(+)-pentazocine from sigma1 receptor in guinea pig brain membranes incubated for 1 hr by liquid scintillation counting method B 8.6 pKi 2.5 nM Ki ACS Med Chem Lett (2020) 11: 889-894 [PMID:32435401]
ChEMBL Displacement of [3H]-(+)-pentazocine from sigma 1 receptor in guinea pig brain membrane after 150 mins by liquid scintillation counting B 8.66 pKi 2.2 nM Ki Eur J Med Chem (2011) 46: 433-438 [PMID:21055848]
ChEMBL Displacement of [3H]-(+)-pentazocine from sigma 1 receptor in guinea pig brain membranes after 150 mins B 8.66 pKi 2.2 nM Ki J Med Chem (2011) 54: 3669-3673 [PMID:21476493]
ChEMBL Displacement of [3H](+)-pentazocine from sigma 1 receptor in guinea pig brain membrane B 8.66 pKi 2.2 nM Ki Eur J Med Chem (2007) 42: 1247-1262 [PMID:17420073]
ChEMBL Displacement of [3H]-(+)-pentazocine from sigma1 receptor in guinea pig brain membrane after 150 mins by liquid scintillation counting method B 8.66 pKi 2.2 nM Ki J Med Chem (2018) 61: 372-384 [PMID:29220177]
ChEMBL Displacement of [3H](+)-pentazocine from sigma 1 receptor in guinea pig brain membrane by liquid scintillation analyzer B 8.66 pKi 2.2 nM Ki Eur J Med Chem (2009) 44: 519-525 [PMID:18499305]
ChEMBL Displacement of [3H](+)-pentazocine from sigma 1 receptor in guinea pig brain membranes after 150 mins by microbeta scintillation counting method B 8.66 pKi 2.2 nM Ki J Med Chem (2021) 64: 13622-13632 [PMID:34477381]
ChEMBL Displacement of [3H](+)-pentazocine from sigma 1 opioid receptor in guinea pig brain membrane B 8.72 pKi 1.9 nM Ki Bioorg Med Chem (2008) 16: 2992-3001 [PMID:18221879]
ChEMBL Displacement of [3H]-(+)-pentazocine from sigma 1 receptor in guinea pig brain membranes after 2 hrs by scintillation counting B 8.72 pKi 1.9 nM Ki Bioorg Med Chem (2016) 24: 4045-4055 [PMID:27396684]
ChEMBL Displacement of [3H](+)-pentazocine from sigma 1 receptor in guinea pig brain membrane B 8.72 pKi 1.9 nM Ki J Med Chem (2007) 50: 6144-6153 [PMID:17967001]
ChEMBL Displacement of [3H]-(+)-pentazocine from sigma1 receptor in guinea pig brain membranes incubated for 150 mins by scintillation counting method B 8.8 pKi 1.6 nM Ki Eur J Med Chem (2019) 174: 226-235 [PMID:31042618]
ChEMBL Displacement of [3H]-pentazocine from guinea pig sigma1 receptor by liquid scintillation counting B 8.82 pKi 1.5 nM Ki J Med Chem (2011) 54: 1555-1564 [PMID:21348515]
ChEMBL Displacement of [3H](+)-pentazocine from sigma 1 receptor in guinea pig brain homogenates after 1 hr by liquid scintillation counting B 8.84 pKi 1.45 nM Ki Bioorg Med Chem (2010) 18: 5291-5300 [PMID:20542439]
ChEMBL Displacement of [3H](+)-pentazocine from sigma 1-type opioid receptor in guinea pig brain homogenates B 8.84 pKi 1.45 nM Ki Bioorg Med Chem (2009) 17: 1222-1231 [PMID:19119012]
ChEMBL Displacement of [3H]-(+)-pentazocine from sigma-1 receptor in guinea pig brain membranes incubated for 1 hr in presence of 250 uM phenytoin liquid scintillation counting method B 8.85 pKi 1.4 nM Ki J Med Chem (2021) 64: 890-904 [PMID:33372782]
ChEMBL Displacement of [3H]-(+)-pentazocine from sigma-1 receptor in guinea pig brain membranes incubated for 1 hr by liquid scintillation counting method B 8.89 pKi 1.3 nM Ki J Med Chem (2021) 64: 890-904 [PMID:33372782]
ChEMBL Displacement of [3H]-(+)-pentazocine from guinea pig brain sigma1 receptor after 150 mins by scintillation counting analysis B 8.89 pKi 1.3 nM Ki Bioorg Med Chem (2014) 22: 393-397 [PMID:24290063]
