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

Click here for a description of the charts and data table

Please tell us if you are using this feature and what you think!

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]
There should be some charts here, you may need to enable JavaScript!
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 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]