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Assay Detail

CHEMBL4136378

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

Binding
Displacement of [125I]-Deltorphin II from mouse FLAG-tagged delta-type opioid receptor expressed in HEK293 cell membranes after 60 mins by gamma counting analysis
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Delta-type opioid receptor (CHEMBL3222)
Type SINGLE PROTEIN
Organism Mus musculus

Publication

χ-Space Screening of Dermorphin-Based Tetrapeptides through Use of Constrained Arylazepinone and Quinolinone Scaffolds.
Van der Poorten O, Van Den Hauwe R, Eiselt E, Betti C, Guillemyn K, Chung NN, Hallé F, Bihel F, Schiller PW, Tourwé D, Sarret P, Gendron L, Ballet S.
ACS Med Chem Lett (2017) 8 : 1177 -1182
PubMed 29152051 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 7.65 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4165323 1 9.00
CHEMBL4166388 1 8.83
CHEMBL4173234 1 8.68
CHEMBL4164236 1 7.22
CHEMBL4161890 1 6.82
CHEMBL4169811 1 6.78
CHEMBL4174890 1 6.20

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4165323 IC50 = 1.0 nM 9.00
CHEMBL4166388 IC50 = 1.47 nM 8.83
CHEMBL4173234 IC50 = 2.07 nM 8.68
CHEMBL4164236 IC50 = 60.7 nM 7.22
CHEMBL4161890 IC50 = 153.0 nM 6.82
CHEMBL4169811 IC50 = 167.0 nM 6.78
CHEMBL4174890 IC50 = 630.0 nM 6.20