ChEMBL Displacement of [3H]-(+)-pentazocine from Sigma1-receptor in guinea pig brain membrane B 9.08 pKi 0.83 nM Ki Bioorg Med Chem (2011) 19: 1852-1859 [PMID:21376604]
ChEMBL Displacement of [3H](+)-PTZ from sigma1 receptor in Hartley guinea pig brain B 9.08 pKi 0.83 nM Ki Bioorg Med Chem (2008) 16: 755-761 [PMID:18029187]
σ2/Sigma intracellular receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105907] [GtoPdb: 2553] [UniProtKB: Q5BJF2]
ChEMBL Binding affinity to sigma-2 receptor (unknown origin) B 6.66 pKi 221 nM Ki J Med Chem (2020) 63: 15187-15217 [PMID:33111525]
ChEMBL Displacement of [3H]-DTG from sigma-2 receptor in human Jurkat cell membrane incubated for 1 hr by liquid scintillation counting method B 7.08 pKi 83 nM Ki J Med Chem (2021) 64: 890-904 [PMID:33372782]
ChEMBL Displacement of [3H]-DTG from sigma2 receptor (unknown origin) incubated for 120 mins by scintillation counting method B 7.75 pKi 17.6 nM Ki Eur J Med Chem (2019) 174: 226-235 [PMID:31042618]
ChEMBL Displacement of [3H]-DTG from sigma 2 receptor (unknown origin) after 120 mins by liquid scintillation counting method B 7.8 pKi 16 nM Ki J Med Chem (2017) 60: 9531-9544 [PMID:29172528]
ChEMBL Displacement of [3H]-di-o-tolylguanidine from sigma2 receptor (unknown origin) incubated for 1 hr in presence of (+)SKF10047 by liquid scintillation counting method B 7.8 pKi 16 nM Ki ACS Med Chem Lett (2020) 11: 889-894 [PMID:32435401]
σ2/Sigma intracellular receptor 2 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105864] [GtoPdb: 2553] [UniProtKB: Q5U3Y7]
ChEMBL Displacement of [3H]-DTG from sigma2 receptor in rat brain membranes after 120 mins in presence of (+)-pentazocine by radioligand binding assay B 7.09 pKi 80.6 nM Ki Eur J Med Chem (2019) 165: 250-257 [PMID:30685525]
ChEMBL Displacement of [3H]-di-o-tolylguanidine from sigma2 receptor in rat liver membrane incubated for 120 mins measured for 5 mins by scintillation counting method B 7.11 pKi 78 nM Ki Bioorg Med Chem (2017) 25: 2472-2481 [PMID:28320613]
ChEMBL Displacement of [3H]-DTG from sigma2 receptor in rat liver membranes after 120 mins by liquid scintillation counting B 7.11 pKi 78 nM Ki Bioorg Med Chem (2017) 25: 4778-4799 [PMID:28764962]
ChEMBL Displacement of [3H]-DTG from sigma 2 receptor in rat liver membranes after 120 mins by scintillation counting analysis B 7.11 pKi 78 nM Ki Bioorg Med Chem (2018) 26: 501-508 [PMID:29254894]
ChEMBL Displacement of [3H]DTG from sigma2 receptor in Sprague-Dawley rat liver membranes after 120 mins by scintillation counting analysis B 7.11 pKi 78 nM Ki Medchemcomm (2016) 7: 2368-2380
ChEMBL Displacement of [3H]-di-o-tolylguanidine from sigma-2 receptor in rat liver membranes incubated for 120 mins measured for 5 mins by scintillation counting method B 7.11 pKi 78 nM Ki Eur J Med Chem (2018) 144: 672-681 [PMID:29289890]
ChEMBL Displacement of [3H]-di-o-tolylguanidine from sigma2 receptor in rat liver membranes in the presence of sigma1 receptor ligand (+)-pentazocine incubated for 120 mins by scintillation counting method B 7.11 pKi 78 nM Ki Eur J Med Chem (2019) 180: 268-282 [PMID:31319263]
ChEMBL Displacement of [3H]di-o-tolylguanidine from sigma2 receptor in rat liver membranes measured after 120 mins by solid scintillation counting method B 7.11 pKi 78 nM Ki Bioorg Med Chem (2019) 27: 115146-115146 [PMID:31648876]
ChEMBL Displacement of [3H]-Di-o-tolylguanidine from sigma-2 receptor in rat liver membranes after 120 mins by scintillation counting method B 7.11 pKi 78 nM Ki Bioorg Med Chem (2019) 27: 3559-3567 [PMID:31255496]
