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Assay Detail

CHEMBL4178993

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

Binding
Antagonist activity at rat TRPV1 expressed in CHO cells assessed as inhibition of capsaicin-induced intracellular calcium level preincubated for 6 mins followed by capsaicin addition by Fluo-4 dye based FLIPR assay
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Cell Type CHO
Confidence 9 — Direct single protein target
Curated By Autocuration

Publication

Pyrazole C-region analogues of 2-(3-fluoro-4-methylsulfonylaminophenyl)propanamides as potent TRPV1 antagonists.
Lee S, Kim C, Ann J, Thorat SA, Kim E, Park J, Choi S, Blumberg PM, Frank-Foltyn R, Bahrenberg G, Stockhausen H, Christoph T, Lee J.
Bioorg Med Chem Lett (2017) 27 : 4383 -4388
PubMed 28838698 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 2 10.00 10.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3689037 1 10.00
CHEMBL3689046 1 10.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3689037 Ki = 0.1 nM 10.00
CHEMBL3689046 Ki = 0.1 nM 10.00