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Assay Detail

CHEMBL955667

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

Binding
Displacement of [3H]DAMGO from mu opioid receptor in rat brain membrane
5
Total Activities
5
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

Synthesis and in vitro evaluation of a library of modified endomorphin 1 peptides.
Koda Y, Del Borgo M, Wessling ST, Lazarus LH, Okada Y, Toth I, Blanchfield JT.
Bioorg Med Chem (2008) 16 : 6286 -6296
PubMed 18468445 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 5 8.48 10.17

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL412923 1 10.17
CHEMBL316446 ENDOMORPHIN-1 1 8.94
CHEMBL471806 1 8.54
CHEMBL505960 1 7.83
CHEMBL499141 1 6.94

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL412923 Ki = 0.067 nM 10.17
CHEMBL316446 ENDOMORPHIN-1 Ki = 1.15 nM 8.94
CHEMBL471806 Ki = 2.86 nM 8.54
CHEMBL505960 Ki = 14.8 nM 7.83
CHEMBL499141 Ki = 115.0 nM 6.94