ChEMBL Displacement of [3H]DTG from sigma2 receptor in rat liver membranes after 120 mins by scintillation counting method B 7.11 pKi 78 nM Ki J Med Chem (2019) 62: 893-907 [PMID:30543421]
ChEMBL Displacement of [3H]-di-o-tolylguanidine from sigma2 receptor in rat liver membranes incubated for 120 mins by scintillation counting method B 7.11 pKi 78 nM Ki Eur J Med Chem (2019) 177: 47-62 [PMID:31129453]
ChEMBL Displacement of [3H]-di-o-tolylguanidine from sigma2 receptor in rat liver membrane by solid scintillation counting method B 7.11 pKi 78 nM Ki Eur J Med Chem (2021) 219: 113443-113443 [PMID:33901806]
ChEMBL Displacement of [3H]DTG from sigma 2 receptor in rat liver membranes incubated for 120 mins by scintillation counting method B 7.11 pKi 78 nM Ki Eur J Med Chem (2020) 190: 112138-112138 [PMID:32070917]
ChEMBL Displacement of [3H]-di-o-tolylguanidine from sigma2 receptor in rat liver membrane incubated for 120 mins by liquid scintillation counting method relative to control B 7.11 pKi 78 nM Ki Eur J Med Chem (2021) 210: 112950-112950 [PMID:33148494]
ChEMBL Displacement of [3H]DTG from sigma-2 receptor in rat liver membranes after 120 mins by microbeta scintillation counting method B 7.11 pKi 78 nM Ki Bioorg Med Chem (2017) 25: 3384-3395 [PMID:28501431]
ChEMBL Displacement of [3H]-di-o-tolylguanidine from sigma2 receptor in rat liver membranes incubated for 120 mins in the presence of sigma1 receptor ligand (+)-pentazocine by scintillation counting method B 7.11 pKi 78 nM Ki Bioorg Med Chem (2020) 28: 115245-115245 [PMID:31843460]
ChEMBL Displacement of [3H]-Di-o-tolylguanidine from sigma-2 receptor in rat liver membranes after 120 mins by scintillation counting method B 7.11 pKi 78 nM Ki ACS Med Chem Lett (2020) 11: 651-656 [PMID:32435366]
ChEMBL Displacement of [3H]DTG from sigma2 receptor in rat liver membranes after 60 mins by liquid scintillation counting method B 7.36 pKi 43.9 nM Ki J Med Chem (2018) 61: 6937-6943 [PMID:29969030]
ChEMBL Displacement of [125I]-RHM-4 from sigma 2 receptor in rat liver membranes after 120 mins by microbeta scintillation counting method B 7.45 pKi 35.22 nM Ki Eur J Med Chem (2021) 209: 112906-112906 [PMID:33049607]
ChEMBL Displacement of (+)-[3H]DTG from sigma 2 receptor in SPRD rat liver membrane incubated for 2 hrs by liquid scintillation counting method B 7.69 pKi 20.5 nM Ki RSC Med Chem (2021) 12: 1000-1004 [PMID:34223165]
sigma non-opioid intracellular receptor 1/Sigma opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL287] [GtoPdb: 2552] [UniProtKB: Q99720]
ChEMBL Displacement of [3H]-(+)-pentazocine from sigma-1 receptor in human RPMI8226 cell membranes after 120 mins by scintillation counting analysis B 7.4 pKi 40 nM Ki J Med Chem (2014) 57: 2884-2894 [PMID:24617836]
ChEMBL Displacement of [3H](+)-Pentazocine from sigma 1 receptor in human RPMI8226 cell membranes B 7.4 pKi 40 nM Ki J Med Chem (2016) 59: 5505-5519 [PMID:27156565]
ChEMBL Inhibitory constant against sigma receptor type 2 using 3 nM [3H]ditolylguanidine B 7.8 pKi 16 nM Ki J Med Chem (2005) 48: 266-273 [PMID:15634021]
ChEMBL Displacement of [3H](+)-pentazocine from human sigma 1 receptor in human Jurkat cell membranes incubated for 2 hrs by liquid scintillation counting B 7.92 pKi 11.9 nM Ki Eur J Med Chem (2015) 89: 198-206 [PMID:25462240]
