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Assay Detail

CHEMBL4409283

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

Binding
Inhibition of mu opioid receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of forskolin-stimulated beta arrestin 2 recruitment preincubated for 30 mins followed by forskolin-stimulation and measured after 60 mins
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Progress in the development of more effective and safer analgesics for pain management.
Turnaturi R, Chiechio S, Salerno L, Rescifina A, Pittalà V, Cantarella G, Tomarchio E, Parenti C, Pasquinucci L.
Eur J Med Chem (2019) 183 : 111701 -111701
PubMed 31550662 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 7 7.06 7.28

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4467777 1 7.28
CHEMBL4533745 1 7.28
CHEMBL4577586 1 7.28
CHEMBL4581231 1 7.28
CHEMBL4456635 1 7.28
CHEMBL4530626 1 6.69
CHEMBL4462475 1 6.34

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4467777 EC50 = 52.41 nM 7.28
CHEMBL4533745 EC50 = 52.41 nM 7.28
CHEMBL4577586 EC50 = 52.41 nM 7.28
CHEMBL4581231 EC50 = 52.41 nM 7.28
CHEMBL4456635 EC50 = 52.41 nM 7.28
CHEMBL4530626 EC50 = 203.4 nM 6.69
CHEMBL4462475 EC50 = 455.6 nM 6.34