4α-PDD [Ligand Id: 2500] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL118987 (4Alpha-Phorbol-Didecanoate)
  • TRPV4 in Human [GtoPdb: 510] [UniProtKB: Q9HBA0]
  • 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 in Human [GtoPdb: 510] [UniProtKB: Q9HBA0]
GtoPdb - - 6.5 pEC50 - - - Br J Pharmacol (2003) 140: 413-21 [PMID:12970074]
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 Y556A mutant expressed in HEK293 cells assessed as increase in intracellular calcium concentration B 5.2 pEC50 6300 nM EC50 J Med Chem (2009) 52: 2933-2939 [PMID:19361196]
ChEMBL Activation of mouse TRPV4 W586A mutant expressed in HEK293 cells assessed as increase in intracellular calcium concentration B 5.22 pEC50 >6000 nM EC50 J Med Chem (2009) 52: 2933-2939 [PMID:19361196]
ChEMBL Activation of mouse wild type TRPV4 expressed in HEK293 cells assessed as increase in intracellular calcium concentration B 6.43 pEC50 370 nM EC50 J Med Chem (2009) 52: 2933-2939 [PMID:19361196]
ChEMBL Agonist activity at mouse TRPV4 B 6.43 pEC50 370 nM EC50 Bioorg Med Chem Lett (2020) 30: 127022-127022 [PMID:32063431]
ChEMBL Activation of mouse TRPV4 S557A mutant expressed in HEK293 cells assessed as increase in intracellular calcium concentration B 6.49 pEC50 320 nM EC50 J Med Chem (2009) 52: 2933-2939 [PMID:19361196]
GtoPdb - - 6.7 pEC50 - - - J Biol Chem (2002) 277: 13569-77 [PMID:11827975]

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]