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Assay Detail

CHEMBL4032004

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Functional
Agonist activity at recombinant human MOR expressed in CHO cell membranes after 60 mins by [35S]GTPgammaS binding assay
16
Total Activities
8
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
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
EC50 8 8.78 9.89
Activity 8 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4103328 2 9.89
CHEMBL607351 2 9.49
CHEMBL4065490 2 8.86
CHEMBL607405 2 8.84
CHEMBL4088589 2 8.53
CHEMBL326684 2 8.48
CHEMBL963 OXYMORPHONE 4.0 2 8.11
CHEMBL4074110 2 8.05

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4103328 EC50 = 0.13 nM 9.89
CHEMBL607351 EC50 = 0.32 nM 9.49
CHEMBL4065490 EC50 = 1.37 nM 8.86
CHEMBL607405 EC50 = 1.45 nM 8.84
CHEMBL4088589 EC50 = 2.95 nM 8.53
CHEMBL326684 EC50 = 3.28 nM 8.48
CHEMBL963 OXYMORPHONE EC50 = 7.8 nM 8.11
CHEMBL4074110 EC50 = 8.99 nM 8.05
CHEMBL963 OXYMORPHONE Activity - -
CHEMBL4074110 Activity - -
CHEMBL607405 Activity - -
CHEMBL4065490 Activity - -
CHEMBL607351 Activity - -
CHEMBL4103328 Activity - -
CHEMBL326684 Activity - -
CHEMBL4088589 Activity - -