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Assay Detail

CHEMBL5046497

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

Functional
Agonist activity at human mu opioid receptor expressed in HEK293T cells assessed as arrestin-3 recruitment preincubated for 5 mins with coelenterazine followed by compound addition and measured after 10 mins by BRET assay
9
Total Activities
9
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type HEK293T
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Novel Dual-Target μ-Opioid Receptor and Dopamine D<sub>3</sub> Receptor Ligands as Potential Nonaddictive Pharmacotherapeutics for Pain Management.
Bonifazi A, Battiti FO, Sanchez J, Zaidi SA, Bow E, Makarova M, Cao J, Shaik AB, Sulima A, Rice KC, Katritch V, Canals M, Lane JR, Newman AH.
J Med Chem (2021) 64 : 7778 -7808
PubMed 34011153 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
pEC50 5 - -
EC50 4 7.05 7.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5080654 1 7.70
CHEMBL70 MORPHINE 4.0 1 7.10
CHEMBL5085974 1 7.08
CHEMBL5075990 1 6.32
CHEMBL5089655 1 -
CHEMBL5073754 1 -
CHEMBL5082465 1 -
CHEMBL5077114 1 -
CHEMBL5086564 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5080654 EC50 = 19.95 nM 7.70
CHEMBL70 MORPHINE EC50 = 79.43 nM 7.10
CHEMBL5085974 EC50 = 83.18 nM 7.08
CHEMBL5075990 EC50 = 478.63 nM 6.32
CHEMBL5089655 pEC50 - -
CHEMBL5073754 pEC50 - -
CHEMBL5082465 pEC50 - -
CHEMBL5077114 pEC50 - -
CHEMBL5086564 pEC50 - -