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Assay Detail

CHEMBL745615

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

Binding
Compound was tested in vitro for binding affinity towards mu opioid receptor by measuring displacement of [3H]DAGO from guinea pig brain membranes
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Cavia porcellus
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

Mu-type opioid receptor (CHEMBL4354)
Type SINGLE PROTEIN
Organism Cavia porcellus

Publication

Octahydro-1,2,3,4,4a,5,11,11a-pyrido[3,4-c][1,5]benzoxazepines: conformationally restricted fentanyl analogs
Kudzma LV, Evans SM, Turnbull SP, Severnak SA, Ezell EF
Bioorg Med Chem Lett (1995) 5 : 1177 -1182
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 8.35 8.51

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL596 FENTANYL 4.0 1 8.51
CHEMBL2079638 1 8.29
CHEMBL2079569 1 8.24

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL596 FENTANYL IC50 = 3.1 nM 8.51
CHEMBL2079638 IC50 = 5.1 nM 8.29
CHEMBL2079569 IC50 = 5.8 nM 8.24