thioridazine [Ligand Id: 100] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL479 (Dl-thioridazine, Mellaril-s, Mellerette, Melleril, Novoridazine, Rideril, Sonapax, Thioridazine, Thioridazine prolongatum, Thioril, Tioridazina, TP-21)
  • 5-HT1A receptor in Human [GtoPdb: 1] [UniProtKB: P08908]
  • 5-HT1A receptor/5-hydroxytryptamine receptor 1A in Rat [ChEMBL: CHEMBL273] [GtoPdb: 1] [UniProtKB: P19327]
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  • 5-HT2A receptor/5-hydroxytryptamine receptor 2A in Human [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223]
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  • 5-HT2B receptor/5-hydroxytryptamine receptor 2B in Human [ChEMBL: CHEMBL1833] [GtoPdb: 7] [UniProtKB: P41595]
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  • 5-HT2C receptor/5-hydroxytryptamine receptor 2C in Human [ChEMBL: CHEMBL225] [GtoPdb: 8] [UniProtKB: P28335]
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  • 5-HT6 receptor/5-hydroxytryptamine receptor 6 in Human [ChEMBL: CHEMBL3371] [GtoPdb: 11] [UniProtKB: P50406]
  • 5-HT6 receptor in Rat [GtoPdb: 11] [UniProtKB: P31388]
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  • 5-HT7 receptor/5-hydroxytryptamine receptor 7 in Human [ChEMBL: CHEMBL3155] [GtoPdb: 12] [UniProtKB: P34969]
  • 5-HT7 receptor in Rat [GtoPdb: 12] [UniProtKB: P32305]
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  • A1 receptor/Adenosine receptor A1 in Rat [ChEMBL: CHEMBL318] [GtoPdb: 18] [UniProtKB: P25099]
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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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  • β1-adrenoceptor/Beta-1 adrenergic receptor in Rat [ChEMBL: CHEMBL3252] [GtoPdb: 28] [UniProtKB: P18090]
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  • β2-adrenoceptor/Beta-2 adrenergic receptor in Rat [ChEMBL: CHEMBL3754] [GtoPdb: 29] [UniProtKB: P10608]
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  • ABCG2/Broad substrate specificity ATP-binding cassette transporter ABCG2 in Human [ChEMBL: CHEMBL5393] [GtoPdb: 792] [UniProtKB: Q9UNQ0]
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  • D1 receptor/D(1A) dopamine receptor in Human [ChEMBL: CHEMBL2056] [GtoPdb: 214] [UniProtKB: P21728]
  • D1 receptor/D(1A) dopamine receptor in Rat [ChEMBL: CHEMBL265] [GtoPdb: 214] [UniProtKB: P18901]
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  • D2 receptor/D(2) dopamine receptor in Human [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416]
  • D2 receptor/D(2) dopamine receptor in Rat [ChEMBL: CHEMBL339] [GtoPdb: 215] [UniProtKB: P61169]
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  • D3 receptor/D(3) dopamine receptor in Human [ChEMBL: CHEMBL234] [GtoPdb: 216] [UniProtKB: P35462]
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  • D4 receptor/D(4) dopamine receptor in Human [ChEMBL: CHEMBL219] [GtoPdb: 217] [UniProtKB: P21917]
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  • epidermal growth factor receptor/Epidermal growth factor receptor in Human [ChEMBL: CHEMBL203] [GtoPdb: 1797] [UniProtKB: P00533]
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  • GABAA receptor γ1 subunit/Gamma-aminobutyric acid receptor subunit gamma-1 in Rat [ChEMBL: CHEMBL296] [GtoPdb: 413] [UniProtKB: P23574]
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  • H1 receptor/Histamine H1 receptor in Human [ChEMBL: CHEMBL231] [GtoPdb: 262] [UniProtKB: P35367]
  • H1 receptor/Histamine H1 receptor in Rat [ChEMBL: CHEMBL4701] [GtoPdb: 262] [UniProtKB: P31390]
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  • H2 receptor/Histamine H2 receptor in Human [ChEMBL: CHEMBL1941] [GtoPdb: 263] [UniProtKB: P25021]