ChEMBL Displacement of [3H](+)Pentazocine from sigma 1 receptor in human Jurkat cells after 120 mins by liquid scintillation counting analysis B 7.92 pKi 11.9 nM Ki Eur J Med Chem (2015) 92: 575-582 [PMID:25602932]
ChEMBL The compound was tested for its binding affinity towards Sigma opioid receptor in guinea pig brain membranes B 7.98 pKi 10.4 nM Ki J Med Chem (1991) 34: 3360-3365 [PMID:1662725]
ChEMBL Displacement of [3H]Haloperidol from sigma 1 receptor in human jurkat cells after 4 hrs B 8.06 pKi 8.8 nM Ki Bioorg Med Chem Lett (2013) 23: 1834-1838 [PMID:23403082]
ChEMBL Displacement of [3H](+)-pentazocine from sigma1 receptor in human Jurkat cell membrane B 8.11 pKi 7.76 nM Ki J Med Chem (2010) 53: 1261-1269 [PMID:20067271]
ChEMBL Displacement of [3H]-(+)-pentazocine from recombinant human sigma1 receptor expressed in HEK293 cell membranes after 120 mins by microbeta scintillation counting method B 8.15 pKi 7 nM Ki Bioorg Med Chem (2019) 27: 1824-1835 [PMID:30904383]
ChEMBL Binding affinity to sigma-1 receptor (unknown origin) B 8.19 pKi 6.4 nM Ki J Med Chem (2020) 63: 15187-15217 [PMID:33111525]
ChEMBL Binding affinity to sigma-1 receptor (unknown origin) by radioligand displacement assay B 8.2 pKi 6.3 nM Ki Bioorg Med Chem Lett (2016) 26: 889-893 [PMID:26750254]
ChEMBL Binding affinity for Sigma opioid receptor type 2 in guinea pig brain homogenate with 4 nM [3H]-(+)-DTG B 8.22 pKi 6 nM Ki Bioorg Med Chem Lett (1994) 4: 2185-2188
ChEMBL Displacement of (+)-[3H]pentazocine from human sigma1 receptor expressed in HEK293 cell membranes after 60 mins by liquid scintillation counting method B 8.23 pKi 5.9 nM Ki J Med Chem (2018) 61: 6937-6943 [PMID:29969030]
ChEMBL DRUGMATRIX: Sigma1 radioligand binding (ligand: [3H] Haloperidol) B 8.25 pKi 5.67 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL Inhibition of [3H]DTG binding to Sigma opioid receptor B 8.3 pKi 5 nM Ki J Med Chem (1991) 34: 1855-1859 [PMID:1648139]
ChEMBL Binding affinity against sigma receptor of MCF cells B 8.34 pKi 4.6 nM Ki J Med Chem (1994) 37: 1737-1739 [PMID:8021913]
ChEMBL Inhibitory activity against sigma receptor isolated from guinea pig brain cortex membrane using [3H]DTG as radioligand B 8.38 pKi 4.2 nM Ki J Med Chem (1996) 39: 176-182 [PMID:8568804]
ChEMBL Ability to displace [3H](+)-pentazocine at sigma receptor in guinea pig brain membrane was determined B 8.43 pKi 3.7 nM Ki J Med Chem (1993) 36: 2311-2320 [PMID:8360875]
ChEMBL Binding affinity was evaluated against sigma-1 binding site in guinea pig, using [3H]- -(+)- Pentazocine B 8.43 pKi 3.7 nM Ki J Med Chem (1993) 36: 566-571 [PMID:8496936]
ChEMBL Binding affinity towards sigma 1 receptor was determined in guinea pig brain membrane using [3H](+)-pentazocine as radioligand B 8.43 pKi 3.7 nM Ki J Med Chem (1994) 37: 314-321 [PMID:8295220]
ChEMBL Binding affinity for sigma receptor using [3H](+)-pentazocine in guinea pig brain homogenates B 8.43 pKi 3.7 nM Ki J Med Chem (1992) 35: 4334-4343 [PMID:1447735]
ChEMBL Compound was evaluated for its in vitro competition binding studies using sigma-ligand (0.05-10000 nM) - [3H](+)-pentazocine (sigma1 receptor) in guinea pig brain membranes B 8.43 pKi 3.7 nM Ki J Med Chem (1998) 41: 2445-2450 [PMID:9651150]
ChEMBL Displacement of [3H]pentazocine from human sigma 1 receptor expressed in HEK293 cell membrane incubated for 2 hrs by liquid scintillation counting method B 8.45 pKi 3.53 nM Ki RSC Med Chem (2021) 12: 1000-1004 [PMID:34223165]
