Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL4032001

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

Binding
Displacement of [3H]-HS665 from recombinant human KOR expressed in CHO cell membranes after 30 mins by liquid scintillation counting
8
Total Activities
8
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

Synthesis, Pharmacology, and Molecular Docking Studies on 6-Desoxo-N-methylmorphinans as Potent μ-Opioid Receptor Agonists.
Dumitrascuta M, Ben Haddou T, Guerrieri E, Noha SM, Schläfer L, Schmidhammer H, Spetea M.
J Med Chem (2017) 60 : 9407 -9412
PubMed 29053268 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 8 8.20 9.07

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4103328 1 9.07
CHEMBL607351 1 8.90
CHEMBL4065490 1 8.40
CHEMBL4088589 1 8.10
CHEMBL607405 1 8.00
CHEMBL326684 1 7.82
CHEMBL4074110 1 7.67
CHEMBL963 OXYMORPHONE 4.0 1 7.60

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4103328 Ki = 0.85 nM 9.07
CHEMBL607351 Ki = 1.27 nM 8.90
CHEMBL4065490 Ki = 3.99 nM 8.40
CHEMBL4088589 Ki = 7.92 nM 8.10
CHEMBL607405 Ki = 10.1 nM 8.00
CHEMBL326684 Ki = 15.1 nM 7.82
CHEMBL4074110 Ki = 21.6 nM 7.67
CHEMBL963 OXYMORPHONE Ki = 25.3 nM 7.60