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Assay Detail

CHEMBL893242

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 membrane
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Expert

Target

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

Publication

In-vitro investigation of oxazol and urea analogues of morphinan at opioid receptors.
Peng X, Knapp BI, Bidlack JM, Neumeyer JL.
Bioorg Med Chem (2007) 15 : 4106 -4112
PubMed 17433695 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 14 8.31 10.21

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL49269 CYCLORPHAN 1 10.21
CHEMBL301160 BUTORPHAN 1 9.64
CHEMBL299220 1 8.89
CHEMBL242968 1 8.85
CHEMBL242756 1 8.82
CHEMBL394573 1 8.49
CHEMBL49143 1 8.43
CHEMBL390912 1 8.24
CHEMBL390866 1 8.15
CHEMBL428038 1 7.92
CHEMBL243195 1 7.66
CHEMBL242757 1 7.40
CHEMBL390911 1 6.82
CHEMBL242967 1 6.80

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL49269 CYCLORPHAN Ki = 0.062 nM 10.21
CHEMBL301160 BUTORPHAN Ki = 0.23 nM 9.64
CHEMBL299220 Ki = 1.3 nM 8.89
CHEMBL242968 Ki = 1.4 nM 8.85
CHEMBL242756 Ki = 1.5 nM 8.82
CHEMBL394573 Ki = 3.2 nM 8.49
CHEMBL49143 Ki = 3.7 nM 8.43
CHEMBL390912 Ki = 5.8 nM 8.24
CHEMBL390866 Ki = 7.1 nM 8.15
CHEMBL428038 Ki = 12.0 nM 7.92
CHEMBL243195 Ki = 22.0 nM 7.66
CHEMBL242757 Ki = 40.0 nM 7.40
CHEMBL390911 Ki = 150.0 nM 6.82
CHEMBL242967 Ki = 160.0 nM 6.80