chlorpromazine [Ligand Id: 83] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL71 (Aminazine, Chlorpromazine, Chlorpromazine hibenzate, Chlorpromazine phenolphthalinate, Chlorpromazine tannate, Chlorpromazinum, Elmarin, Esmind, Fenactil, J2.794D, Largactil, Largactilothiazine, Megaphen, Novomazina, NSC-167745, NSC-226514, Propaphenin, Sanopron, SKF-2601A, Sonazine, Thorazine, Wintermin)
  • Acetylcholine receptor protein alpha chain in Torpedo californica [ChEMBL: CHEMBL3097] [UniProtKB: P02710]
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  • 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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  • Arachidonate 15-lipoxygenase in Rabbit [ChEMBL: CHEMBL4358] [UniProtKB: P12530]
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  • δ receptor/Delta opioid receptor in Human [ChEMBL: CHEMBL236] [GtoPdb: 317] [UniProtKB: P41143]
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  • D1 receptor/Dopamine D1 receptor in Human [ChEMBL: CHEMBL2056] [GtoPdb: 214] [UniProtKB: P21728]
  • D1 receptor/Dopamine D1 receptor in Rat [ChEMBL: CHEMBL265] [GtoPdb: 214] [UniProtKB: P18901]
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  • 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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  • D3 receptor/Dopamine D3 receptor in Human [ChEMBL: CHEMBL234] [GtoPdb: 216] [UniProtKB: P35462]
  • D3 receptor in Rat [GtoPdb: 216] [UniProtKB: P19020]
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  • D4 receptor/Dopamine D4 receptor in Human [ChEMBL: CHEMBL219] [GtoPdb: 217] [UniProtKB: P21917]
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  • D5 receptor/Dopamine D5 receptor in Human [ChEMBL: CHEMBL1850] [GtoPdb: 218] [UniProtKB: P21918]
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  • epidermal growth factor receptor/Epidermal growth factor receptor erbB1 in Human [ChEMBL: CHEMBL203] [GtoPdb: 1797] [UniProtKB: P00533]
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  • H1 receptor/Histamine H1 receptor in Human [ChEMBL: CHEMBL231] [GtoPdb: 262] [UniProtKB: P35367]
  • 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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  • H3 receptor/Histamine H3 receptor in Human [ChEMBL: CHEMBL264] [GtoPdb: 264] [UniProtKB: Q9Y5N1]
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  • κ receptor/Kappa opioid receptor in Human [ChEMBL: CHEMBL237] [GtoPdb: 318] [UniProtKB: P41145]
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  • MC3 receptor/Melanocortin receptor 3 in Human [ChEMBL: CHEMBL4644] [GtoPdb: 284] [UniProtKB: P41968]
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  • MC4 receptor/Melanocortin receptor 4 in Human [ChEMBL: CHEMBL259] [GtoPdb: 285] [UniProtKB: P32245]
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  • MC5 receptor/Melanocortin receptor 5 in Human [ChEMBL: CHEMBL4608] [GtoPdb: 286] [UniProtKB: P33032]
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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]
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  • M2 receptor/Muscarinic acetylcholine receptor M2 in Human [ChEMBL: CHEMBL211] [GtoPdb: 14] [UniProtKB: P08172]
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  • M3 receptor/Muscarinic acetylcholine receptor M3 in Human [ChEMBL: CHEMBL245] [GtoPdb: 15] [UniProtKB: P20309]
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  • M4 receptor/Muscarinic acetylcholine receptor M4 in Human [ChEMBL: CHEMBL1821] [GtoPdb: 16] [UniProtKB: P08173]
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  • M5 receptor/Muscarinic acetylcholine receptor M5 in Human [ChEMBL: CHEMBL2035] [GtoPdb: 17] [UniProtKB: P08912]
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  • NK2 receptor/Neurokinin 2 receptor in Human [ChEMBL: CHEMBL2327] [GtoPdb: 361] [UniProtKB: P21452]
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  • NET/Norepinephrine transporter in Human [ChEMBL: CHEMBL222] [GtoPdb: 926] [UniProtKB: P23975]
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  • Pleiotropic ABC efflux transporter of multiple drugs in Saccharomyces cerevisiae S288c [ChEMBL: CHEMBL1697658] [UniProtKB: P33302]
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  • K2P2.1/Potassium channel subfamily K member 2 in Human [ChEMBL: CHEMBL2321615] [GtoPdb: 514] [UniProtKB: O95069]
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  • erb-b2 receptor tyrosine kinase 2/Receptor protein-tyrosine kinase erbB-2 in Human [ChEMBL: CHEMBL1824] [GtoPdb: 2019] [UniProtKB: P04626]
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  • Sarcoplasmic/endoplasmic reticulum calcium ATP-ase in Rabbit [ChEMBL: CHEMBL4693] [UniProtKB: P04191]
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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]
  • 5-HT2A receptor in Rat [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]
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  • 5-HT6 receptor/Serotonin 6 (5-HT6) receptor in Human [ChEMBL: CHEMBL3371] [GtoPdb: 11] [UniProtKB: P50406]
  • 5-HT6 receptor in Rat [GtoPdb: 11] [UniProtKB: P31388]
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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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  • SERT/Serotonin transporter in Human [ChEMBL: CHEMBL228] [GtoPdb: 928] [UniProtKB: P31645]
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  • sigma non-opioid intracellular receptor 1/Sigma opioid receptor in Human [ChEMBL: CHEMBL287] [GtoPdb: 2552] [UniProtKB: Q99720]
