ChEMBL ligand: CHEMBL3613642
TRPM8/Transient receptor potential cation channel subfamily M member 8 in Human [ChEMBL: CHEMBL1075319] [GtoPdb: 500] [UniProtKB: Q7Z2W7] There should be some charts here, you may need to enable JavaScript!
TRPV3/Transient receptor potential cation channel subfamily V member 3 in Human [ChEMBL: CHEMBL5522] [GtoPdb: 509] [UniProtKB: Q8NET8] There should be some charts here, you may need to enable JavaScript!
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!
TRPV1/Vanilloid receptor in Human [ChEMBL: CHEMBL4794] [GtoPdb: 507] [UniProtKB: Q8NER1] 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
TRPM8/Transient receptor potential cation channel subfamily M member 8 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1075319] [GtoPdb: 500] [UniProtKB: Q7Z2W7]
ChEMBL	Antagonist activity at human TRPM8 receptor expressed in HEK293 cells assessed as inhibition of menthol-stimulated calcium flux after 10 mins	B	4.52	pIC50	30000	nM	IC50	Bioorg Med Chem Lett (2015) 25: 4011-4015 [PMID:26235950]
TRPV3/Transient receptor potential cation channel subfamily V member 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5522] [GtoPdb: 509] [UniProtKB: Q8NET8]
ChEMBL	Antagonist activity at human TRPV3 receptor expressed in HEK293 cells assessed as inhibition of capsaicin-stimulated calcium flux after 10 mins	B	4.52	pIC50	>30000	nM	IC50	Bioorg Med Chem Lett (2015) 25: 4011-4015 [PMID:26235950]
TRPV4/Transient receptor potential cation channel subfamily V member 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3119] [GtoPdb: 510] [UniProtKB: Q9HBA0]
GtoPdb	-	-	6.2	pIC50	-	-	-	Bioorg Med Chem Lett (2015) 25: 4011-5 [PMID:26235950]
ChEMBL	Antagonist activity at human TRPV4 expressed in HEK293 cells assessed as inhibition of 20% hypotonic solution-induced Ca2+ influx	B	6.24	pIC50	570	nM	IC50	Bioorg Med Chem Lett (2015) 25: 4011-4015 [PMID:26235950]
ChEMBL	Antagonist activity at human TRPV4 receptor expressed in HEK293 cells assessed as inhibition of EC80 of 4alpha-PDD-stimulated calcium flux after 10 mins	B	6.38	pIC50	420	nM	IC50	Bioorg Med Chem Lett (2015) 25: 4011-4015 [PMID:26235950]
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 receptor expressed in HEK293 cells assessed as inhibition of EC80 of 4alpha-PDD-stimulated calcium flux after 10 mins	B	6.49	pIC50	320	nM	IC50	Bioorg Med Chem Lett (2015) 25: 4011-4015 [PMID:26235950]
GtoPdb	-	-	6.5	pIC50	-	-	-	Bioorg Med Chem Lett (2015) 25: 4011-5 [PMID:26235950]
ChEMBL	Antagonist activity at mouse TRPV4 receptor expressed in HEK293 cells assessed as inhibition of 4alpha-PDD-stimulated calcium flux after 10 mins	B	7.24	pIC50	57	nM	IC50	Bioorg Med Chem Lett (2015) 25: 4011-4015 [PMID:26235950]
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 20% hypotonic solution-induced Ca2+ influx	B	5.68	pIC50	2100	nM	IC50	Bioorg Med Chem Lett (2015) 25: 4011-4015 [PMID:26235950]
ChEMBL	Antagonist activity at rat TRPV4 receptor expressed in HEK293 cells assessed as inhibition of EC80 of 4alpha-PDD-stimulated calcium flux after 10 mins	B	6.18	pIC50	660	nM	IC50	Bioorg Med Chem Lett (2015) 25: 4011-4015 [PMID:26235950]
ChEMBL	Antagonist activity at rat TRPV4 receptor expressed in HEK293 cells assessed as inhibition of 4alpha-PDD-stimulated calcium flux after 10 mins	B	6.92	pIC50	120	nM	IC50	Bioorg Med Chem Lett (2015) 25: 4011-4015 [PMID:26235950]
TRPV1/Vanilloid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4794] [GtoPdb: 507] [UniProtKB: Q8NER1]
ChEMBL	Antagonist activity at human TRPV1 receptor expressed in HEK293 cells assessed as inhibition of capsaicin-stimulated calcium flux after 10 mins	B	5	pIC50	>10000	nM	IC50	Bioorg Med Chem Lett (2015) 25: 4011-4015 [PMID:26235950]

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]