fluphenazine [Ligand Id: 204] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL726 (Flufenazina, Fluphenazine, NSC-62323)
  • 5-HT1A receptor/5-hydroxytryptamine receptor 1A in Human [ChEMBL: CHEMBL214] [GtoPdb: 1] [UniProtKB: P08908]
  • 5-HT1A receptor/5-hydroxytryptamine receptor 1A in Rat [ChEMBL: CHEMBL273] [GtoPdb: 1] [UniProtKB: P19327]
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  • 5-HT1B receptor/5-hydroxytryptamine receptor 1B in Rat [ChEMBL: CHEMBL3459] [GtoPdb: 2] [UniProtKB: P28564]
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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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  • A3 receptor/Adenosine receptor A3 in Human [ChEMBL: CHEMBL256] [GtoPdb: 21] [UniProtKB: P0DMS8]
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  • α1A-adrenoceptor/Alpha-1A adrenergic receptor in Human [ChEMBL: CHEMBL229] [GtoPdb: 22] [UniProtKB: P35348]
  • 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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  • ABCB1/ATP-dependent translocase ABCB1 in Human [ChEMBL: CHEMBL4302] [GtoPdb: 768] [UniProtKB: P08183]
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  • β3-adrenoceptor/Beta-3 adrenergic receptor in Human [ChEMBL: CHEMBL246] [GtoPdb: 30] [UniProtKB: P13945]
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  • D1 receptor/D(1A) dopamine receptor in Human [ChEMBL: CHEMBL2056] [GtoPdb: 214] [UniProtKB: P21728]
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  • D5 receptor/D(1B) dopamine receptor in Human [ChEMBL: CHEMBL1850] [GtoPdb: 218] [UniProtKB: P21918]
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  • D2 receptor/D(2) dopamine receptor in Human [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416]
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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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  • δ receptor/Delta-type opioid receptor in Human [ChEMBL: CHEMBL236] [GtoPdb: 317] [UniProtKB: P41143]
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  • epidermal growth factor receptor/Epidermal growth factor receptor 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]
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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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  • histone deacetylase 6/Histone deacetylase 6 in Human [ChEMBL: CHEMBL1865] [GtoPdb: 2618] [UniProtKB: Q9UBN7]
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  • κ receptor/Kappa-type opioid receptor in Human [ChEMBL: CHEMBL237] [GtoPdb: 318] [UniProtKB: P41145]
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  • MC5 receptor/Melanocortin receptor 5 in Human [ChEMBL: CHEMBL4608] [GtoPdb: 286] [UniProtKB: P33032]
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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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  • μ receptor/Mu-type opioid receptor in Human [ChEMBL: CHEMBL233] [GtoPdb: 319] [UniProtKB: P35372]
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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 tyrosine-protein kinase erbB-2 in Human [ChEMBL: CHEMBL1824] [GtoPdb: 2019] [UniProtKB: P04626]
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  • Sarcoplasmic/endoplasmic reticulum calcium ATPase 1 in Rabbit [ChEMBL: CHEMBL4693] [UniProtKB: P04191]
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  • sigma non-opioid intracellular receptor 1/Sigma non-opioid intracellular receptor 1 in Human [ChEMBL: CHEMBL287] [GtoPdb: 2552] [UniProtKB: Q99720]
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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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  • NK2 receptor/Substance-K receptor in Human [ChEMBL: CHEMBL2327] [GtoPdb: 361] [UniProtKB: P21452]
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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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  • Kv11.1/Voltage-gated inwardly rectifying potassium channel KCNH2 in Human [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
