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Assay Detail

CHEMBL893243

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

Binding
Displacement of [3H]U69,593 from human kappa 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

Kappa-type opioid receptor (CHEMBL237)
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 8.83 10.47

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL49269 CYCLORPHAN 1 10.47
CHEMBL242756 1 10.31
CHEMBL301160 BUTORPHAN 1 10.10
CHEMBL299220 1 9.74
CHEMBL242968 1 9.21
CHEMBL390866 1 9.10
CHEMBL49143 1 8.74
CHEMBL390912 1 8.72
CHEMBL428038 1 8.64
CHEMBL242757 1 8.18
CHEMBL394573 1 8.05
CHEMBL243195 1 7.70
CHEMBL242967 1 7.33
CHEMBL390911 1 7.28

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL49269 CYCLORPHAN Ki = 0.034 nM 10.47
CHEMBL242756 Ki = 0.049 nM 10.31
CHEMBL301160 BUTORPHAN Ki = 0.079 nM 10.10
CHEMBL299220 Ki = 0.18 nM 9.74
CHEMBL242968 Ki = 0.61 nM 9.21
CHEMBL390866 Ki = 0.79 nM 9.10
CHEMBL49143 Ki = 1.8 nM 8.74
CHEMBL390912 Ki = 1.9 nM 8.72
CHEMBL428038 Ki = 2.3 nM 8.64
CHEMBL242757 Ki = 6.6 nM 8.18
CHEMBL394573 Ki = 8.9 nM 8.05
CHEMBL243195 Ki = 20.0 nM 7.70
CHEMBL242967 Ki = 47.0 nM 7.33
CHEMBL390911 Ki = 52.0 nM 7.28