ChEMBL Compound was tested for its binding affinity towards sigma 1 receptor using [3H](+)-pentazocine from guinea pig brain B 8.49 pKi 3.2 nM Ki J Med Chem (1998) 41: 1557-1560 [PMID:9572880]
ChEMBL Compound tested for binding affinity towards sigma 1 receptor in quinea pig brain membranes using [3H](+)-pentazocine as the radioligand. B 8.6 pKi 2.53 nM Ki J Med Chem (1998) 41: 2361-2370 [PMID:9632369]
ChEMBL Binding affinity for sigma 1 opioid receptor, measured on guinea pig brain membranes using [3H]- (+)-pentazocine as radioligand B 8.6 pKi 2.53 nM Ki J Med Chem (2001) 44: 4404-4415 [PMID:11728186]
ChEMBL Displacement of [3H]-Pentazocine from sigma 1 receptor (unknown origin) expressed in HEK293T cell membranes B 8.61 pKi 2.46 nM Ki Bioorg Med Chem (2019) 27: 2629-2636 [PMID:30987780]
ChEMBL Displacement of [3H]-Pentazocine from sigma 1 receptor (unknown origin) expressed in HEK293T cell membranes B 8.61 pKi 2.46 nM Ki Bioorg Med Chem (2019) 27: 2629-2636 [PMID:30987780]
ChEMBL Displacement of [3H]-pentazocine from sigma-1 receptor in human Jurkat cell membrane incubated for 2 hr by liquid scintillation counting method B 8.64 pKi 2.3 nM Ki J Med Chem (2021) 64: 890-904 [PMID:33372782]
ChEMBL Ability to displace [3H](+)-pentazocine from Sigma opioid receptor type 1 of guinea pig brain B 8.66 pKi 2.2 nM Ki J Med Chem (2002) 45: 4923-4930 [PMID:12383018]
ChEMBL Sigma opioid receptor type 1 affinity in guinea pig brain by employing [3H](+)-pentazocine as radioligand. B 8.66 pKi 2.2 nM Ki J Med Chem (2002) 45: 438-448 [PMID:11784148]
ChEMBL Inhibitory constant against sigma receptor type 1 using 3 nM [3H]pentazocine B 8.66 pKi 2.2 nM Ki J Med Chem (2005) 48: 266-273 [PMID:15634021]
ChEMBL Displacement of [3H]-(+)-pentazocine from human sigma1 receptor transfected in HEK293 cells after 120 mins by liquid scintillation counting analysis B 8.68 pKi 2.1 nM Ki J Med Chem (2013) 56: 3656-3665 [PMID:23560650]
ChEMBL Displacement of [3H](+)pentazocine from human sigma 1 receptor transfected in HEK293 cell membranes after 120 mins by scintillation counter B 8.68 pKi 2.1 nM Ki J Med Chem (2012) 55: 8211-8224 [PMID:22784008]
ChEMBL Displacement of [3H]-(+)-pentazocine from human sigma-1 receptor expressed in HEK293 membranes incubated for 120 mins by liquid scintillation counting method B 8.7 pKi 2 nM Ki J Med Chem (2020) 63: 2434-2454 [PMID:31743642]
ChEMBL Displacement of [3H]-(+)-pentazocine from human sigma1 receptor expressed in HEK293 cell membranes incubated for 120 mins by liquid scintillation counting method B 8.7 pKi 2 nM Ki J Med Chem (2020) 63: 14979-14988 [PMID:33237785]
ChEMBL Inhibition of sigma 1 receptor B 8.72 pKi 1.9 nM Ki J Med Chem (2011) 54: 2529-2591 [PMID:21413808]
ChEMBL Inhibition of [3H]- pentazocine binding against alpha-1 from guinea pig brain B 8.74 pKi 1.8 nM Ki J Med Chem (1999) 42: 5181-5187 [PMID:10602703]
ChEMBL Displacement of [3H](+)Pentazocine from sigma 1 receptor (unknown origin) B 8.78 pKi 1.66 nM Ki Bioorg Med Chem Lett (2014) 24: 576-579 [PMID:24365159]
ChEMBL Displacement of [3H]-(+)-pentazocine from sigma-1 receptor in human Jurkat cell membranes after 2 hrs by liquid scintillation counting method B 8.8 pKi 1.6 nM Ki Eur J Med Chem (2019) 162: 234-248 [PMID:30447434]
ChEMBL Inhibition of [3H]pentazocine binding to sigma-1 sites in guinea pig brain membranes B 8.8 pKi 1.6 nM Ki J Med Chem (1998) 41: 1574-1580 [PMID:9572883]
