4α-PDH [Ligand Id: 4105] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL490470 (4Alpha-Phorbol 12,13-Dihexanoate)
  • TRPV4/Transient receptor potential cation channel subfamily V member 4 in Mouse [ChEMBL: CHEMBL6126] [GtoPdb: 510] [UniProtKB: Q9EPK8]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
TRPV4/Transient receptor potential cation channel subfamily V member 4 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6126] [GtoPdb: 510] [UniProtKB: Q9EPK8]
ChEMBL Activation of mouse TRPV4 W586A mutant expressed in HEK293 cells assessed as increase in intracellular calcium concentration B 5.55 pEC50 2840 nM EC50 J Med Chem (2009) 52: 2933-2939 [PMID:19361196]
ChEMBL Activation of mouse TRPV4 Y556A mutant expressed in HEK293 cells assessed as increase in intracellular calcium concentration B 5.55 pEC50 2790 nM EC50 J Med Chem (2009) 52: 2933-2939 [PMID:19361196]
ChEMBL Activation of mouse TRPV4 S557A mutant expressed in HEK293 cells assessed as increase in intracellular calcium concentration B 6.44 pEC50 360 nM EC50 J Med Chem (2009) 52: 2933-2939 [PMID:19361196]
GtoPdb - - 7.1 pEC50 79.4 nM EC50 J Med Chem (2009) 52: 2933-9 [PMID:19361196]
ChEMBL Activation of mouse wild type TRPV4 expressed in HEK293 cells assessed as increase in intracellular calcium concentration B 7.15 pEC50 70 nM EC50 J Med Chem (2009) 52: 2933-2939 [PMID:19361196]

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]