RS 39604 [Ligand Id: 254] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL83954 (RS-23597-190)
  • 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]
  • Serotonin 4 (5-HT4) receptor in Guinea pig [ChEMBL: CHEMBL5017] [UniProtKB: O70528]
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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 5.7 pKi 1995.26 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 Binding affinity at 5HT4 receptor B 7.5 pKi 31.62 nM Ki Bioorg. Med. Chem. (2009) 17: 2607-2622 [PMID:19261477]
GtoPdb - - 8.7 pKi - - - Br J Pharmacol (2000) 129: 771-81 [PMID:10683202];
Br J Pharmacol (2000) 131: 827-35 [PMID:11030734];
Br J Pharmacol (2004) 143: 361-70 [PMID:15351779]
5-HT4 receptor/Serotonin 4 (5-HT4) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4317] [GtoPdb: 9] [UniProtKB: Q62758]
ChEMBL Binding affinity towards 5-hydroxytryptamine 4 receptor was determined in rat striatal membranes using [3H]GR-113808 as radioligand B 7.55 pKi 28.1 nM Ki J. Med. Chem. (1997) 40: 608-621 [PMID:9046352]
Serotonin 4 (5-HT4) receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5017] [UniProtKB: O70528]
ChEMBL Displacement of [3H]GR113808 from serotonin 5-HT4 receptor in Dunkin-Hartley guinea pigs striatal nuclei membranes incubated for 2 hrs by liquid scintillation counting B 7.72 pKi 19 nM Ki MedChemComm (2017) 8: 647-651 [PMID:30108781]
ChEMBL Displacement of [3H]-GR113808 from 5-HT4R in Dunkin-Hartley guinea pig straitum nuclear membranes after 2 hrs by filter binding method B 7.72 pKi 19 nM Ki MedChemComm (2018) 9: 1466-1471 [PMID:30288221]
ChEMBL 5-hydroxytryptamine 4 receptor agonist activity, concentration which gave 50% increase in the response to electrically-stimulated myenteric plexus and longitudinal muscle of the guinea pig ileum F 7.52 pEC50 30 nM EC50 J. Med. Chem. (1997) 40: 608-621 [PMID:9046352]

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]