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Assay Detail

CHEMBL3412243

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Binding
Antagonist activity at human TRPV1 expressed in CHO cells assessed as inhibition of pH-induced activity by FLIPR assay
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Publication

Pyridine C-region analogs of 2-(3-fluoro-4-methylsulfonylaminophenyl)propanamides as potent TRPV1 antagonists.
Ryu H, Seo S, Lee JY, Ha TH, Lee S, Jung A, Ann J, Kim SE, Yoon S, Hong M, Blumberg PM, Frank-Foltyn R, Bahrenberg G, Schiene K, Stockhausen H, Christoph T, Frormann S, Lee J.
Eur J Med Chem (2015) 93 : 101 -108
PubMed 25659771 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 7.87 8.08

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3407762 1 8.08
CHEMBL2177428 1 7.80
CHEMBL3407765 1 7.73

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3407762 IC50 = 8.3 nM 8.08
CHEMBL2177428 IC50 = 15.8 nM 7.80
CHEMBL3407765 IC50 = 18.5 nM 7.73