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Assay Detail

CHEMBL955666

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 SHSY5Y cells
12
Total Activities
12
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

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 12 8.08 10.23

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL412923 1 10.23
CHEMBL509528 1 10.09
CHEMBL316446 ENDOMORPHIN-1 1 8.96
CHEMBL471806 1 8.67
CHEMBL510939 1 8.54
CHEMBL500704 1 8.52
CHEMBL505960 1 7.81
CHEMBL499141 1 6.94
CHEMBL503367 1 6.92
CHEMBL446814 1 6.83
CHEMBL451830 1 6.82
CHEMBL526349 1 6.58

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL412923 Ki = 0.059 nM 10.23
CHEMBL509528 Ki = 0.081 nM 10.09
CHEMBL316446 ENDOMORPHIN-1 Ki = 1.11 nM 8.96
CHEMBL471806 Ki = 2.15 nM 8.67
CHEMBL510939 Ki = 2.92 nM 8.54
CHEMBL500704 Ki = 3.02 nM 8.52
CHEMBL505960 Ki = 15.4 nM 7.81
CHEMBL499141 Ki = 115.0 nM 6.94
CHEMBL503367 Ki = 121.0 nM 6.92
CHEMBL446814 Ki = 148.0 nM 6.83
CHEMBL451830 Ki = 151.0 nM 6.82
CHEMBL526349 Ki = 266.0 nM 6.58