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Assay Detail

CHEMBL3636668

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

Binding
Displacement of [3H]DAMGO from rat mu-opioid receptor expressed in CHO cells after 90 mins by scintillation counter
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Cell Type CHO
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Structure-Activity Relationships of the Peptide Kappa Opioid Receptor Antagonist Zyklophin.
Joshi AA, Murray TF, Aldrich JV.
J Med Chem (2015) 58 : 8783 -8795
PubMed 26491810 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 17 5.37 6.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3634917 1 6.80
CHEMBL3634918 1 5.83
CHEMBL3634916 1 5.61
CHEMBL3632647 1 5.59
CHEMBL3634930 1 5.58
CHEMBL3634928 1 5.50
CHEMBL2372399 ZYKLOPHIN 1 5.36
CHEMBL3634929 1 5.08
CHEMBL3634921 1 5.07
CHEMBL3634922 1 4.97
CHEMBL3634920 1 4.96
CHEMBL3634919 1 4.96
CHEMBL3634927 1 4.95
CHEMBL3634925 1 4.94
CHEMBL3634923 1 -
CHEMBL3634924 1 -
CHEMBL3634926 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3634917 Ki = 157.0 nM 6.80
CHEMBL3634918 Ki = 1490.0 nM 5.83
CHEMBL3634916 Ki = 2440.0 nM 5.61
CHEMBL3632647 Ki = 2550.0 nM 5.59
CHEMBL3634930 Ki = 2610.0 nM 5.58
CHEMBL3634928 Ki = 3200.0 nM 5.50
CHEMBL2372399 ZYKLOPHIN Ki = 4380.0 nM 5.36
CHEMBL3634929 Ki = 8260.0 nM 5.08
CHEMBL3634921 Ki = 8470.0 nM 5.07
CHEMBL3634922 Ki = 10600.0 nM 4.97
CHEMBL3634920 Ki = 10900.0 nM 4.96
CHEMBL3634919 Ki = 11000.0 nM 4.96
CHEMBL3634927 Ki = 11300.0 nM 4.95
CHEMBL3634925 Ki = 11500.0 nM 4.94
CHEMBL3634923 Ki > 10000.0 nM -
CHEMBL3634924 Ki > 10000.0 nM -
CHEMBL3634926 Ki > 10000.0 nM -