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

CHEMBL748537

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

Binding
Inhibitory concentration against Opioid receptor kappa 1 using [3H]- U-69,593 radioligand
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Cavia porcellus
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

Kappa-type opioid receptor (CHEMBL3952)
Type SINGLE PROTEIN
Organism Cavia porcellus

Publication

Isothiocyanate-substituted benzyl ether opioid receptor ligands derived from 6 beta-naltrexol.
Davis RD, Nelson WL.
J Med Chem (1995) 38 : 570 -579
PubMed 7853350 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 11 8.25 9.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL19019 NALTREXONE 4.0 1 9.30
CHEMBL2112732 1 8.70
CHEMBL440765 U-69593 1 8.68
CHEMBL468469 1 8.59
CHEMBL152351 1 8.22
CHEMBL347674 1 8.13
CHEMBL345208 1 8.09
CHEMBL154510 1 7.77
CHEMBL352224 1 7.68
CHEMBL152327 1 7.37
CHEMBL31421 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL19019 NALTREXONE IC50 = 0.5 nM 9.30
CHEMBL2112732 IC50 = 2.0 nM 8.70
CHEMBL440765 U-69593 IC50 = 2.1 nM 8.68
CHEMBL468469 IC50 = 2.6 nM 8.59
CHEMBL152351 IC50 = 6.0 nM 8.22
CHEMBL347674 IC50 = 7.4 nM 8.13
CHEMBL345208 IC50 = 8.2 nM 8.09
CHEMBL154510 IC50 = 17.0 nM 7.77
CHEMBL352224 IC50 = 21.0 nM 7.68
CHEMBL152327 IC50 = 43.0 nM 7.37
CHEMBL31421 IC50 > 1000.0 nM -