AC-42 [Ligand Id: 289] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL1242950
  • 5-HT1A receptor/5-hydroxytryptamine receptor 1A in Human [ChEMBL: CHEMBL214] [GtoPdb: 1] [UniProtKB: P08908]
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  • 5-HT1B receptor/5-hydroxytryptamine receptor 1B in Human [ChEMBL: CHEMBL1898] [GtoPdb: 2] [UniProtKB: P28222]
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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-HT3A/5-hydroxytryptamine receptor 3A in Human [ChEMBL: CHEMBL1899] [GtoPdb: 373] [UniProtKB: P46098]
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  • 5-HT4 receptor/5-hydroxytryptamine receptor 4 in Human [ChEMBL: CHEMBL1875] [GtoPdb: 9] [UniProtKB: Q13639]
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  • 5-HT7 receptor/5-hydroxytryptamine receptor 7 in Human [ChEMBL: CHEMBL3155] [GtoPdb: 12] [UniProtKB: P34969]
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  • acetylcholinesterase (Yt blood group)/Acetylcholinesterase in Human [ChEMBL: CHEMBL220] [GtoPdb: 2465] [UniProtKB: P22303]
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  • A1 receptor/Adenosine receptor A1 in Human [ChEMBL: CHEMBL226] [GtoPdb: 18] [UniProtKB: P30542]
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  • A2A receptor/Adenosine receptor A2a in Human [ChEMBL: CHEMBL251] [GtoPdb: 19] [UniProtKB: P29274]
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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]
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  • α1B-adrenoceptor/Alpha-1B adrenergic receptor in Human [ChEMBL: CHEMBL232] [GtoPdb: 23] [UniProtKB: P35368]
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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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  • Monoamine oxidase A/Amine oxidase [flavin-containing] A in Human [ChEMBL: CHEMBL1951] [GtoPdb: 2489] [UniProtKB: P21397]
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  • β1-adrenoceptor/Beta-1 adrenergic receptor in Human [ChEMBL: CHEMBL213] [GtoPdb: 28] [UniProtKB: P08588]
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  • β2-adrenoceptor/Beta-2 adrenergic receptor in Human [ChEMBL: CHEMBL210] [GtoPdb: 29] [UniProtKB: P07550]
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  • CB1 receptor/Cannabinoid receptor 1 in Human [ChEMBL: CHEMBL218] [GtoPdb: 56] [UniProtKB: P21554]
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  • D1 receptor/D(1A) dopamine receptor in Human [ChEMBL: CHEMBL2056] [GtoPdb: 214] [UniProtKB: P21728]
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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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  • ETA receptor/Endothelin-1 receptor in Human [ChEMBL: CHEMBL252] [GtoPdb: 219] [UniProtKB: P25101]
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  • CCK2 receptor/Gastrin/cholecystokinin type B receptor in Human [ChEMBL: CHEMBL298] [GtoPdb: 77] [UniProtKB: P32239]
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  • CHT/High affinity choline transporter 1 in Human [ChEMBL: CHEMBL4507] [GtoPdb: 914] [UniProtKB: Q9GZV3]
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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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  • κ receptor/Kappa-type opioid receptor in Human [ChEMBL: CHEMBL237] [GtoPdb: 318] [UniProtKB: P41145]
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  • MC4 receptor/Melanocortin receptor 4 in Human [ChEMBL: CHEMBL259] [GtoPdb: 285] [UniProtKB: P32245]
