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Assay Detail

CHEMBL3630761

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Binding
Antagonist activity at human TRPV1 heterologously expressed in CHO cells assessed as inhibition of low 45 degC heat -induced activation
2
Total Activities
2
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

Structure activity relationships of benzyl C-region analogs of 2-(3-fluoro-4-methylsulfonamidophenyl)propanamides as potent TRPV1 antagonists.
Ann J, Jung A, Kim MY, Kim HM, Ryu H, Kim S, Kang DW, Hong S, Cui M, Choi S, Blumberg PM, Frank-Foltyn R, Bahrenberg G, Stockhausen H, Christoph T, Lee J.
Bioorg Med Chem (2015) 23 : 6844 -6854
PubMed 26474664 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 7.79 8.14

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3627723 1 8.14
CHEMBL3627950 1 7.43

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3627723 IC50 = 7.3 nM 8.14
CHEMBL3627950 IC50 = 37.2 nM 7.43