5-HT1A receptor/5-hydroxytryptamine receptor 1A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL214] [GtoPdb: 1] [UniProtKB: P08908]
ChEMBL Binding affinity to 5HT1A receptor (unknown origin) assessed as inhibition constant B 6.84 pKi 145.7 nM Ki J Med Chem (2024) 67: 12463-12484 [PMID:39038276]
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 6.03 pKi 939 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1A radioligand binding (ligand: [3H] 8-OH-DPAT) B 5.78 pIC50 1644 nM IC50 DrugMatrix in vitro pharmacology data
5-HT1B receptor/5-hydroxytryptamine receptor 1B in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3459] [GtoPdb: 2] [UniProtKB: P28564]
ChEMBL DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol) B 6.06 pKi 869 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol) B 5.72 pIC50 1912 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 - - 7.5 pKi - - - Neuropsychopharmacology (2003) 28: 519-26 [PMID:12629531]
ChEMBL Binding affinity to 5HT2A (unknown origin) assessed as inhibition constant B 7.52 pKi 30 nM Ki J Med Chem (2024) 67: 12463-12484 [PMID:39038276]
ChEMBL DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2A radioligand binding (ligand: [3H] Ketanserin) B 8.84 pKi 1.46 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2A radioligand binding (ligand: [3H] Ketanserin) B 8.29 pIC50 5.1 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 7.6 pKi 25 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide) B 7.41 pIC50 39 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]
ChEMBL DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2C radioligand binding (ligand: [3H] Mesulergine) B 7.46 pKi 35 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2C radioligand binding (ligand: [3H] Mesulergine) B 7.17 pIC50 67 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]
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]
GtoPdb - - 7.4 pKi - - - Psychopharmacology (Berl) (2005) 179: 461-9 [PMID:15821958]
ChEMBL Binding affinity to 5HT6 (unknown origin) assessed as inhibition constant B 7.42 pKi 38 nM Ki J Med Chem (2024) 67: 12463-12484 [PMID:39038276]
ChEMBL DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide) B 7.62 pKi 24 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide) B 7.28 pIC50 52 nM IC50 DrugMatrix in vitro pharmacology data
5-HT6 receptor in Rat [GtoPdb: 11] [UniProtKB: P31388]
GtoPdb - - 7.8 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 - - 7.9 pKi - - - Psychopharmacology (Berl) (2005) 179: 461-9 [PMID:15821958]
ChEMBL Binding affinity to 5HT7 receptor (unknown origin) assessed as inhibition constant B 8.1 pKi 8 nM Ki J Med Chem (2024) 67: 12463-12484 [PMID:39038276]
5-HT7 receptor in Rat [GtoPdb: 12] [UniProtKB: P32305]
GtoPdb - - 8.1 pKi - - - J Pharmacol Exp Ther (1994) 268: 1403-10 [PMID:7908055]
A3 receptor/Adenosine receptor A3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL256] [GtoPdb: 21] [UniProtKB: P0DMS8]
ChEMBL DRUGMATRIX: Adenosine A3 radioligand binding (ligand: AB-MECA) B 5.17 pKi 6746 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Adenosine A3 radioligand binding (ligand: AB-MECA) B 4.92 pIC50 11935 nM IC50 DrugMatrix in vitro pharmacology data
α1A-adrenoceptor/Alpha-1A adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL229] [GtoPdb: 22] [UniProtKB: P35348]
ChEMBL Binding affinity to alpha1A adrenergic receptor (unknown origin) assessed as inhibition constant B 8.19 pKi 6.5 nM Ki J Med Chem (2024) 67: 12463-12484 [PMID:39038276]
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 8.02 pKi 9.58 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin) B 7.62 pIC50 24 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 7.72 pKi 19 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Alpha-1B adrenergic receptor radioligand binding (ligand: prazosin) B 7.47 pIC50 34 nM IC50 DrugMatrix in vitro pharmacology data