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  • MT1 receptor/Melatonin receptor type 1A in Human [ChEMBL: CHEMBL1945] [GtoPdb: 287] [UniProtKB: P48039]
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  • mitogen-activated protein kinase 14/Mitogen-activated protein kinase 14 in Human [ChEMBL: CHEMBL260] [GtoPdb: 1499] [UniProtKB: Q16539]
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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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  • μ receptor/Mu-type opioid receptor in Human [ChEMBL: CHEMBL233] [GtoPdb: 319] [UniProtKB: P35372]
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  • nicotinic acetylcholine receptor β2 subunit/nicotinic acetylcholine receptor α4 subunit/Neuronal acetylcholine receptor; alpha4/beta2 in Human [ChEMBL: CHEMBL1907589] [GtoPdb: 472465] [UniProtKB: P17787P43681]
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  • Y1 receptor/Neuropeptide Y receptor type 1 in Human [ChEMBL: CHEMBL4777] [GtoPdb: 305] [UniProtKB: P25929]
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  • NTS1 receptor/Neurotensin receptor type 1 in Human [ChEMBL: CHEMBL4123] [GtoPdb: 309] [UniProtKB: P30989]
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  • Ribosyldihydronicotinamide dehydrogenase [quinone] in Human [ChEMBL: CHEMBL3959] [UniProtKB: P16083]
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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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  • NK1 receptor/Substance-P receptor in Human [ChEMBL: CHEMBL249] [GtoPdb: 360] [UniProtKB: P25103]
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  • LYN proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase Lyn in Human [ChEMBL: CHEMBL3905] [GtoPdb: 2060] [UniProtKB: P07948]
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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 human 5-HT1A receptor by radioligand displacement assay B 6.55 pKi 280 nM Ki J Med Chem (2010) 53: 6386-6397 [PMID:20684563]
5-HT1B receptor/5-hydroxytryptamine receptor 1B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1898] [GtoPdb: 2] [UniProtKB: P28222]
ChEMBL Binding affinity to 5-HT1B receptor by radioligand displacement assay B 6 pKi >=1000 nM Ki J Med Chem (2010) 53: 6386-6397 [PMID:20684563]
5-HT2A receptor/5-hydroxytryptamine receptor 2A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223]
ChEMBL Binding affinity to human 5-HT2A agonist site receptor by radioligand displacement assay B 6 pKi >=1000 nM Ki J Med Chem (2010) 53: 6386-6397 [PMID:20684563]
5-HT2B receptor/5-hydroxytryptamine receptor 2B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1833] [GtoPdb: 7] [UniProtKB: P41595]
ChEMBL Binding affinity to human 5-HT2B agonist site receptor by radioligand displacement assay B 6 pKi >=1000 nM Ki J Med Chem (2010) 53: 6386-6397 [PMID:20684563]
5-HT2C receptor/5-hydroxytryptamine receptor 2C in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL225] [GtoPdb: 8] [UniProtKB: P28335]
ChEMBL Binding affinity to human 5HT2C receptor agonist site by radioligand displacement assay B 6 pKi >=1000 nM Ki J Med Chem (2010) 53: 6386-6397 [PMID:20684563]
5-HT3A/5-hydroxytryptamine receptor 3A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1899] [GtoPdb: 373] [UniProtKB: P46098]
ChEMBL Binding affinity to human 5-HT3 receptor by radioligand displacement assay B 6 pKi >=1000 nM Ki J Med Chem (2010) 53: 6386-6397 [PMID:20684563]
5-HT4 receptor/5-hydroxytryptamine receptor 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1875] [GtoPdb: 9] [UniProtKB: Q13639]
ChEMBL Binding affinity to human 5-HT4e receptor by radioligand displacement assay B 6 pKi >=1000 nM Ki J Med Chem (2010) 53: 6386-6397 [PMID:20684563]