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  • κ receptor/Kappa-type opioid receptor in Human [ChEMBL: CHEMBL237] [GtoPdb: 318] [UniProtKB: P41145]
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  • MALT1 paracaspase/Mucosa-associated lymphoid tissue lymphoma translocation protein 1 in Human [ChEMBL: CHEMBL3632452] [GtoPdb: 2983] [UniProtKB: Q9UDY8]
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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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  • Pleiotropic ABC efflux transporter of multiple drugs in Saccharomyces cerevisiae S288c [ChEMBL: CHEMBL1697658] [UniProtKB: P33302]
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  • Pim-1 proto-oncogene, serine/threonine kinase/Serine/threonine-protein kinase pim-1 in Human [ChEMBL: CHEMBL2147] [GtoPdb: 2158] [UniProtKB: P11309]
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  • sigma non-opioid intracellular receptor 1/Sigma non-opioid intracellular receptor 1 in Human [ChEMBL: CHEMBL287] [GtoPdb: 2552] [UniProtKB: Q99720]
  • sigma non-opioid intracellular receptor 1/Sigma non-opioid intracellular receptor 1 in Rat [ChEMBL: CHEMBL3602] [GtoPdb: 2552] [UniProtKB: Q9R0C9]
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  • Nav1.5/Sodium channel protein type 5 subunit alpha in Human [ChEMBL: CHEMBL1980] [GtoPdb: 582] [UniProtKB: Q14524]
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  • DAT/Sodium-dependent dopamine transporter in Human [ChEMBL: CHEMBL238] [GtoPdb: 927] [UniProtKB: Q01959]
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  • NET/Sodium-dependent noradrenaline transporter in Human [ChEMBL: CHEMBL222] [GtoPdb: 926] [UniProtKB: P23975]
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  • SERT/Sodium-dependent serotonin transporter in Human [ChEMBL: CHEMBL228] [GtoPdb: 928] [UniProtKB: P31645]
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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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  • Cav1.2/Voltage-dependent L-type calcium channel subunit alpha-1C in Human [ChEMBL: CHEMBL1940] [GtoPdb: 529] [UniProtKB: Q13936]
  • Voltage-dependent L-type calcium channel subunit alpha-1C in Guinea pig [ChEMBL: CHEMBL2366456] [UniProtKB: O35505]
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  • Kv11.1/Voltage-gated inwardly rectifying potassium channel KCNH2 in Human [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809]
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  • D5 receptor in Human [GtoPdb: 218] [UniProtKB: P21918]
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  • Kir3.2 in Mouse [GtoPdb: 435] [UniProtKB: P48542]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
5-HT1A receptor in Human [GtoPdb: 1] [UniProtKB: P08908]
GtoPdb - - 7.1 pKi - - - Eur J Pharmacol (1998) 355: 245-56 [PMID:9760039]
5-HT1A receptor/5-hydroxytryptamine receptor 1A 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 7.47 pKi 34 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1A radioligand binding (ligand: [3H] 8-OH-DPAT) B 7.22 pIC50 60 nM IC50 DrugMatrix in vitro pharmacology data
5-HT2A receptor/5-hydroxytryptamine receptor 2A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223]
GtoPdb - - 8 pKi - - - Neuropsychopharmacology (2003) 28: 519-26 [PMID:12629531];
Eur J Pharmacol (2002) 450: 37-41 [PMID:12176106]
ChEMBL DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2A radioligand binding (ligand: [3H] Ketanserin) B 8.9 pKi 1.25 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2A radioligand binding (ligand: [3H] Ketanserin) B 8.36 pIC50 4.37 nM IC50 DrugMatrix in vitro pharmacology data
