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

CHEMBL907191

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

Functional
Activity at human recombinant kappa opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S binding
23
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type CHO
Confidence 9 — Direct single protein target
Curated By Expert

Target

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

Publication

Structural determinants of opioid activity in derivatives of 14-aminomorphinones: effects of changes to the chain linking of the C14-amino group to the aryl ring.
Rennison D, Moynihan H, Traynor JR, Lewis JW, Husbands SM.
J Med Chem (2006) 49 : 6104 -6110
PubMed 17004724 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 23 8.09 10.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL386492 CLOCINNAMOX 1 10.00
CHEMBL217395 1 9.54
CHEMBL217658 1 9.47
CHEMBL217102 1 9.36
CHEMBL217479 1 9.23
CHEMBL448428 1 8.95
CHEMBL19019 NALTREXONE 4.0 1 8.73
CHEMBL384497 1 8.73
CHEMBL216558 1 8.46
CHEMBL277530 1 8.04
CHEMBL386272 1 8.01
CHEMBL217710 1 7.86
CHEMBL383896 1 7.78
CHEMBL263482 1 7.70
CHEMBL217790 1 7.58
CHEMBL387101 1 7.36
CHEMBL216365 1 6.97
CHEMBL215926 1 6.70
CHEMBL411089 1 6.68
CHEMBL384118 1 6.41
CHEMBL387016 1 6.39
CHEMBL267027 1 -
CHEMBL443311 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL386492 CLOCINNAMOX IC50 = 0.1 nM 10.00
CHEMBL217395 IC50 = 0.29 nM 9.54
CHEMBL217658 IC50 = 0.34 nM 9.47
CHEMBL217102 IC50 = 0.44 nM 9.36
CHEMBL217479 IC50 = 0.59 nM 9.23
CHEMBL448428 IC50 = 1.12 nM 8.95
CHEMBL19019 NALTREXONE IC50 = 1.86 nM 8.73
CHEMBL384497 IC50 = 1.87 nM 8.73
CHEMBL216558 IC50 = 3.45 nM 8.46
CHEMBL277530 IC50 = 9.07 nM 8.04
CHEMBL386272 IC50 = 9.81 nM 8.01
CHEMBL217710 IC50 = 13.8 nM 7.86
CHEMBL383896 IC50 = 16.7 nM 7.78
CHEMBL263482 IC50 = 20.2 nM 7.70
CHEMBL217790 IC50 = 26.2 nM 7.58
CHEMBL387101 IC50 = 43.4 nM 7.36
CHEMBL216365 IC50 = 106.0 nM 6.97
CHEMBL215926 IC50 = 202.0 nM 6.70
CHEMBL411089 IC50 = 208.0 nM 6.68
CHEMBL384118 IC50 = 387.0 nM 6.41
CHEMBL387016 IC50 = 410.0 nM 6.39
CHEMBL267027 IC50 = 0.003 nM -
CHEMBL443311 IC50 = 0.006 nM -