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Assay Detail

CHEMBL887389

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

Binding
Displacement of [3H]U-69593 from human kappa opioid receptors expressed in CHO cell membrane
13
Total Activities
13
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 Expert

Target

Kappa-type opioid receptor (CHEMBL237)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

High-affinity carbamate analogues of morphinan at opioid receptors.
Peng X, Knapp BI, Bidlack JM, Neumeyer JL.
Bioorg Med Chem Lett (2007) 17 : 1508 -1511
PubMed 17276685 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 13 9.30 10.47

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL49269 CYCLORPHAN 1 10.47
CHEMBL397035 1 10.34
CHEMBL242048 1 10.29
CHEMBL301160 BUTORPHAN 1 10.10
CHEMBL263096 1 9.85
CHEMBL427862 1 9.85
CHEMBL394624 1 9.52
CHEMBL242046 1 9.09
CHEMBL592 LEVORPHANOL 4.0 1 8.64
CHEMBL245049 1 8.48
CHEMBL241824 1 8.47
CHEMBL242047 1 8.37
CHEMBL241823 1 7.44

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL49269 CYCLORPHAN Ki = 0.034 nM 10.47
CHEMBL397035 Ki = 0.046 nM 10.34
CHEMBL242048 Ki = 0.051 nM 10.29
CHEMBL301160 BUTORPHAN Ki = 0.079 nM 10.10
CHEMBL263096 Ki = 0.14 nM 9.85
CHEMBL427862 Ki = 0.14 nM 9.85
CHEMBL394624 Ki = 0.3 nM 9.52
CHEMBL242046 Ki = 0.81 nM 9.09
CHEMBL592 LEVORPHANOL Ki = 2.3 nM 8.64
CHEMBL245049 Ki = 3.3 nM 8.48
CHEMBL241824 Ki = 3.4 nM 8.47
CHEMBL242047 Ki = 4.3 nM 8.37
CHEMBL241823 Ki = 36.0 nM 7.44