5-HT2B receptor/5-hydroxytryptamine receptor 2B 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 7.09 pKi 82 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide) B 6.89 pIC50 129 nM IC50 DrugMatrix in vitro pharmacology data
5-HT2C receptor/5-hydroxytryptamine receptor 2C in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL225] [GtoPdb: 8] [UniProtKB: P28335]
GtoPdb - - 7.3 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 7.64 pKi 23 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2C radioligand binding (ligand: [3H] Mesulergine) B 7.36 pIC50 44 nM IC50 DrugMatrix in vitro pharmacology data
5-HT6 receptor/5-hydroxytryptamine receptor 6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3371] [GtoPdb: 11] [UniProtKB: P50406]
GtoPdb - - 7.2 pKi - - - Psychopharmacology (Berl) (2005) 179: 461-9 [PMID:15821958]
ChEMBL DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide) B 7.48 pKi 33 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide) B 7.15 pIC50 71 nM IC50 DrugMatrix in vitro pharmacology data
5-HT6 receptor in Rat [GtoPdb: 11] [UniProtKB: P31388]
GtoPdb - - 8.2 pKi - - - J Pharmacol Exp Ther (1994) 268: 1403-10 [PMID:7908055]
5-HT7 receptor/5-hydroxytryptamine receptor 7 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3155] [GtoPdb: 12] [UniProtKB: P34969]
GtoPdb - - 7.1 pKi - - - Psychopharmacology (Berl) (2005) 179: 461-9 [PMID:15821958]
ChEMBL Binding affinity towards human 5-hydroxytryptamine 7 receptor B 7.15 pKi 70 nM Ki J Med Chem (2003) 46: 2795-2812 [PMID:12825922]
5-HT7 receptor in Rat [GtoPdb: 12] [UniProtKB: P32305]
GtoPdb - - 7.2 pKi - - - J Pharmacol Exp Ther (1994) 268: 1403-10 [PMID:7908055]
A1 receptor/Adenosine receptor A1 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL318] [GtoPdb: 18] [UniProtKB: P25099]
ChEMBL Displacement of [3H]-CHA (N6-Cyclohexyl adenosine) from adenosine A1 receptor in rat brain B 5 pIC50 >10000 nM IC50 J Med Chem (1988) 31: 454-461 [PMID:2892936]
aldehyde oxidase 1/Aldehyde oxidase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3257] [GtoPdb: 3186] [UniProtKB: Q06278]
ChEMBL Noncompetitive type inhibition of human AOX assessed as inhibitor dissociation constant by measuring changes in intercept of the double reciprocal plot using phthalazine as substrate by Michaelis-Menten analysis B 5.89 pKi 1.3 uM Kii J Med Chem (2021) 64: 13025-13037 [PMID:34415167]
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 8.69 pKi 2.06 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin) B 8.29 pIC50 5.09 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 8.59 pKi 2.6 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Alpha-1B adrenergic receptor radioligand binding (ligand: prazosin) B 8.33 pIC50 4.69 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 8.54 pKi 2.9 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Alpha-1D adrenergic receptor radioligand binding (ligand: prazosin) B 8.23 pIC50 5.89 nM IC50 DrugMatrix in vitro pharmacology data
α2A-adrenoceptor/Alpha-2A adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1867] [GtoPdb: 25] [UniProtKB: P08913]
ChEMBL DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912) B 7.3 pKi 50 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912) B 6.88 pIC50 133 nM IC50 DrugMatrix in vitro pharmacology data
α2B-adrenoceptor/Alpha-2B adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1942] [GtoPdb: 26] [UniProtKB: P18089]
