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Assay Detail

CHEMBL993513

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

Binding
Displacement of [3H]DAMGO from mu opioid receptor expressed in CHO cells
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
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
Ki 11 8.43 9.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL476600 1 9.85
CHEMBL19019 NALTREXONE 4.0 1 9.59
CHEMBL473136 1 9.39
CHEMBL472843 1 8.84
CHEMBL476603 1 8.80
CHEMBL500766 1 8.70
CHEMBL473253 1 8.57
CHEMBL515621 1 8.25
CHEMBL516085 1 7.17
CHEMBL516263 1 6.91
CHEMBL513990 1 6.65

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL476600 Ki = 0.14 nM 9.85
CHEMBL19019 NALTREXONE Ki = 0.26 nM 9.59
CHEMBL473136 Ki = 0.41 nM 9.39
CHEMBL472843 Ki = 1.44 nM 8.84
CHEMBL476603 Ki = 1.59 nM 8.80
CHEMBL500766 Ki = 2.02 nM 8.70
CHEMBL473253 Ki = 2.69 nM 8.57
CHEMBL515621 Ki = 5.58 nM 8.25
CHEMBL516085 Ki = 68.4 nM 7.17
CHEMBL516263 Ki = 123.23 nM 6.91
CHEMBL513990 Ki = 225.27 nM 6.65