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Assay Detail

CHEMBL755961

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

Binding
Binding affinity of Opioid receptor mu 1 by the displacement of mu-selective [3H]DAGO from brain membrane preparations.
5
Total Activities
5
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

Mu-type opioid receptor (CHEMBL4354)
Type SINGLE PROTEIN
Organism Cavia porcellus

Publication

Hybrid bivalent ligands with opiate and enkephalin pharmacophores.
Portoghese PS, Larson DL, Ronsisvalle G, Schiller PW, Nguyen TM, Lemieux C, Takemori AE.
J Med Chem (1987) 30 : 1991 -1994
PubMed 2444704 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 5 7.99 8.74

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL607319 1 8.74
CHEMBL607322 1 8.26
CHEMBL607321 1 7.96
CHEMBL607320 1 7.72
CHEMBL60377 1 7.28

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL607319 Ki = 1.81 nM 8.74
CHEMBL607322 Ki = 5.48 nM 8.26
CHEMBL607321 Ki = 11.1 nM 7.96
CHEMBL607320 Ki = 19.1 nM 7.72
CHEMBL60377 Ki = 52.9 nM 7.28