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Assay Detail

CHEMBL4038748

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

Binding
Displacement of [3H]U-69593 from recombinant human kappa opioid receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counter analysis
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Kappa-type opioid receptor (CHEMBL237)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Design and characterization of opioid ligands based on cycle-in-macrocycle scaffold.
Adamska-Bartłomiejczyk A, De Marco R, Gentilucci L, Kluczyk A, Janecka A.
Bioorg Med Chem (2017) 25 : 2399 -2405
PubMed 28318893 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 5 6.09 8.63

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1927270 1 8.63
CHEMBL4083221 1 6.05
CHEMBL4095366 1 5.33
CHEMBL4085033 1 5.26
CHEMBL4074931 1 5.17

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1927270 Ki = 2.36 nM 8.63
CHEMBL4083221 Ki = 884.0 nM 6.05
CHEMBL4095366 Ki = 4625.0 nM 5.33
CHEMBL4085033 Ki = 5461.0 nM 5.26
CHEMBL4074931 Ki = 6717.0 nM 5.17