asenapine [Ligand Id: 22] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL504548 |
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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 | Displacement of [3H]SCH-23390 from human cloned D1 dopamine receptor expressed in HEKT cells incubated for 90 mins by scintillation counting based radioligand binding assay | B | 8.05 | pKi | 8.9 | nM | Ki | Medchemcomm (2015) 6: 1679-1686 |
| D2 receptor/Dopamine D2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416] | ||||||||
| ChEMBL | Displacement of [3H]N-methylspiperone from human cloned D2 dopamine receptor expressed in human fibroblasts incubated for 90 mins by scintillation counting based radioligand binding assay | B | 8.05 | pKi | 8.9 | nM | Ki | Medchemcomm (2015) 6: 1679-1686 |
| GtoPdb | - | - | 8.92 | pKi | 1.2 | nM | Ki | J Psychopharmacol (Oxford) (2009) 23: 65-73 [PMID:18308814] |
| D3 receptor/Dopamine D3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL234] [GtoPdb: 216] [UniProtKB: P35462] | ||||||||
| ChEMBL | Displacement of [3H]N-methylspiperone from human cloned D3 dopamine receptor expressed in HEKT cells incubated for 90 mins by scintillation counting based radioligand binding assay | B | 8.03 | pKi | 9.4 | nM | Ki | Medchemcomm (2015) 6: 1679-1686 |
| D4 receptor/Dopamine D4 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL219] [GtoPdb: 217] [UniProtKB: P21917] | ||||||||
| ChEMBL | Displacement of [3H]N-methylspiperone from human D4 dopamine receptor incubated for 90 mins by scintillation counting based radioligand binding assay | B | 8.05 | pKi | 9 | nM | Ki | Medchemcomm (2015) 6: 1679-1686 |
| H1 receptor/Histamine H1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL231] [GtoPdb: 262] [UniProtKB: P35367] | ||||||||
| ChEMBL | Binding affinity to H1 histamine receptor (unknown origin) | B | 9 | pKi | 1 | nM | Ki | Bioorg Med Chem Lett (2021) 31: 127681-127681 [PMID:33189775] |
| GtoPdb | - | - | 9.8 | pKi | - | - | - | Psychopharmacology (Berl.) (1996) 124: 57-73 [PMID:8935801] |
| 5-HT1A receptor in Human [GtoPdb: 1] [UniProtKB: P08908] | ||||||||
| GtoPdb | - | - | 8.3 | pKi | - | - | - |
Eur J Pharmacol (1998) 355: 245-56 [PMID:9760039]; Psychopharmacology (Berl.) (1996) 124: 57-73 [PMID:8935801] |
| 5-HT1B receptor in Human [GtoPdb: 2] [UniProtKB: P28222] | ||||||||
| GtoPdb | - | - | 8.1 | pKi | - | - | - | Psychopharmacology (Berl.) (1996) 124: 57-73 [PMID:8935801] |
| 5-HT1D receptor in Human [GtoPdb: 3] [UniProtKB: P28221] | ||||||||
| GtoPdb | - | - | 8.4 | pKi | - | - | - | Psychopharmacology (Berl.) (1996) 124: 57-73 [PMID:8935801] |
| 5-ht1e receptor in Human [GtoPdb: 4] [UniProtKB: P28566] | ||||||||
| GtoPdb | - | - | 8 | pKi | - | - | - | Psychopharmacology (Berl.) (1996) 124: 57-73 [PMID:8935801] |
| 5-HT2A receptor in Human [GtoPdb: 6] [UniProtKB: P28223] | ||||||||
| GtoPdb | - | - | 10.22 | pKi | 0.06 | nM | Ki | J Psychopharmacol (Oxford) (2009) 23: 65-73 [PMID:18308814] |
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]
