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Assay Detail

CHEMBL834471

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

Functional
Inhibition of mu opioid receptor mediated GTPgammaS binding to CHO cell membranes
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Rationale, design, and synthesis of novel phenyl imidazoles as opioid receptor agonists for gastrointestinal disorders.
Breslin HJ, Miskowski TA, Rafferty BM, Coutinho SV, Palmer JM, Wallace NH, Schneider CR, Kimball ES, Zhang SP, Li J, Colburn RW, Stone DJ, Martinez RP, He W.
J Med Chem (2004) 47 : 5009 -5020
PubMed 15456245 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 8 6.25 7.24

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL841 LOPERAMIDE 4.0 1 7.24
CHEMBL366311 1 6.82
CHEMBL186527 1 5.89
CHEMBL188558 1 5.67
CHEMBL361274 1 5.62
CHEMBL361033 1 -
CHEMBL408680 1 -
CHEMBL362514 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL841 LOPERAMIDE EC50 = 58.0 nM 7.24
CHEMBL366311 EC50 = 153.0 nM 6.82
CHEMBL186527 EC50 = 1300.0 nM 5.89
CHEMBL188558 EC50 = 2120.0 nM 5.67
CHEMBL361274 EC50 = 2400.0 nM 5.62
CHEMBL361033 EC50 > 10000.0 nM -
CHEMBL408680 EC50 > 10000.0 nM -
CHEMBL362514 EC50 > 10000.0 nM -