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Assay Detail

CHEMBL4125103

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Binding
Antagonist activity at recombinant human TRPV1 expressed in CHOK1 cells assessed as reduction in temperature-induced Ca2+ flux after 15 mins at 45 degC by fluo-4-based FLIPR assay
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 2-(3,5-difluoro-4-methylsulfonaminophenyl)propanamides as potent TRPV1 antagonists.
Kim C, Ann J, Lee S, Sun W, Blumberg PM, Frank-Foltyn R, Bahrenberg G, Stockhausen H, Christoph T, Lee J.
Bioorg Med Chem Lett (2018) 28 : 2539 -2542
PubMed 29884534 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 8.09 8.09

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4125690 1 8.09

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4125690 IC50 = 8.1 nM 8.09