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Assay Detail

CHEMBL3369378

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

Binding
Displacement of [3H]DAMGO from MOR in rat brain membranes
3
Total Activities
3
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

Mu-type opioid receptor (CHEMBL270)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Antinociceptive and antidepressant-like action of endomorphin-2 analogs with proline surrogates in position 2.
Perlikowska R, Piekielna J, Mazur M, Koralewski R, Olczak J, do Rego JC, Fichna J, Modranka J, Janecki T, Janecka A.
Bioorg Med Chem (2014) 22 : 4803 -4809
PubMed 25047937 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 8.90 9.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL333357 ENDOMORPHIN 2 1 9.10
CHEMBL3327220 1 9.07
CHEMBL3327221 1 8.54

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL333357 ENDOMORPHIN 2 IC50 = 0.79 nM 9.10
CHEMBL3327220 IC50 = 0.85 nM 9.07
CHEMBL3327221 IC50 = 2.91 nM 8.54