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Assay Detail

CHEMBL5033288

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

Binding
Displacement of [3H]-diprenorphine from mouse KOR expressed in HEK293 cell membranes by radioligand binding assay relative to control
21
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Mus musculus
Cell Type HEK293
Subcellular Cell membrane
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
Ki 21 6.73 9.51

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL415330 1 9.51
CHEMBL5071625 1 7.68
CHEMBL5070568 1 7.01
CHEMBL5077697 2 6.92
CHEMBL5091699 1 6.77
CHEMBL5070898 1 6.66
CHEMBL5087018 1 6.66
CHEMBL5088478 1 6.19
CHEMBL5075196 1 5.64
CHEMBL5093924 1 5.60
CHEMBL5079877 1 5.50
CHEMBL5087338 1 -
CHEMBL5076587 1 -
CHEMBL5076021 1 -
CHEMBL5081959 1 -
CHEMBL5070737 1 -
CHEMBL5083929 1 -
CHEMBL5075574 1 -
CHEMBL5080221 1 -
CHEMBL453539 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL415330 Ki = 0.31 nM 9.51
CHEMBL5071625 Ki = 21.0 nM 7.68
CHEMBL5070568 Ki = 97.0 nM 7.01
CHEMBL5077697 Ki = 120.0 nM 6.92
CHEMBL5091699 Ki = 170.0 nM 6.77
CHEMBL5070898 Ki = 220.0 nM 6.66
CHEMBL5087018 Ki = 220.0 nM 6.66
CHEMBL5077697 Ki = 250.0 nM 6.60
CHEMBL5088478 Ki = 650.0 nM 6.19
CHEMBL5075196 Ki = 2300.0 nM 5.64
CHEMBL5093924 Ki = 2500.0 nM 5.60
CHEMBL5079877 Ki = 3200.0 nM 5.50
CHEMBL5087338 Ki > 10000.0 nM -
CHEMBL5076587 Ki > 10000.0 nM -
CHEMBL5076021 Ki > 10000.0 nM -
CHEMBL5081959 Ki > 10000.0 nM -
CHEMBL5070737 Ki > 10000.0 nM -
CHEMBL5083929 Ki > 10000.0 nM -
CHEMBL5075574 Ki > 10000.0 nM -
CHEMBL5080221 Ki > 10000.0 nM -
CHEMBL453539 Ki > 30000.0 nM -