α1D-adrenoceptor/Alpha-1D adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL223] [GtoPdb: 24] [UniProtKB: P25100]
ChEMBL DRUGMATRIX: Alpha-1D adrenergic receptor radioligand binding (ligand: prazosin) B 7.8 pKi 16 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Alpha-1D adrenergic receptor radioligand binding (ligand: prazosin) B 7.48 pIC50 33 nM IC50 DrugMatrix in vitro pharmacology data
α2A-adrenoceptor/Alpha-2A adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1867] [GtoPdb: 25] [UniProtKB: P08913]
ChEMBL Binding affinity to alpha2A adrenergic receptor (unknown origin) assessed as inhibition constant B 6.5 pKi 314.1 nM Ki J Med Chem (2024) 67: 12463-12484 [PMID:39038276]
ChEMBL DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912) B 7.1 pKi 80 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912) B 6.67 pIC50 215 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 Binding affinity to alpha2B adrenergic receptor (unknown origin) assessed as inhibition constant B 7.09 pKi 81.6 nM Ki J Med Chem (2024) 67: 12463-12484 [PMID:39038276]
ChEMBL DRUGMATRIX: Alpha-2B adrenergic receptor radioligand binding (ligand: Rauwolscine) B 7.89 pKi 13 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Alpha-2B adrenergic receptor radioligand binding (ligand: Rauwolscine) B 7.54 pIC50 29 nM IC50 DrugMatrix in vitro pharmacology data
α2C-adrenoceptor/Alpha-2C adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1916] [GtoPdb: 27] [UniProtKB: P18825]
ChEMBL Binding affinity to alpha2C adrenergic receptor (unknown origin) assessed as inhibition constant B 7.54 pKi 28.8 nM Ki J Med Chem (2024) 67: 12463-12484 [PMID:39038276]
ChEMBL DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912) B 7.66 pKi 22 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912) B 6.81 pIC50 154 nM IC50 DrugMatrix in vitro pharmacology data
Androgen receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3072] [GtoPdb: 628] [UniProtKB: P15207]
ChEMBL Displacement of [3H]mibolerone from rat androgen receptor B 6.1 pKi 800 nM Ki Proc Natl Acad Sci U S A (2007) 104: 11927-11932 [PMID:17606915]
ABCB1/ATP-dependent translocase ABCB1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4302] [GtoPdb: 768] [UniProtKB: P08183]
ChEMBL TP_TRANSPORTER: inhibition of Rhodamine 123 efflux in NIH-3T3-G185 cells F 4.98 pIC50 10400 nM IC50 Biochem Biophys Res Commun (2001) 289: 580-585 [PMID:11716514]
ChEMBL TP_TRANSPORTER: inhibition of Daunorubicin efflux in NIH-3T3-G185 cells F 5.19 pIC50 6500 nM IC50 Biochem Biophys Res Commun (2001) 289: 580-585 [PMID:11716514]
ChEMBL TP_TRANSPORTER: inhibition of LDS-751 efflux in NIH-3T3-G185 cells F 5.24 pIC50 5700 nM IC50 Biochem Biophys Res Commun (2001) 289: 580-585 [PMID:11716514]
β3-adrenoceptor/Beta-3 adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL246] [GtoPdb: 30] [UniProtKB: P13945]
ChEMBL DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol) B 4.66 pKi 22116 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol) B 4.53 pIC50 29488 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]
ChEMBL Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK cells B 6.75 pKi 179 nM Ki Bioorg Med Chem Lett (2009) 19: 538-542 [PMID:19091563]
ChEMBL Binding affinity to D1 receptor (unknown origin) assessed as inhibition constant B 6.75 pKi 179 nM Ki J Med Chem (2024) 67: 12463-12484 [PMID:39038276]
GtoPdb - - 7.7 pKi - - - Nature (1991) 350: 614-9 [PMID:1826762]
ChEMBL DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390) B 7.96 pKi 11 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390) B 7.64 pIC50 23 nM IC50 DrugMatrix in vitro pharmacology data
D5 receptor/D(1B) dopamine 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 7.68 pKi 21 nM Ki Bioorg Med Chem Lett (2009) 19: 538-542 [PMID:19091563]
ChEMBL Binding affinity to D5 receptor (unknown origin) assessed as inhibition constant B 7.68 pKi 21 nM Ki J Med Chem (2024) 67: 12463-12484 [PMID:39038276]
GtoPdb - - 7.9 pKi - - - Nature (1991) 350: 614-9 [PMID:1826762]
D2 receptor/D(2) dopamine receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416]