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  • Organic cation transporter 1/Solute carrier family 22 member 1 in Human [ChEMBL: CHEMBL5685] [GtoPdb: 1019] [UniProtKB: O15245]
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  • sphingomyelin phosphodiesterase 1/Sphingomyelin phosphodiesterase in Human [ChEMBL: CHEMBL2760] [GtoPdb: 2514] [UniProtKB: P17405]
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  • Trypanothione reductase in Trypanosoma cruzi [ChEMBL: CHEMBL5131] [UniProtKB: P28593]
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  • FYN proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase FYN in Human [ChEMBL: CHEMBL1841] [GtoPdb: 2026] [UniProtKB: P06241]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
Acetylcholine receptor protein alpha chain in Torpedo californica (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3097] [UniProtKB: P02710]
ChEMBL Displacement of [3H]PCP from nAChR in Torpedo nobiliana electric organs membranes by scintillation counting method B 4.79 pIC50 16400 nM IC50 J Pestic Sci (1995) 20: 49-56
ChEMBL Displacement of [3H]PCP from nAChR in Torpedo nobiliana electric organs membranes in presence of 100 uM carbachol by scintillation counting method B 5.89 pIC50 1280 nM IC50 J Pestic Sci (1995) 20: 49-56
α1A-adrenoceptor/Alpha-1a adrenergic receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL319] [GtoPdb: 22] [UniProtKB: P43140]
ChEMBL DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin) B 8.46 pKi 3.46 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin) B 8.07 pIC50 8.54 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 8.3 pKi 4.96 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Alpha-1B adrenergic receptor radioligand binding (ligand: prazosin) B 8.05 pIC50 8.97 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 8.71 pKi 1.96 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Alpha-1D adrenergic receptor radioligand binding (ligand: prazosin) B 8.4 pIC50 3.99 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]
GtoPdb - - 6.6 pKi - - - Mol Pharmacol (1992) 42: 1-5 [PMID:1353247];
Eur J Pharmacol (1994) 252: 43-9 [PMID:7908642];
Pharmacol Res Perspect (2022) 10: e00936 [PMID:35224877]
ChEMBL DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912) B 6.88 pKi 132 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912) B 6.45 pIC50 352 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 7.92 pKi 12 nM Ki DrugMatrix in vitro pharmacology data
GtoPdb - - 8.3 pKi - - - Mol Pharmacol (1992) 42: 1-5 [PMID:1353247];
Eur J Pharmacol (1994) 252: 43-9 [PMID:7908642];
Pharmacol Res Perspect (2022) 10: e00936 [PMID:35224877]
ChEMBL DRUGMATRIX: Alpha-2B adrenergic receptor radioligand binding (ligand: Rauwolscine) B 7.59 pIC50 26 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 7.27 pKi 54 nM Ki DrugMatrix in vitro pharmacology data
GtoPdb - - 7.4 pKi - - - Mol Pharmacol (1992) 42: 1-5 [PMID:1353247];
Eur J Pharmacol (1994) 252: 43-9 [PMID:7908642];
Pharmacol Res Perspect (2022) 10: e00936 [PMID:35224877]
ChEMBL DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912) B 6.43 pIC50 374 nM IC50 DrugMatrix in vitro pharmacology data
Arachidonate 15-lipoxygenase in Rabbit (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4358] [UniProtKB: P12530]
ChEMBL DRUGMATRIX: Lipoxygenase 15-LO enzyme inhibition (substrate: Linoleic acid) B 4.8 pIC50 15951 nM IC50 DrugMatrix in vitro pharmacology data
ABCB11/Bile salt export pump in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6020] [GtoPdb: 778] [UniProtKB: O95342]
ChEMBL TP_TRANSPORTER: increase in dihydrofluorescein intracellular accumulation (dihydrofluorescein: 1 uM) in SK-E2 cells (expressing BSEP) F 4.47 pIC50 33500 nM IC50 Pharm Res (2003) 20: 537-544 [PMID:12739759]
ChEMBL TP_TRANSPORTER: increase in bodipy intracellular accumulation (Bodipy: 0.2 uM) in SK-E2 cells (expressing BSEP) F 4.51 pIC50 30900 nM IC50 Pharm Res (2003) 20: 537-544 [PMID:12739759]
Calmodulin in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6093] [UniProtKB: P0DP23]
ChEMBL Binding affinity to human calmodulin expressed in Escherichia coli using M124C-mBBr fluorescent biosensor by spectrofluorometer analysis B 5.91 pKd 1240 nM Kd J Nat Prod (2013) 76: 1454-1460 [PMID:23876004]
ChEMBL Inhibition of recombinant calmodulin mediated bovine brain PDE1 activation assessed as effect on inorganic phosphate release using variable calmodulin level by spectrophotometry B 4.71 pKi 19280 nM Ki Bioorg Med Chem (2009) 17: 2167-2174 [PMID:19013822]
ChEMBL Inhibition of Calmodulin-dependent PDE1 activity assessed as inorganic phosphate release after 30 min B 4.99 pIC50 10300 nM IC50 Eur J Med Chem (2011) 46: 2699-2708 [PMID:21514702]
ChEMBL Binding affinity to CaM (unknown origin) by equilibrium dialysis method B 5.1 pIC50 8000 nM IC50 Eur J Med Chem (2016) 116: 36-45 [PMID:27043269]
ChEMBL Inhibition of recombinant calmodulin mediated bovine brain PDE1 activation assessed as effect on inorganic phosphate release by spectrophotometry B 5.14 pIC50 7260 nM IC50 Bioorg Med Chem (2009) 17: 2167-2174 [PMID:19013822]
Calmodulin in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6092] [UniProtKB: P62157]
ChEMBL Binding affinity to bovine brain CaM by FTPFACE analysis B 5.51 pKd 3100 nM Kd Eur J Med Chem (2016) 116: 36-45 [PMID:27043269]
ChEMBL Displacement of [3H]W-7 from bovine brain CaM B 5.6 pIC50 2500 nM IC50 Eur J Med Chem (2016) 116: 36-45 [PMID:27043269]
