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Assay Detail

CHEMBL751038

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

Binding
Competitive binding displacement analyses was performed from permanently transfected HEK293 cells expressing Opioid receptor kappa 1
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type HEK293
Confidence 8 — Homologous single protein target
Curated By Expert

Target

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

Publication

High-affinity, non-peptide agonists for the ORL1 (orphanin FQ/nociceptin) receptor.
Röver S, Adam G, Cesura AM, Galley G, Jenck F, Monsma FJ, Wichmann J, Dautzenberg FM.
J Med Chem (2000) 43 : 1329 -1338
PubMed 10753470 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 6 7.90 8.28

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL284414 1 8.28
CHEMBL28198 1 8.26
CHEMBL27460 1 7.97
CHEMBL26638 1 7.77
CHEMBL283432 1 7.76
CHEMBL27716 1 7.33

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL284414 Ki = 5.3 nM 8.28
CHEMBL28198 Ki = 5.5 nM 8.26
CHEMBL27460 Ki = 10.7 nM 7.97
CHEMBL26638 Ki = 17.0 nM 7.77
CHEMBL283432 Ki = 17.5 nM 7.76
CHEMBL27716 Ki = 46.3 nM 7.33