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Assay Detail

CHEMBL756522

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

Binding
Displacement of [3H]dalamid ([D-Ala2,Met5] enkephalinamide) from opioid receptors of rat brain membrane
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 5 — Multiple protein complex / RNA
Curated By Autocuration

Target

Opioid receptor (CHEMBL2094129)
Type PROTEIN FAMILY
Organism Rattus norvegicus

Publication

Probes for narcotic receptor mediated phenomena. 13. Potential irreversible narcotic antagonist-based ligands derived from 6,14-endo-ethenotetrahydronororipavine with 7-(methoxyfumaroyl)amino, (bromoacetyl)amino, or isothiocyanate electrophiles: chemistry, biochemistry, and pharmacology.
Lessor RA, Bajwa BS, Rice KC, Jacobson AE, Streaty RA, Klee WA, Smith CB, Aceto MD, May EL, Harris LS.
J Med Chem (1986) 29 : 2136 -2141
PubMed 3023609 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 14 7.57 8.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1908349 NALORPHINE HYDROCHLORIDE -1.0 1 8.82
CHEMBL2096625 1 8.52
CHEMBL2310921 1 8.22
CHEMBL3038189 1 8.22
CHEMBL2310915 1 8.15
CHEMBL3038190 1 8.15
CHEMBL2310917 1 7.30
CHEMBL2310916 1 7.05
CHEMBL2310918 1 7.05
CHEMBL2310922 1 7.00
CHEMBL2310919 1 7.00
CHEMBL2310920 1 6.89
CHEMBL3038192 1 6.89
CHEMBL3038191 1 6.75

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1908349 NALORPHINE HYDROCHLORIDE EC50 = 1.5 nM 8.82
CHEMBL2096625 EC50 = 3.0 nM 8.52
CHEMBL2310921 EC50 = 6.0 nM 8.22
CHEMBL3038189 EC50 = 6.0 nM 8.22
CHEMBL2310915 EC50 = 7.0 nM 8.15
CHEMBL3038190 EC50 = 7.0 nM 8.15
CHEMBL2310917 EC50 = 50.0 nM 7.30
CHEMBL2310916 EC50 = 90.0 nM 7.05
CHEMBL2310918 EC50 = 90.0 nM 7.05
CHEMBL2310922 EC50 = 100.0 nM 7.00
CHEMBL2310919 EC50 = 100.0 nM 7.00
CHEMBL2310920 EC50 = 130.0 nM 6.89
CHEMBL3038192 EC50 = 130.0 nM 6.89
CHEMBL3038191 EC50 = 180.0 nM 6.75