zotepine [Ligand Id: 103] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL285802 (Zotepine, Zoleptil 25, Zoleptil 50, Zoleptil 100)
  • D1 receptor/Dopamine D1 receptor in Human [ChEMBL: CHEMBL2056] [GtoPdb: 214] [UniProtKB: P21728]
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  • D2 receptor/Dopamine D2 receptor in Human [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416]
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  • D3 receptor/Dopamine D3 receptor in Human [ChEMBL: CHEMBL234] [GtoPdb: 216] [UniProtKB: P35462]
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  • D4 receptor/Dopamine D4 receptor in Human [ChEMBL: CHEMBL219] [GtoPdb: 217] [UniProtKB: P21917]
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  • H1 receptor/Histamine H1 receptor in Human [ChEMBL: CHEMBL231] [GtoPdb: 262] [UniProtKB: P35367]
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  • M4 receptor/Muscarinic acetylcholine receptor M4 in Human [ChEMBL: CHEMBL1821] [GtoPdb: 16] [UniProtKB: P08173]
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  • 5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Human [ChEMBL: CHEMBL214] [GtoPdb: 1] [UniProtKB: P08908]
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  • 5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Human [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223]
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  • 5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Human [ChEMBL: CHEMBL225] [GtoPdb: 8] [UniProtKB: P28335]
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  • 5-HT1B receptor in Human [GtoPdb: 2] [UniProtKB: P28222]
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  • 5-HT1D receptor in Human [GtoPdb: 3] [UniProtKB: P28221]
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  • 5-ht1e receptor in Human [GtoPdb: 4] [UniProtKB: P28566]
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  • 5-HT6 receptor in Human [GtoPdb: 11] [UniProtKB: P50406]
  • 5-HT6 receptor in Rat [GtoPdb: 11] [UniProtKB: P31388]
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  • 5-HT7 receptor in Human [GtoPdb: 12] [UniProtKB: P34969]
  • 5-HT7 receptor in Rat [GtoPdb: 12] [UniProtKB: P32305]
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  • α2B-adrenoceptor in Human [GtoPdb: 26] [UniProtKB: P18089]
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  • NET in Human [GtoPdb: 926] [UniProtKB: P23975]
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  • SERT in Human [GtoPdb: 928] [UniProtKB: P31645]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
D1 receptor/Dopamine D1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2056] [GtoPdb: 214] [UniProtKB: P21728]
ChEMBL Binding affinity towards human Dopamine receptor D1 B 7.08 pKi 84 nM Ki J. Med. Chem. (2004) 47: 1303-1314 [PMID:14998318]
ChEMBL Binding affinity against dopamine receptor D1 B 7.54 pKi 29 nM Ki J. Med. Chem. (2001) 44: 477-501 [PMID:11170639]
D2 receptor/Dopamine D2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416]
ChEMBL Binding affinity towards human Dopamine receptor D2 B 7.89 pKi 13 nM Ki J. Med. Chem. (2004) 47: 1303-1314 [PMID:14998318]
ChEMBL Binding affinity towards human D2 dopamine receptor. B 7.96 pKi 11 nM Ki J. Med. Chem. (2001) 44: 477-501 [PMID:11170639]
GtoPdb - - 7.96 pKi 11 nM Ki Psychopharmacology (Berl.) (1996) 124: 57-73 [PMID:8935801]
D3 receptor/Dopamine D3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL234] [GtoPdb: 216] [UniProtKB: P35462]
ChEMBL Binding affinity towards human Dopamine receptor D3 B 7.8 pKi 16 nM Ki J. Med. Chem. (2004) 47: 1303-1314 [PMID:14998318]
GtoPdb - - 8.19 pKi 6.4 nM Ki Psychopharmacology (Berl.) (1996) 124: 57-73 [PMID:8935801]
ChEMBL Binding affinity towards human dopamine receptor D3 B 8.19 pKi 6.4 nM Ki J. Med. Chem. (2001) 44: 477-501 [PMID:11170639]
