zotepine [Ligand Id: 103] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL285802 (Nipolept, Setous, Zoleptil 100, Zoleptil 25, Zoleptil 50, Zotepin, Zotepine) |
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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 33:
Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
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]
