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Assay Detail

CHEMBL1056142

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

Binding
Displacement of [3H]U69593 from human kappa opioid receptor expressed in CHO cells after 60 mins by liquid scintillation counting
12
Total Activities
12
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 Intermediate

Target

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

Publication

Univalent and bivalent ligands of butorphan: characteristics of the linking chain determine the affinity and potency of such opioid ligands.
Decker M, Fulton BS, Zhang B, Knapp BI, Bidlack JM, Neumeyer JL.
J Med Chem (2009) 52 : 7389 -7396
PubMed 19634902 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 12 9.17 10.31

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL147511 1 10.31
CHEMBL301160 BUTORPHAN 1 10.10
CHEMBL584791 1 9.89
CHEMBL566346 1 9.54
CHEMBL565679 1 9.38
CHEMBL584790 1 9.33
CHEMBL582930 1 9.21
CHEMBL566762 1 9.03
CHEMBL575031 1 8.66
CHEMBL584792 1 8.47
CHEMBL575647 1 8.33
CHEMBL573918 1 7.75

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL147511 Ki = 0.049 nM 10.31
CHEMBL301160 BUTORPHAN Ki = 0.079 nM 10.10
CHEMBL584791 Ki = 0.13 nM 9.89
CHEMBL566346 Ki = 0.29 nM 9.54
CHEMBL565679 Ki = 0.42 nM 9.38
CHEMBL584790 Ki = 0.47 nM 9.33
CHEMBL582930 Ki = 0.62 nM 9.21
CHEMBL566762 Ki = 0.94 nM 9.03
CHEMBL575031 Ki = 2.2 nM 8.66
CHEMBL584792 Ki = 3.4 nM 8.47
CHEMBL575647 Ki = 4.7 nM 8.33
CHEMBL573918 Ki = 18.0 nM 7.75