5-HT7 receptor/5-hydroxytryptamine receptor 7 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3155] [GtoPdb: 12] [UniProtKB: P34969]
ChEMBL Binding affinity to human 5-HT7 receptor by radioligand displacement assay B 6 pKi >=1000 nM Ki J Med Chem (2010) 53: 6386-6397 [PMID:20684563]
acetylcholinesterase (Yt blood group)/Acetylcholinesterase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL220] [GtoPdb: 2465] [UniProtKB: P22303]
ChEMBL Binding affinity to human acetylcholine esterase by radioligand displacement assay B 6 pKi >=1000 nM Ki J Med Chem (2010) 53: 6386-6397 [PMID:20684563]
A1 receptor/Adenosine receptor A1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL226] [GtoPdb: 18] [UniProtKB: P30542]
ChEMBL Binding affinity to human adenosine A1 receptor by radioligand displacement assay B 6 pKi >=1000 nM Ki J Med Chem (2010) 53: 6386-6397 [PMID:20684563]
ChEMBL Binding affinity to human adenosine A1 receptor agonist site by radioligand displacement assay B 6 pKi >=1000 nM Ki J Med Chem (2010) 53: 6386-6397 [PMID:20684563]
A2A receptor/Adenosine receptor A2a in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL251] [GtoPdb: 19] [UniProtKB: P29274]
ChEMBL Binding affinity to human adenosine A2A receptor by radioligand displacement assay B 6 pKi >=1000 nM Ki J Med Chem (2010) 53: 6386-6397 [PMID:20684563]
A3 receptor/Adenosine receptor A3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL256] [GtoPdb: 21] [UniProtKB: P0DMS8]
ChEMBL Binding affinity to human adenosine A3 receptor by radioligand displacement assay B 6 pKi >=1000 nM Ki J Med Chem (2010) 53: 6386-6397 [PMID:20684563]
α1A-adrenoceptor/Alpha-1A adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL229] [GtoPdb: 22] [UniProtKB: P35348]
ChEMBL Binding affinity to human adrenergic alpha1A receptor by radioligand displacement assay B 7.74 pKi 18 nM Ki J Med Chem (2010) 53: 6386-6397 [PMID:20684563]
α1B-adrenoceptor/Alpha-1B adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL232] [GtoPdb: 23] [UniProtKB: P35368]
ChEMBL Binding affinity to human adrenergic Alpha-1B receptor by radioligand displacement assay B 7.19 pKi 65 nM Ki J Med Chem (2010) 53: 6386-6397 [PMID:20684563]
α1D-adrenoceptor/Alpha-1D adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL223] [GtoPdb: 24] [UniProtKB: P25100]
ChEMBL Binding affinity to human adrenergic Alpha-1D receptor by radioligand displacement assay B 7.4 pKi 40 nM Ki J Med Chem (2010) 53: 6386-6397 [PMID:20684563]
α2A-adrenoceptor/Alpha-2A adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1867] [GtoPdb: 25] [UniProtKB: P08913]
ChEMBL Binding affinity to human adrenergic alpha2A receptor by radioligand displacement assay B 6.28 pKi 530 nM Ki J Med Chem (2010) 53: 6386-6397 [PMID:20684563]
α2B-adrenoceptor/Alpha-2B adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1942] [GtoPdb: 26] [UniProtKB: P18089]
ChEMBL Binding affinity to adrenergic alpha2B receptor by radioligand displacement assay B 6.08 pKi 840 nM Ki J Med Chem (2010) 53: 6386-6397 [PMID:20684563]
Monoamine oxidase A/Amine oxidase [flavin-containing] A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1951] [GtoPdb: 2489] [UniProtKB: P21397]
ChEMBL Binding affinity to MAOA by radioligand displacement assay B 6 pKi >=1000 nM Ki J Med Chem (2010) 53: 6386-6397 [PMID:20684563]
β1-adrenoceptor/Beta-1 adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL213] [GtoPdb: 28] [UniProtKB: P08588]
ChEMBL Binding affinity to human adrenergic beta-1 receptor by radioligand displacement assay B 6 pKi >=1000 nM Ki J Med Chem (2010) 53: 6386-6397 [PMID:20684563]
