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Assay Detail

CHEMBL945979

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

Binding
Displacement of [3H]DAMGO from mu opioid receptor in rat brain membranes
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Novel highly potent mu-opioid receptor antagonist based on endomorphin-2 structure.
Fichna J, do-Rego JC, Janecki T, Staniszewska R, Poels J, Broeck JV, Costentin J, Schiller PW, Janecka A.
Bioorg Med Chem Lett (2008) 18 : 1350 -1353
PubMed 18207400 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 8.68 11.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL254927 1 11.00
CHEMBL333357 ENDOMORPHIN 2 1 9.10
CHEMBL254919 1 8.82
CHEMBL254926 1 5.81

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL254927 IC50 = 0.01 nM 11.00
CHEMBL333357 ENDOMORPHIN 2 IC50 = 0.79 nM 9.10
CHEMBL254919 IC50 = 1.52 nM 8.82
CHEMBL254926 IC50 = 1560.0 nM 5.81