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Assay Detail

CHEMBL1117042

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

Binding
Inhibition of rat brain mTOR assessed as p70S6K-GST protein phosphorylation after 30 mins by ELISA
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Serine/threonine-protein kinase mTOR (CHEMBL1075134)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Discovery of 2-ureidophenyltriazines bearing bridged morpholines as potent and selective ATP-competitive mTOR inhibitors.
Zask A, Verheijen JC, Richard DJ, Kaplan J, Curran K, Toral-Barza L, Lucas J, Hollander I, Yu K.
Bioorg Med Chem Lett (2010) 20 : 2644 -2647
PubMed 20227881 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 12 8.15 9.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1092653 1 9.30
CHEMBL1088973 1 9.00
CHEMBL1088970 1 8.77
CHEMBL1088974 1 8.70
CHEMBL1092642 1 8.60
CHEMBL1092909 1 8.59
CHEMBL1092908 1 8.55
CHEMBL1088972 1 7.46
CHEMBL1088919 1 7.36
CHEMBL586702 ZSTK-474 2.0 1 7.35
CHEMBL1089219 1 7.22
CHEMBL1088971 1 6.89

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1092653 IC50 = 0.5 nM 9.30
CHEMBL1088973 IC50 = 1.0 nM 9.00
CHEMBL1088970 IC50 = 1.7 nM 8.77
CHEMBL1088974 IC50 = 2.0 nM 8.70
CHEMBL1092642 IC50 = 2.5 nM 8.60
CHEMBL1092909 IC50 = 2.6 nM 8.59
CHEMBL1092908 IC50 = 2.8 nM 8.55
CHEMBL1088972 IC50 = 35.0 nM 7.46
CHEMBL1088919 IC50 = 44.0 nM 7.36
CHEMBL586702 ZSTK-474 IC50 = 45.0 nM 7.35
CHEMBL1089219 IC50 = 60.0 nM 7.22
CHEMBL1088971 IC50 = 130.0 nM 6.89