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Assay Detail

CHEMBL750000

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

Binding
Inhibition of [3H]DPDPE binding to guinea pig brain membrane Opioid receptor delta 1 at 1.0 nM
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Cavia porcellus
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Delta-type opioid receptor (CHEMBL236)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Electrophilic opioid ligands. Oxygen tethered alpha-methylene-gamma-lactone, acrylate, isothiocyanate, and epoxide derivatives of 6 beta-naltrexol.
Dasher WE, Klein P, Nelson WL.
J Med Chem (1992) 35 : 2374 -2384
PubMed 1320121 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 12 8.03 8.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL76023 1 8.85
CHEMBL350384 BREMAZOCINE 2.0 1 8.82
CHEMBL2310843 1 8.21
CHEMBL78932 1 8.14
CHEMBL310785 1 8.11
CHEMBL78796 1 8.04
CHEMBL311912 1 7.92
CHEMBL80434 1 7.89
CHEMBL19019 NALTREXONE 4.0 1 7.82
CHEMBL80531 1 7.72
CHEMBL140278 1 7.64
CHEMBL80 NALOXONE 4.0 1 7.21

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL76023 IC50 = 1.4 nM 8.85
CHEMBL350384 BREMAZOCINE IC50 = 1.5 nM 8.82
CHEMBL2310843 IC50 = 6.2 nM 8.21
CHEMBL78932 IC50 = 7.2 nM 8.14
CHEMBL310785 IC50 = 7.7 nM 8.11
CHEMBL78796 IC50 = 9.1 nM 8.04
CHEMBL311912 IC50 = 12.0 nM 7.92
CHEMBL80434 IC50 = 13.0 nM 7.89
CHEMBL19019 NALTREXONE IC50 = 15.0 nM 7.82
CHEMBL80531 IC50 = 19.0 nM 7.72
CHEMBL140278 IC50 = 23.0 nM 7.64
CHEMBL80 NALOXONE IC50 = 62.0 nM 7.21