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Assay Detail

CHEMBL865710

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

Functional
Activity against mu opioid receptor by stimulation of [35S]GTP-gamma-S binding in CHO-hgamma cells
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Cavia porcellus
Cell Type CHO-hgamma
Confidence 9 — Direct single protein target
Curated By Expert

Target

Mu-type opioid receptor (CHEMBL4354)
Type SINGLE PROTEIN
Organism Cavia porcellus

Publication

Identification of potent phenyl imidazoles as opioid receptor agonists.
Breslin HJ, Cai C, Miskowski TA, Coutinho SV, Zhang SP, Hornby P, He W.
Bioorg Med Chem Lett (2006) 16 : 2505 -2508
PubMed 16483774 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 8 7.17 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL377069 1 8.70
CHEMBL205049 1 8.05
CHEMBL208454 1 7.57
CHEMBL204996 1 7.00
CHEMBL366311 1 6.85
CHEMBL205388 1 6.81
CHEMBL427214 1 6.79
CHEMBL361274 1 5.61

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL377069 EC50 = 2.0 nM 8.70
CHEMBL205049 EC50 = 9.0 nM 8.05
CHEMBL208454 EC50 = 27.0 nM 7.57
CHEMBL204996 EC50 = 100.0 nM 7.00
CHEMBL366311 EC50 = 142.0 nM 6.85
CHEMBL205388 EC50 = 155.0 nM 6.81
CHEMBL427214 EC50 = 161.0 nM 6.79
CHEMBL361274 EC50 = 2445.0 nM 5.61