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Assay Detail

CHEMBL3390730

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

Binding
Displacement of [3H]DAMGO from MOR in Wistar rat brain membranes by liquid scintillation counting method
6
Total Activities
6
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 side-chain-linked opioid analogs utilizing cis- and trans-4-aminocyclohexyl-D-alanine.
Piekielna J, Gentilucci L, De Marco R, Perlikowska R, Adamska A, Olczak J, Mazur M, Artali R, Modranka J, Janecki T, Tömböly C, Janecka A.
Bioorg Med Chem (2014) 22 : 6545 -6551
PubMed 25456075 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 9.43 10.66

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3355781 1 10.66
CHEMBL3355780 1 10.40
CHEMBL1927270 1 9.25
CHEMBL333357 ENDOMORPHIN 2 1 9.10
CHEMBL3355779 1 8.68
CHEMBL3355778 1 8.49

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3355781 IC50 = 0.022 nM 10.66
CHEMBL3355780 IC50 = 0.04 nM 10.40
CHEMBL1927270 IC50 = 0.56 nM 9.25
CHEMBL333357 ENDOMORPHIN 2 IC50 = 0.79 nM 9.10
CHEMBL3355779 IC50 = 2.08 nM 8.68
CHEMBL3355778 IC50 = 3.2 nM 8.49