δ receptor/Delta opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL236] [GtoPdb: 317] [UniProtKB: P41143]
ChEMBL DRUGMATRIX: Opiate delta1 (OP1, DOP) radioligand binding (ligand: [3H] Naltrindole) B 5.13 pKi 7365 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Opiate delta1 (OP1, DOP) radioligand binding (ligand: [3H] Naltrindole) B 4.68 pIC50 20894 nM IC50 DrugMatrix in vitro pharmacology data
D1 receptor/Dopamine D1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2056] [GtoPdb: 214] [UniProtKB: P21728]
ChEMBL DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390) B 6.95 pKi 112 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK cells B 7.02 pKi 96 nM Ki Bioorg Med Chem Lett (2009) 19: 538-542 [PMID:19091563]
GtoPdb - - 7.1 pKi - - - Nature (1991) 350: 614-9 [PMID:1826762]
ChEMBL DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390) B 6.65 pIC50 225 nM IC50 DrugMatrix in vitro pharmacology data
D1 receptor/Dopamine D1 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL265] [GtoPdb: 214] [UniProtKB: P18901]
ChEMBL Inhibition of [3H]SCH-23,390 binding to Dopamine receptor D1 at 0.25 nM B 7.3 pKi 50 nM Ki J Med Chem (1988) 31: 1941-1946 [PMID:3050089]
ChEMBL Binding affinity against dopamine receptor D1 B 7.45 pKi 35.48 nM Ki J Med Chem (1994) 37: 519-525 [PMID:7907148]
ChEMBL In vitro binding affinity against Dopamine receptor D1 in rat striatal tissue B 7.46 pKi 35 nM Ki J Med Chem (1993) 36: 2107-2114 [PMID:8101877]
ChEMBL Binding affinity against Dopamine receptor D1 by using [3H]SCH-23390 as radioligand B 8.67 pIC50 2.15 nM IC50 J Med Chem (1995) 38: 318-327 [PMID:7830274]
D2 receptor/Dopamine D2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416]
GtoPdb - - 7.6 pKi - - - J Pharmacol Exp Ther (1994) 268: 417-26 [PMID:8301582];
Eur J Pharmacol (1992) 225: 331-7 [PMID:1354163]
ChEMBL DRUGMATRIX: Dopamine D2L radioligand binding (ligand: [3H] Spiperone) B 7.74 pKi 18 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL Displacement of [3H]spiperone from human dopamine D2 receptor short form expressed in CHO cells B 8 pKi 10 nM Ki J Med Chem (2007) 50: 5103-5108 [PMID:17880057]
ChEMBL Displacement of [3H]spiperone from dopamine D2-like receptor in porcine striata homogenate B 8.1 pKi 8 nM Ki J Med Chem (2006) 49: 6848-6857 [PMID:17154515]
ChEMBL Displacement of [3H]spiperone from human D2 receptor transfected in HEK cells B 8.21 pKi 6.1 nM Ki J Med Chem (2014) 57: 4368-4381 [PMID:24779610]
ChEMBL Displacement of [3H]spiperone from human dopamine D2 receptor expressed in CHO cells B 8.39 pKi 4.06 nM Ki Bioorg Med Chem Lett (2009) 19: 538-542 [PMID:19091563]
ChEMBL Displacement of [3H]-methylspiperone from human D2 receptor transfected in CHO-K1 cells measured after 60 mins by scintillation counting method B 8.63 pKi 2.34 nM Ki J Med Chem (2021) 64: 12603-12629 [PMID:34436892]
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 8.74 pKi 1.8 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 8.74 pKi 1.8 nM Ki Eur J Med Chem (2019) 166: 144-158 [PMID:30703658]
ChEMBL Displacement of [3H]-N-methylspiperone from human dopamine D2long receptor expressed in HEK293 cells after 30 mins by scintillation counting B 8.92 pKi 1.2 nM Ki Bioorg Med Chem (2012) 20: 6366-6374 [PMID:23018094]
ChEMBL DRUGMATRIX: Dopamine D2L radioligand binding (ligand: [3H] Spiperone) B 7.27 pIC50 54 nM IC50 DrugMatrix in vitro pharmacology data
ChEMBL Binding affinity to dopamine D2 receptor (unknown origin) by radioligand binding assay B 7.92 pIC50 12 nM IC50 J Med Chem (2013) 56: 8955-8971 [PMID:23919353]
ChEMBL Antagonist activity at human D2 receptor expressed in CHO-K1 cells co-expressing Galphaqi5 assessed as decrease in apomorphine-induced calcium mobilization preincubated for 30 mins followed by apomorphine challenge measured for 30 secs by aequorin-derived luminescence assay F 8.52 pIC50 3 nM IC50 Bioorg Med Chem Lett (2018) 28: 2039-2049 [PMID:29730027]
ChEMBL Antagonist activity against human recombinant dopmaine D2L receptor expressed in CHOK1 cells assessed as reduction in apomorphine-induced increase in intracellular Ca2+ levels by aequorin based radiometric and luminescence plate counting method F 9 pIC50 1 nM IC50 Eur J Med Chem (2015) 92: 221-235 [PMID:25557493]
ChEMBL Antagonist activity at human dopamine D2 receptor expressed in CHOK1 cells assessed as inhibition of apomorphine-induced calcium mobilization by radiometric and luminescence plate counting method F 9 pIC50 1 nM IC50 Eur J Med Chem (2015) 92: 221-235 [PMID:25557493]
Dopamine D2 receptor in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3998] [UniProtKB: P20288]
ChEMBL Competition in vitro with the dopamine receptor D2 antagonist [3H]spiperone, for binding sites on calf caudate membranes. B 7.1 pIC50 80 nM IC50 J Med Chem (1993) 36: 912-918 [PMID:8096548]
D2 receptor/Dopamine D2 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL339] [GtoPdb: 215] [UniProtKB: P61169]
ChEMBL Tested for Competitive binding inhibition of [3H]spiperone to Dopamine receptor D2 in rat striatal membrane. B 7.3 pKi 50 nM Ki Bioorg Med Chem Lett (1993) 3: 1241-1244
GtoPdb - - 7.5 pKi - - - Nature (1990) 347: 146-51 [PMID:1975644]
ChEMBL In vitro binding affinity for dopamine receptor D2 of rat nucleus accumbens labeled with [3H]spiperone B 8 pKi 10 nM Ki J Med Chem (1987) 30: 1100-1105 [PMID:2884314]
ChEMBL Binding affinity towards dopamine receptor D2 by displacing [3H]spiperone radioligand in rat striatum B 8.11 pKi 7.8 nM Ki J Med Chem (1992) 35: 552-558 [PMID:1346653]
ChEMBL Inhibition of [3H]spiperone binding to Dopamine receptor D2 at 0.02 nM B 8.3 pKi 4.97 nM Ki J Med Chem (1988) 31: 1941-1946 [PMID:3050089]
