PF-04995274 [Ligand Id: 9059] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL2152922 (Pf-04995274)
  • 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-HT4 receptor/Serotonin 4 (5-HT4) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1875] [GtoPdb: 9] [UniProtKB: Q13639]
ChEMBL Displacement of [3H]GR113808 from human 5HT4B receptor expressed in HEK293 cells after 30 mins by liquid scintillation counting B 9.34 pKi 0.46 nM Ki J Med Chem (2012) 55: 9240-9254 [PMID:22974325]
ChEMBL Displacement of [3H]GR113808 from human 5HT4A receptor expressed in HEK293 cells after 30 mins by liquid scintillation counting B 9.44 pKi 0.36 nM Ki J Med Chem (2012) 55: 9240-9254 [PMID:22974325]
ChEMBL Displacement of [3H]GR113808 from human 5HT4E receptor expressed in CHO cells after 30 mins by liquid scintillation counting B 9.49 pKi 0.32 nM Ki J Med Chem (2012) 55: 9240-9254 [PMID:22974325]
GtoPdb Measured at the 5-HT4d receptor. - 9.82 pKi 0.15 nM Ki J Med Chem (2012) 55: 9240-54 [PMID:22974325]
ChEMBL Displacement of [3H]GR113808 from human 5HT4D receptor expressed in HEK293 cells after 30 mins by liquid scintillation counting B 9.82 pKi 0.15 nM Ki J Med Chem (2012) 55: 9240-9254 [PMID:22974325]
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 8.82 pEC50 1.5 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 8.89 pEC50 1.3 nM EC50 Eur J Med Chem (2015) 103: 289-301 [PMID:26363507]
ChEMBL Agonist activity at human 5HT4A receptor expressed in HEK293 cells assessed as increase in cAMP production after 30 mins by HTRF assay F 9.33 pEC50 0.47 nM EC50 J Med Chem (2012) 55: 9240-9254 [PMID:22974325]
ChEMBL Agonist activity at human 5HT4B receptor expressed in HEK293 cells assessed as increase in cAMP production after 30 mins by HTRF assay F 9.44 pEC50 0.36 nM EC50 J Med Chem (2012) 55: 9240-9254 [PMID:22974325]
ChEMBL Agonist activity at 5-HT4E receptor (unknown origin) B 9.59 pEC50 0.26 nM EC50 J Med Chem (2018) 61: 4993-5008 [PMID:29763304]
ChEMBL Agonist activity at human 5HT4E receptor expressed in HEK293 cells assessed as increase in cAMP production after 30 mins by HTRF assay F 9.59 pEC50 0.26 nM EC50 J Med Chem (2012) 55: 9240-9254 [PMID:22974325]
ChEMBL Partial agonist activity at human 5HT4D receptor expressed in HEK293 cells assessed as cAMP production after 30 mins by HTRF assay F 9.7 pEC50 0.2 nM EC50 J Med Chem (2012) 55: 9240-9254 [PMID:22974325]
5-HT4 receptor/Serotonin 4 (5-HT4) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4317] [GtoPdb: 9] [UniProtKB: Q62758]
ChEMBL Displacement of [3H]GR113808 from 5HT4 receptor in rat striatal membrane after 30 mins by liquid scintillation counting B 9.52 pKi 0.3 nM Ki J Med Chem (2012) 55: 9240-9254 [PMID:22974325]
ChEMBL Agonist activity at rat 5HT4L receptor expressed in HEK293 cells assessed as increase in cAMP production after 30 mins by HTRF assay F 9.19 pEC50 0.65 nM EC50 J Med Chem (2012) 55: 9240-9254 [PMID:22974325]
ChEMBL Agonist activity at rat 5HT4E receptor expressed in HEK293 cells assessed as increase in cAMP production after 30 mins by HTRF assay F 9.21 pEC50 0.62 nM EC50 J Med Chem (2012) 55: 9240-9254 [PMID:22974325]
ChEMBL Agonist activity at rat 5HT4S receptor expressed in HEK293 cells assessed as increase in cAMP production after 30 mins by HTRF assay F 9.23 pEC50 0.59 nM EC50 J Med Chem (2012) 55: 9240-9254 [PMID:22974325]

ChEMBL data shown on this page come from version 33:

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]