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Assay Detail

CHEMBL3616044

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Antagonist activity at human TRPM8 receptor expressed in HEK293 cells assessed as inhibition of menthol-stimulated calcium flux after 10 mins
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Publication

Identification of orally-bioavailable antagonists of the TRPV4 ion-channel.
Wei ZL, Nguyen MT, O'Mahony DJ, Acevedo A, Zipfel S, Zhang Q, Liu L, Dourado M, Chi C, Yip V, DeFalco J, Gustafson A, Emerling DE, Kelly MG, Kincaid J, Vincent F, Duncton MA.
Bioorg Med Chem Lett (2015) 25 : 4011 -4015
PubMed 26235950 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 4.52 4.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3613642 1 4.52

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3613642 IC50 = 30000.0 nM 4.52