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Assay Detail

CHEMBL865906

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

Binding
Inhibition of mu opioid receptor
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Expert

Target

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

Publication

Derivatives of tramadol for increased duration of effect.
Shao L, Abolin C, Hewitt MC, Koch P, Varney M.
Bioorg Med Chem Lett (2006) 16 : 691 -694
PubMed 16257206 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 6.28 7.37

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL201556 1 7.37
CHEMBL1400 O-DESMETHYL TRAMADOL 1 7.33
CHEMBL379021 1 5.28
CHEMBL1237044 TRAMADOL 4.0 1 5.12
CHEMBL438627 1 -
CHEMBL201531 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL201556 IC50 = 43.0 nM 7.37
CHEMBL1400 O-DESMETHYL TRAMADOL IC50 = 47.0 nM 7.33
CHEMBL379021 IC50 = 5300.0 nM 5.28
CHEMBL1237044 TRAMADOL IC50 = 7600.0 nM 5.12
CHEMBL438627 IC50 > 10000.0 nM -
CHEMBL201531 IC50 > 10000.0 nM -