ChEMBL Binding affinity measured at the sigma receptor by the inhibition of [3H]-3-PPP binding to guinea pig cerebellum using unlabeled 3-PPP for nonspecific binding. B 8.82 pKi 1.5 nM Ki J Med Chem (1998) 41: 5402-5409 [PMID:9876110]
ChEMBL Binding affinity for sigma-1 receptor measured on guinea pig brain membranes using [3H](+)-pentazocine as radioligand B 8.82 pKi 1.5 nM Ki J Med Chem (2001) 44: 1815-1826 [PMID:11356115]
ChEMBL Displacement of [3H](+)Pentazocine from sigma 1 receptor (unknown origin) B 8.92 pKi 1.2 nM Ki Bioorg Med Chem Lett (2014) 24: 576-579 [PMID:24365159]
ChEMBL Displacement of [3H](+)-pentazocine from human sigma1 receptor by PDSP assay B 8.96 pKi 1.1 nM Ki Bioorg Med Chem (2016) 24: 2060-2071 [PMID:27032890]
ChEMBL Binding affinity for Sigma opioid receptor type 1 in guinea pig brain homogenate with 0.5 nM [3H](+)-PENT B 9.22 pKi 0.6 nM Ki Bioorg Med Chem Lett (1994) 4: 2185-2188
ChEMBL The compound was evaluated for affinity at sigma-1 site by inhibition of [3H](+)-pentazocine (PENT) binding in guinea pig brain. B 9.22 pKi 0.6 nM Ki J Med Chem (1994) 37: 1964-1970 [PMID:8027978]
ChEMBL Inhibition of [3H]pentazocine binding to Sigma opioid receptor type 1 B 9.36 pKi 0.44 nM Ki Bioorg Med Chem Lett (1997) 7: 2303-2306
ChEMBL Tested for [3H](+)-pentazocine binding to sigma-1 receptor in guinea pig brain membrane B 9.48 pKi 0.33 nM Ki J Med Chem (1993) 36: 3929-3936 [PMID:7902870]
ChEMBL Displacement of [3H]-(+)-pentazocine from sigma1 in human MDA-MB-468 cell membranes B 9.68 pKi 0.21 nM Ki Bioorg Med Chem Lett (2017) 27: 2216-2220 [PMID:28385503]
ChEMBL Affinity for sigma receptor type 1 of guinea pig using [3H]ifenprodil or (+)-[3H]pentazocine radioligand B 9.7 pKi 0.2 nM Ki J Med Chem (2005) 48: 4754-4764 [PMID:16033255]
ChEMBL Displacement of [3H](+)-pentazocine from sigma 1 opioid receptor in human Jurkat cells by scintillation counting B 6.64 pIC50 230 nM IC50 Eur J Med Chem (2010) 45: 256-263 [PMID:19875205]
ChEMBL The compound was tested for affinity towards sigma-3 receptor B 6.67 pIC50 213.8 nM IC50 J Med Chem (1994) 37: 4109-4117 [PMID:7990111]
ChEMBL Displacement of [3H]Haloperidol from sigma 1 receptor in human jurkat cells after 4 hrs B 7.68 pIC50 21 nM IC50 Bioorg Med Chem Lett (2013) 23: 1834-1838 [PMID:23403082]
ChEMBL Inhibition of specific binding of [3H]3-PPP to sigma binding site in Guinea pig brain membranes B 7.77 pIC50 17 nM IC50 J Med Chem (1992) 35: 4683-4689 [PMID:1469697]
ChEMBL DRUGMATRIX: Sigma1 radioligand binding (ligand: [3H] Haloperidol) B 7.89 pIC50 13 nM IC50 DrugMatrix in vitro pharmacology data
ChEMBL Inhibition of specific binding of [125I]-PIPAG to sigma binding site in Guinea pig brain membranes B 8.1 pIC50 8 nM IC50 J Med Chem (1992) 35: 4683-4689 [PMID:1469697]
ChEMBL In vitro binding affinity measured on sigma opioid receptor using [3H]DTG as radioligand B 8.25 pIC50 5.64 nM IC50 J Med Chem (1995) 38: 942-949 [PMID:7699710]
ChEMBL Displacement of [3H]DTG from sigma opioid receptor of homogenized guinea pig whole brain B 8.3 pIC50 5 nM IC50 J Med Chem (1991) 34: 1867-1870 [PMID:1648140]
ChEMBL Inhibition of specific binding of [3H]DTG to sigma binding site in Guinea pig brain membranes B 8.3 pIC50 5 nM IC50 J Med Chem (1992) 35: 4683-4689 [PMID:1469697]
ChEMBL Inhibition of specific binding of [3H]NANM of sigma binding site in Guinea pig brain membranes B 8.4 pIC50 4 nM IC50 J Med Chem (1992) 35: 4683-4689 [PMID:1469697]