ChEMBL Compound was evaluated for the binding affinity against [3H]U-86,170-labeled dopamine receptor D2 in cloned CHO cells B 8.52 pKi 3 nM Ki J Med Chem (1993) 36: 1053-1068 [PMID:8097537]
ChEMBL Compound was evaluated for binding affinity towards Dopamine receptor D2 in striatal membranes, using [3H]- spiperone as radioligand in the presence of sodium chloride B 8.66 pKi 2.19 nM Ki J Med Chem (1991) 34: 1612-1624 [PMID:1827843]
ChEMBL In vitro binding affinity against Dopamine D2 receptor in rat striatal tissue. B 8.7 pKi 2.01 nM Ki J Med Chem (1993) 36: 2107-2114 [PMID:8101877]
ChEMBL Binding affinity against dopamine D2 receptor B 8.7 pKi 2 nM Ki J Med Chem (1994) 37: 519-525 [PMID:7907148]
ChEMBL Compound was evaluated for binding affinity towards Dopamine receptor D2 in striatal membranes, using [3H]- spiperone as radioligand in the absence of sodium chloride B 8.75 pKi 1.77 nM Ki J Med Chem (1991) 34: 1612-1624 [PMID:1827843]
ChEMBL Compound was tested for inhibitory activity against the binding of [3H]spiperone to Dopamine receptor D2 in rat striatal membranes B 8.92 pKi 1.2 nM Ki J Med Chem (1987) 30: 1631-1635 [PMID:2887659]
ChEMBL Compound was tested in vitro for its affinity towards rat striatal Dopamine receptor D2 labeled with [3H]- spiperone B 7.4 pIC50 40 nM IC50 J Med Chem (1986) 29: 359-369 [PMID:2869146]
ChEMBL Ability to bind at dopamine receptor D2 of rat corpus striatum by displacing [3H]spiperone B 7.4 pIC50 40 nM IC50 J Med Chem (1989) 32: 1147-1156 [PMID:2542551]
D3 receptor/Dopamine D3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL234] [GtoPdb: 216] [UniProtKB: P35462]
GtoPdb - - 7.5 pKi - - - J Pharmacol Exp Ther (1994) 268: 417-26 [PMID:8301582];
Eur J Pharmacol (1992) 225: 331-7 [PMID:1354163]
ChEMBL Displacement of [3H]N-methylspiperone from human dopamine D3 receptor expressed in HEK293T cell membranes by radioligand binding assay B 7.83 pKi 14.79 nM Ki Bioorg Med Chem Lett (2018) 28: 1897-1902 [PMID:29631959]
ChEMBL Displacement of [3H]N-methylspiperone from human dopamine D3 receptor by PDSP assay B 7.96 pKi 11 nM Ki Bioorg Med Chem (2016) 24: 2060-2071 [PMID:27032890]
ChEMBL Displacement of [3H]N-methylspiperone from human dopamine D3 receptor expressed in HEK293T cell membranes by radioligand binding assay B 8.12 pKi 7.6 nM Ki Bioorg Med Chem Lett (2018) 28: 1897-1902 [PMID:29631959]
ChEMBL Displacement of [3H]spiperone from human dopamine D3 receptor expressed in CHO cells B 8.16 pKi 6.9 nM Ki Bioorg Med Chem Lett (2009) 19: 538-542 [PMID:19091563]
ChEMBL DRUGMATRIX: Dopamine D3 radioligand binding (ligand: [3H] Spiperone) B 8.38 pKi 4.21 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL Displacement of [3H]-N-methylspiperone from human dopamine D3 receptor expressed in HEK293 cells after 30 mins by scintillation counting B 8.42 pKi 3.8 nM Ki Bioorg Med Chem (2012) 20: 6366-6374 [PMID:23018094]
ChEMBL Displacement of [3H]N-Methylspiperone from dopamine D3 receptor (unknown origin) B 8.48 pKi 3.31 nM Ki Bioorg Med Chem Lett (2014) 24: 576-579 [PMID:24365159]
ChEMBL Displacement of [3H]N-Methylspiperone from dopamine D3 receptor (unknown origin) B 8.48 pKi 3.3 nM Ki Bioorg Med Chem Lett (2014) 24: 576-579 [PMID:24365159]
ChEMBL Displacement of [125I]iodosulpiride from human Dopamine receptor D3 expressed in CHO cells B 8.52 pKi 3 nM Ki J Med Chem (2003) 46: 4377-4392 [PMID:14521403]
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 DRUGMATRIX: Dopamine D3 radioligand binding (ligand: [3H] Spiperone) B 7.92 pIC50 12 nM IC50 DrugMatrix in vitro pharmacology data
D3 receptor in Rat [GtoPdb: 216] [UniProtKB: P19020]
GtoPdb - - 7.2 pKi - - - Nature (1990) 347: 146-51 [PMID:1975644]
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 6.32 pKi 479 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL Displacement of [3H]N-Methylspiperone from dopamine D4 receptor (unknown origin) B 7.5 pKi 31.62 nM Ki Bioorg Med Chem Lett (2014) 24: 576-579 [PMID:24365159]
ChEMBL Displacement of [3H]N-Methylspiperone from dopamine D4 receptor (unknown origin) B 7.52 pKi 30 nM Ki Bioorg Med Chem Lett (2014) 24: 576-579 [PMID:24365159]
ChEMBL Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells B 7.6 pKi 25.12 nM Ki J Med Chem (2007) 50: 5103-5108 [PMID:17880057]
GtoPdb - - 7.8 pKi - - - Eur J Pharmacol (1993) 236: 483-6 [PMID:8102973]
ChEMBL DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone) B 5.86 pIC50 1365 nM IC50 DrugMatrix in vitro pharmacology data
D5 receptor/Dopamine D5 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1850] [GtoPdb: 218] [UniProtKB: P21918]
ChEMBL Displacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK cells B 6.76 pKi 172 nM Ki Bioorg Med Chem Lett (2009) 19: 538-542 [PMID:19091563]
GtoPdb - - 6.9 pKi - - - Nature (1991) 350: 614-9 [PMID:1826762]
DAT/Dopamine transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL238] [GtoPdb: 927] [UniProtKB: Q01959]
ChEMBL DRUGMATRIX: Dopamine Transporter radioligand binding (ligand: [125I] RTI-55) B 5.68 pKi 2100 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Dopamine Transporter radioligand binding (ligand: [125I] RTI-55) B 5.58 pIC50 2643 nM IC50 DrugMatrix in vitro pharmacology data
epidermal growth factor receptor/Epidermal growth factor receptor erbB1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL203] [GtoPdb: 1797] [UniProtKB: P00533]
ChEMBL DRUGMATRIX: Protein Tyrosine Kinase, EGF Receptor enzyme inhibition (substrate: Poly(Glu:Tyr)) B 4.54 pIC50 28868 nM IC50 DrugMatrix in vitro pharmacology data