ChEMBL DRUGMATRIX: Alpha-2B adrenergic receptor radioligand binding (ligand: Rauwolscine) B 6.76 pKi 174 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Alpha-2B adrenergic receptor radioligand binding (ligand: Rauwolscine) B 6.42 pIC50 380 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 7.6 pKi 25 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912) B 6.77 pIC50 171 nM IC50 DrugMatrix in vitro pharmacology data
β1-adrenoceptor/Beta-1 adrenergic receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3252] [GtoPdb: 28] [UniProtKB: P18090]
ChEMBL Displacement of [3H]DHA (Dihydroalprenolol) from beta-1 adrenergic receptor in rat brain B 5 pIC50 >10000 nM IC50 J Med Chem (1988) 31: 454-461 [PMID:2892936]
β2-adrenoceptor/Beta-2 adrenergic receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3754] [GtoPdb: 29] [UniProtKB: P10608]
ChEMBL Displacement of [3H]DHA (Dihydroalprenolol) from beta-2 adrenergic receptor in rat brain B 5 pIC50 >10000 nM IC50 J Med Chem (1988) 31: 454-461 [PMID:2892936]
ABCG2/Broad substrate specificity ATP-binding cassette transporter ABCG2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5393] [GtoPdb: 792] [UniProtKB: Q9UNQ0]
ChEMBL Inhibition of ABCG2 (unknown origin) expressed in human HEK293 cells membrane vesicles assessed inhibition of BCRP- mediated transport of 3[H]-E1S for 1 mins using [3H]-estrone sulfate as substrate by rapid filtration technique B 5.18 pIC50 6600 nM IC50 Eur J Med Chem (2022) 237: 114346-114346 [PMID:35483322]
CYP1A2/Cytochrome P450 1A2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3356] [GtoPdb: 1319] [UniProtKB: P05177]
ChEMBL DRUGMATRIX: CYP450, 1A2 enzyme inhibition (substrate: 3-Cyano-7-ethoxycoumarin) B 5.03 pIC50 9332.3 nM IC50 DrugMatrix in vitro pharmacology data
CYP2C19/Cytochrome P450 2C19 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3622] [GtoPdb: 1328] [UniProtKB: P33261]
ChEMBL DRUGMATRIX: CYP450, 2C19 enzyme inhibition (substrate: 3-Cyano-7-ethoxycoumarin) B 5.2 pIC50 6377.8 nM IC50 DrugMatrix in vitro pharmacology data
CYP2D6/Cytochrome P450 2D6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL289] [GtoPdb: 1329] [UniProtKB: P10635]
ChEMBL DRUGMATRIX: CYP450, 2D6 enzyme inhibition (substrate: 3-Cyano-7-ethoxycoumarin) B 5.75 pIC50 1772.6 nM IC50 DrugMatrix in vitro pharmacology data
D1 receptor/D(1A) dopamine receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2056] [GtoPdb: 214] [UniProtKB: P21728]
GtoPdb - - 7 pKi - - - Nature (1991) 350: 614-9 [PMID:1826762]
ChEMBL DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390) B 7.01 pKi 97 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390) B 6.71 pIC50 194 nM IC50 DrugMatrix in vitro pharmacology data
D1 receptor/D(1A) dopamine receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL265] [GtoPdb: 214] [UniProtKB: P18901]
ChEMBL Affinity for displacement of [3H]clonidine labeled Dopamine receptor D1 B 5.89 pIC50 1300 nM IC50 J Med Chem (1987) 30: 1807-1812 [PMID:2888897]
ChEMBL Displacement of [3H]cis-flupenthixol from Dopamine receptor D1 in rat brain B 7.1 pIC50 80 nM IC50 J Med Chem (1988) 31: 454-461 [PMID:2892936]
ChEMBL Affinity for displacement of [3H]WB-4101 labeled Dopamine receptor D1 B 7.76 pIC50 17.3 nM IC50 J Med Chem (1987) 30: 1807-1812 [PMID:2888897]
D2 receptor/D(2) dopamine receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416]
ChEMBL Binding affinity towards Dopamine receptor D2 B 7.57 pKi 27 nM Ki J Med Chem (2003) 46: 2017-2022 [PMID:12747773]
ChEMBL DRUGMATRIX: Dopamine D2L radioligand binding (ligand: [3H] Spiperone) B 7.92 pKi 12 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Dopamine D2L radioligand binding (ligand: [3H] Spiperone) B 7.46 pIC50 35 nM IC50 DrugMatrix in vitro pharmacology data
D2 receptor/D(2) dopamine receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL339] [GtoPdb: 215] [UniProtKB: P61169]
