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 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]