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Assay Detail

CHEMBL3637629

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Binding
Binding affinity to kappa opioid receptor (unknown origin)
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

Conformationally restricted κ-opioid receptor agonists: Synthesis and pharmacological evaluation of diastereoisomeric and enantiomeric decahydroquinoxalines.
Molenveld P, Bouzanne des Mazery R, Sterk GJ, Storcken RP, Autar R, van Oss B, van der Haas RN, Fröhlich R, Schepmann D, Wünsch B, Soeberdt M.
Bioorg Med Chem Lett (2015) 25 : 5326 -5330
PubMed 26411794 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 5 6.73 8.03

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3299005 1 8.03
CHEMBL267495 NALFURAFINE 4.0 1 6.77
CHEMBL58033 (-)-U-50488 1 6.47
CHEMBL603370 1 6.44
CHEMBL3634396 1 5.92

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3299005 Ki = 9.4 nM 8.03
CHEMBL267495 NALFURAFINE Ki = 170.0 nM 6.77
CHEMBL58033 (-)-U-50488 Ki = 340.0 nM 6.47
CHEMBL603370 Ki = 360.0 nM 6.44
CHEMBL3634396 Ki = 1200.0 nM 5.92