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Assay Detail

CHEMBL1019883

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

Binding
Displacement of [3H]U69593 form kappa opioid receptor in guinea pig brain
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Cavia porcellus
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Kappa-type opioid receptor (CHEMBL3952)
Type SINGLE PROTEIN
Organism Cavia porcellus

Publication

Syntheses and opioid receptor binding properties of carboxamido-substituted opioids.
Wentland MP, Lou R, Lu Q, Bu Y, VanAlstine MA, Cohen DJ, Bidlack JM.
Bioorg Med Chem Lett (2009) 19 : 203 -208
PubMed 19027293 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 10 8.69 10.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2367604 1 10.05
CHEMBL517166 1 10.05
CHEMBL55033 1 9.21
CHEMBL461229 1 9.15
CHEMBL2107292 KETAZOCINE 2.0 1 9.00
CHEMBL464071 1 8.82
CHEMBL511691 1 8.74
CHEMBL459746 1 8.55
CHEMBL70 MORPHINE 4.0 1 7.62
CHEMBL505011 1 5.70

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2367604 Ki = 0.09 nM 10.05
CHEMBL517166 Ki = 0.089 nM 10.05
CHEMBL55033 Ki = 0.62 nM 9.21
CHEMBL461229 Ki = 0.7 nM 9.15
CHEMBL2107292 KETAZOCINE Ki = 1.0 nM 9.00
CHEMBL464071 Ki = 1.5 nM 8.82
CHEMBL511691 Ki = 1.8 nM 8.74
CHEMBL459746 Ki = 2.8 nM 8.55
CHEMBL70 MORPHINE Ki = 24.0 nM 7.62
CHEMBL505011 Ki = 2000.0 nM 5.70