asenapine [Ligand Id: 22] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL504548
  • 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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  • 5-HT1A receptor in Human [GtoPdb: 1] [UniProtKB: P08908]
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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-HT2A receptor in Human [GtoPdb: 6] [UniProtKB: P28223]
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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 32:

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]