ChEMBL Compound was tested in vitro for its affinity towards rat striatal Dopamine receptor D2 labeled with [3H]- spiperone B 7.22 pIC50 60 nM IC50 J Med Chem (1986) 29: 359-369 [PMID:2869146]
ChEMBL In vitro inhibitory against radioligand [3H]spiperone binding to rat striatal Dopamine receptor D2 B 7.22 pIC50 60 nM IC50 J Med Chem (1992) 35: 4516-4525 [PMID:1361578]
ChEMBL Displacement of [3H]haloperidol from Dopamine receptor D2 in rat brain B 8.4 pIC50 4 nM IC50 J Med Chem (1988) 31: 454-461 [PMID:2892936]
ChEMBL In vitro binding affinity against Dopamine receptor D2 by displacement of [3H]haloperidol from rat striatal membranes. B 8.55 pIC50 2.8 nM IC50 J Med Chem (1987) 30: 1807-1812 [PMID:2888897]
D3 receptor/D(3) dopamine receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL234] [GtoPdb: 216] [UniProtKB: P35462]
ChEMBL DRUGMATRIX: Dopamine D3 radioligand binding (ligand: [3H] Spiperone) B 8.47 pKi 3.36 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Dopamine D3 radioligand binding (ligand: [3H] Spiperone) B 8 pIC50 9.89 nM IC50 DrugMatrix in vitro pharmacology data
D4 receptor/D(4) dopamine receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL219] [GtoPdb: 217] [UniProtKB: P21917]
ChEMBL DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone) B 6.29 pKi 515 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone) B 5.83 pIC50 1468 nM IC50 DrugMatrix in vitro pharmacology data
epidermal growth factor receptor/Epidermal growth factor receptor 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 5.53 pIC50 2947 nM IC50 DrugMatrix in vitro pharmacology data
GABAA receptor γ1 subunit/Gamma-aminobutyric acid receptor subunit gamma-1 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL296] [GtoPdb: 413] [UniProtKB: P23574]
ChEMBL Inhibition of [3H]muscimol binding to Gamma-aminobutyric acid (GABA-A) receptor B 6 pIC50 >1000 nM IC50 J Med Chem (1986) 29: 359-369 [PMID:2869146]
H1 receptor/Histamine H1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL231] [GtoPdb: 262] [UniProtKB: P35367]
GtoPdb - - 7.7 pKi - - - Neuropsychopharmacology (2003) 28: 519-26 [PMID:12629531]
ChEMBL DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine) B 8.08 pKi 8.41 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine) B 7.14 pIC50 72 nM IC50 DrugMatrix in vitro pharmacology data
H1 receptor/Histamine H1 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4701] [GtoPdb: 262] [UniProtKB: P31390]
ChEMBL Binding affinity against Histamine H1 receptor was measured using radioligand ([3H]pyrilamine) binding assay B 7 pIC50 99 nM IC50 J Med Chem (1986) 29: 359-369 [PMID:2869146]
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 6.03 pKi 934 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine) B 6.02 pIC50 950 nM IC50 DrugMatrix in vitro pharmacology data
κ receptor/Kappa-type 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 6 pKi 996 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Opiate kappa (OP2, KOP) radioligand binding (ligand: [3H] Diprenorphine) B 5.6 pIC50 2490 nM IC50 DrugMatrix in vitro pharmacology data
MALT1 paracaspase/Mucosa-associated lymphoid tissue lymphoma translocation protein 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3632452] [GtoPdb: 2983] [UniProtKB: Q9UDY8]
ChEMBL Inhibition of N-terminal his-tagged GCN4 leucine zipper fused human MALT1 (340-281 residues) expressed in Escherichia coli using Ac-LVSR-AMC as substrate by HTS assay B 5.39 pIC50 4100 nM IC50 J Med Chem (2021) 64: 9217-9237 [PMID:34181850]
ChEMBL Inhibition of MALT1 (unknown origin) B 5.46 pIC50 3430 nM IC50 Bioorg Med Chem Lett (2021) 41: 127996-127996 [PMID:33775836]
