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Assay Detail

CHEMBL5253118

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Binding
Agonist activity at human kappa opioid receptor expressed in CHO-K1 cells assessed as ERK phosphorylation incubated for 2 hrs by Alphascreen surefire method
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type CHO-K1
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Conopeptide-Derived κ-Opioid Agonists (Conorphins): Potent, Selective, and Metabolic Stable Dynorphin A Mimetics with Antinociceptive Properties.
Brust A, Croker DE, Colless B, Ragnarsson L, Andersson Å, Jain K, Garcia-Caraballo S, Castro J, Brierley SM, Alewood PF, Lewis RJ.
J Med Chem (2016) 59 : 2381 -2395
PubMed 26859603 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 9 6.79 9.44

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5281912 1 9.44
CHEMBL5282326 1 9.21
CHEMBL5273273 1 9.02
CHEMBL5289642 1 6.35
CHEMBL5268886 1 5.96
CHEMBL5267287 1 5.80
CHEMBL5281790 1 5.23
CHEMBL5283510 1 5.13
CHEMBL5282726 1 5.01

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5281912 EC50 = 0.36 nM 9.44
CHEMBL5282326 EC50 = 0.62 nM 9.21
CHEMBL5273273 EC50 = 0.95 nM 9.02
CHEMBL5289642 EC50 = 450.0 nM 6.35
CHEMBL5268886 EC50 = 1105.0 nM 5.96
CHEMBL5267287 EC50 = 1580.0 nM 5.80
CHEMBL5281790 EC50 = 5864.0 nM 5.23
CHEMBL5283510 EC50 = 7486.0 nM 5.13
CHEMBL5282726 EC50 = 9848.0 nM 5.01