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Assay Detail

CHEMBL757491

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

Binding
The compound was evaluated for binding affinity against opioid receptor mu in guinea pig brain membranes using [3H]- DAMGO as ligand
7
Total Activities
7
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

Opioid agonist and antagonist activities of morphindoles related to naltrindole.
Portoghese PS, Larson DL, Sultana M, Takemori AE.
J Med Chem (1992) 35 : 4325 -4329
PubMed 1333013 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 7 6.99 8.42

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL567175 NALTRINDOLE 1 8.42
CHEMBL607339 1 6.76
CHEMBL344000 1 6.43
CHEMBL401093 OXYMORPHINDOLE 1 6.33
CHEMBL47545 1 -
CHEMBL607395 1 -
CHEMBL607393 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL567175 NALTRINDOLE Ki = 3.8 nM 8.42
CHEMBL607339 Ki = 173.0 nM 6.76
CHEMBL344000 Ki = 375.0 nM 6.43
CHEMBL401093 OXYMORPHINDOLE Ki = 468.0 nM 6.33
CHEMBL47545 Ki > 1000.0 nM -
CHEMBL607395 Ki > 1000.0 nM -
CHEMBL607393 Ki > 1000.0 nM -