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Assay Detail

CHEMBL3824993

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

Binding
Displacement of [3H]-resiniferatoxin from human TRPV1 expressed in CHO cells incubated for 60 mins by scintillation counting analysis
12
Total Activities
12
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

Discovery of N-(3-fluoro-4-methylsulfonamidomethylphenyl)urea as a potent TRPV1 antagonistic template.
Ann J, Sun W, Zhou X, Jung A, Baek J, Lee S, Kim C, Yoon S, Hong S, Choi S, Turcios NA, Herold BK, Esch TE, Lewin NE, Abramovitz A, Pearce LV, Blumberg PM, Lee J.
Bioorg Med Chem Lett (2016) 26 : 3603 -3607
PubMed 27317643 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 12 7.15 8.53

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2177429 1 8.53
CHEMBL3694601 1 8.17
CHEMBL2177428 1 8.10
CHEMBL3822842 1 7.50
CHEMBL3823425 1 7.27
CHEMBL3822908 1 7.23
CHEMBL3824160 1 7.08
CHEMBL3823983 1 6.68
CHEMBL3822749 1 6.64
CHEMBL3823968 1 6.39
CHEMBL3822592 1 6.31
CHEMBL3822772 1 5.94

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2177429 Ki = 2.95 nM 8.53
CHEMBL3694601 Ki = 6.77 nM 8.17
CHEMBL2177428 Ki = 7.9 nM 8.10
CHEMBL3822842 Ki = 31.6 nM 7.50
CHEMBL3823425 Ki = 54.0 nM 7.27
CHEMBL3822908 Ki = 59.0 nM 7.23
CHEMBL3824160 Ki = 83.0 nM 7.08
CHEMBL3823983 Ki = 210.0 nM 6.68
CHEMBL3822749 Ki = 230.0 nM 6.64
CHEMBL3823968 Ki = 410.0 nM 6.39
CHEMBL3822592 Ki = 490.0 nM 6.31
CHEMBL3822772 Ki = 1160.0 nM 5.94