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Assay Detail

CHEMBL928097

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

Binding
Displacement of [3H]naloxone from mu opioid receptor in rat brain membrane
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

Blood-brain barrier penetration by two dermorphin tetrapeptide analogues: role of lipophilicity vs structural flexibility.
Ballet S, Misicka A, Kosson P, Lemieux C, Chung NN, Schiller PW, Lipkowski AW, Tourwé D.
J Med Chem (2008) 51 : 2571 -2574
PubMed 18370374 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 4.75 5.01

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL70 MORPHINE 4.0 1 5.01
CHEMBL409225 1 4.68
CHEMBL260120 1 4.55

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL70 MORPHINE IC50 = 9770.0 nM 5.01
CHEMBL409225 IC50 = 20800.0 nM 4.68
CHEMBL260120 IC50 = 28100.0 nM 4.55