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Assay Detail

CHEMBL1763481

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

Binding
Inhibition of mTOR in human U-87 cells assessed as inhibition of phosphorylation of 4EBP1 at T37/46
39
Total Activities
39
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type U-87
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Discovery of triazine-benzimidazoles as selective inhibitors of mTOR.
Peterson EA, Andrews PS, Be X, Boezio AA, Bush TL, Cheng AC, Coats JR, Colletti AE, Copeland KW, DuPont M, Graceffa R, Grubinska B, Harmange JC, Kim JL, Mullady EL, Olivieri P, Schenkel LB, Stanton MK, Teffera Y, Whittington DA, Cai T, La DS.
Bioorg Med Chem Lett (2011) 21 : 2064 -2070
PubMed 21376583 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 39 5.85 7.01

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1762790 1 7.01
CHEMBL1762788 1 6.82
CHEMBL1760154 1 6.47
CHEMBL1760172 1 6.47
CHEMBL1760155 1 6.47
CHEMBL1762782 1 6.42
CHEMBL1615183 1 6.41
CHEMBL1760169 1 6.22
CHEMBL1760168 1 6.22
CHEMBL1762778 1 6.15
CHEMBL1760157 1 6.02
CHEMBL1762785 1 5.92
CHEMBL1760170 1 5.89
CHEMBL1760171 1 5.85
CHEMBL1760156 1 5.82
CHEMBL1760158 1 5.82
CHEMBL1615182 1 5.77
CHEMBL1762775 1 5.54
CHEMBL1760161 1 5.48
CHEMBL1762781 1 5.46
CHEMBL1760153 1 5.41
CHEMBL1760162 1 5.38
CHEMBL1760159 1 5.28
CHEMBL1760163 1 5.28
CHEMBL1762783 1 5.20
CHEMBL1760160 1 5.19
CHEMBL1762786 1 5.05
CHEMBL1762787 1 4.67
CHEMBL1762774 1 -
CHEMBL1760167 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1762790 IC50 = 97.0 nM 7.01
CHEMBL1762788 IC50 = 150.0 nM 6.82
CHEMBL1760172 IC50 = 340.0 nM 6.47
CHEMBL1760155 IC50 = 340.0 nM 6.47
CHEMBL1760154 IC50 = 340.0 nM 6.47
CHEMBL1762782 IC50 = 380.0 nM 6.42
CHEMBL1615183 IC50 = 390.0 nM 6.41
CHEMBL1760169 IC50 = 600.0 nM 6.22
CHEMBL1760168 IC50 = 600.0 nM 6.22
CHEMBL1762778 IC50 = 710.0 nM 6.15
CHEMBL1760157 IC50 = 960.0 nM 6.02
CHEMBL1762785 IC50 = 1200.0 nM 5.92
CHEMBL1760170 IC50 = 1300.0 nM 5.89
CHEMBL1760171 IC50 = 1400.0 nM 5.85
CHEMBL1760158 IC50 = 1500.0 nM 5.82
CHEMBL1760156 IC50 = 1500.0 nM 5.82
CHEMBL1615182 IC50 = 1700.0 nM 5.77
CHEMBL1762775 IC50 = 2900.0 nM 5.54
CHEMBL1760161 IC50 = 3300.0 nM 5.48
CHEMBL1762781 IC50 = 3500.0 nM 5.46
CHEMBL1760153 IC50 = 3900.0 nM 5.41
CHEMBL1760162 IC50 = 4200.0 nM 5.38
CHEMBL1760159 IC50 = 5300.0 nM 5.28
CHEMBL1760163 IC50 = 5300.0 nM 5.28
CHEMBL1762783 IC50 = 6300.0 nM 5.20
CHEMBL1760160 IC50 = 6500.0 nM 5.19
CHEMBL1762786 IC50 = 8900.0 nM 5.05
CHEMBL1762787 IC50 = 21500.0 nM 4.67
CHEMBL1762779 IC50 > 25000.0 nM -
CHEMBL1762780 IC50 > 25000.0 nM -
CHEMBL1762784 IC50 > 25000.0 nM -
CHEMBL1762777 IC50 > 25000.0 nM -
CHEMBL1762789 IC50 > 25000.0 nM -
CHEMBL1762776 IC50 > 25000.0 nM -
CHEMBL1760164 IC50 > 25000.0 nM -
CHEMBL1760165 IC50 > 25000.0 nM -
CHEMBL1760166 IC50 > 25000.0 nM -
CHEMBL1760167 IC50 > 25000.0 nM -
CHEMBL1762774 IC50 > 25000.0 nM -