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Assay Detail

CHEMBL3812007

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

Binding
Agonist activity at human MOR expressed in CHO cell membranes after 60 mins by [35S]GTP-gamma-S binding assay
6
Total Activities
3
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
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

Discovery of Potent and Selective Agonists of δ Opioid Receptor by Revisiting the "Message-Address" Concept.
Shen Q, Qian Y, Huang X, Xu X, Li W, Liu J, Fu W.
ACS Med Chem Lett (2016) 7 : 391 -396
PubMed 27096047 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Emax 3 - -
EC50 3 6.71 7.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL38874 DAMGO 2 7.52
CHEMBL1400 O-DESMETHYL TRAMADOL 2 6.62
CHEMBL1066 (R,R)-TRAMADOL 2 6.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL38874 DAMGO EC50 = 30.0 nM 7.52
CHEMBL1400 O-DESMETHYL TRAMADOL EC50 = 240.0 nM 6.62
CHEMBL1066 (R,R)-TRAMADOL EC50 = 1000.0 nM 6.00
CHEMBL38874 DAMGO Emax = 225.0 % -
CHEMBL1400 O-DESMETHYL TRAMADOL Emax = 220.0 % -
CHEMBL1066 (R,R)-TRAMADOL Emax = 220.0 % -