D4 receptor/Dopamine D4 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL219] [GtoPdb: 217] [UniProtKB: P21917]
ChEMBL Binding affinity towards human dopamine-4.2 receptor B 7.41 pKi 39 nM Ki J. Med. Chem. (2004) 47: 1303-1314 [PMID:14998318]
ChEMBL Binding affinity towards human dopamine receptor D4 B 7.41 pKi 39 nM Ki J. Med. Chem. (2001) 44: 477-501 [PMID:11170639]
GtoPdb - - 7.41 pKi 39 nM Ki Psychopharmacology (Berl.) (1996) 124: 57-73 [PMID:8935801]
H1 receptor/Histamine H1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL231] [GtoPdb: 262] [UniProtKB: P35367]
ChEMBL Binding affinity towards human histamine H1 receptor B 8.47 pKi 3.4 nM Ki J. Med. Chem. (2004) 47: 1303-1314 [PMID:14998318]
GtoPdb - - 9.2 pKi - - - Psychopharmacology (Berl.) (1996) 124: 57-73 [PMID:8935801]
ChEMBL Binding affinity towards human H1 receptor B 9.21 pKi 0.62 nM Ki J. Med. Chem. (2001) 44: 477-501 [PMID:11170639]
M4 receptor/Muscarinic acetylcholine receptor M4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1821] [GtoPdb: 16] [UniProtKB: P08173]
ChEMBL Binding affinity towards human muscarinic receptor B 6.26 pKi 550 nM Ki J. Med. Chem. (2004) 47: 1303-1314 [PMID:14998318]
5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL214] [GtoPdb: 1] [UniProtKB: P08908]
ChEMBL Binding affinity towards human 5-hydroxytryptamine 1 receptor B 6.48 pKi 330 nM Ki J. Med. Chem. (2001) 44: 477-501 [PMID:11170639]
GtoPdb - - 6.5 pKi - - - Psychopharmacology (Berl.) (1996) 124: 57-73 [PMID:8935801]
5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223]
ChEMBL Binding affinity for human 5-hydroxytryptamine 2A receptor B 8.57 pKi 2.7 nM Ki J. Med. Chem. (2001) 44: 477-501 [PMID:11170639]
GtoPdb - - 8.6 pKi - - - Psychopharmacology (Berl.) (1996) 124: 57-73 [PMID:8935801]
ChEMBL Binding affinity towards human serotonin 5-hydroxytryptamine 2A receptor B 9.04 pKi 0.91 nM Ki J. Med. Chem. (2004) 47: 1303-1314 [PMID:14998318]
ChEMBL Antagonist activity at 5HT2A receptor F 9.3 pKi 0.5 nM Ki Bioorg. Med. Chem. (2009) 17: 7802-7815 [PMID:19836247]
5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL225] [GtoPdb: 8] [UniProtKB: P28335]
ChEMBL Binding affinity towards human serotonin 5-hydroxytryptamine 2C receptor B 8.54 pKi 2.9 nM Ki J. Med. Chem. (2004) 47: 1303-1314 [PMID:14998318]
GtoPdb - - 8.6 pKi - - - J Pharmacol Exp Ther (2000) 295: 226-32 [PMID:10991983]
5-HT1B receptor in Human [GtoPdb: 2] [UniProtKB: P28222]
GtoPdb - - 7.2 pKi - - - Psychopharmacology (Berl.) (1996) 124: 57-73 [PMID:8935801]
5-HT1D receptor in Human [GtoPdb: 3] [UniProtKB: P28221]
GtoPdb - - 9.3 pKi - - - Psychopharmacology (Berl.) (1996) 124: 57-73 [PMID:8935801]
5-ht1e receptor in Human [GtoPdb: 4] [UniProtKB: P28566]
GtoPdb - - 6.5 pKi - - - Psychopharmacology (Berl.) (1996) 124: 57-73 [PMID:8935801]
5-HT6 receptor in Human [GtoPdb: 11] [UniProtKB: P50406]
GtoPdb - - 8.3 pKi - - - Psychopharmacology (Berl.) (2005) 179: 461-9 [PMID:15821958]
5-HT6 receptor in Rat [GtoPdb: 11] [UniProtKB: P31388]
GtoPdb - - 8.9 pKi - - - J Pharmacol Exp Ther (1994) 268: 1403-10 [PMID:7908055]
5-HT7 receptor in Human [GtoPdb: 12] [UniProtKB: P34969]
GtoPdb - - 8.4 pKi - - - Psychopharmacology (Berl.) (2005) 179: 461-9 [PMID:15821958]
5-HT7 receptor in Rat [GtoPdb: 12] [UniProtKB: P32305]
GtoPdb - - 8.8 pKi - - - J Pharmacol Exp Ther (1994) 268: 1403-10 [PMID:7908055]
α2B-adrenoceptor in Human [GtoPdb: 26] [UniProtKB: P18089]
GtoPdb - - 8.2 pKi 5.7 nM Ki Psychopharmacology (Berl.) (1996) 124: 57-73 [PMID:8935801]
NET in Human [GtoPdb: 926] [UniProtKB: P23975]
GtoPdb - - 7.15 pIC50 71 nM IC50 J Pharmacol Exp Ther (2010) 333: 772-81 [PMID:20223878]
SERT in Human [GtoPdb: 928] [UniProtKB: P31645]
GtoPdb - - 5.14 pIC50 7270 nM IC50 J Pharmacol Exp Ther (2010) 333: 772-81 [PMID:20223878]

ChEMBL data shown on this page come from version 28:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]