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Assay Detail

CHEMBL843459

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

Binding
Tested for binding activity against mu opioid receptor using [3H]DAMGO ligand
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Mu-type opioid receptor (CHEMBL233)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis of naltrexone-derived delta-opioid antagonists. Role of conformation of the delta address moiety.
Portoghese PS, Sultana M, Moe ST, Takemori AE.
J Med Chem (1994) 37 : 579 -585
PubMed 8126697 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 8 8.62 9.72

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL610550 1 9.72
CHEMBL610046 1 8.85
CHEMBL610293 1 8.85
CHEMBL610292 1 8.85
CHEMBL101519 1 8.72
CHEMBL610290 1 8.28
CHEMBL252172 BNTX 1 7.88
CHEMBL567175 NALTRINDOLE 1 7.84

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL610550 Ki = 0.19 nM 9.72
CHEMBL610046 Ki = 1.4 nM 8.85
CHEMBL610293 Ki = 1.4 nM 8.85
CHEMBL610292 Ki = 1.4 nM 8.85
CHEMBL101519 Ki = 1.9 nM 8.72
CHEMBL610290 Ki = 5.2 nM 8.28
CHEMBL252172 BNTX Ki = 13.3 nM 7.88
CHEMBL567175 NALTRINDOLE Ki = 14.4 nM 7.84