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Assay Detail

CHEMBL934449

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Binding
Inhibition of mTOR
45
Total Activities
45
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

Synthesis and structure-activity relationships of ring-opened 17-hydroxywortmannins: potent phosphoinositide 3-kinase inhibitors with improved properties and anticancer efficacy.
Zask A, Kaplan J, Toral-Barza L, Hollander I, Young M, Tischler M, Gaydos C, Cinque M, Lucas J, Yu K.
J Med Chem (2008) 51 : 1319 -1323
PubMed 18269228 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 45 5.75 6.71

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL273832 1 6.71
CHEMBL271780 1 6.60
CHEMBL405230 1 6.25
CHEMBL271982 1 6.21
CHEMBL271184 1 6.16
CHEMBL409671 1 6.12
CHEMBL271544 1 6.09
CHEMBL272816 1 6.09
CHEMBL410637 1 6.08
CHEMBL410071 1 6.08
CHEMBL411950 1 6.08
CHEMBL272898 1 6.06
CHEMBL406237 1 6.05
CHEMBL271430 1 6.02
CHEMBL260313 1 6.02
CHEMBL408074 1 5.92
CHEMBL271413 1 5.92
CHEMBL405258 1 5.87
CHEMBL409427 1 5.83
CHEMBL429577 1 5.83
CHEMBL273038 1 5.77
CHEMBL270039 1 5.75
CHEMBL409620 1 5.73
CHEMBL407215 1 5.64
CHEMBL407214 1 5.63
CHEMBL270553 1 5.61
CHEMBL410643 1 5.54
CHEMBL411907 SONOLISIB 2.0 1 5.51
CHEMBL272595 1 5.45
CHEMBL272897 1 5.45

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL273832 IC50 = 193.0 nM 6.71
CHEMBL271780 IC50 = 249.0 nM 6.60
CHEMBL405230 IC50 = 568.0 nM 6.25
CHEMBL271982 IC50 = 619.0 nM 6.21
CHEMBL271184 IC50 = 692.0 nM 6.16
CHEMBL409671 IC50 = 767.0 nM 6.12
CHEMBL271544 IC50 = 820.0 nM 6.09
CHEMBL272816 IC50 = 816.0 nM 6.09
CHEMBL410637 IC50 = 829.0 nM 6.08
CHEMBL410071 IC50 = 822.0 nM 6.08
CHEMBL411950 IC50 = 831.0 nM 6.08
CHEMBL272898 IC50 = 878.0 nM 6.06
CHEMBL406237 IC50 = 890.0 nM 6.05
CHEMBL271430 IC50 = 961.0 nM 6.02
CHEMBL260313 IC50 = 960.0 nM 6.02
CHEMBL408074 IC50 = 1200.0 nM 5.92
CHEMBL271413 IC50 = 1210.0 nM 5.92
CHEMBL405258 IC50 = 1350.0 nM 5.87
CHEMBL409427 IC50 = 1470.0 nM 5.83
CHEMBL429577 IC50 = 1480.0 nM 5.83
CHEMBL273038 IC50 = 1690.0 nM 5.77
CHEMBL270039 IC50 = 1800.0 nM 5.75
CHEMBL409620 IC50 = 1870.0 nM 5.73
CHEMBL407215 IC50 = 2290.0 nM 5.64
CHEMBL407214 IC50 = 2330.0 nM 5.63
CHEMBL270553 IC50 = 2450.0 nM 5.61
CHEMBL410643 IC50 = 2920.0 nM 5.54
CHEMBL411907 SONOLISIB IC50 = 3100.0 nM 5.51
CHEMBL272595 IC50 = 3560.0 nM 5.45
CHEMBL272897 IC50 = 3570.0 nM 5.45
CHEMBL271257 IC50 = 5600.0 nM 5.25
CHEMBL270746 IC50 = 6500.0 nM 5.19
CHEMBL409251 IC50 = 8700.0 nM 5.06
CHEMBL272593 IC50 = 12600.0 nM 4.90
CHEMBL272281 IC50 = 13900.0 nM 4.86
CHEMBL272197 IC50 = 14000.0 nM 4.85
CHEMBL271190 IC50 = 28600.0 nM 4.54
CHEMBL406655 IC50 > 20000.0 nM -
CHEMBL271191 IC50 > 20000.0 nM -
CHEMBL272190 IC50 > 20000.0 nM -
CHEMBL428873 IC50 > 20000.0 nM -
CHEMBL409294 IC50 > 20000.0 nM -
CHEMBL410644 IC50 > 20000.0 nM -
CHEMBL405157 IC50 > 1690.0 nM -
CHEMBL412076 IC50 > 18700.0 nM -