GluN2D/GluN3B/GluN1/GluN2A/GluN2B/GluN2C/GluN3A/Glutamate [NMDA] receptor in Human (target type: PROTEIN COMPLEX GROUP) [ChEMBL: CHEMBL2094124] [GtoPdb: 459461455456457458460] [UniProtKB: O15399O60391Q05586Q12879Q13224Q14957Q8TCU5]
ChEMBL Binding affinity against dextromethorpin binding site associated with N-methyl-D-aspartate glutamate receptor from guinea pig mitochondrial pellet P2 determined using [3H]1 as radioligand. B 5.96 pIC50 1100 nM IC50 J Med Chem (1992) 35: 4135-4142 [PMID:1433216]
ChEMBL Inhibition of [3H]1 binding to dextromethorpin binding site of guinea pig microsomal pellet P3 N-methyl-D-aspartate glutamate receptor B 6.22 pIC50 600 nM IC50 J Med Chem (1992) 35: 4135-4142 [PMID:1433216]
GluN1/GluN2A/GluN2B/GluN2C/GluN2D/GluN3B/GluN3A/Glutamate NMDA receptor in Rat (target type: PROTEIN COMPLEX GROUP) [ChEMBL: CHEMBL1907608] [GtoPdb: 455456457458459461460] [UniProtKB: P35439Q00959Q00960Q00961Q62645Q8VHN2Q9R1M7]
ChEMBL Displacement of [3H]MK-801 from NMDA receptor in Wistar rat brain membranes by scintillation counting analysis B 4.68 pIC50 21000 nM IC50 Bioorg Med Chem Lett (2015) 25: 4131-4135 [PMID:26296478]
ChEMBL Binding affinity against dextromethorpin binding site of N-methyl-D-aspartate glutamate receptor from rat brain using [3H]1 B 5.89 pIC50 1300 nM IC50 J Med Chem (1992) 35: 4135-4142 [PMID:1433216]
Kv11.1/HERG in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809]
ChEMBL DRUGMATRIX: Potassium Channel HERG radioligand binding (ligand: [3H] Astemizole) B 5.32 pKi 4774.3 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Potassium Channel HERG radioligand binding (ligand: [3H] Astemizole) B 5.23 pIC50 5827.5 nM IC50 DrugMatrix in vitro pharmacology data
ChEMBL Inhibition of human Potassium channel HERG expressed in mammalian cells B 5.83 pIC50 1479.11 nM IC50 Bioorg Med Chem Lett (2003) 13: 2773-2775 [PMID:12873512]
ChEMBL Inhibition of partially open human voltage-gated potassium channel subunit Kv11.1 (ERG K+ channel) F 5.83 pIC50 1479.11 nM IC50 Bioorg Med Chem Lett (2005) 15: 1737-1741 [PMID:15745831]
ChEMBL Inhibitory concentration against potassium channel HERG B 5.83 pIC50 1479.11 nM IC50 Bioorg Med Chem Lett (2005) 15: 2886-2890 [PMID:15911273]
ChEMBL Inhibition of human ERG expressed in CHO cells by whole cell patch clamp technique B 5.83 pIC50 1479.11 nM IC50 Bioorg Med Chem (2008) 16: 6252-6260 [PMID:18448342]
ChEMBL Inhibition of human ERG in MCF7 cells B 5.83 pIC50 1479.11 nM IC50 Eur J Med Chem (2009) 44: 1926-1932 [PMID:19110341]
ChEMBL Inhibition of human ERG B 5.83 pIC50 1479.11 nM IC50 Eur J Med Chem (2011) 46: 618-630 [PMID:21185626]
ChEMBL Inhibition of hERG K channel F 5.83 pIC50 1470 nM IC50 Cardiovasc Res (2011) 91: 53-61 [PMID:21300721]
ChEMBL K+ channel blocking activity in Chinese hamster ovary cells expressing HERG Kv11.1 F 5.83 pIC50 1470 nM IC50 J Med Chem (2002) 45: 3844-3853 [PMID:12190308]
H1 receptor/Histamine H1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL231] [GtoPdb: 262] [UniProtKB: P35367]
GtoPdb - - 8.2 pKi - - - Neuropsychopharmacology (2003) 28: 519-26 [PMID:12629531]
ChEMBL Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO cells B 8.37 pKi 4.25 nM Ki Bioorg Med Chem Lett (2009) 19: 538-542 [PMID:19091563]
ChEMBL DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine) B 8.71 pKi 1.96 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine) B 7.77 pIC50 17 nM IC50 DrugMatrix in vitro pharmacology data
ChEMBL Binding affinity to histamine H1 receptor (unknown origin) by radioligand binding assay B 7.92 pIC50 12 nM IC50 J Med Chem (2013) 56: 8955-8971 [PMID:23919353]
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 7.3 pKi 50.12 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 5.59 pKi 2582 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine) B 5.58 pIC50 2626 nM IC50 DrugMatrix in vitro pharmacology data
H3 receptor/Histamine H3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL264] [GtoPdb: 264] [UniProtKB: Q9Y5N1]
ChEMBL Displacement of [125I]iodoproxyfan from human histamine H3 receptor expressed in CHO/HEK293 cells B 6 pKi >1000 nM Ki Bioorg Med Chem Lett (2009) 19: 538-542 [PMID:19091563]
κ receptor/Kappa opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL237] [GtoPdb: 318] [UniProtKB: P41145]
ChEMBL DRUGMATRIX: Opiate kappa (OP2, KOP) radioligand binding (ligand: [3H] Diprenorphine) B 5.35 pKi 4433 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Opiate kappa (OP2, KOP) radioligand binding (ligand: [3H] Diprenorphine) B 4.96 pIC50 11082 nM IC50 DrugMatrix in vitro pharmacology data
MC3 receptor/Melanocortin receptor 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4644] [GtoPdb: 284] [UniProtKB: P41968]
ChEMBL DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH) B 4.67 pKi 21244 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH) B 4.61 pIC50 24343 nM IC50 DrugMatrix in vitro pharmacology data
MC4 receptor/Melanocortin receptor 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL259] [GtoPdb: 285] [UniProtKB: P32245]
ChEMBL DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH) B 4.84 pKi 14619 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH) B 4.82 pIC50 15204 nM IC50 DrugMatrix in vitro pharmacology data
MC5 receptor/Melanocortin receptor 5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4608] [GtoPdb: 286] [UniProtKB: P33032]
ChEMBL DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH) B 5.15 pKi 7145 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH) B 5.12 pIC50 7617 nM IC50 DrugMatrix in vitro pharmacology data
