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Assay Detail

CHEMBL5033291

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

Functional
Agonist activity at mouse KOR expressed in HEK293 cell assessed as inhibition of cAMP concentration incubated for 1 hrs by time-resolved fluorescence resonance energy transfer assay
21
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Mus musculus
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Kappa-type opioid receptor (CHEMBL4329)
Type SINGLE PROTEIN
Organism Mus musculus

Publication

Design of a Stable Cyclic Peptide Analgesic Derived from Sunflower Seeds that Targets the κ-Opioid Receptor for the Treatment of Chronic Abdominal Pain.
Muratspahić E, Tomašević N, Koehbach J, Duerrauer L, Hadžić S, Castro J, Schober G, Sideromenos S, Clark RJ, Brierley SM, Craik DJ, Gruber CW.
J Med Chem (2021) 64 : 9042 -9055
PubMed 34162205 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 21 6.37 8.55

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL415330 1 8.55
CHEMBL5071625 1 7.35
CHEMBL5070568 1 5.89
CHEMBL5079877 1 5.85
CHEMBL5075196 1 5.82
CHEMBL5070898 1 5.77
CHEMBL5093924 1 5.33
CHEMBL453539 1 -
CHEMBL5080221 1 -
CHEMBL5075574 1 -
CHEMBL5083929 1 -
CHEMBL5070737 1 -
CHEMBL5081959 1 -
CHEMBL5076021 1 -
CHEMBL5076587 1 -
CHEMBL5087018 1 -
CHEMBL5091699 1 -
CHEMBL5077697 2 -
CHEMBL5088478 1 -
CHEMBL5087338 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL415330 EC50 = 2.8 nM 8.55
CHEMBL5071625 EC50 = 45.0 nM 7.35
CHEMBL5070568 EC50 = 1300.0 nM 5.89
CHEMBL5079877 EC50 = 1400.0 nM 5.85
CHEMBL5075196 EC50 = 1500.0 nM 5.82
CHEMBL5070898 EC50 = 1700.0 nM 5.77
CHEMBL5093924 EC50 = 4700.0 nM 5.33
CHEMBL453539 EC50 - -
CHEMBL5080221 EC50 - -
CHEMBL5075574 EC50 - -
CHEMBL5083929 EC50 - -
CHEMBL5070737 EC50 - -
CHEMBL5081959 EC50 - -
CHEMBL5076021 EC50 - -
CHEMBL5076587 EC50 - -
CHEMBL5087018 EC50 - -
CHEMBL5091699 EC50 - -
CHEMBL5077697 EC50 - -
CHEMBL5077697 EC50 - -
CHEMBL5088478 EC50 - -
CHEMBL5087338 EC50 - -