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Assay Detail

CHEMBL2188275

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Functional
Antagonist activity at human TRPV1 expressed in CHOK1 cells assessed as inhibition of capsaicin-induced activity by FLIPR assay
ChEMBL ↗
85
Total Activities
85
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type CHO-K1
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Transient receptor potential cation channel subfamily V member 1 (CHEMBL4794) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

2-(3-fluoro-4-methylsulfonylaminophenyl)propanamides as potent transient receptor potential vanilloid 1 (TRPV1) antagonists: structure-activity relationships of 2-amino derivatives in the N-(6-trifluoromethylpyridin-3-ylmethyl) C-region.
Kim MS, Ryu H, Kang DW, Cho SH, Seo S, Park YS, Kim MY, Kwak EJ, Kim YS, Bhondwe RS, Kim HS, Park SG, Son K, Choi S, DeAndrea-Lazarus IA, Pearce LV, Blumberg PM, Frank R, Bahrenberg G, Stockhausen H, Kögel BY, Schiene K, Christoph T, Lee J.
J Med Chem (2012) 55 : 8392 -8408
PubMed 22957803 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 85 8.56 9.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2178059 — — 1 9.70
CHEMBL2177441 — — 1 9.70
CHEMBL2177440 — — 1 9.70
CHEMBL2177429 — — 1 9.70
CHEMBL2178063 — — 1 9.70
CHEMBL2178068 — — 1 9.52
CHEMBL2177435 — — 1 9.52
CHEMBL2177424 — — 1 9.52
CHEMBL2177425 — — 1 9.52
CHEMBL2177432 — — 1 9.52
CHEMBL2177428 — — 1 9.52
CHEMBL2177402 — — 1 9.40
CHEMBL2177423 — — 1 9.37
CHEMBL2177404 — — 1 9.30
CHEMBL2177434 — — 1 9.22
CHEMBL2178064 — — 1 9.22
CHEMBL2178067 — — 1 9.22
CHEMBL2177405 — — 1 9.22
CHEMBL2177419 — — 1 9.15
CHEMBL2179146 — — 1 9.15
CHEMBL2177433 — — 1 9.15
CHEMBL2177418 — — 1 9.10
CHEMBL2177427 — — 1 9.10
CHEMBL2178065 — — 1 9.10
CHEMBL2178066 — — 1 9.05
CHEMBL2179150 — — 1 8.96
CHEMBL191247 — — 1 8.92
CHEMBL2177400 — — 1 8.89
CHEMBL2177409 — — 1 8.89
CHEMBL2177401 — — 1 8.85

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2178059 — Ki = 0.2 nM 9.70
CHEMBL2178063 — Ki = 0.2 nM 9.70
CHEMBL2177429 — Ki = 0.2 nM 9.70
CHEMBL2177441 — Ki = 0.2 nM 9.70
CHEMBL2177440 — Ki = 0.2 nM 9.70
CHEMBL2178068 — Ki = 0.3 nM 9.52
CHEMBL2177435 — Ki = 0.3 nM 9.52
CHEMBL2177424 — Ki = 0.3 nM 9.52
CHEMBL2177425 — Ki = 0.3 nM 9.52
CHEMBL2177432 — Ki = 0.3 nM 9.52
CHEMBL2177428 — Ki = 0.3 nM 9.52
CHEMBL2177402 — Ki = 0.4 nM 9.40
CHEMBL2177423 — Ki = 0.43 nM 9.37
CHEMBL2177404 — Ki = 0.5 nM 9.30
CHEMBL2177405 — Ki = 0.6 nM 9.22
CHEMBL2178064 — Ki = 0.6 nM 9.22
CHEMBL2178067 — Ki = 0.6 nM 9.22
CHEMBL2177434 — Ki = 0.6 nM 9.22
CHEMBL2177419 — Ki = 0.7 nM 9.15
CHEMBL2179146 — Ki = 0.7 nM 9.15
CHEMBL2177433 — Ki = 0.7 nM 9.15
CHEMBL2177418 — Ki = 0.8 nM 9.10
CHEMBL2177427 — Ki = 0.8 nM 9.10
CHEMBL2178065 — Ki = 0.8 nM 9.10
CHEMBL2178066 — Ki = 0.9 nM 9.05
CHEMBL2179150 — Ki = 1.1 nM 8.96
CHEMBL191247 — Ki = 1.2 nM 8.92
CHEMBL2177400 — Ki = 1.3 nM 8.89
CHEMBL2177409 — Ki = 1.3 nM 8.89
CHEMBL2177401 — Ki = 1.43 nM 8.85
CHEMBL2177410 — Ki = 1.4 nM 8.85
CHEMBL2179153 — Ki = 1.4 nM 8.85
CHEMBL2178072 — Ki = 1.4 nM 8.85
CHEMBL2177431 — Ki = 1.5 nM 8.82
CHEMBL2177437 — Ki = 1.7 nM 8.77
CHEMBL2177414 — Ki = 2.0 nM 8.70
CHEMBL2179154 — Ki = 2.1 nM 8.68
CHEMBL2177415 — Ki = 2.1 nM 8.68
CHEMBL2179151 — Ki = 2.3 nM 8.64
CHEMBL2177439 — Ki = 2.4 nM 8.62
CHEMBL2179149 — Ki = 2.4 nM 8.62
CHEMBL2177408 — Ki = 2.4 nM 8.62
CHEMBL2179152 — Ki = 2.5 nM 8.60
CHEMBL2178071 — Ki = 2.6 nM 8.59
CHEMBL2177398 — Ki = 2.8 nM 8.55
CHEMBL2177426 — Ki = 2.9 nM 8.54
CHEMBL2177412 — Ki = 3.0 nM 8.52
CHEMBL2179148 — Ki = 3.3 nM 8.48
CHEMBL2179147 — Ki = 3.4 nM 8.47
CHEMBL2178062 — Ki = 3.5 nM 8.46