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Assay Detail

CHEMBL5253448

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Binding
Antagonist activity at TRPM8 (unknown origin)
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Publication

Transient Receptor Potential Melastatin 8 Channel (TRPM8) Modulation: Cool Entryway for Treating Pain and Cancer.
Pérez de Vega MJ, Gómez-Monterrey I, Ferrer-Montiel A, González-Muñiz R.
J Med Chem (2016) 59 : 10006 -10029
PubMed 27437828 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 16 6.66 9.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5275380 1 9.52
CHEMBL3353597 1 8.08
CHEMBL190461 CANNABIDIOL 4.0 1 7.22
CHEMBL375696 1 6.82
CHEMBL465718 DELTA9-TETRAHYDROCANNABINOLIC ACID A 1 6.82
CHEMBL5269402 1 6.82
CHEMBL497318 CANNABIGEROL 2.0 1 6.80
CHEMBL465 DRONABINOL 4.0 1 6.80
CHEMBL808 ECONAZOLE 4.0 1 6.38
CHEMBL5284265 1 6.16
CHEMBL258502 1 6.10
CHEMBL1779158 1 6.10
CHEMBL294199 CAPSAICIN 4.0 1 6.00
CHEMBL5274774 1 5.22
CHEMBL104 CLOTRIMAZOLE 4.0 1 5.10
CHEMBL5267089 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5275380 IC50 = 0.3 nM 9.52
CHEMBL3353597 IC50 = 8.3 nM 8.08
CHEMBL190461 CANNABIDIOL IC50 = 60.0 nM 7.22
CHEMBL375696 IC50 = 150.0 nM 6.82
CHEMBL465718 DELTA9-TETRAHYDROCANNABINOLIC ACID A IC50 = 150.0 nM 6.82
CHEMBL5269402 IC50 = 150.0 nM 6.82
CHEMBL497318 CANNABIGEROL IC50 = 160.0 nM 6.80
CHEMBL465 DRONABINOL IC50 = 160.0 nM 6.80
CHEMBL808 ECONAZOLE IC50 = 420.0 nM 6.38
CHEMBL5284265 IC50 = 700.0 nM 6.16
CHEMBL258502 IC50 = 800.0 nM 6.10
CHEMBL1779158 IC50 = 800.0 nM 6.10
CHEMBL294199 CAPSAICIN IC50 = 1000.0 nM 6.00
CHEMBL5274774 IC50 = 6000.0 nM 5.22
CHEMBL104 CLOTRIMAZOLE IC50 = 8000.0 nM 5.10
CHEMBL5267089 IC50 < 20.0 nM -