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Assay Detail

CHEMBL2445667

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

Binding
Inhibition of human TRPM8 (unknown origin) expressed in HEK293 cells assessed as inhibition of WS12-induced Ca2+ elevation by FLIPR assay
ChEMBL ↗
68
Total Activities
47
Compounds Tested
3
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Transient receptor potential cation channel subfamily M member 8 (CHEMBL1075319) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Serendipity in drug-discovery: a new series of 2-(benzyloxy)benzamides as TRPM8 antagonists.
Brown A, Ellis D, Favor DA, Kirkup T, Klute W, MacKenny M, McMurray G, Stennett A.
Bioorg Med Chem Lett (2013) 23 : 6118 -6122
PubMed 24080460 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kb 44 - -
IC50 21 6.41 7.82
EC50 3 6.48 7.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2442021 — — 2 7.82
CHEMBL2442013 — — 2 7.71
CHEMBL2442019 — — 2 7.68
CHEMBL2442017 — — 2 7.52
CHEMBL2441929 ACOLTREMON 2.0 1 7.40
CHEMBL2442022 — — 2 7.12
CHEMBL2442016 — — 2 7.07
CHEMBL2442015 — — 2 7.01
CHEMBL2442014 — — 2 6.59
CHEMBL2442020 — — 2 6.54
CHEMBL258405 ICILLIN 3.0 1 6.52
CHEMBL2442018 — — 2 6.36
CHEMBL2442011 — — 2 6.31
CHEMBL2442030 — — 2 6.23
CHEMBL2442037 — — 2 5.91
CHEMBL2442051 — — 2 5.91
CHEMBL2442033 — — 2 5.87
CHEMBL2442032 — — 2 5.85
CHEMBL2442012 — — 2 5.73
CHEMBL2442034 — — 2 5.70
CHEMBL256087 MENTHOL 4.0 1 5.52
CHEMBL2442036 — — 2 5.50
CHEMBL2442010 — — 2 5.17
CHEMBL2442031 — — 2 5.06
CHEMBL2442052 — — 1 -
CHEMBL2442050 — — 1 -
CHEMBL2442048 — — 1 -
CHEMBL2442049 — — 1 -
CHEMBL2442047 — — 1 -
CHEMBL2442046 — — 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2442021 — IC50 = 15.1 nM 7.82
CHEMBL2442013 — IC50 = 19.3 nM 7.71
CHEMBL2442019 — IC50 = 21.1 nM 7.68
CHEMBL2442017 — IC50 = 29.9 nM 7.52
CHEMBL2441929 ACOLTREMON EC50 = 40.0 nM 7.40
CHEMBL2442022 — IC50 = 76.2 nM 7.12
CHEMBL2442016 — IC50 = 85.4 nM 7.07
CHEMBL2442015 — IC50 = 96.9 nM 7.01
CHEMBL2442014 — IC50 = 254.0 nM 6.59
CHEMBL2442020 — IC50 = 291.0 nM 6.54
CHEMBL258405 ICILLIN EC50 = 300.0 nM 6.52
CHEMBL2442018 — IC50 = 435.0 nM 6.36
CHEMBL2442011 — IC50 = 493.0 nM 6.31
CHEMBL2442030 — IC50 = 593.0 nM 6.23
CHEMBL2442051 — IC50 = 1240.0 nM 5.91
CHEMBL2442037 — IC50 = 1230.0 nM 5.91
CHEMBL2442033 — IC50 = 1360.0 nM 5.87
CHEMBL2442032 — IC50 = 1400.0 nM 5.85
CHEMBL2442012 — IC50 = 1850.0 nM 5.73
CHEMBL2442034 — IC50 = 2010.0 nM 5.70
CHEMBL256087 MENTHOL EC50 = 3000.0 nM 5.52
CHEMBL2442036 — IC50 = 3150.0 nM 5.50
CHEMBL2442010 — IC50 = 6780.0 nM 5.17
CHEMBL2442031 — IC50 = 8780.0 nM 5.06
CHEMBL2442044 — Kb = 4860.0 nM -
CHEMBL2442045 — Kb = 2600.0 nM -
CHEMBL2442046 — Kb > 5000.0 nM -
CHEMBL2442047 — Kb > 5000.0 nM -
CHEMBL2442049 — Kb = 1400.0 nM -
CHEMBL2442048 — Kb = 1130.0 nM -
CHEMBL2442050 — Kb < 100.0 nM -
CHEMBL2442051 — Kb = 443.0 nM -
CHEMBL2442052 — Kb = 8.4 nM -
CHEMBL2442019 — Kb = 17.8 nM -
CHEMBL2441930 — Kb = 7.8 nM -
CHEMBL2442010 — Kb = 4590.0 nM -
CHEMBL2442011 — Kb = 491.0 nM -
CHEMBL2442042 — Kb > 5000.0 nM -
CHEMBL2442040 — Kb > 5000.0 nM -
CHEMBL2442041 — Kb > 10000.0 nM -
CHEMBL2442038 — Kb > 10000.0 nM -
CHEMBL2442039 — Kb > 10000.0 nM -
CHEMBL2442035 — Kb > 10000.0 nM -
CHEMBL2442036 — Kb = 3670.0 nM -
CHEMBL2442037 — Kb = 1430.0 nM -
CHEMBL2442033 — Kb = 794.0 nM -
CHEMBL2442034 — Kb = 2250.0 nM -
CHEMBL2442031 — Kb = 5130.0 nM -
CHEMBL2442032 — Kb = 1560.0 nM -
CHEMBL2442043 — Kb > 10000.0 nM -