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

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ChEMBL ligand: CHEMBL243712 (Solian 50, APD421, APD-421, Barhemsys, Solian, Solian 100, Amisulpride, Solian 200, Solian 400, DAN-2163)
  • D2 receptor/Dopamine D2 receptor in Human [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416]
  • 7.9
1 CHEMBL243712_lig_chart_1 Dopamine D2 receptor Human
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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]
  • 7.4
2 CHEMBL243712_lig_chart_2 Dopamine D3 receptor HumanRat
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  • 5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Human [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223]
  • This target only has 1 pki data point
  • 6.2
3 CHEMBL243712_lig_chart_3 Serotonin 2a (5-HT2a) receptor Human
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  • 5-HT2B receptor/Serotonin 2b (5-HT2b) receptor in Human [ChEMBL: CHEMBL1833] [GtoPdb: 7] [UniProtKB: P41595]
  • This target only has 1 pki data point
  • 6.5
4 CHEMBL243712_lig_chart_4 Serotonin 2b (5-HT2b) receptor Human
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  • 5-HT7 receptor/Serotonin 7 (5-HT7) receptor in Human [ChEMBL: CHEMBL3155] [GtoPdb: 12] [UniProtKB: P34969]
  • This target only has 1 pki data point
  • 7.6
5 CHEMBL243712_lig_chart_5 Serotonin 7 (5-HT7) receptor Human
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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 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 B 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]
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 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]