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Assay Detail

CHEMBL751053

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

Binding
Concentration required for inhibition of [3H]DAMGO binding to Opioid receptor mu 1 in rat brain membranes
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Tissue Brain
Subcellular Brain membranes
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

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

Publication

Synthesis and binding activity of endomorphin-1 analogues containing beta-amino acids.
Cardillo G, Gentilucci L, Melchiorre P, Spampinato S.
Bioorg Med Chem Lett (2000) 10 : 2755 -2758
PubMed 11133084 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 7.27 8.74

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL313820 1 8.74
CHEMBL38874 DAMGO 1 8.01
CHEMBL316446 ENDOMORPHIN-1 1 7.25
CHEMBL316447 1 7.14
CHEMBL329996 1 6.33
CHEMBL92693 1 6.17

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL313820 IC50 = 1.8 nM 8.74
CHEMBL38874 DAMGO IC50 = 9.89 nM 8.01
CHEMBL316446 ENDOMORPHIN-1 IC50 = 56.0 nM 7.25
CHEMBL316447 IC50 = 72.0 nM 7.14
CHEMBL329996 IC50 = 470.0 nM 6.33
CHEMBL92693 IC50 = 680.0 nM 6.17