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Assay Detail

CHEMBL1022992

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
7
Total Activities
7
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

14 beta-O-cinnamoylnaltrexone and related dihydrocodeinones are mu opioid receptor partial agonists with predominant antagonist activity.
Moynihan H, Jales AR, Greedy BM, Rennison D, Broadbear JH, Purington L, Traynor JR, Woods JH, Lewis JW, Husbands SM.
J Med Chem (2009) 52 : 1553 -1557
PubMed 19253983 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 7 8.78 9.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL19019 NALTREXONE 4.0 1 9.70
CHEMBL514774 1 9.47
CHEMBL474755 1 8.60
CHEMBL386492 CLOCINNAMOX 1 8.52
CHEMBL512526 1 8.46
CHEMBL471543 1 8.38
CHEMBL386272 1 8.32

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL19019 NALTREXONE Ki = 0.2 nM 9.70
CHEMBL514774 Ki = 0.34 nM 9.47
CHEMBL474755 Ki = 2.5 nM 8.60
CHEMBL386492 CLOCINNAMOX Ki = 3.0 nM 8.52
CHEMBL512526 Ki = 3.5 nM 8.46
CHEMBL471543 Ki = 4.2 nM 8.38
CHEMBL386272 Ki = 4.8 nM 8.32