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Assay Detail

CHEMBL756018

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

Binding
In vitro binding affinity against Opioid receptors from bovine caudate nucleus determined in presence of [3H]- bremazocine (0.5 nM)
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Bos taurus
Confidence 4 — Cell-line / Tissue
Curated By Autocuration

Target

Opioid receptors; mu/kappa/delta (CHEMBL2095181)
Type PROTEIN FAMILY
Organism Homo sapiens

Publication

Conjugate addition ligands of opioid antagonists. Methacrylate esters and ethers of 6 alpha- and 6 beta-naltrexol.
Olsen LD, Klein P, Nelson WL, Yao YH, Simon EJ.
J Med Chem (1990) 33 : 737 -741
PubMed 2153826 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 8.34 9.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL350384 BREMAZOCINE 2.0 1 9.30
CHEMBL166355 1 8.62
CHEMBL163704 1 8.30
CHEMBL610531 1 8.22
CHEMBL76023 1 7.92
CHEMBL3084322 1 7.70

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL350384 BREMAZOCINE IC50 = 0.5 nM 9.30
CHEMBL166355 IC50 = 2.4 nM 8.62
CHEMBL163704 IC50 = 5.0 nM 8.30
CHEMBL610531 IC50 = 6.0 nM 8.22
CHEMBL76023 IC50 = 12.0 nM 7.92
CHEMBL3084322 IC50 = 20.0 nM 7.70