β2-adrenoceptor/Beta-2 adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL210] [GtoPdb: 29] [UniProtKB: P07550]
ChEMBL Binding affinity to adrenergic beta2 receptor by radioligand displacement assay B 6 pKi >=1000 nM Ki J Med Chem (2010) 53: 6386-6397 [PMID:20684563]
CB1 receptor/Cannabinoid receptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL218] [GtoPdb: 56] [UniProtKB: P21554]
ChEMBL Binding affinity to human CB1 receptor by radioligand displacement assay B 6 pKi >=1000 nM Ki J Med Chem (2010) 53: 6386-6397 [PMID:20684563]
D1 receptor/D(1A) dopamine receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2056] [GtoPdb: 214] [UniProtKB: P21728]
ChEMBL Binding affinity to human dopamine D1 receptor by radioligand displacement assay B 6 pKi >=1000 nM Ki J Med Chem (2010) 53: 6386-6397 [PMID:20684563]
D2 receptor/D(2) dopamine receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416]
ChEMBL Binding affinity to human D2S agonist site receptor by radioligand displacement assay B 6 pKi >=1000 nM Ki J Med Chem (2010) 53: 6386-6397 [PMID:20684563]
ChEMBL Binding affinity to human dopamine D2S receptor by radioligand displacement assay B 7.11 pKi 77 nM Ki J Med Chem (2010) 53: 6386-6397 [PMID:20684563]
D3 receptor/D(3) dopamine receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL234] [GtoPdb: 216] [UniProtKB: P35462]
ChEMBL Binding affinity to human dopamine D3 receptor by radioligand displacement assay B 6 pKi >=1000 nM Ki J Med Chem (2010) 53: 6386-6397 [PMID:20684563]
D4 receptor/D(4) dopamine receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL219] [GtoPdb: 217] [UniProtKB: P21917]
ChEMBL Binding affinity to human D4.4 receptor by radioligand displacement assay B 7.96 pKi 11 nM Ki J Med Chem (2010) 53: 6386-6397 [PMID:20684563]
ETA receptor/Endothelin-1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL252] [GtoPdb: 219] [UniProtKB: P25101]
ChEMBL Binding affinity to human ETA receptor by radioligand displacement assay B 6 pKi >=1000 nM Ki J Med Chem (2010) 53: 6386-6397 [PMID:20684563]
CCK2 receptor/Gastrin/cholecystokinin type B receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL298] [GtoPdb: 77] [UniProtKB: P32239]
ChEMBL Binding affinity to human CCK2 receptor by radioligand displacement assay B 6 pKi >=1000 nM Ki J Med Chem (2010) 53: 6386-6397 [PMID:20684563]
Glucocorticoid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2034] [GtoPdb: 625] [UniProtKB: P04150]
ChEMBL Binding affinity to human glucocorticoid receptor by radioligand displacement assay B 6 pKi >=1000 nM Ki J Med Chem (2010) 53: 6386-6397 [PMID:20684563]
CHT/High affinity choline transporter 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4507] [GtoPdb: 914] [UniProtKB: Q9GZV3]
ChEMBL Binding affinity to human choline transporter (CHT1) by radioligand displacement assay B 6 pKi >=1000 nM Ki J Med Chem (2010) 53: 6386-6397 [PMID:20684563]
H1 receptor/Histamine H1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL231] [GtoPdb: 262] [UniProtKB: P35367]
ChEMBL Binding affinity to human histamine H1 receptor by radioligand displacement assay B 6.21 pKi 610 nM Ki J Med Chem (2010) 53: 6386-6397 [PMID:20684563]
H2 receptor/Histamine H2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1941] [GtoPdb: 263] [UniProtKB: P25021]
ChEMBL Binding affinity to human histamine H2 receptor by radioligand displacement assay B 6 pKi >=1000 nM Ki J Med Chem (2010) 53: 6386-6397 [PMID:20684563]
H3 receptor/Histamine H3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL264] [GtoPdb: 264] [UniProtKB: Q9Y5N1]
