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Assay Detail

CHEMBL950282

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

Binding
Displacement of [3H]DAMGO from human mu opioid receptor expressed in CHO cells
28
Total Activities
28
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type CHO
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Synthesis and biological evaluation of alpha- and beta-6-amido derivatives of 17-cyclopropylmethyl-3, 14beta-dihydroxy-4, 5alpha-epoxymorphinan: potential alcohol-cessation agents.
Ghirmai S, Azar MR, Polgar WE, Berzetei-Gurske I, Cashman JR.
J Med Chem (2008) 51 : 1913 -1924
PubMed 18298057 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 28 9.53 10.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL409458 1 10.30
CHEMBL438413 1 10.22
CHEMBL272215 1 10.00
CHEMBL412050 1 9.92
CHEMBL410526 1 9.92
CHEMBL273105 1 9.89
CHEMBL410122 1 9.89
CHEMBL411927 1 9.80
CHEMBL429929 1 9.80
CHEMBL271815 1 9.74
CHEMBL407466 1 9.72
CHEMBL411738 1 9.72
CHEMBL410884 1 9.68
CHEMBL271797 1 9.68
CHEMBL271811 1 9.59
CHEMBL270918 1 9.57
CHEMBL19019 NALTREXONE 4.0 1 9.52
CHEMBL260528 1 9.51
CHEMBL429588 1 9.42
CHEMBL272051 1 9.37
CHEMBL443326 1 9.37
CHEMBL409036 1 9.19
CHEMBL272181 1 9.17
CHEMBL271755 1 9.04
CHEMBL982 NALMEFENE 4.0 1 9.04
CHEMBL411916 1 8.92
CHEMBL406116 1 8.83
CHEMBL272021 1 8.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL409458 Ki = 0.05 nM 10.30
CHEMBL438413 Ki = 0.06 nM 10.22
CHEMBL272215 Ki = 0.1 nM 10.00
CHEMBL412050 Ki = 0.12 nM 9.92
CHEMBL410526 Ki = 0.12 nM 9.92
CHEMBL273105 Ki = 0.13 nM 9.89
CHEMBL410122 Ki = 0.13 nM 9.89
CHEMBL411927 Ki = 0.16 nM 9.80
CHEMBL429929 Ki = 0.16 nM 9.80
CHEMBL271815 Ki = 0.18 nM 9.74
CHEMBL407466 Ki = 0.19 nM 9.72
CHEMBL411738 Ki = 0.19 nM 9.72
CHEMBL410884 Ki = 0.21 nM 9.68
CHEMBL271797 Ki = 0.21 nM 9.68
CHEMBL271811 Ki = 0.26 nM 9.59
CHEMBL270918 Ki = 0.27 nM 9.57
CHEMBL19019 NALTREXONE Ki = 0.3 nM 9.52
CHEMBL260528 Ki = 0.31 nM 9.51
CHEMBL429588 Ki = 0.38 nM 9.42
CHEMBL272051 Ki = 0.43 nM 9.37
CHEMBL443326 Ki = 0.43 nM 9.37
CHEMBL409036 Ki = 0.64 nM 9.19
CHEMBL272181 Ki = 0.67 nM 9.17
CHEMBL271755 Ki = 0.92 nM 9.04
CHEMBL982 NALMEFENE Ki = 0.91 nM 9.04
CHEMBL411916 Ki = 1.2 nM 8.92
CHEMBL406116 Ki = 1.49 nM 8.83
CHEMBL272021 Ki = 10.08 nM 8.00