ChEMBL ligand: CHEMBL2133556

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] 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 Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3119] [GtoPdb: 510] [UniProtKB: Q9HBA0]
ChEMBL	Antagonist activity at human TRPV4	B	6.69	pIC50	202.9	nM	IC50	Eur J Med Chem (2023) 249: 115137-115137 [PMID:36696767]
ChEMBL	Antagonist activity at TRPV4 (unknown origin) expressed in Flp-In-CHO cells assessed as inhibition of GSK1016790A induced Ca2+ influx by calcium imaging method	B	7.13	pIC50	73.58	nM	IC50	Eur J Med Chem (2023) 249: 115137-115137 [PMID:36696767]
ChEMBL	Antagonist activity at recombinant human TRPV4 expressed in CHOK1 cells assessed as inhibition of 4alphaPDD-induced activation pretreated for 5 mins followed by 4alphaPDD stimulation measured for 5 mins by FLIPR assay	B	7.24	pIC50	57	nM	IC50	Bioorg Med Chem (2017) 25: 2177-2190 [PMID:28284871]
ChEMBL	Antagonist activity at human TRPV4 assessed as inhibition of 4alpha-PDD-induced activation	B	7.24	pIC50	57	nM	IC50	Bioorg Med Chem Lett (2016) 26: 4936-4941 [PMID:27634196]
ChEMBL	Antagonist activity at human recombinant TRPV4 expressed in CHO-K1 cells assessed as blockade of 1000 nM 4alphaPDD-induced calcium mobilization by FLIPR assay	B	7.24	pIC50	57	nM	IC50	Bioorg Med Chem Lett (2016) 26: 4930-4935 [PMID:27637151]
GtoPdb	-	-	7.3	pIC50	48	nM	IC50	Proc Natl Acad Sci USA (2010) 107: 19084-9 [PMID:20956320]
ChEMBL	Antagonist activity at TRPV4 (unknown origin)	B	7.32	pIC50	48	nM	IC50	Bioorg Med Chem Lett (2020) 30: 127022-127022 [PMID:32063431]
ChEMBL	Antagonist activity at human TRPV4 expressed in HEK293 cells assessed as inhibition of 4alpha-PDD-induced current at holding potential of -40 mV by Whole cell patch-clamp method	B	7.32	pIC50	48	nM	IC50	ACS Med Chem Lett (2017) 8: 549-554 [PMID:28523109]
ChEMBL	Antagonist activity at recombinant human TRPV4 expressed in CHOK1 cells assessed as inhibition of hypotonicity-induced activation pretreated for 5 mins followed by hypotonic solution addition measured for 5 mins by FLIPR assay	B	7.54	pIC50	29	nM	IC50	Bioorg Med Chem (2017) 25: 2177-2190 [PMID:28284871]
ChEMBL	Antagonist activity at human TRPV4	B	7.74	pIC50	18	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]
ChEMBL	Antagonist activity at mouse TRPV4 expressed in HEK293 cells assessed as inhibition of 4alpha-PDD-induced current at holding potential of -40 mV by Whole cell patch-clamp method	B	7.77	pIC50	17	nM	IC50	ACS Med Chem Lett (2017) 8: 549-554 [PMID:28523109]
ChEMBL	Antagonist activity at mouse TRPV4	B	7.77	pIC50	17	nM	IC50	Bioorg Med Chem (2020) 28: 115609-115609 [PMID:32690264]
GtoPdb	-	-	7.8	pIC50	-	-	-	Proc Natl Acad Sci USA (2010) 107: 19084-9 [PMID:20956320]
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 recombinant rat TRPV4 expressed in CHOK1 cells assessed as inhibition of 4alphaPDD-induced activation pretreated for 5 mins followed by 4alphaPDD stimulation measured for 5 mins by FLIPR assay	B	6.74	pIC50	180	nM	IC50	Bioorg Med Chem (2017) 25: 2177-2190 [PMID:28284871]
ChEMBL	Antagonist activity at rat TRPV4 expressed in HEK293 cells assessed as inhibition of 4alpha-PDD-induced current at holding potential of -40 mV by Whole cell patch-clamp method	B	6.88	pIC50	133	nM	IC50	ACS Med Chem Lett (2017) 8: 549-554 [PMID:28523109]
ChEMBL	Antagonist activity at rat TRPV4	B	6.88	pIC50	133	nM	IC50	Bioorg Med Chem (2020) 28: 115609-115609 [PMID:32690264]
GtoPdb	-	-	6.9	pIC50	-	-	-	Proc Natl Acad Sci USA (2010) 107: 19084-9 [PMID:20956320]

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]