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Assay Detail

CHEMBL4371545

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

Binding
Agonist activity at GFP-tagged rat kappa opioid receptor expressed in HEK293 cells assessed as increase in ERK1/2 phosphorylation after 5 mins by Western blot analysis
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Kappa-type opioid receptor (CHEMBL3614)
Type SINGLE PROTEIN
Organism Rattus norvegicus

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 1 9.30 9.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL267495 NALFURAFINE 4.0 1 9.30

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL267495 NALFURAFINE EC50 = 0.5 nM 9.30