GtoPdb - - 8.84 pKi 1.44 nM Ki Bioorg Med Chem (2007) 15: 7258-73 [PMID:17826096]
ChEMBL Displacement of [3H]spiperone from human dopamine D2 receptor expressed in CHO cells B 8.84 pKi 1.44 nM Ki Bioorg Med Chem Lett (2009) 19: 538-542 [PMID:19091563]
ChEMBL Binding affinity to D2 receptor (unknown origin) assessed as inhibition constant B 8.84 pKi 1.44 nM Ki J Med Chem (2024) 67: 12463-12484 [PMID:39038276]
ChEMBL DRUGMATRIX: Dopamine D2L radioligand binding (ligand: [3H] Spiperone) B 9.27 pKi 0.54 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Dopamine D2L radioligand binding (ligand: [3H] Spiperone) B 8.79 pIC50 1.62 nM IC50 DrugMatrix in vitro pharmacology data
D3 receptor/D(3) dopamine receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL234] [GtoPdb: 216] [UniProtKB: P35462]
ChEMBL Displacement of [3H]spiperone from human dopamine D3 receptor expressed in CHO cells B 8.49 pKi 3.21 nM Ki Bioorg Med Chem Lett (2009) 19: 538-542 [PMID:19091563]
ChEMBL Binding affinity to D3 receptor (unknown origin) assessed as inhibition constant B 8.49 pKi 3.2 nM Ki J Med Chem (2024) 67: 12463-12484 [PMID:39038276]
ChEMBL DRUGMATRIX: Dopamine D3 radioligand binding (ligand: [3H] Spiperone) B 9.69 pKi 0.2 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Dopamine D3 radioligand binding (ligand: [3H] Spiperone) B 9.23 pIC50 0.59 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 5.69 pKi 2061 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL Binding affinity to D4 receptor (unknown origin) assessed as inhibition constant B 6.89 pKi 130 nM Ki J Med Chem (2024) 67: 12463-12484 [PMID:39038276]
ChEMBL DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone) B 5.23 pIC50 5877 nM IC50 DrugMatrix in vitro pharmacology data
δ receptor/Delta-type 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 5.07 pKi 8473 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Opiate delta1 (OP1, DOP) radioligand binding (ligand: [3H] Naltrindole) B 4.62 pIC50 24036 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 4.4 pIC50 40107 nM IC50 DrugMatrix in vitro pharmacology data
H1 receptor/Histamine H1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL231] [GtoPdb: 262] [UniProtKB: P35367]
ChEMBL Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO cells B 7.4 pKi 40 nM Ki Bioorg Med Chem Lett (2009) 19: 538-542 [PMID:19091563]
ChEMBL Binding affinity to H1 receptor (unknown origin) assessed as inhibition constant B 7.68 pKi 21 nM Ki J Med Chem (2024) 67: 12463-12484 [PMID:39038276]
GtoPdb - - 7.7 pKi - - - Neuropsychopharmacology (2003) 28: 519-26 [PMID:12629531]
ChEMBL DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine) B 8.33 pKi 4.66 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine) B 7.4 pIC50 40 nM IC50 DrugMatrix in vitro pharmacology data
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 5.92 pKi 1205 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine) B 5.91 pIC50 1226 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]
histone deacetylase 6/Histone deacetylase 6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1865] [GtoPdb: 2618] [UniProtKB: Q9UBN7]
ChEMBL Determination of IC50 values for inhibition of enzymatic assay of human HDAC6 with custom peptide substrate B 5.25 pIC50 5624 nM IC50 HDAC6 screening dataset using tau-based substrate in an enzymatic assay yields selective inhibitors and activators
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 5 pKi 9891 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Opiate kappa (OP2, KOP) radioligand binding (ligand: [3H] Diprenorphine) B 4.61 pIC50 24727 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 5.05 pKi 8929 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH) B 5.02 pIC50 9518 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 DRUGMATRIX: Muscarinic M1 radioligand binding (ligand: [3H] N-Methylscopolamine) B 6.19 pKi 646 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Muscarinic M1 radioligand binding (ligand: [3H] N-Methylscopolamine) B 5.57 pIC50 2683 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 5.58 pKi 2660 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Muscarinic M2 radioligand binding (ligand: [3H] N-Methylscopolamine) B 5.13 pIC50 7481 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 6 pKi 1002 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine) B 5.33 pIC50 4728 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 6.32 pKi 484 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine) B 5.46 pIC50 3468 nM IC50 DrugMatrix in vitro pharmacology data