μ receptor/Mu opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL233] [GtoPdb: 319] [UniProtKB: P35372]
ChEMBL DRUGMATRIX: Opiate mu (OP3, MOP) radioligand binding (ligand: [3H] Diprenorphine) B 5.23 pKi 5844 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Opiate mu (OP3, MOP) radioligand binding (ligand: [3H] Diprenorphine) B 4.84 pIC50 14397 nM IC50 DrugMatrix in vitro pharmacology data
M1 receptor/Muscarinic acetylcholine receptor M1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL216] [GtoPdb: 13] [UniProtKB: P11229]
ChEMBL Displacement of [3H]pirenzepine from human M1 receptor expressed in CHO cells B 6.9 pKi 125.89 nM Ki J Med Chem (2007) 50: 5103-5108 [PMID:17880057]
ChEMBL DRUGMATRIX: Muscarinic M1 radioligand binding (ligand: [3H] N-Methylscopolamine) B 7.7 pKi 20 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Muscarinic M1 radioligand binding (ligand: [3H] N-Methylscopolamine) B 7.08 pIC50 83 nM IC50 DrugMatrix in vitro pharmacology data
M2 receptor/Muscarinic acetylcholine receptor M2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL211] [GtoPdb: 14] [UniProtKB: P08172]
ChEMBL DRUGMATRIX: Muscarinic M2 radioligand binding (ligand: [3H] N-Methylscopolamine) B 6.63 pKi 232 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Muscarinic M2 radioligand binding (ligand: [3H] N-Methylscopolamine) B 6.19 pIC50 652 nM IC50 DrugMatrix in vitro pharmacology data
M3 receptor/Muscarinic acetylcholine receptor M3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL245] [GtoPdb: 15] [UniProtKB: P20309]
ChEMBL DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine) B 7.36 pKi 44 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine) B 6.69 pIC50 206 nM IC50 DrugMatrix in vitro pharmacology data
M4 receptor/Muscarinic acetylcholine receptor M4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1821] [GtoPdb: 16] [UniProtKB: P08173]
ChEMBL Displacement of [3H]4-DAMP from human M4 receptor expressed in CHO cells B 6.8 pKi 158.49 nM Ki J Med Chem (2007) 50: 5103-5108 [PMID:17880057]
ChEMBL DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine) B 7.68 pKi 21 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine) B 6.83 pIC50 149 nM IC50 DrugMatrix in vitro pharmacology data
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 7.74 pKi 18 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine) B 7.6 pIC50 25 nM IC50 DrugMatrix in vitro pharmacology data
NK2 receptor/Neurokinin 2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2327] [GtoPdb: 361] [UniProtKB: P21452]
ChEMBL DRUGMATRIX: Tachykinin NK2 radioligand binding (ligand: [3H] SR-48968) B 5.04 pKi 9065 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Tachykinin NK2 radioligand binding (ligand: [3H] SR-48968) B 4.57 pIC50 27195 nM IC50 DrugMatrix in vitro pharmacology data
NET/Norepinephrine transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL222] [GtoPdb: 926] [UniProtKB: P23975]
ChEMBL DRUGMATRIX: Norepinephrine Transporter radioligand binding (ligand: [125I] RTI-55) B 7.72 pKi 19 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Norepinephrine Transporter radioligand binding (ligand: [125I] RTI-55) B 7.72 pIC50 19 nM IC50 DrugMatrix in vitro pharmacology data
ABCB1/P-glycoprotein 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4302] [GtoPdb: 768] [UniProtKB: P08183]
ChEMBL Concentration giving half of the maximal ATPase activity calculated for the high-affinity binding site of the CHO P-Glycoprotein (P-gp) in two-affinity model B 4.91 pKi 12200 nM Ki J Med Chem (2002) 45: 5671-5686 [PMID:12477351]
ChEMBL High affinity constant at binding site of human P-Glycoprotein (P-gp) in two-affinity model B 6.22 pKi 600 nM Ki J Med Chem (2002) 45: 5671-5686 [PMID:12477351]
Plasmodium falciparum (target type: ORGANISM) [ChEMBL: CHEMBL364]
ChEMBL Antimicrobial activity against Plasmodium falciparum F 4.55 pIC50 28000 nM IC50 Bioorg Med Chem (2010) 18: 2225-2231 [PMID:20185316]
ChEMBL DNDI: Malaria in Vitro, 72 hour F 5.52 pIC50 3030 nM IC50 Antiprotozoal Activity Profiling of Approved Drugs: A Starting Point toward Drug Repositioning
Pleiotropic ABC efflux transporter of multiple drugs in Saccharomyces cerevisiae S288c (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1697658] [UniProtKB: P33302]
ChEMBL Inhibition of Pdr5p-mediated rhodamine 6G transport in Saccharomyces cerevisiae MKPDR5h plasma membrane by spectrofluorometric assay B 5.35 pIC50 4500 nM IC50 Antimicrob Agents Chemother (2009) 53: 1516-1527 [PMID:19188399]
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 5.57 pIC50 2700 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 5.7 pEC50 2000 nM EC50 J Med Chem (2003) 46: 3563-3564 [PMID:12904059]
Prion protein in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3698] [UniProtKB: P04925]
ChEMBL Activity at mouse prion protein expressed in Escherichia coli B 5.7 pEC50 2000 nM EC50 J Med Chem (2018) 61: 1276-1284 [PMID:29328660]
erb-b2 receptor tyrosine kinase 2/Receptor protein-tyrosine kinase erbB-2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1824] [GtoPdb: 2019] [UniProtKB: P04626]
ChEMBL DRUGMATRIX: Protein Tyrosine Kinase, ERBB2 (HER2) enzyme inhibition (substrate: Poly(Glu:Tyr)) B 4.71 pIC50 19366 nM IC50 DrugMatrix in vitro pharmacology data
Sarcoplasmic/endoplasmic reticulum calcium ATP-ase in Rabbit (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4693] [UniProtKB: P04191]
ChEMBL Inhibition of rabbit skeletal muscle microsomes SERCA1a incubated for 10 mins by enzyme-coupled method B 4.64 pIC50 23000 nM IC50 J Med Chem (2020) 63: 1937-1963 [PMID:32030976]
