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Assay Detail

CHEMBL4031999

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

Binding
Displacement of [3H]-DAMGO from recombinant human MOR expressed in CHO cell membranes after 60 mins by liquid scintillation counting
16
Total Activities
8
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Synthesis, Pharmacology, and Molecular Docking Studies on 6-Desoxo-N-methylmorphinans as Potent μ-Opioid Receptor Agonists.
Dumitrascuta M, Ben Haddou T, Guerrieri E, Noha SM, Schläfer L, Schmidhammer H, Spetea M.
J Med Chem (2017) 60 : 9407 -9412
PubMed 29053268 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 8 9.42 10.32
Inhibition 8 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4103328 2 10.32
CHEMBL4065490 2 9.62
CHEMBL326684 2 9.60
CHEMBL607405 2 9.49
CHEMBL4088589 2 9.47
CHEMBL607351 2 9.35
CHEMBL4074110 2 8.78
CHEMBL963 OXYMORPHONE 4.0 2 8.75

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4103328 Ki = 0.048 nM 10.32
CHEMBL4065490 Ki = 0.24 nM 9.62
CHEMBL326684 Ki = 0.25 nM 9.60
CHEMBL607405 Ki = 0.32 nM 9.49
CHEMBL4088589 Ki = 0.34 nM 9.47
CHEMBL607351 Ki = 0.45 nM 9.35
CHEMBL4074110 Ki = 1.65 nM 8.78
CHEMBL963 OXYMORPHONE Ki = 1.79 nM 8.75
CHEMBL963 OXYMORPHONE Inhibition - % -
CHEMBL4074110 Inhibition - % -
CHEMBL607405 Inhibition - % -
CHEMBL4065490 Inhibition - % -
CHEMBL607351 Inhibition - % -
CHEMBL4103328 Inhibition - % -
CHEMBL326684 Inhibition - % -
CHEMBL4088589 Inhibition - % -