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Assay Detail

CHEMBL887072

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

Functional
Agonist activity at human cloned mu opioid receptor assessed as stimulation of [35S]GTPgammaS binding
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

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

Publication

Further studies of tyrosine surrogates in opioid receptor peptide ligands.
Dolle RE, Michaut M, Martinez-Teipel B, Belanger S, Graczyk TM, DeHaven RN.
Bioorg Med Chem Lett (2007) 17 : 2656 -2660
PubMed 17350835 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 21 6.62 7.31

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL247758 1 7.31
CHEMBL391580 1 6.85
CHEMBL246739 1 6.75
CHEMBL247760 1 6.60
CHEMBL246956 1 6.57
CHEMBL246572 1 6.46
CHEMBL13786 1 6.21
CHEMBL247368 1 6.20
CHEMBL246479 1 -
CHEMBL31421 1 -
CHEMBL2372104 1 -
CHEMBL247363 1 -
CHEMBL247163 1 -
CHEMBL247562 1 -
CHEMBL246682 1 -
CHEMBL393867 1 -
CHEMBL247064 1 -
CHEMBL395863 1 -
CHEMBL392275 1 -
CHEMBL246740 1 -
CHEMBL247759 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL247758 EC50 = 49.0 nM 7.31
CHEMBL391580 EC50 = 140.0 nM 6.85
CHEMBL246739 EC50 = 180.0 nM 6.75
CHEMBL247760 EC50 = 250.0 nM 6.60
CHEMBL246956 EC50 = 270.0 nM 6.57
CHEMBL246572 EC50 = 350.0 nM 6.46
CHEMBL13786 EC50 = 620.0 nM 6.21
CHEMBL247368 EC50 = 630.0 nM 6.20
CHEMBL246479 EC50 - -
CHEMBL31421 EC50 - -
CHEMBL2372104 EC50 - -
CHEMBL247363 EC50 - -
CHEMBL247163 EC50 - -
CHEMBL247562 EC50 - -
CHEMBL246682 EC50 - -
CHEMBL393867 EC50 - -
CHEMBL247064 EC50 - -
CHEMBL395863 EC50 - -
CHEMBL392275 EC50 - -
CHEMBL246740 EC50 - -
CHEMBL247759 EC50 - -