RN1734 [Ligand Id: 4294] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL2324347
  • TRPV4/Transient receptor potential cation channel subfamily V member 4 in Human [ChEMBL: CHEMBL3119] [GtoPdb: 510] [UniProtKB: Q9HBA0]
  • TRPV4/Transient receptor potential cation channel subfamily V member 4 in Mouse [ChEMBL: CHEMBL6126] [GtoPdb: 510] [UniProtKB: Q9EPK8]
  • TRPV4/Transient receptor potential cation channel subfamily V member 4 in Rat [ChEMBL: CHEMBL2775] [GtoPdb: 510] [UniProtKB: Q9ERZ8]
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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 Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3119] [GtoPdb: 510] [UniProtKB: Q9HBA0]
GtoPdb - - 5.6 pIC50 2300 nM IC50 Biochem Biophys Res Commun (2009) 389: 490-4 [PMID:19737537]
ChEMBL Inhibition of TRPV4 (unknown origin) B 5.64 pIC50 2300 nM IC50 J Med Chem (2013) 56: 593-624 [PMID:23121096]
ChEMBL Antagonist activity at human TRPV4 expressed in HEK293 cells assessed as inhibition of 4alpha-PDD-induced intracellular calcium after 10 mins in presence of 45Ca2+ by microbeta liquid scintillation counting method B 5.64 pIC50 2300 nM IC50 ACS Med Chem Lett (2017) 8: 549-554 [PMID:28523109]
ChEMBL Antagonist activity at TRPV4 (unknown origin) B 5.64 pIC50 2300 nM IC50 Bioorg Med Chem Lett (2020) 30: 127022-127022 [PMID:32063431]
ChEMBL Antagonist activity at human TRPV4 B 5.64 pIC50 2300 nM IC50 Bioorg Med Chem (2020) 28: 115609-115609 [PMID:32690264]
TRPV4/Transient receptor potential cation channel subfamily V member 4 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6126] [GtoPdb: 510] [UniProtKB: Q9EPK8]
GtoPdb - - 5.2 pIC50 - - - Biochem Biophys Res Commun (2009) 389: 490-4 [PMID:19737537]
ChEMBL Antagonist activity at mouse TRPV4 expressed in HEK293 cells assessed as inhibition of 4alpha-PDD-induced intracellular calcium after 10 mins in presence of 45Ca2+ by microbeta liquid scintillation counting method B 5.23 pIC50 5900 nM IC50 ACS Med Chem Lett (2017) 8: 549-554 [PMID:28523109]
ChEMBL Antagonist activity at mouse TRPV4 B 5.23 pIC50 5900 nM IC50 Bioorg Med Chem (2020) 28: 115609-115609 [PMID:32690264]
TRPV4/Transient receptor potential cation channel subfamily V member 4 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2775] [GtoPdb: 510] [UniProtKB: Q9ERZ8]
ChEMBL Antagonist activity at rat TRPV4 expressed in HEK293 cells assessed as inhibition of 4alpha-PDD-induced intracellular calcium after 10 mins in presence of 45Ca2+ by microbeta liquid scintillation counting method B 5.49 pIC50 3200 nM IC50 ACS Med Chem Lett (2017) 8: 549-554 [PMID:28523109]
ChEMBL Antagonist activity at rat TRPV4 B 5.49 pIC50 3200 nM IC50 Bioorg Med Chem (2020) 28: 115609-115609 [PMID:32690264]
GtoPdb - - 5.5 pIC50 - - - Biochem Biophys Res Commun (2009) 389: 490-4 [PMID:19737537]

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]