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Assay Detail

CHEMBL4322959

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

Binding
Antagonist activity at human TRPV4 channel transfected in HEK cells assessed as inhibition of GSK634775-evoked Ca2+ influx by FLIPR method
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Publication

Discovery of GSK3527497: A Candidate for the Inhibition of Transient Receptor Potential Vanilloid-4 (TRPV4).
Brooks CA, Barton LS, Behm DJ, Brnardic EJ, Costell MH, Holt DA, Jolivette LJ, Matthews JM, McAtee JJ, McCleland BW, Patterson JR, Pero JE, Rivero RA, Roethke TJ, Sanchez RM, Shenje R, Terrell LR, Lawhorn BG.
J Med Chem (2019) 62 : 9270 -9280
PubMed 31532662 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 7.40 7.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4073922 1 7.40

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4073922 IC50 = 40.0 nM 7.40