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Assay Detail

CHEMBL4193818

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

Binding
Displacement of [3H]DAMGO from MOR in Wistar rat whole brain membranes after 45 mins by liquid scintillation counting method
5
Total Activities
5
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

Cyclic Biphalin Analogues Incorporating a Xylene Bridge: Synthesis, Characterization, and Biological Profile.
Stefanucci A, Carotenuto A, Macedonio G, Novellino E, Pieretti S, Marzoli F, Szűcs E, Erdei AI, Zádor F, Benyhe S, Mollica A.
ACS Med Chem Lett (2017) 8 : 858 -863
PubMed 28835802 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 5 8.75 9.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL200199 BIPHALIN 1 9.10
CHEMBL4213910 1 8.88
CHEMBL4209510 1 8.79
CHEMBL4204649 1 8.76
CHEMBL4217792 1 8.22

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL200199 BIPHALIN Ki = 0.79 nM 9.10
CHEMBL4213910 Ki = 1.33 nM 8.88
CHEMBL4209510 Ki = 1.61 nM 8.79
CHEMBL4204649 Ki = 1.73 nM 8.76
CHEMBL4217792 Ki = 6.06 nM 8.22