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, Clorpromazina, 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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  • aldehyde oxidase 1/Aldehyde oxidase in Human [ChEMBL: CHEMBL3257] [GtoPdb: 3186] [UniProtKB: Q06278]
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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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  • lysine demethylase 1A/Lysine-specific histone demethylase 1 in Human [ChEMBL: CHEMBL6136] [GtoPdb: 2669] [UniProtKB: O60341]
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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
aldehyde oxidase 1/Aldehyde oxidase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3257] [GtoPdb: 3186] [UniProtKB: Q06278]
ChEMBL Inhibition of human liver AOX using phthalazine as substrate incubated for 2.5 mins by HPLC-MS analysis B 6 pIC50 <1000 nM IC50 Eur J Med Chem (2020) 187: 111948-111948 [PMID:31877540]
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 assessed as inhibition constant B 7.96 pKi 11 nM Ki J Med Chem (2023) 66: 10060-10079 [PMID:37421373]
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: 459, 461, 455, 456, 457, 458, 460] [UniProtKB: O15399, O60391, Q05586, Q12879, Q13224, Q14957, Q8TCU5]
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: 455, 456, 457, 458, 459, 461, 460] [UniProtKB: P35439, Q00959, Q00960, Q00961, Q62645, Q8VHN2, Q9R1M7]
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
lysine demethylase 1A/Lysine-specific histone demethylase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6136] [GtoPdb: 2669] [UniProtKB: O60341]
ChEMBL Inhibition of recombinant LSD1 (unknown origin) expressed in Escherichia coli BL21 (DE3) using H3K4me2 peptide as substrate incubated for 30 mins by fluorescence based microplate reader assay B 5.29 pIC50 5135 nM IC50 J Med Chem (2023) 66: 3896-3916 [PMID:36856685]
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 34:

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