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Assay Detail

CHEMBL1067293

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Binding
Inhibition of mTOR
26
Total Activities
26
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Serine/threonine-protein kinase mTOR (CHEMBL2842)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of 2-arylthieno[3,2-d]pyrimidines containing 8-oxa-3-azabi-cyclo[3.2.1]octane in the 4-position as potent inhibitors of mTOR with selectivity over PI3K.
Verheijen JC, Yu K, Toral-Barza L, Hollander I, Zask A.
Bioorg Med Chem Lett (2010) 20 : 375 -379
PubMed 19897362 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 26 8.33 9.54

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL595256 1 9.54
CHEMBL593157 1 9.47
CHEMBL592917 1 9.36
CHEMBL594431 1 9.35
CHEMBL594549 1 9.22
CHEMBL594793 1 9.17
CHEMBL595053 1 9.15
CHEMBL595287 1 9.15
CHEMBL606131 1 9.05
CHEMBL594244 1 9.00
CHEMBL594571 1 8.90
CHEMBL604167 1 8.85
CHEMBL594173 1 8.43
CHEMBL594606 1 8.33
CHEMBL605915 1 7.96
CHEMBL596426 1 7.80
CHEMBL605529 1 7.70
CHEMBL593186 1 7.66
CHEMBL596430 1 7.58
CHEMBL595288 1 7.50
CHEMBL595743 1 7.46
CHEMBL510164 1 7.31
CHEMBL593156 1 7.24
CHEMBL603212 1 7.24
CHEMBL594844 1 7.21
CHEMBL594350 1 7.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL595256 IC50 = 0.29 nM 9.54
CHEMBL593157 IC50 = 0.34 nM 9.47
CHEMBL592917 IC50 = 0.44 nM 9.36
CHEMBL594431 IC50 = 0.45 nM 9.35
CHEMBL594549 IC50 = 0.6 nM 9.22
CHEMBL594793 IC50 = 0.68 nM 9.17
CHEMBL595053 IC50 = 0.7 nM 9.15
CHEMBL595287 IC50 = 0.7 nM 9.15
CHEMBL606131 IC50 = 0.9 nM 9.05
CHEMBL594244 IC50 = 1.0 nM 9.00
CHEMBL594571 IC50 = 1.25 nM 8.90
CHEMBL604167 IC50 = 1.4 nM 8.85
CHEMBL594173 IC50 = 3.7 nM 8.43
CHEMBL594606 IC50 = 4.7 nM 8.33
CHEMBL605915 IC50 = 11.0 nM 7.96
CHEMBL596426 IC50 = 16.0 nM 7.80
CHEMBL605529 IC50 = 20.0 nM 7.70
CHEMBL593186 IC50 = 22.0 nM 7.66
CHEMBL596430 IC50 = 26.5 nM 7.58
CHEMBL595288 IC50 = 32.0 nM 7.50
CHEMBL595743 IC50 = 35.0 nM 7.46
CHEMBL510164 IC50 = 49.0 nM 7.31
CHEMBL593156 IC50 = 58.0 nM 7.24
CHEMBL603212 IC50 = 57.0 nM 7.24
CHEMBL594844 IC50 = 61.0 nM 7.21
CHEMBL594350 IC50 = 100.0 nM 7.00