prucalopride [Ligand Id: 243] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL117287 (Prucalopride, R093877, R-093877, Resolor)
  • 5-HT3A/Serotonin 3a (5-HT3a) receptor in Human [ChEMBL: CHEMBL1899] [GtoPdb: 373] [UniProtKB: P46098]
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  • 5-HT4 receptor/Serotonin 4 (5-HT4) receptor in Human [ChEMBL: CHEMBL1875] [GtoPdb: 9] [UniProtKB: Q13639]
  • 5-HT4 receptor/Serotonin 4 (5-HT4) receptor in Rat [ChEMBL: CHEMBL4317] [GtoPdb: 9] [UniProtKB: Q62758]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
5-HT3A/Serotonin 3a (5-HT3a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1899] [GtoPdb: 373] [UniProtKB: P46098]
ChEMBL Binding affinity at 5HT3 receptor B 5.4 pKi 3981.07 nM Ki Bioorg. Med. Chem. (2009) 17: 2607-2622 [PMID:19261477]
5-HT4 receptor/Serotonin 4 (5-HT4) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1875] [GtoPdb: 9] [UniProtKB: Q13639]
ChEMBL Tested for selectivity for 5-hydroxytryptamine 4 receptor B 6 pKi >1000 nM Ki J. Med. Chem. (2003) 46: 319-344 [PMID:12540230]
ChEMBL Tested for selectivity for 5-hydroxytryptamine 4 receptor B 6 pKi >1000 nM Ki J. Med. Chem. (2003) 46: 319-344 [PMID:12540230]
ChEMBL Tested for selectivity for 5-hydroxytryptamine 4 receptor B 6.96 pKi 110 nM Ki J. Med. Chem. (2003) 46: 319-344 [PMID:12540230]
ChEMBL Tested for agonist activity against 5-hydroxytryptamine 4 receptor F 8.12 pKi 7.5 nM Ki J. Med. Chem. (2003) 46: 319-344 [PMID:12540230]
ChEMBL Binding affinity at 5HT4 receptor B 8.6 pKi 2.51 nM Ki Bioorg. Med. Chem. (2009) 17: 2607-2622 [PMID:19261477]
GtoPdb - - 8.6 pKi - - - J Neurochem (2000) 74: 478-89 [PMID:10646498];
Eur J Pharmacol (2001) 423: 71-83 [PMID:11438309]
ChEMBL Agonist activity at 5-HT4E receptor (unknown origin) B 7.59 pEC50 26 nM EC50 J Med Chem (2018) 61: 4993-5008 [PMID:29763304]
ChEMBL Agonist activity at human 5HT4e receptor expressed in CHO cells assessed as cAMP level after 4 hrs by luciferase reporter gene assay F 8.28 pEC50 5.2 nM EC50 Eur. J. Med. Chem. (2015) 103: 289-301 [PMID:26363507]
ChEMBL Agonist activity at recombinant human 5-HT4E receptor expressed in CHO cells assessed as induction of c-AMP accumulation after 4 hrs by luciferase reporter assay B 8.28 pEC50 5.2 nM EC50 J Med Chem (2018) 61: 4993-5008 [PMID:29763304]
5-HT4 receptor/Serotonin 4 (5-HT4) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4317] [GtoPdb: 9] [UniProtKB: Q62758]
ChEMBL Agonist activity at rat 5HT4e receptor expressed in HEK293 cells assessed as cAMP level after 30 mins by HTRF assay F 7.59 pEC50 26 nM EC50 Eur. J. Med. Chem. (2015) 103: 289-301 [PMID:26363507]

ChEMBL data shown on this page come from version 31:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, Cibrián-Uhalte E, Davies M, Dedman N, Karlsson A, Magariños 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]