ChEMBL Binding affinity to human histamine H3 receptor by radioligand displacement assay B 6 pKi >=1000 nM Ki J Med Chem (2010) 53: 6386-6397 [PMID:20684563]
κ receptor/Kappa-type opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL237] [GtoPdb: 318] [UniProtKB: P41145]
ChEMBL Binding affinity to kappa opioid receptor by radioligand displacement assay B 6 pKi >=1000 nM Ki J Med Chem (2010) 53: 6386-6397 [PMID:20684563]
MC4 receptor/Melanocortin receptor 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL259] [GtoPdb: 285] [UniProtKB: P32245]
ChEMBL Binding affinity to human MC4 receptor by radioligand displacement assay B 6 pKi >=1000 nM Ki J Med Chem (2010) 53: 6386-6397 [PMID:20684563]
MT1 receptor/Melatonin receptor type 1A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1945] [GtoPdb: 287] [UniProtKB: P48039]
ChEMBL Binding affinity to human MT1 receptor by radioligand displacement assay B 6 pKi >=1000 nM Ki J Med Chem (2010) 53: 6386-6397 [PMID:20684563]
mitogen-activated protein kinase 14/Mitogen-activated protein kinase 14 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL260] [GtoPdb: 1499] [UniProtKB: Q16539]
ChEMBL Binding affinity to p38alpha by radioligand displacement assay B 6 pKi >=1000 nM Ki J Med Chem (2010) 53: 6386-6397 [PMID:20684563]
M1 receptor/Muscarinic acetylcholine receptor M1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL216] [GtoPdb: 13] [UniProtKB: P11229]
ChEMBL Binding affinity to human muscarinic M1 receptor by radioligand displacement assay B 6 pKi >=1000 nM Ki J Med Chem (2010) 53: 6386-6397 [PMID:20684563]
GtoPdb - - 6.2 pKi - - - Mol Pharmacol (2006) 69: 236-46 [PMID:16207821]
GtoPdb - - 6.2 pKi - - - Mol Pharmacol (2006) 69: 236-46 [PMID:16207821]
ChEMBL Agonist activity at human muscarinic M1 receptor Y381A mutant expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assay F 6.3 pEC50 500 nM EC50 J Med Chem (2010) 53: 6386-6397 [PMID:20684563]
ChEMBL Agonist activity at human muscarinic M1 receptor expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assay F 6.82 pEC50 150 nM EC50 J Med Chem (2010) 53: 6386-6397 [PMID:20684563]
M2 receptor/Muscarinic acetylcholine receptor M2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL211] [GtoPdb: 14] [UniProtKB: P08172]
ChEMBL Binding affinity to human muscarinic M2 receptor by radioligand displacement assay B 6 pKi >=1000 nM Ki J Med Chem (2010) 53: 6386-6397 [PMID:20684563]
ChEMBL Displacement of [3H]-AFDX-384 from human muscarinic M2 receptor expressed in CHO-K1 cells B 6.01 pKi 980 nM Ki J Med Chem (2010) 53: 6386-6397 [PMID:20684563]
M3 receptor/Muscarinic acetylcholine receptor M3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL245] [GtoPdb: 15] [UniProtKB: P20309]
ChEMBL Displacement of [3H]-4-DAMP from human muscarinic M3 receptor expressed in BHK-21 cells B 5.55 pKi 2800 nM Ki J Med Chem (2010) 53: 6386-6397 [PMID:20684563]
ChEMBL Binding affinity to human muscarinic M3 receptor by radioligand displacement assay B 6 pKi >=1000 nM Ki J Med Chem (2010) 53: 6386-6397 [PMID:20684563]
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 muscarinic M4 receptor expressed in BHK-21 cells B 5.85 pKi 1400 nM Ki J Med Chem (2010) 53: 6386-6397 [PMID:20684563]
ChEMBL Binding affinity to human muscarinic M4 receptor by radioligand displacement assay B 6 pKi >=1000 nM Ki J Med Chem (2010) 53: 6386-6397 [PMID:20684563]
M5 receptor/Muscarinic acetylcholine receptor M5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2035] [GtoPdb: 17] [UniProtKB: P08912]
ChEMBL Displacement of [3H]-4-DAMP from human muscarinic M5 receptor expressed in BHK-21 cells B 5.35 pKi 4500 nM Ki J Med Chem (2010) 53: 6386-6397 [PMID:20684563]
