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Assay Detail

CHEMBL1036849

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

Binding
Displacement of [3H]DAMGO from mu opioid receptor in Wistar rat brain membrane
10
Total Activities
10
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

Biological activity of endomorphin and [Dmt1]endomorphin analogs with six-membered proline surrogates in position 2.
Perlikowska R, Gach K, Fichna J, Toth G, Walkowiak B, do-Rego JC, Janecka A.
Bioorg Med Chem (2009) 17 : 3789 -3794
PubMed 19435668 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 10 8.49 10.46

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL505175 1 10.46
CHEMBL505420 1 10.40
CHEMBL499209 1 9.42
CHEMBL316446 ENDOMORPHIN-1 1 9.37
CHEMBL333357 ENDOMORPHIN 2 1 9.16
CHEMBL503762 1 8.45
CHEMBL449143 1 7.69
CHEMBL452372 1 7.10
CHEMBL510205 1 6.44
CHEMBL510728 1 6.40

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL505175 IC50 = 0.035 nM 10.46
CHEMBL505420 IC50 = 0.04 nM 10.40
CHEMBL499209 IC50 = 0.38 nM 9.42
CHEMBL316446 ENDOMORPHIN-1 IC50 = 0.43 nM 9.37
CHEMBL333357 ENDOMORPHIN 2 IC50 = 0.69 nM 9.16
CHEMBL503762 IC50 = 3.55 nM 8.45
CHEMBL449143 IC50 = 20.4 nM 7.69
CHEMBL452372 IC50 = 79.95 nM 7.10
CHEMBL510205 IC50 = 360.0 nM 6.44
CHEMBL510728 IC50 = 400.6 nM 6.40