ChEMBL Inhibitory activity against opioid receptor sigma 1 in guinea pig cerebral cortex using [3H](+)-pentazocine as radio ligand at pH 7.5 for 150 min at 22 degree C B 8.68 pIC50 2.1 nM IC50 Bioorg Med Chem Lett (2005) 15: 4828-4832 [PMID:16140009]
ChEMBL Inhibitory concentration against opioid receptor sigma 1 of guinea pig cerebral cortex using [3H](+)-pentazocine upon incubation for 150 minutes at 22 degree C B 8.68 pIC50 2.1 nM IC50 Bioorg Med Chem Lett (2005) 15: 4833-4837 [PMID:16140011]
sigma non-opioid intracellular receptor 1/Sigma opioid receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3602] [GtoPdb: 2552] [UniProtKB: Q9R0C9]
ChEMBL Binding affinity was measured on Sigma receptor type 2 with rat liver membranes and [3H]- DTG as ligand. B 7.33 pKi 46.5 nM Ki J Med Chem (2000) 43: 3913-3922 [PMID:11052796]
ChEMBL Binding affinity of compound towards sigma receptor using [3H]DTG (4 nM) ligand in hippocampus rat was determined B 7.42 pKi 38 nM Ki J Med Chem (1997) 40: 952-960 [PMID:9083484]
ChEMBL Ability to displace [3H]ditolylguanidine in the presence of 100 nM (+)-pentazocine from Sigma opioid receptor type 2 of rat liver B 7.47 pKi 34.2 nM Ki J Med Chem (2002) 45: 4923-4930 [PMID:12383018]
ChEMBL Sigma opioid receptor type 2 affinity in rat liver by employing [3H]ditolylguanidine as radioligand B 7.47 pKi 34.2 nM Ki J Med Chem (2002) 45: 438-448 [PMID:11784148]
ChEMBL Inhibitory activity against Opioid receptor sigma 1 isolated from whole rat membranes using [3H](+)-pentazocine as radioligand B 8 pKi 10 nM Ki J Med Chem (1996) 39: 176-182 [PMID:8568804]
ChEMBL Displacement of [3H]pentazocine from sigma 1 receptor in rat brain membrane after 2.5 hrs by microbeta scintillation counting analysis B 8.15 pKi 7 nM Ki ACS Med Chem Lett (2012) 3: 1054-1058 [PMID:23641311]
ChEMBL Displacement of [3H]-pentazocine from sigma 1 opioid receptor in rat liver homogenate by liquid scintillation counting B 8.24 pKi 5.7 nM Ki ACS Med Chem Lett (2011) 2: 834-839 [PMID:24900272]
ChEMBL Displacement of [3H](+)-pentazocine from sigma 1 receptor in rat liver membrane B 8.24 pKi 5.7 nM Ki Eur J Med Chem (2009) 44: 124-130 [PMID:18440098]
ChEMBL Displacement of [3H](+)-pentazocine from sigma1 receptor in rat liver membrane by liquid scintillation counting B 8.24 pKi 5.7 nM Ki J Med Chem (2009) 52: 5380-5393 [PMID:19673530]
ChEMBL Displacement of (+)-[3H]pentazocine from sigma1 receptor in rat brain membranes after 60 mins by liquid scintillation counting method B 8.27 pKi 5.39 nM Ki J Med Chem (2018) 61: 6937-6943 [PMID:29969030]
ChEMBL Displacement of (+)-[3H]pentazocine from rat brain sigma1 receptor by competitive binding assay B 8.31 pKi 4.95 nM Ki J Med Chem (2013) 56: 3478-3491 [PMID:23566245]
ChEMBL Displacement of (+)-[3H]pentazocine from sigma1 receptor in rat brain membranes B 8.31 pKi 4.95 nM Ki Bioorg Med Chem (2013) 21: 215-222 [PMID:23199475]
ChEMBL Displacement of (+)-[3H]pentazocine from sigma1 receptor in Sprague-Dawley rat cerebral membrane after 90 mins by liquid scintillation counting B 8.46 pKi 3.5 nM Ki Bioorg Med Chem (2012) 20: 4936-4941 [PMID:22831799]
ChEMBL Displacement of [3H](+)-pentazocine from sigma1 receptor in rat brain membranes after 120 mins by radioligand binding assay B 8.47 pKi 3.35 nM Ki Eur J Med Chem (2019) 165: 250-257 [PMID:30685525]
ChEMBL Displacement of [3H](+)-pentazocine from opioid sigma1 receptor in rat brain homogenate B 8.47 pKi 3.35 nM Ki J Med Chem (2008) 51: 1482-1486 [PMID:18278854]
