Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL969336

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

Binding
Displacement of [3H]DAMGO from mu opioid receptor in human SH-SY5Y cells
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type SH-SY5Y
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Mu-type opioid receptor (CHEMBL233)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Internalisation of the mu-opioid receptor by endomorphin-1 and leu-enkephalin is dependant on aromatic amino acid residues.
Del Borgo MP, Blanchfield JT, Toth I.
Bioorg Med Chem (2008) 16 : 4341 -4346
PubMed 18329886 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 9 7.17 8.84

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL316446 ENDOMORPHIN-1 1 8.84
CHEMBL35838 [LEU5]ENKEPHALIN 1 7.94
CHEMBL504973 1 7.92
CHEMBL500212 1 7.43
CHEMBL512955 1 7.14
CHEMBL455502 1 6.95
CHEMBL387816 1 6.65
CHEMBL466147 1 6.15
CHEMBL445690 1 5.50

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL316446 ENDOMORPHIN-1 Ki = 1.45 nM 8.84
CHEMBL35838 [LEU5]ENKEPHALIN Ki = 11.4 nM 7.94
CHEMBL504973 Ki = 12.1 nM 7.92
CHEMBL500212 Ki = 37.3 nM 7.43
CHEMBL512955 Ki = 72.7 nM 7.14
CHEMBL455502 Ki = 112.5 nM 6.95
CHEMBL387816 Ki = 225.9 nM 6.65
CHEMBL466147 Ki = 705.0 nM 6.15
CHEMBL445690 Ki = 3190.0 nM 5.50