amisulpride [Ligand Id: 963] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL243712 (Aminosultopride, Amisulpride, APD-421, APD421, Barhemsys, DAN-2163, Deniban, NSC-760085, Socian, Solian, Solian 100, Solian 200, Solian 400, Solian 50, Sulamid)
  • 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]
  • D3 receptor in Rat [GtoPdb: 216] [UniProtKB: P19020]
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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-HT2B receptor/Serotonin 2b (5-HT2b) receptor in Human [ChEMBL: CHEMBL1833] [GtoPdb: 7] [UniProtKB: P41595]
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  • 5-HT7 receptor/Serotonin 7 (5-HT7) receptor in Human [ChEMBL: CHEMBL3155] [GtoPdb: 12] [UniProtKB: P34969]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
D2 receptor/Dopamine D2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416]
GtoPdb - - 7.8 pKi - - - Nature (1990) 347: 146-51 [PMID:1975644]
ChEMBL Displacement of [3H]spiperone from human dopamine D2 receptor short form expressed in CHO cells B 7.9 pKi 12.59 nM Ki J Med Chem (2007) 50: 5103-5108 [PMID:17880057]
GtoPdb - - 8 pKi - - - Eur J Pharmacol (1992) 225: 331-7 [PMID:1354163];
Mol Pharmacol (1993) 43: 749-54 [PMID:8099194]
ChEMBL Displacement of [3H]N-methyl-spiperone from D2R (unknown origin) assessed as inhibition constant by competition binding assay B 8.52 pKi 3 nM Ki Bioorg Med Chem Lett (2021) 49: 128275-128275 [PMID:34311086]
ChEMBL Antagonistic activity at D2 receptor (unknown origin) expressed in CHOK1 cells co-expressing G-alpha 15 assessed as inhibition of dopamine-induced calcium flux by fluo-4 dye based FLIPR assay F 8.52 pIC50 3.04 nM IC50 Eur J Med Chem (2016) 123: 332-353 [PMID:27487565]
D3 receptor/Dopamine D3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL234] [GtoPdb: 216] [UniProtKB: P35462]
ChEMBL Displacement of [3H]spiperone from human dopamine D3 receptor expressed in CHO cells B 8.4 pKi 3.98 nM Ki J Med Chem (2007) 50: 5103-5108 [PMID:17880057]
ChEMBL Displacement of [3H]N-methyl-spiperone from D3R (unknown origin) assessed as inhibition constant by competition binding assay B 8.46 pKi 3.5 nM Ki Bioorg Med Chem Lett (2021) 49: 128275-128275 [PMID:34311086]
D3 receptor in Rat [GtoPdb: 216] [UniProtKB: P19020]
GtoPdb - - 7.4 pKi - - - Nature (1990) 347: 146-51 [PMID:1975644]
5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223]
ChEMBL Displacement of [3H]ketanserin from human 5HT2A receptor expressed in CHO cells B 6.2 pKi 630.96 nM Ki J Med Chem (2007) 50: 5103-5108 [PMID:17880057]
5-HT2B receptor/Serotonin 2b (5-HT2b) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1833] [GtoPdb: 7] [UniProtKB: P41595]
ChEMBL Displacement of [3H]DOI from 5HT2B receptor expressed in CHO cells B 6.5 pKi 316.23 nM Ki J Med Chem (2007) 50: 5103-5108 [PMID:17880057]
5-HT7 receptor/Serotonin 7 (5-HT7) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3155] [GtoPdb: 12] [UniProtKB: P34969]
ChEMBL Displacement of [3H]LSD from human 5HT7 receptor expressed in CHO cells B 7.6 pKi 25.12 nM Ki J Med Chem (2007) 50: 5103-5108 [PMID:17880057]
ChEMBL Displacement of [3H]LSD from 5-HT7R (unknown origin) assessed as inhibition constant by competition binding assay B 7.94 pKi 11.5 nM Ki Bioorg Med Chem Lett (2021) 49: 128275-128275 [PMID:34311086]

ChEMBL data shown on this page come from version 34:

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]