ChEMBL Displacement of (-)-[3H]pentazocine from sigma 1 receptor in rat brain membrane after 120 mins B 8.47 pKi 3.35 nM Ki Eur J Med Chem (2011) 46: 5154-5161 [PMID:21899931]
ChEMBL Displacement of [3H](+)-pentazocine from Sigma1 receptor in rat brain homogenate B 8.47 pKi 3.35 nM Ki J Med Chem (2012) 55: 8272-8282 [PMID:22853801]
ChEMBL Displacement of [3H](+)-pentazocine from Sigma1 receptor in rat liver homogenate B 8.48 pKi 3.3 nM Ki J Med Chem (2012) 55: 8272-8282 [PMID:22853801]
ChEMBL Binding affinity was measured on Sigma receptor type 1 with guinea pig membranes and [3H]- pentazocine as ligand. B 8.53 pKi 2.95 nM Ki J Med Chem (2000) 43: 3913-3922 [PMID:11052796]
ChEMBL Displacement of [3H](+)-pentazocine from sigma 1 receptor in rat brain membrane after 2.5 hrs by scintillation counting B 8.77 pKi 1.7 nM Ki Bioorg Med Chem (2012) 20: 6856-6861 [PMID:23084435]
ChEMBL Displacement of [3H](+)-pentazocine from sigma 1 receptor in rat brain homogenate B 9.05 pKi 0.9 nM Ki Bioorg Med Chem Lett (2011) 21: 3622-3626 [PMID:21555222]
ChEMBL Binding affinity towards Sigma receptor type 2 in whole rat brain homogenates except cerebellum using radioligand ([3H]DTG) binding assay. B 7.77 pIC50 17 nM IC50 J Med Chem (1995) 38: 2009-2017 [PMID:7783132]
ChEMBL Binding effinity for sigma receptor using 2 nM of [3H]-DTG as radioligand, in membranes from brain minus cerebellum B 7.77 pIC50 17 nM IC50 J Med Chem (1993) 36: 3188-3196 [PMID:8230107]
ChEMBL Inhibitory activity against Sigma opioid receptor B 8.52 pIC50 3 nM IC50 J Med Chem (1991) 34: 1855-1859 [PMID:1648139]
ChEMBL Compound was tested in vitro for its ability to displace radioligand (+)-[3H]-3-PPP from rat cortical sigma receptor B 8.85 pIC50 1.4 nM IC50 J Med Chem (1992) 35: 4516-4525 [PMID:1361578]
ChEMBL Compound was evaluated for the binding affinity towards Sigma receptor type 1 using radioligand ([3H]-(+)- Pentazocine) binding assay. B 9.19 pIC50 0.65 nM IC50 J Med Chem (1995) 38: 2009-2017 [PMID:7783132]
ChEMBL Binding affinity towards sigma receptor binding site 1 using [3H](+)-pentazocine B 9.19 pIC50 0.65 nM IC50 J Med Chem (1995) 38: 1998-2008 [PMID:7783131]
Transporter in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6184] [UniProtKB: Q63380]
ChEMBL Binding affinity to rat NET B 5.26 pKi 5500 nM Ki Bioorg Med Chem (2008) 16: 7291-7301 [PMID:18595716]
Vesicular acetylcholine transporter in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2125] [GtoPdb: 1013] [UniProtKB: Q62666]
ChEMBL Displacement of (-)-[3H]vesamicol from rat VAChT expressed in rat PC12 cell membranes after 60 mins by liquid scintillation counting method B 6.41 pKi 391 nM Ki J Med Chem (2018) 61: 6937-6943 [PMID:29969030]
Zinc finger protein 664 in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105757] [UniProtKB: Q60493]
ChEMBL Displacement of [3H]-(+)-pentazocine from sigma1-type opioid receptor in guinea pig cortex membranes after 120 mins by solid scintillation counting B 8.18 pKi 6.6 nM Ki J Med Chem (2017) 60: 2526-2551 [PMID:28218838]
5-HT1D receptor in Human [GtoPdb: 3] [UniProtKB: P28221]
GtoPdb - - 6.6 pKi - - - Psychopharmacology (Berl.) (1996) 124: 57-73 [PMID:8935801]
Kir3.2 in Mouse [GtoPdb: 435] [UniProtKB: P48542]
GtoPdb - - 4.1 pEC50 - - - Br J Pharmacol (2000) 129: 1716-22 [PMID:10780978]
Kv10.1 in Human [GtoPdb: 570] [UniProtKB: O95259]
GtoPdb - - 6.2 pIC50 - - - Br J Pharmacol (2003) 138: 161-71 [PMID:12522086]

ChEMBL data shown on this page come from version 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]