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Assay Detail

CHEMBL3268177

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

Functional
Antagonist activity at kappa opioid receptor in guinea pig caudate assessed as inhibition of U69593-stimulated [35S]-GTP[gammaS] binding
9
Total Activities
9
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
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

Antagonists of the kappa opioid receptor.
Urbano M, Guerrero M, Rosen H, Roberts E.
Bioorg Med Chem Lett (2014) 24 : 2021 -2032
PubMed 24690494 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ke 8 - -
Ki 1 10.70 10.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL415247 JDTIC 1.0 1 10.70
CHEMBL10986 1 -
CHEMBL3264437 1 -
CHEMBL2111681 1 -
CHEMBL326471 1 -
CHEMBL10872 1 -
CHEMBL2112472 1 -
CHEMBL3264438 1 -
CHEMBL575508 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL415247 JDTIC Ki = 0.02 nM 10.70
CHEMBL10986 Ke = 4.7 nM -
CHEMBL3264437 Ke = 44.6 nM -
CHEMBL2111681 Ke = 30.0 nM -
CHEMBL326471 Ke = 4.2 nM -
CHEMBL10872 Ke = 11.5 nM -
CHEMBL2112472 Ke = 19.6 nM -
CHEMBL3264438 Ke = 0.16 nM -
CHEMBL575508 Ke = 0.37 nM -