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Assay Detail

CHEMBL892731

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

Binding
Displacement of [3H]deltorphin2 from delta opioid receptor in rat brain membrane
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Tissue Brain
Subcellular Membrane
Confidence 9 — Direct single protein target
Curated By Expert

Target

Delta-type opioid receptor (CHEMBL269)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Differential receptor binding characteristics of consecutive phenylalanines in micro-opioid specific peptide ligand endomorphin-2.
Honda T, Shirasu N, Isozaki K, Kawano M, Shigehiro D, Chuman Y, Fujita T, Nose T, Shimohigashi Y.
Bioorg Med Chem (2007) 15 : 3883 -3888
PubMed 17395470 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 18 5.14 6.14

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL38874 DAMGO 1 6.14
CHEMBL223552 1 5.50
CHEMBL316446 ENDOMORPHIN-1 1 5.45
CHEMBL242974 1 5.24
CHEMBL242980 1 5.09
CHEMBL333357 ENDOMORPHIN 2 1 4.99
CHEMBL242979 1 4.94
CHEMBL397448 1 4.93
CHEMBL438833 1 4.82
CHEMBL242981 1 4.26
CHEMBL242087 1 -
CHEMBL242089 1 -
CHEMBL242330 1 -
CHEMBL390914 1 -
CHEMBL242984 1 -
CHEMBL243200 1 -
CHEMBL243201 1 -
CHEMBL364703 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL38874 DAMGO IC50 = 727.0 nM 6.14
CHEMBL223552 IC50 = 3150.0 nM 5.50
CHEMBL316446 ENDOMORPHIN-1 IC50 = 3580.0 nM 5.45
CHEMBL242974 IC50 = 5720.0 nM 5.24
CHEMBL242980 IC50 = 8040.0 nM 5.09
CHEMBL333357 ENDOMORPHIN 2 IC50 = 10300.0 nM 4.99
CHEMBL242979 IC50 = 11400.0 nM 4.94
CHEMBL397448 IC50 = 11700.0 nM 4.93
CHEMBL438833 IC50 = 15200.0 nM 4.82
CHEMBL242981 IC50 = 54500.0 nM 4.26
CHEMBL242087 IC50 > 1000000.0 nM -
CHEMBL242089 IC50 > 1000000.0 nM -
CHEMBL242330 IC50 > 1000000.0 nM -
CHEMBL390914 IC50 > 1000000.0 nM -
CHEMBL242984 IC50 > 1000000.0 nM -
CHEMBL243200 IC50 > 1000000.0 nM -
CHEMBL243201 IC50 > 1000000.0 nM -
CHEMBL364703 IC50 > 1000000.0 nM -