ChEMBL Binding affinity to human muscarinic M5 receptor by radioligand displacement assay B 6 pKi >=1000 nM Ki J Med Chem (2010) 53: 6386-6397 [PMID:20684563]
μ receptor/Mu-type opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL233] [GtoPdb: 319] [UniProtKB: P35372]
ChEMBL Binding affinity to human mu opioid receptor agonist site by radioligand displacement assay B 6 pKi >=1000 nM Ki J Med Chem (2010) 53: 6386-6397 [PMID:20684563]
nicotinic acetylcholine receptor β2 subunit/nicotinic acetylcholine receptor α4 subunit/Neuronal acetylcholine receptor; alpha4/beta2 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL1907589] [GtoPdb: 472465] [UniProtKB: P17787P43681]
ChEMBL Binding affinity to nAChR alpha4beta2 receptor by radioligand displacement assay B 6 pKi >=1000 nM Ki J Med Chem (2010) 53: 6386-6397 [PMID:20684563]
Y1 receptor/Neuropeptide Y receptor type 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4777] [GtoPdb: 305] [UniProtKB: P25929]
ChEMBL Binding affinity to human neuropeptide Y1 receptor by radioligand displacement assay B 6 pKi >=1000 nM Ki J Med Chem (2010) 53: 6386-6397 [PMID:20684563]
NTS1 receptor/Neurotensin receptor type 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4123] [GtoPdb: 309] [UniProtKB: P30989]
ChEMBL Binding affinity to human UT1 receptor by radioligand displacement assay B 6 pKi >=1000 nM Ki J Med Chem (2010) 53: 6386-6397 [PMID:20684563]
Nischarin in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3923] [UniProtKB: Q9Y2I1]
ChEMBL Binding affinity to I1 receptor by radioligand displacement assay B 6 pKi >=1000 nM Ki J Med Chem (2010) 53: 6386-6397 [PMID:20684563]
Ribosyldihydronicotinamide dehydrogenase [quinone] in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3959] [UniProtKB: P16083]
ChEMBL Binding affinity to ML2 (MT3) receptor by radioligand displacement assay B 6 pKi >=1000 nM Ki J Med Chem (2010) 53: 6386-6397 [PMID:20684563]
DAT/Sodium-dependent dopamine transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL238] [GtoPdb: 927] [UniProtKB: Q01959]
ChEMBL Binding affinity to human dopamine transporter by radioligand displacement assay B 6 pKi >=1000 nM Ki J Med Chem (2010) 53: 6386-6397 [PMID:20684563]
NET/Sodium-dependent noradrenaline transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL222] [GtoPdb: 926] [UniProtKB: P23975]
ChEMBL Binding affinity to human NE transporter by radioligand displacement assay B 6 pKi >=1000 nM Ki J Med Chem (2010) 53: 6386-6397 [PMID:20684563]
SERT/Sodium-dependent serotonin transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL228] [GtoPdb: 928] [UniProtKB: P31645]
ChEMBL Binding affinity to human 5-HT transporter by radioligand displacement assay B 6 pKi >=1000 nM Ki J Med Chem (2010) 53: 6386-6397 [PMID:20684563]
NK2 receptor/Substance-K receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2327] [GtoPdb: 361] [UniProtKB: P21452]
ChEMBL Binding affinity to human NK2 receptor by radioligand displacement assay B 6 pKi >=1000 nM Ki J Med Chem (2010) 53: 6386-6397 [PMID:20684563]
NK1 receptor/Substance-P receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL249] [GtoPdb: 360] [UniProtKB: P25103]
ChEMBL Binding affinity to human NK1 receptor by radioligand displacement assay B 6 pKi >=1000 nM Ki J Med Chem (2010) 53: 6386-6397 [PMID:20684563]
LYN proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase Lyn in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3905] [GtoPdb: 2060] [UniProtKB: P07948]
ChEMBL Binding affinity to Lyn by radioligand displacement assay B 6 pKi >=1000 nM Ki J Med Chem (2010) 53: 6386-6397 [PMID:20684563]

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]