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Assay Detail

CHEMBL958391

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

Functional
Agonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Syntheses of novel high affinity ligands for opioid receptors.
Wentland MP, Lou R, Lu Q, Bu Y, Denhardt C, Jin J, Ganorkar R, VanAlstine MA, Guo C, Cohen DJ, Bidlack JM.
Bioorg Med Chem Lett (2009) 19 : 2289 -2294
PubMed 19282177 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 10 8.06 9.07

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL511645 1 9.07
CHEMBL471048 1 8.80
CHEMBL398707 HYDROMORPHONE 4.0 1 8.59
CHEMBL512150 1 8.51
CHEMBL56695 1 8.31
CHEMBL470005 1 8.00
CHEMBL19019 NALTREXONE 4.0 1 7.80
CHEMBL895 NALBUPHINE 4.0 1 7.34
CHEMBL38874 DAMGO 1 7.26
CHEMBL471049 1 6.96

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL511645 EC50 = 0.86 nM 9.07
CHEMBL471048 EC50 = 1.6 nM 8.80
CHEMBL398707 HYDROMORPHONE EC50 = 2.6 nM 8.59
CHEMBL512150 EC50 = 3.1 nM 8.51
CHEMBL56695 EC50 = 4.9 nM 8.31
CHEMBL470005 EC50 = 10.0 nM 8.00
CHEMBL19019 NALTREXONE EC50 = 16.0 nM 7.80
CHEMBL895 NALBUPHINE EC50 = 46.0 nM 7.34
CHEMBL38874 DAMGO EC50 = 55.0 nM 7.26
CHEMBL471049 EC50 = 110.0 nM 6.96