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Assay Detail

CHEMBL758274

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

Binding
Inhibitory potency against Opioid receptor mu 1 in longitudinal muscle preparation of guinea pig ileum
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Cavia porcellus
Tissue Ileum
Confidence 9 — Direct single protein target
Curated By Expert

Target

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

Publication

Evidence of the preferential involvement of mu receptors in analgesia using enkephalins highly selective for peripheral mu or delta receptors.
Gacel G, Fournié-Zaluski MC, Fellion E, Roques BP.
J Med Chem (1981) 24 : 1119 -1124
PubMed 6276540 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 10 7.02 8.14

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL274204 1 8.14
CHEMBL13894 1 7.66
CHEMBL340032 DADLE 1 7.32
CHEMBL70 MORPHINE 4.0 1 7.16
CHEMBL280274 1 7.00
CHEMBL14094 1 6.74
CHEMBL13786 1 6.70
CHEMBL14036 1 6.62
CHEMBL14230 1 6.44
CHEMBL14204 1 6.42

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL274204 IC50 = 7.2 nM 8.14
CHEMBL13894 IC50 = 21.9 nM 7.66
CHEMBL340032 DADLE IC50 = 47.8 nM 7.32
CHEMBL70 MORPHINE IC50 = 70.0 nM 7.16
CHEMBL280274 IC50 = 100.0 nM 7.00
CHEMBL14094 IC50 = 182.0 nM 6.74
CHEMBL13786 IC50 = 200.0 nM 6.70
CHEMBL14036 IC50 = 240.0 nM 6.62
CHEMBL14230 IC50 = 360.0 nM 6.44
CHEMBL14204 IC50 = 380.0 nM 6.42