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 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 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]
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]
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 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]