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Assay Detail

CHEMBL4058231

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

Binding
Displacement of [3H]-(+)-U69,593 from KOR in guinea pig brain membranes by liquid scintillation counting analysis
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Development of novel LP1-based analogues with enhanced delta opioid receptor profile.
Pasquinucci L, Turnaturi R, Prezzavento O, Arena E, Aricò G, Georgoussi Z, Parenti R, Cantarella G, Parenti C.
Bioorg Med Chem (2017) 25 : 4745 -4752
PubMed 28734666 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 6 7.53 8.65

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4079574 1 8.65
CHEMBL4066846 1 8.14
CHEMBL4077833 1 7.98
CHEMBL4102093 1 7.82
CHEMBL3759092 1 6.96
CHEMBL4060120 1 5.64

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4079574 Ki = 2.22 nM 8.65
CHEMBL4066846 Ki = 7.3 nM 8.14
CHEMBL4077833 Ki = 10.51 nM 7.98
CHEMBL4102093 Ki = 15.22 nM 7.82
CHEMBL3759092 Ki = 110.0 nM 6.96
CHEMBL4060120 Ki = 2276.0 nM 5.64