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Assay Detail

CHEMBL3374353

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

Binding
Antagonist activity at human TRPV1 expressed in CHO cells assessed as inhibition of N-arachidonoyl dopamine-induced increase in intracellular Ca2+ level by FLIPR assay
1
Total Activities
1
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

2-Alkyl/alkenyl substituted pyridine C-region analogues of 2-(3-fluoro-4-methylsulfonylaminophenyl)propanamides as highly potent TRPV1 antagonists.
Ryu H, Seo S, Cho SH, Kim HS, Jung A, Kang DW, Son K, Cui M, Hong SH, Sharma PK, Choi S, Blumberg PM, Frank-Foltyn R, Bahrenberg G, Stockhausen H, Schiene K, Christoph T, Frormann S, Lee J.
Bioorg Med Chem Lett (2014) 24 : 4039 -4043
PubMed 24948568 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 1 9.70 9.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3314389 1 9.70

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3314389 Ki = 0.2 nM 9.70