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Assay Detail

CHEMBL751070

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

Binding
Inhibitory concentration against [3H]DAMGO binding to Opioid receptor mu 1 in rat brain membrane
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Beta-casomorphins: substitution of phenylalanine with beta-homo phenylalanine increases the mu-type opioid receptor affinity.
Longobardo L, Melck D, Siciliano R, Santini A, Di Marzo V, Cammarota G.
Bioorg Med Chem Lett (2000) 10 : 1185 -1188
PubMed 10866377 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 5.29 5.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3142988 1 5.70
CHEMBL2370579 1 5.40
CHEMBL2370515 1 5.35
CHEMBL2370605 1 4.70

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3142988 IC50 = 2000.0 nM 5.70
CHEMBL2370579 IC50 = 4000.0 nM 5.40
CHEMBL2370515 IC50 = 4500.0 nM 5.35
CHEMBL2370605 IC50 = 20000.0 nM 4.70