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Assay Detail

CHEMBL687941

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

Functional
Mu opioid receptor agonist activity as inhibition of electrically stimulated mysenteric plexus in guinea pig ileum
8
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
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

Synthesis and biological evaluation of a metazocine-containing enkephalinamide. Evidence for nonidentical roles of the tyramine moiety in opiates and opioid peptides.
Ramakrishnan K, Portoghese PS.
J Med Chem (1982) 25 : 1423 -1427
PubMed 7154002 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 6.31 7.76

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL595972 1 7.76
CHEMBL70 MORPHINE 4.0 1 7.24
CHEMBL257661 METAZOCINE 2.0 1 7.03
CHEMBL441776 2 6.29
CHEMBL285083 1 5.55
CHEMBL284060 1 5.21
CHEMBL2372185 1 5.10

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL595972 IC50 = 17.4 nM 7.76
CHEMBL70 MORPHINE IC50 = 57.3 nM 7.24
CHEMBL257661 METAZOCINE IC50 = 94.0 nM 7.03
CHEMBL441776 IC50 = 510.0 nM 6.29
CHEMBL441776 IC50 = 510.0 nM 6.29
CHEMBL285083 IC50 = 2820.0 nM 5.55
CHEMBL284060 IC50 = 6090.0 nM 5.21
CHEMBL2372185 IC50 = 7970.0 nM 5.10