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Assay Detail

CHEMBL755495

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

Binding
In vitro binding affinity against Opioid receptor kappa 1 in rat brain homogenates.
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Tissue Brain
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

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

Publication

3-Alkyl ethers of clocinnamox: delayed long-term mu-antagonists with variable mu efficacy.
Husbands SM, Sadd J, Broadbear JH, Woods JH, Martin J, Traynor JR, Aceto MD, Bowman ER, Harris LS, Lewis JW.
J Med Chem (1998) 41 : 3493 -3498
PubMed 9719602 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 8 7.62 8.27

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL386492 CLOCINNAMOX 1 8.27
CHEMBL610543 1 7.83
CHEMBL610544 1 7.75
CHEMBL610030 1 7.75
CHEMBL610546 1 7.72
CHEMBL610028 1 7.72
CHEMBL610286 1 7.02
CHEMBL610287 1 6.88

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL386492 CLOCINNAMOX Ki = 5.4 nM 8.27
CHEMBL610543 Ki = 14.9 nM 7.83
CHEMBL610544 Ki = 17.9 nM 7.75
CHEMBL610030 Ki = 18.0 nM 7.75
CHEMBL610546 Ki = 19.1 nM 7.72
CHEMBL610028 Ki = 19.1 nM 7.72
CHEMBL610286 Ki = 95.4 nM 7.02
CHEMBL610287 Ki = 131.2 nM 6.88