M1 receptor/Muscarinic acetylcholine receptor M1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL216] [GtoPdb: 13] [UniProtKB: P11229]
ChEMBL DRUGMATRIX: Muscarinic M1 radioligand binding (ligand: [3H] N-Methylscopolamine) B 8.77 pKi 1.69 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Muscarinic M1 radioligand binding (ligand: [3H] N-Methylscopolamine) B 8.15 pIC50 7.02 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 7.42 pKi 38 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Muscarinic M2 radioligand binding (ligand: [3H] N-Methylscopolamine) B 6.97 pIC50 106 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 7.72 pKi 19 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine) B 7.05 pIC50 90 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 DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine) B 7.96 pKi 11 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine) B 7.1 pIC50 80 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 8.18 pKi 6.64 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine) B 8.03 pIC50 9.25 nM IC50 DrugMatrix in vitro pharmacology data
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 5.89 pIC50 1300 nM IC50 Antimicrob Agents Chemother (2009) 53: 1516-1527 [PMID:19188399]
Pim-1 proto-oncogene, serine/threonine kinase/Serine/threonine-protein kinase pim-1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2147] [GtoPdb: 2158] [UniProtKB: P11309]
ChEMBL Inhibition of PIM-1 (unknown origin) after 1 hr by HTRF assay B 5.16 pIC50 6890 nM IC50 Medchemcomm (2014) 5: 507-511
sigma non-opioid intracellular receptor 1/Sigma non-opioid intracellular receptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL287] [GtoPdb: 2552] [UniProtKB: Q99720]
ChEMBL DRUGMATRIX: Sigma1 radioligand binding (ligand: [3H] Haloperidol) B 6.82 pKi 153 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Sigma1 radioligand binding (ligand: [3H] Haloperidol) B 6.44 pIC50 363 nM IC50 DrugMatrix in vitro pharmacology data
sigma non-opioid intracellular receptor 1/Sigma non-opioid intracellular receptor 1 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3602] [GtoPdb: 2552] [UniProtKB: Q9R0C9]
ChEMBL Displacement of (+)-[3H]-3-PPP from rat cortical sigma site F 6.12 pIC50 750 nM IC50 J Med Chem (1992) 35: 4516-4525 [PMID:1361578]
Nav1.5/Sodium channel protein type 5 subunit alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1980] [GtoPdb: 582] [UniProtKB: Q14524]
ChEMBL Inhibition of sodium current measured using whole-cell patch clamp experiments in HEK-293 cells stably transfected with hNaV1.5 cDNA F 5.74 pIC50 1830 nM IC50 Cardiovasc Res (2011) 91: 53-61 [PMID:21300721]
DAT/Sodium-dependent 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 5.72 pKi 1888 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Dopamine Transporter radioligand binding (ligand: [125I] RTI-55) B 5.62 pIC50 2376 nM IC50 DrugMatrix in vitro pharmacology data
NET/Sodium-dependent noradrenaline transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL222] [GtoPdb: 926] [UniProtKB: P23975]
ChEMBL DRUGMATRIX: Norepinephrine Transporter radioligand binding (ligand: [125I] RTI-55) B 5.81 pKi 1538 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Norepinephrine Transporter radioligand binding (ligand: [125I] RTI-55) B 5.81 pIC50 1551 nM IC50 DrugMatrix in vitro pharmacology data
SERT/Sodium-dependent serotonin transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL228] [GtoPdb: 928] [UniProtKB: P31645]
ChEMBL DRUGMATRIX: Transporter, Serotonin (5-Hydroxytryptamine) (SERT) radioligand binding (ligand: [3H] Paroxetine) B 6.4 pKi 399 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Transporter, Serotonin (5-Hydroxytryptamine) (SERT) radioligand binding (ligand: [3H] Paroxetine) B 6.12 pIC50 751 nM IC50 DrugMatrix in vitro pharmacology data
