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Assay Detail

CHEMBL5030192

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

Binding
Displacement of [3H]DPDPE from DOR in Wistar rat brain membranes measured after 3 hrs by scintillation counting method
8
Total Activities
8
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 Autocuration

Target

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

Publication

Novel Cyclic Endomorphin Analogues with Multiple Modifications and Oligoarginine Vector Exhibit Potent Antinociception with Reduced Opioid-like Side Effects.
Zhang YZ, Wang MM, Wang SY, Wang XF, Yang WJ, Zhao YN, Han FT, Zhang Y, Gu N, Wang CL.
J Med Chem (2021) 64 : 16801 -16819
PubMed 34781680 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 8 5.33 5.68

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5076581 1 5.68
CHEMBL5085104 1 5.37
CHEMBL316446 ENDOMORPHIN-1 1 5.21
CHEMBL333357 ENDOMORPHIN 2 1 5.06
CHEMBL5080666 1 -
CHEMBL5084034 1 -
CHEMBL5080233 1 -
CHEMBL5078349 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5076581 Ki = 2087.0 nM 5.68
CHEMBL5085104 Ki = 4274.0 nM 5.37
CHEMBL316446 ENDOMORPHIN-1 Ki = 6105.0 nM 5.21
CHEMBL333357 ENDOMORPHIN 2 Ki = 8770.0 nM 5.06
CHEMBL5080666 Ki > 10000.0 nM -
CHEMBL5084034 Ki > 10000.0 nM -
CHEMBL5080233 Ki > 10000.0 nM -
CHEMBL5078349 Ki > 10000.0 nM -