5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL214] [GtoPdb: 1] [UniProtKB: P08908]
ChEMBL Compound was evaluated for the binding affinity against [3H]8-OH-DPAT-labeled 5-hydroxytryptamine 1A receptor sites in cloned CHO cells B 6.17 pKi 673 nM Ki J Med Chem (1993) 36: 1053-1068 [PMID:8097537]
GtoPdb - - 6.2 pKi - - - Eur J Pharmacol (1998) 355: 245-56 [PMID:9760039]
5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL273] [GtoPdb: 1] [UniProtKB: P19327]
ChEMBL DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1A radioligand binding (ligand: [3H] 8-OH-DPAT) B 5.57 pKi 2677 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL The compound was tested for its binding affinity towards 5-hydroxytryptamine 1A receptor by displacing [3H]WB-4101 radioligand in rat hippocampus B 6.75 pKi 179 nM Ki J Med Chem (1992) 35: 552-558 [PMID:1346653]
ChEMBL DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1A radioligand binding (ligand: [3H] 8-OH-DPAT) B 5.33 pIC50 4685 nM IC50 DrugMatrix in vitro pharmacology data
ChEMBL Ability to bind at 5-hydroxytryptamine 1A receptor of rat hippocampus by displacing [3H]8-OH-DPAT B 6.43 pIC50 372 nM IC50 J Med Chem (1989) 32: 1147-1156 [PMID:2542551]
5-HT1B receptor/Serotonin 1b (5-HT1b) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3459] [GtoPdb: 2] [UniProtKB: P28564]
ChEMBL DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol) B 5.74 pKi 1837 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol) B 5.39 pIC50 4041 nM IC50 DrugMatrix in vitro pharmacology data
5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223]
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 7.92 pKi 12.02 nM Ki J Med Chem (2021) 64: 12603-12629 [PMID:34436892]
GtoPdb - - 8.1 pKi - - - Neuropsychopharmacology (2003) 28: 519-26 [PMID:12629531]
ChEMBL Displacement of [3H]ketanserin from human 5HT2A 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]Ketanserin from 5-HT2A receptor (unknown origin) B 8.23 pKi 5.9 nM Ki Bioorg Med Chem Lett (2014) 24: 576-579 [PMID:24365159]
ChEMBL Displacement of [3H]Ketanserin from 5-HT2A receptor (unknown origin) B 8.23 pKi 5.89 nM Ki Bioorg Med Chem Lett (2014) 24: 576-579 [PMID:24365159]
ChEMBL DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2A radioligand binding (ligand: [3H] Ketanserin) B 8.96 pKi 1.1 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2A radioligand binding (ligand: [3H] Ketanserin) B 8.41 pIC50 3.85 nM IC50 DrugMatrix in vitro pharmacology data
ChEMBL Binding affinity to 5HT2A receptor (unknown origin) by radioligand binding assay B 8.47 pIC50 3.4 nM IC50 J Med Chem (2013) 56: 8955-8971 [PMID:23919353]
5-HT2A receptor in Rat [GtoPdb: 6] [UniProtKB: P14842]
GtoPdb - - 8.7 pKi - - - J Pharmacol Exp Ther (1998) 286: 85-90 [PMID:9655845]
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 7.1 pKi 80 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL Displacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation counting B 7.28 pKi 52 nM Ki J Med Chem (2010) 53: 7573-7586 [PMID:20958049]
ChEMBL Displacement of [3H]DOI from 5HT2B receptor expressed in CHO cells B 7.4 pKi 39.81 nM Ki J Med Chem (2007) 50: 5103-5108 [PMID:17880057]
ChEMBL DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide) B 6.9 pIC50 126 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 5HT2C receptor expressed in CHO cells B 7.4 pKi 39.81 nM Ki J Med Chem (2007) 50: 5103-5108 [PMID:17880057]
ChEMBL Displacement of [3H]Mesulergine from 5-HT2C receptor (unknown origin) B 7.52 pKi 30.2 nM Ki Bioorg Med Chem Lett (2014) 24: 576-579 [PMID:24365159]
ChEMBL Displacement of [3H]Mesulergine from 5-HT2C receptor (unknown origin) B 7.52 pKi 30 nM Ki Bioorg Med Chem Lett (2014) 24: 576-579 [PMID:24365159]
ChEMBL Displacement of [3H]mesulergine from 5-HT2C receptor after 1.5 hrs by scintillation counting B 7.57 pKi 27 nM Ki Bioorg Med Chem (2011) 19: 5756-5762 [PMID:21907583]
GtoPdb - - 8.2 pKi - - - Neuropsychopharmacology (2003) 28: 519-26 [PMID:12629531];
J Pharmacol Exp Ther (2000) 295: 226-32 [PMID:10991983]
ChEMBL DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2C radioligand binding (ligand: [3H] Mesulergine) B 8.56 pKi 2.74 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2C radioligand binding (ligand: [3H] Mesulergine) B 8.28 pIC50 5.24 nM IC50 DrugMatrix in vitro pharmacology data
5-HT6 receptor/Serotonin 6 (5-HT6) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3371] [GtoPdb: 11] [UniProtKB: P50406]
ChEMBL Displacement of [3H]LSD from 5-HT6 receptor (unknown origin) B 7.22 pKi 60.26 nM Ki Bioorg Med Chem Lett (2014) 24: 576-579 [PMID:24365159]
ChEMBL Displacement of [3H]LSD from 5-HT6 receptor (unknown origin) B 7.22 pKi 60 nM Ki Bioorg Med Chem Lett (2014) 24: 576-579 [PMID:24365159]
ChEMBL Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells B 7.3 pKi 50.12 nM Ki J Med Chem (2007) 50: 5103-5108 [PMID:17880057]
ChEMBL Binding affinity for human 5-hydroxytryptamine 6 receptor B 7.3 pKi <50 nM Ki J Med Chem (2005) 48: 1781-1795 [PMID:15771424]
ChEMBL DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide) B 7.59 pKi 26 nM Ki DrugMatrix in vitro pharmacology data
GtoPdb - - 7.8 pKi - - - J Neurochem (1996) 66: 47-56 [PMID:8522988];
Psychopharmacology (Berl.) (2005) 179: 461-9 [PMID:15821958]
ChEMBL Binding affinity towards human 5-hydroxytryptamine 6 receptor B 8.4 pKi 4 nM Ki J Med Chem (2003) 46: 2795-2812 [PMID:12825922]
ChEMBL DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide) B 7.24 pIC50 57 nM IC50 DrugMatrix in vitro pharmacology data
