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Assay Detail

CHEMBL779645

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

Functional
Concentration of drug required to inhibit the stereospecific binding of [3H]naloxone (5 nM) to homogenates of rat brain minus cerebellum in the presence of 100 mM NaCl
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Rattus norvegicus
Tissue Brain
Confidence 1 — Organism
Curated By Intermediate

Target

Rattus norvegicus (CHEMBL376)
Type ORGANISM
Organism Rattus norvegicus

Publication

5-Aryl-3-azabicyclo[3.2.0]heptan-6-one ketals, compounds with morphine-like analgesic activity.
McKenzie TC, Epstein JW, Fanshawe WJ, Dixon JS, Osterberg AC, Wennogle LP, Regan BA, Abel MS, Meyerson LR.
J Med Chem (1984) 27 : 628 -632
PubMed 6325691 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 5.93 7.47

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1254682 LEVALLORPHAN 4.0 1 7.47
CHEMBL80 NALOXONE 4.0 1 7.38
CHEMBL485 CODEINE 4.0 1 4.66
CHEMBL156381 1 4.20

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1254682 LEVALLORPHAN IC50 = 34.0 nM 7.47
CHEMBL80 NALOXONE IC50 = 42.0 nM 7.38
CHEMBL485 CODEINE IC50 = 22000.0 nM 4.66
CHEMBL156381 IC50 = 62531.0 nM 4.20