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Assay Detail

CHEMBL2389488

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Binding
Antagonist activity at human TRPV1 expressed in CHOK1 cells assessed as inhibition of pH 6 to 6.3-induced activity by FLIPR assay
ChEMBL ↗
67
Total Activities
67
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
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 TRPV1 antagonists: structure activity relationships of the 2-oxy pyridine C-region.
Thorat SA, Kang DW, Ryu H, Kim MS, Kim HS, Ann J, Ha T, Kim SE, Son K, Choi S, Blumberg PM, Frank R, Bahrenberg G, Schiene K, Christoph T, Lee J.
Eur J Med Chem (2013) 64 : 589 -602
PubMed 23685943 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 67 7.15 8.29

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2385246 — — 1 8.29
CHEMBL2385249 — — 1 7.94
CHEMBL2385426 — — 1 7.91
CHEMBL2385418 — — 1 7.85
CHEMBL2385409 — — 1 7.82
CHEMBL2385220 — — 1 7.78
CHEMBL2385223 — — 1 7.73
CHEMBL2385250 — — 1 7.71
CHEMBL2385410 — — 1 7.62
CHEMBL2385229 — — 1 7.60
CHEMBL2385424 — — 1 7.56
CHEMBL2385224 — — 1 7.56
CHEMBL2385416 — — 1 7.54
CHEMBL2385425 — — 1 7.52
CHEMBL2385423 — — 1 7.52
CHEMBL2385248 — — 1 7.39
CHEMBL2385419 — — 1 7.37
CHEMBL2385255 — — 1 7.37
CHEMBL2385417 — — 1 7.36
CHEMBL2385235 — — 1 7.36
CHEMBL2385251 — — 1 7.35
CHEMBL2385225 — — 1 7.28
CHEMBL2385408 — — 1 7.28
CHEMBL2385231 — — 1 7.18
CHEMBL2385415 — — 1 7.16
CHEMBL2385233 — — 1 7.16
CHEMBL2385238 — — 1 7.12
CHEMBL2385422 — — 1 7.04
CHEMBL2385236 — — 1 7.03
CHEMBL2385407 — — 1 7.03

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2385246 — IC50 = 5.1 nM 8.29
CHEMBL2385249 — IC50 = 11.6 nM 7.94
CHEMBL2385426 — IC50 = 12.3 nM 7.91
CHEMBL2385418 — IC50 = 14.0 nM 7.85
CHEMBL2385409 — IC50 = 15.1 nM 7.82
CHEMBL2385220 — IC50 = 16.6 nM 7.78
CHEMBL2385223 — IC50 = 18.6 nM 7.73
CHEMBL2385250 — IC50 = 19.7 nM 7.71
CHEMBL2385410 — IC50 = 23.8 nM 7.62
CHEMBL2385229 — IC50 = 25.0 nM 7.60
CHEMBL2385424 — IC50 = 27.3 nM 7.56
CHEMBL2385224 — IC50 = 27.6 nM 7.56
CHEMBL2385416 — IC50 = 28.7 nM 7.54
CHEMBL2385425 — IC50 = 29.9 nM 7.52
CHEMBL2385423 — IC50 = 30.5 nM 7.52
CHEMBL2385248 — IC50 = 40.5 nM 7.39
CHEMBL2385419 — IC50 = 43.1 nM 7.37
CHEMBL2385255 — IC50 = 43.0 nM 7.37
CHEMBL2385417 — IC50 = 43.4 nM 7.36
CHEMBL2385235 — IC50 = 43.7 nM 7.36
CHEMBL2385251 — IC50 = 44.4 nM 7.35
CHEMBL2385225 — IC50 = 53.0 nM 7.28
CHEMBL2385408 — IC50 = 52.6 nM 7.28
CHEMBL2385231 — IC50 = 66.1 nM 7.18
CHEMBL2385233 — IC50 = 69.0 nM 7.16
CHEMBL2385415 — IC50 = 69.8 nM 7.16
CHEMBL2385238 — IC50 = 76.0 nM 7.12
CHEMBL2385422 — IC50 = 90.1 nM 7.04
CHEMBL2385236 — IC50 = 93.0 nM 7.03
CHEMBL2385407 — IC50 = 93.4 nM 7.03
CHEMBL2385234 — IC50 = 95.0 nM 7.02
CHEMBL2385237 — IC50 = 114.0 nM 6.94
CHEMBL2385082 — IC50 = 115.0 nM 6.94
CHEMBL2385239 — IC50 = 125.0 nM 6.90
CHEMBL2385230 — IC50 = 132.0 nM 6.88
CHEMBL2385241 — IC50 = 140.0 nM 6.85
CHEMBL2385247 — IC50 = 161.0 nM 6.79
CHEMBL2385406 — IC50 = 161.0 nM 6.79
CHEMBL2385226 — IC50 = 165.0 nM 6.78
CHEMBL2385242 — IC50 = 174.0 nM 6.76
CHEMBL2385228 — IC50 = 182.0 nM 6.74
CHEMBL2385254 — IC50 = 183.0 nM 6.74
CHEMBL2385240 — IC50 = 242.0 nM 6.62
CHEMBL2385421 — IC50 = 277.0 nM 6.56
CHEMBL2385244 — IC50 = 293.0 nM 6.53
CHEMBL2385227 — IC50 = 337.0 nM 6.47
CHEMBL2385219 — IC50 = 342.0 nM 6.47
CHEMBL2385405 — IC50 = 462.0 nM 6.33
CHEMBL2385232 — IC50 = 653.0 nM 6.18
CHEMBL2042264 — IC50 = 1990.0 nM 5.70