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 5.3 pIC50 5050 nM IC50 DrugMatrix in vitro pharmacology data
Cav1.2/Voltage-dependent L-type calcium channel subunit alpha-1C in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1940] [GtoPdb: 529] [UniProtKB: Q13936]
ChEMBL Inhibition of L-type calcium channel measured using 2-electrode voltage-clamp in human embryonic kidney cells heterologically expressing alpha-1C subunit F 5.88 pIC50 1320 nM IC50 J Appl Toxicol (2012) 32: 858-866 [PMID:22761000]
Voltage-dependent L-type calcium channel subunit alpha-1C in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2366456] [UniProtKB: O35505]
ChEMBL Inhibition of calcium current (ICaL) measured using whole-cell patch clamp experiments in isolated guinea pig ventricular myocytes F 5.89 pIC50 1300 nM IC50 Cardiovasc Res (2011) 91: 53-61 [PMID:21300721]
ChEMBL Inhibition of L-type calcium channel measured using whole-cell patch clamp in guinea pig ventricular myocytes F 5.89 pIC50 1300 nM IC50 J Appl Toxicol (2012) 32: 858-866 [PMID:22761000]
Kv11.1/Voltage-gated inwardly rectifying potassium channel KCNH2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809]
ChEMBL DRUGMATRIX: Potassium Channel HERG radioligand binding (ligand: [3H] Astemizole) B 5.89 pKi 1301 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL Displacement of [3H]Astemizole from hERG expressed in HEK293 cells at 10 uM B 6.06 pKi 869 nM Ki Bioorg Med Chem Lett (2006) 16: 5303-5308 [PMID:16908150]
ChEMBL DRUGMATRIX: Potassium Channel HERG radioligand binding (ligand: [3H] Astemizole) B 5.8 pIC50 1588 nM IC50 DrugMatrix in vitro pharmacology data
ChEMBL Inhibition of human Potassium channel HERG expressed in mammalian cells B 6.44 pIC50 363.08 nM IC50 Bioorg Med Chem Lett (2003) 13: 2773-2775 [PMID:12873512]
ChEMBL Inhibition of human ERG expressed in CHO cells by whole cell patch clamp technique B 6.44 pIC50 363.08 nM IC50 Bioorg Med Chem (2008) 16: 6252-6260 [PMID:18448342]
ChEMBL Inhibitory activity against Potassium channel HERG B 6.72 pIC50 191 nM IC50 J Med Chem (2003) 46: 2017-2022 [PMID:12747773]
ChEMBL Inhibitory concentration against potassium channel HERG B 6.72 pIC50 190.55 nM IC50 Bioorg Med Chem Lett (2005) 15: 2886-2890 [PMID:15911273]
ChEMBL Inhibition of human ERG B 7.02 pIC50 95.5 nM IC50 Eur J Med Chem (2011) 46: 618-630 [PMID:21185626]
ChEMBL K+ channel blocking activity in human embryonic kidney cells expressing HERG Kv11.1 F 7.45 pIC50 35.7 nM IC50 J Med Chem (2002) 45: 3844-3853 [PMID:12190308]
ChEMBL Inhibition of partially open human voltage-gated potassium channel subunit Kv11.1 (ERG K+ channel) F 7.45 pIC50 35.48 nM IC50 Bioorg Med Chem Lett (2005) 15: 1737-1741 [PMID:15745831]
ChEMBL Inhibition of human ERG in MCF7 cells B 7.45 pIC50 35.48 nM IC50 Eur J Med Chem (2009) 44: 1926-1932 [PMID:19110341]
ChEMBL Inhibition of human ERG channel B 7.48 pIC50 33.2 nM IC50 J Med Chem (2009) 52: 4266-4276 [PMID:19534531]
ChEMBL Inhibition of human ERG channel B 7.48 pIC50 33.2 nM IC50 J Med Chem (2009) 52: 4266-4276 [PMID:19534531]
ChEMBL Inhibition of hERG K channel F 7.48 pIC50 33 nM IC50 Cardiovasc Res (2011) 91: 53-61 [PMID:21300721]
D5 receptor in Human [GtoPdb: 218] [UniProtKB: P21918]
GtoPdb - - 5.6 pKi - - - Nature (1991) 350: 614-9 [PMID:1826762]
Kir3.2 in Mouse [GtoPdb: 435] [UniProtKB: P48542]
GtoPdb - - 4.2 pEC50 - - - Br J Pharmacol (2000) 129: 1716-22 [PMID:10780978]

ChEMBL data shown on this page come from version 36:

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]