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Assay Detail

CHEMBL753842

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

Binding
Compound was evaluated for binding affinity of Opioid receptor kappa 1 in guinea pig brain membranes
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Cavia porcellus
Tissue Brain
Subcellular Membrane
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

Kappa-type opioid receptor (CHEMBL3952)
Type SINGLE PROTEIN
Organism Cavia porcellus

Publication

An approach to the design of receptor-type-selective non-peptide antagonists of peptidergic receptors: delta opioid antagonists.
Portoghese PS.
J Med Chem (1991) 34 : 1757 -1762
PubMed 1648136 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 4 7.00 7.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL19019 NALTREXONE 4.0 1 7.70
CHEMBL100940 NALTRIBEN 1 6.82
CHEMBL567175 NALTRINDOLE 1 6.48
CHEMBL47545 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL19019 NALTREXONE Ki = 20.0 nM 7.70
CHEMBL100940 NALTRIBEN Ki = 152.0 nM 6.82
CHEMBL567175 NALTRINDOLE Ki = 332.0 nM 6.48
CHEMBL47545 Ki > 1000.0 nM -