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Assay Detail

CHEMBL684402

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

Functional
Tested for potent reversible agonist activity on electrically stimulated guinea pig ileal longitudinal muscle preparation
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Cavia porcellus
Tissue Muscle tissue
Confidence 1 — Organism
Curated By Intermediate

Target

Cavia porcellus (CHEMBL369)
Type ORGANISM
Organism Cavia porcellus

Publication

A novel opioid receptor site directed alkylating agent with irreversible narcotic antagonistic and reversible agonistic activities.
Portoghese PS, Larson DL, Sayre LM, Fries DS, Takemori AE.
J Med Chem (1980) 23 : 233 -234
PubMed 6245210 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 7.70 8.32

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL473136 1 8.32
CHEMBL70 MORPHINE 4.0 1 7.62
CHEMBL78205 1 7.57
CHEMBL19019 NALTREXONE 4.0 1 7.30

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL473136 IC50 = 4.8 nM 8.32
CHEMBL70 MORPHINE IC50 = 24.0 nM 7.62
CHEMBL78205 IC50 = 27.0 nM 7.57
CHEMBL19019 NALTREXONE IC50 = 50.0 nM 7.30