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Assay Detail

CHEMBL2156217

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

Binding
Displacement of [3H]naloxone from MOR in rat brain homogenates by liquid scintillation counting
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Superpotent [Dmt¹] dermorphin tetrapeptides containing the 4-aminotetrahydro-2-benzazepin-3-one scaffold with mixed μ/δ opioid receptor agonistic properties.
Vandormael B, Fourla DD, Gramowski-Voss A, Kosson P, Weiss DG, Schröder OH, Lipkowski A, Georgoussi Z, Tourwé D.
J Med Chem (2011) 54 : 7848 -7859
PubMed 21978284 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 8.74 9.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2151734 1 9.52
CHEMBL2151735 1 9.02
CHEMBL409225 1 7.68
CHEMBL260120 1 -
CHEMBL1834247 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2151734 IC50 = 0.3 nM 9.52
CHEMBL2151735 IC50 = 0.95 nM 9.02
CHEMBL409225 IC50 = 20.8 nM 7.68
CHEMBL260120 IC50 = 28.1 nM -
CHEMBL1834247 IC50 - -