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Assay Detail

CHEMBL757988

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Binding
Compound was evaluated for the binding affinity of Opioid receptor mu 1 by displacing the radioligand [3H]DAMGO from rat brain membrane
5
Total Activities
5
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
Ki 5 6.43 9.28

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL38874 DAMGO 1 9.28
CHEMBL3142988 1 6.14
CHEMBL2370579 1 5.84
CHEMBL2370515 1 5.79
CHEMBL2370605 1 5.12

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL38874 DAMGO Ki = 0.53 nM 9.28
CHEMBL3142988 Ki = 720.0 nM 6.14
CHEMBL2370579 Ki = 1440.0 nM 5.84
CHEMBL2370515 Ki = 1620.0 nM 5.79
CHEMBL2370605 Ki = 7540.0 nM 5.12