μ receptor/Mu-type 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 5.07 pKi 8421 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Opiate mu (OP3, MOP) radioligand binding (ligand: [3H] Diprenorphine) B 4.68 pIC50 20745 nM IC50 DrugMatrix in vitro pharmacology data
Plasmodium falciparum (target type: ORGANISM) [ChEMBL: CHEMBL364]
ChEMBL DNDI: Malaria in Vitro, 72 hour F 6.3 pIC50 500 nM IC50 Antiprotozoal Activity Profiling of Approved Drugs: A Starting Point toward Drug Repositioning
ChEMBL Antiplasmodial activity against Plasmodium falciparum K1 at 0.002 to 100 ug/ml by serial drug dilution assay F 6.3 pIC50 500 nM IC50 Bioorg Med Chem (2017) 25: 6332-6344 [PMID:29042223]
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 5.77 pIC50 1700 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 5.33 pIC50 4700 nM IC50 J Med Chem (2016) 59: 5149-5157 [PMID:26588045]
erb-b2 receptor tyrosine kinase 2/Receptor tyrosine-protein 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 19570 nM IC50 DrugMatrix in vitro pharmacology data
Sarcoplasmic/endoplasmic reticulum calcium ATPase 1 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 4.82 pIC50 15000 nM IC50 J Med Chem (2020) 63: 1937-1963 [PMID:32030976]
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 8.07 pKi 8.57 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Sigma1 radioligand binding (ligand: [3H] Haloperidol) B 7.7 pIC50 20 nM IC50 DrugMatrix in vitro pharmacology data
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 5.79 pKi 1631 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Dopamine Transporter radioligand binding (ligand: [125I] RTI-55) B 5.69 pIC50 2053 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 5.71 pKi 1946 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Norepinephrine Transporter radioligand binding (ligand: [125I] RTI-55) B 5.71 pIC50 1962 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 6.1 pKi 793 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Transporter, Serotonin (5-Hydroxytryptamine) (SERT) radioligand binding (ligand: [3H] Paroxetine) B 5.83 pIC50 1492 nM IC50 DrugMatrix in vitro pharmacology data
NK2 receptor/Substance-K receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2327] [GtoPdb: 361] [UniProtKB: P21452]
ChEMBL DRUGMATRIX: Tachykinin NK2 radioligand binding (ligand: [3H] SR-48968) B 5.13 pKi 7495 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Tachykinin NK2 radioligand binding (ligand: [3H] SR-48968) B 4.65 pIC50 22484 nM IC50 DrugMatrix in vitro pharmacology data
Trypanothione reductase in Trypanosoma cruzi (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5131] [UniProtKB: P28593]
ChEMBL Inhibitory activity against recombinant Trypanosoma cruzi (Trypanosoma cruzi) Trypanothione reductase (linear competitive type) B 4.67 pKi 21200 nM Ki J Med Chem (1998) 41: 148-156 [PMID:9457238]
ChEMBL Inhibitory activity against recombinant Trypanosoma cruzi (Trypanosoma cruzi) Trypanothione reductase B 4.13 pIC50 73700 nM IC50 J Med Chem (1998) 41: 148-156 [PMID:9457238]
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 5.1 pIC50 7990 nM IC50 DrugMatrix in vitro pharmacology data
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 5.33 pKi 4674.6 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Potassium Channel HERG radioligand binding (ligand: [3H] Astemizole) B 5.24 pIC50 5705.8 nM IC50 DrugMatrix in vitro pharmacology data

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]