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Assay Detail

CHEMBL4371532

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

Binding
Agonist activity at human kappa opioid receptor expressed in human U2OS cells assessed as increase in ERK1/2 phosphorylation after 10 mins by Western blot analysis
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type U2OS
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Biased Ligands of G Protein-Coupled Receptors (GPCRs): Structure-Functional Selectivity Relationships (SFSRs) and Therapeutic Potential.
Tan L, Yan W, McCorvy JD, Cheng J.
J Med Chem (2018) 61 : 9841 -9878
PubMed 29939744 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 2 7.38 8.27

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL440765 U-69593 1 8.27
CHEMBL4458783 1 6.48

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL440765 U-69593 EC50 = 5.4 nM 8.27
CHEMBL4458783 EC50 = 329.0 nM 6.48