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Assay Detail

CHEMBL993519

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

Functional
Antagonist activity against mu opioid receptor expressed in CHO cells assessed as inhibition of DAMGO-induced stimulation of [35S]GTPgammaS binding
2
Total Activities
1
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Cell Type CHO
Confidence 8 — Homologous single protein target
Curated By Intermediate

Target

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

Publication

14-O-Heterocyclic-substituted naltrexone derivatives as non-peptide mu opioid receptor selective antagonists: design, synthesis, and biological studies.
Li G, Aschenbach LC, He H, Selley DE, Zhang Y.
Bioorg Med Chem Lett (2009) 19 : 1825 -1829
PubMed 19217280 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ke 1 - -
Kd 1 9.72 9.72

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL476600 2 9.72

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL476600 Kd = 0.1905 nM 9.72
CHEMBL476600 Ke = 0.2 nM -