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Assay Detail

CHEMBL3399796

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

Binding
Displacement of [3H]U69593 from rat recombinant kappa opioid receptor expressed in CHO cells after 60 mins
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Cell Type CHO
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Kappa-type opioid receptor (CHEMBL3614)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Novel fluoroalkyl derivatives of selective kappa opioid receptor antagonist JDTic: Design, synthesis, pharmacology and molecular modeling studies.
Schmitt S, Colloc'h N, Perrio C.
Eur J Med Chem (2015) 90 : 742 -750
PubMed 25513968 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 8 8.62 9.49

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL415247 JDTIC 1.0 1 9.49
CHEMBL58033 (-)-U-50488 1 9.44
CHEMBL3397594 1 8.79
CHEMBL3397593 1 8.26
CHEMBL3397596 1 8.09
CHEMBL3397595 1 7.62
CHEMBL19019 NALTREXONE 4.0 1 -
CHEMBL31421 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL415247 JDTIC Ki = 0.32 nM 9.49
CHEMBL58033 (-)-U-50488 Ki = 0.36 nM 9.44
CHEMBL3397594 Ki = 1.62 nM 8.79
CHEMBL3397593 Ki = 5.51 nM 8.26
CHEMBL3397596 Ki = 8.19 nM 8.09
CHEMBL3397595 Ki = 24.01 nM 7.62
CHEMBL19019 NALTREXONE Ki - -
CHEMBL31421 Ki - -