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Assay Detail

CHEMBL752147

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

Binding
Binding affinity against kappa opioid receptor from calf frontal cortex.
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Bos taurus
Confidence 8 — Homologous single protein target
Curated By Expert

Target

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

Publication

14 beta-[(p-nitrocinnamoyl)amino]morphinones, 14 beta-[(p-nitrocinnamoyl)amino]-7,8-dihydromorphinones, and their codeinone analogues: synthesis and receptor activity.
Sebastian A, Bidlack JM, Jiang Q, Deecher D, Teitler M, Glick SD, Archer S.
J Med Chem (1993) 36 : 3154 -3160
PubMed 7693944 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 17 7.41 8.35

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL110238 1 8.35
CHEMBL107157 1 8.30
CHEMBL607068 1 8.18
CHEMBL317035 1 7.97
CHEMBL611136 1 7.92
CHEMBL106189 1 7.59
CHEMBL106876 1 7.57
CHEMBL610885 1 7.41
CHEMBL108794 1 7.17
CHEMBL107164 1 6.94
CHEMBL108406 1 6.90
CHEMBL105827 1 6.79
CHEMBL110666 1 6.77
CHEMBL323430 1 6.74
CHEMBL413258 1 6.56
CHEMBL320060 1 -
CHEMBL327111 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL110238 IC50 = 4.5 nM 8.35
CHEMBL107157 IC50 = 5.01 nM 8.30
CHEMBL607068 IC50 = 6.6 nM 8.18
CHEMBL317035 IC50 = 10.8 nM 7.97
CHEMBL611136 IC50 = 12.1 nM 7.92
CHEMBL106189 IC50 = 25.5 nM 7.59
CHEMBL106876 IC50 = 27.2 nM 7.57
CHEMBL610885 IC50 = 39.1 nM 7.41
CHEMBL108794 IC50 = 68.0 nM 7.17
CHEMBL107164 IC50 = 116.0 nM 6.94
CHEMBL108406 IC50 = 126.0 nM 6.90
CHEMBL105827 IC50 = 162.0 nM 6.79
CHEMBL110666 IC50 = 171.0 nM 6.77
CHEMBL323430 IC50 = 184.0 nM 6.74
CHEMBL413258 IC50 = 274.0 nM 6.56
CHEMBL320060 IC50 > 1000.0 nM -
CHEMBL327111 IC50 > 1000.0 nM -