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Assay Detail

CHEMBL3762646

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

Binding
Displacement of [3H]nor-BNI from KOR in Dunkin Hartley guinea pig brain homogenates 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
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Synthesis of mixed MOR/KOR efficacy cyclic opioid peptide analogs with antinociceptive activity after systemic administration.
Perlikowska R, Piekielna J, Gentilucci L, De Marco R, Cerlesi MC, Calo G, Artali R, Tömböly C, Kluczyk A, Janecka A.
Eur J Med Chem (2016) 109 : 276 -286
PubMed 26785295 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 6 7.53 8.99

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3759179 1 8.99
CHEMBL1927270 1 8.95
CHEMBL3759167 1 8.75
CHEMBL3758969 1 7.25
CHEMBL3759981 1 6.12
CHEMBL333357 ENDOMORPHIN 2 1 5.11

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3759179 Ki = 1.02 nM 8.99
CHEMBL1927270 Ki = 1.12 nM 8.95
CHEMBL3759167 Ki = 1.78 nM 8.75
CHEMBL3758969 Ki = 56.62 nM 7.25
CHEMBL3759981 Ki = 750.7 nM 6.12
CHEMBL333357 ENDOMORPHIN 2 Ki = 7827.67 nM 5.11