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Assay Detail

CHEMBL1117043

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Binding
Inhibition of PI3K assessed as PIP3 level after 20 mins by HTRF assay
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

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 6.51 8.19

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL586702 ZSTK-474 2.0 1 8.19
CHEMBL1089219 1 7.62
CHEMBL1088970 1 7.06
CHEMBL1088919 1 6.91
CHEMBL1092653 1 6.85
CHEMBL1088974 1 6.82
CHEMBL1092642 1 6.17
CHEMBL1088973 1 6.05
CHEMBL1088971 1 5.74
CHEMBL1092909 1 5.67
CHEMBL1092908 1 5.57
CHEMBL1088972 1 5.46

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL586702 ZSTK-474 IC50 = 6.5 nM 8.19
CHEMBL1089219 IC50 = 24.0 nM 7.62
CHEMBL1088970 IC50 = 87.0 nM 7.06
CHEMBL1088919 IC50 = 124.0 nM 6.91
CHEMBL1092653 IC50 = 142.0 nM 6.85
CHEMBL1088974 IC50 = 150.0 nM 6.82
CHEMBL1092642 IC50 = 680.0 nM 6.17
CHEMBL1088973 IC50 = 899.0 nM 6.05
CHEMBL1088971 IC50 = 1819.0 nM 5.74
CHEMBL1092909 IC50 = 2125.0 nM 5.67
CHEMBL1092908 IC50 = 2692.0 nM 5.57
CHEMBL1088972 IC50 = 3438.0 nM 5.46