5-HT6 receptor in Rat [GtoPdb: 11] [UniProtKB: P31388]
GtoPdb - - 8.4 pKi - - - J Pharmacol Exp Ther (1994) 268: 1403-10 [PMID:7908055]
5-HT7 receptor/Serotonin 7 (5-HT7) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3155] [GtoPdb: 12] [UniProtKB: P34969]
ChEMBL Displacement of [3H]LSD from 5-HT7 receptor (unknown origin) B 6.92 pKi 120.23 nM Ki Bioorg Med Chem Lett (2014) 24: 576-579 [PMID:24365159]
ChEMBL Displacement of [3H]LSD from 5-HT7 receptor (unknown origin) B 6.92 pKi 119 nM Ki Bioorg Med Chem Lett (2014) 24: 576-579 [PMID:24365159]
ChEMBL Displacement of [3H]LSD from human 5HT7 receptor expressed in CHO cells B 7.5 pKi 31.62 nM Ki J Med Chem (2007) 50: 5103-5108 [PMID:17880057]
ChEMBL Displacement of [3H]LSD from 5-HT7 receptor after 1.5 hrs by scintillation counting B 7.57 pKi 27 nM Ki Bioorg Med Chem (2011) 19: 5756-5762 [PMID:21907583]
GtoPdb - - 7.6 pKi - - - Psychopharmacology (Berl.) (2005) 179: 461-9 [PMID:15821958]
ChEMBL Displacement of [3H]-LSD from 5HT7 receptor (unknown origin) expressed in CHOK1 cells B 7.96 pKi 11 nM Ki Bioorg Med Chem (2013) 21: 2568-2576 [PMID:23541835]
ChEMBL Displacement of [3H]-LSD from 5HT7 receptor (unknown origin) expressed in CHOK1 cells B 7.97 pKi 10.72 nM Ki Bioorg Med Chem (2013) 21: 2568-2576 [PMID:23541835]
5-HT7 receptor in Mouse [GtoPdb: 12] [UniProtKB: P32304]
GtoPdb - - 5.3 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]
GtoPdb - - 7.6 pKi - - - J Pharmacol Exp Ther (1994) 268: 1403-10 [PMID:7908055]
ChEMBL Binding affinity towards rat 5-hydroxytryptamine 7 receptor B 7.68 pKi 21 nM Ki J Med Chem (2003) 46: 2795-2812 [PMID:12825922]
SERT/Serotonin transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL228] [GtoPdb: 928] [UniProtKB: P31645]
ChEMBL Displacement of [3H]paraxetine from human 5HT transporter expressed in HEK293 cells B 7.2 pKi 63.1 nM Ki J Med Chem (2007) 50: 5103-5108 [PMID:17880057]
ChEMBL DRUGMATRIX: Transporter, Serotonin (5-Hydroxytryptamine) (SERT) radioligand binding (ligand: [3H] Paroxetine) B 7.68 pKi 21 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL Binding affinity to SERT (unknown origin) by radioligand binding assay B 6.92 pIC50 120 nM IC50 J Med Chem (2013) 56: 8955-8971 [PMID:23919353]
ChEMBL DRUGMATRIX: Transporter, Serotonin (5-Hydroxytryptamine) (SERT) radioligand binding (ligand: [3H] Paroxetine) B 7.41 pIC50 39 nM IC50 DrugMatrix in vitro pharmacology data
sigma non-opioid intracellular receptor 1/Sigma opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL287] [GtoPdb: 2552] [UniProtKB: Q99720]
ChEMBL DRUGMATRIX: Sigma1 radioligand binding (ligand: [3H] Haloperidol) B 6.72 pKi 189 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Sigma1 radioligand binding (ligand: [3H] Haloperidol) B 6.35 pIC50 451 nM IC50 DrugMatrix in vitro pharmacology data
Organic cation transporter 1/Solute carrier family 22 member 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5685] [GtoPdb: 1019] [UniProtKB: O15245]
ChEMBL Inhibition of 4-(4-(dimethylamino)styryl)-N-methylpyridinium uptake at human OCT1 expressed in HEK293 cells by confocal microscopy B 4.57 pIC50 27000 nM IC50 J Med Chem (2008) 51: 5932-5942 [PMID:18788725]
ChEMBL TP_TRANSPORTER: inhibition of TEA uptake in OCT1-expressing HeLa cells F 5.37 pIC50 4300 nM IC50 Mol Pharmacol (2003) 63: 489-498 [PMID:12606755]
sphingomyelin phosphodiesterase 1/Sphingomyelin phosphodiesterase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2760] [GtoPdb: 2514] [UniProtKB: P17405]
ChEMBL Inhibition of mmLDL-stimulated acid sphingomyelinase in human PBMC lysates using 3H-sphingomyelin as substrate preincubated for 30 mins followed by mmLDL stimulation measured after 2 hrs by HPLC method B 4.96 pIC50 11000 nM IC50 Eur J Med Chem (2018) 153: 73-104 [PMID:29031494]
Trypanothione reductase in Trypanosoma cruzi (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5131] [UniProtKB: P28593]
ChEMBL Inhibitory activity against Trypanosoma cruzi trypanothione reductase B 4.97 pKi 10800 nM Ki J Med Chem (2000) 43: 3148-3156 [PMID:10956223]
ChEMBL Inhibitory activity against recombinant Trypanosoma cruzi (Trypanosoma cruzi) Trypanothione reductase (linear competitive type) B 4.97 pKi 10800 nM Ki J Med Chem (1998) 41: 148-156 [PMID:9457238]
ChEMBL Inhibition of Trypanosoma cruzi recombinant trypanothione reductase B 5.49 pKi 3200 nM Ki Bioorg Med Chem (2008) 16: 6689-6695 [PMID:18558492]
ChEMBL Inhibitory activity against recombinant Trypanosoma cruzi (Trypanosoma cruzi) Trypanothione reductase B 4.45 pIC50 35400 nM IC50 J Med Chem (1998) 41: 148-156 [PMID:9457238]
ChEMBL Inhibition of Trypanosoma cruzi recombinant trypanothione reductase B 5.24 pIC50 5800 nM IC50 Bioorg Med Chem (2008) 16: 6689-6695 [PMID:18558492]
FYN proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase FYN in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1841] [GtoPdb: 2026] [UniProtKB: P06241]
ChEMBL DRUGMATRIX: Protein Tyrosine Kinase, Fyn enzyme inhibition (substrate: Poly(Glu:Tyr)) B 5.06 pIC50 8680 nM IC50 DrugMatrix in vitro pharmacology data
TRPV1/Vanilloid receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5102] [GtoPdb: 507] [UniProtKB: O35433]
ChEMBL Displacement of [3H]RTX from rat TRPV1 receptor expressed in CHO cells B 5.89 pKi 1300 nM Ki Bioorg Med Chem (2007) 15: 6043-6053 [PMID:17629487]
ChEMBL Antagonist activity at rat TRPV1 receptor expressed in CHO cells by Ca2+ uptake assay F 6.28 pKi 520 nM Ki Bioorg Med Chem (2007) 15: 6043-6053 [PMID:17629487]

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]