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Assay Detail

CHEMBL755009

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

Binding
In vitro binding activity against opioid receptor mu using [3H]DAGO) as radioligand
5
Total Activities
5
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

New 1-(heterocyclylalkyl)-4-(propionanilido)-4-piperidinyl methyl ester and methylene methyl ether analgesics.
Bagley JR, Thomas SA, Rudo FG, Spencer HK, Doorley BM, Ossipov MH, Jerussi TP, Benvenga MJ, Spaulding T.
J Med Chem (1991) 34 : 827 -841
PubMed 1847432 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 7.16 8.27

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL169366 1 8.27
CHEMBL168723 1 7.99
CHEMBL634 ALFENTANIL 4.0 1 7.82
CHEMBL424400 1 5.92
CHEMBL169587 1 5.80

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL169366 IC50 = 5.4 nM 8.27
CHEMBL168723 IC50 = 10.3 nM 7.99
CHEMBL634 ALFENTANIL IC50 = 15.0 nM 7.82
CHEMBL424400 IC50 = 1200.0 nM 5.92
CHEMBL169587 IC50 = 1600.0 nM 5.80