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Assay Detail

CHEMBL916757

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Binding
Inhibition of ATM kinase
40
Total Activities
40
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Expert

Target

Serine-protein kinase ATM (CHEMBL3797)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Pyranone, thiopyranone, and pyridone inhibitors of phosphatidylinositol 3-kinase related kinases. Structure-activity relationships for DNA-dependent protein kinase inhibition, and identification of the first potent and selective inhibitor of the ataxia telangiectasia mutated kinase.
Hollick JJ, Rigoreau LJ, Cano-Soumillac C, Cockcroft X, Curtin NJ, Frigerio M, Golding BT, Guiard S, Hardcastle IR, Hickson I, Hummersone MG, Menear KA, Martin NM, Matthews I, Newell DR, Ord R, Richardson CJ, Smith GC, Griffin RJ.
J Med Chem (2007) 50 : 1958 -1972
PubMed 17371003 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 40 5.51 7.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL222102 KU-55933 1 7.89
CHEMBL373979 1 5.50
CHEMBL374930 1 5.37
CHEMBL223980 1 5.00
CHEMBL222545 1 4.75
CHEMBL221459 1 4.54
CHEMBL374133 1 -
CHEMBL222179 1 -
CHEMBL374290 1 -
CHEMBL373699 1 -
CHEMBL223667 1 -
CHEMBL375346 1 -
CHEMBL223436 1 -
CHEMBL225796 1 -
CHEMBL221412 1 -
CHEMBL222766 1 -
CHEMBL222765 1 -
CHEMBL223034 1 -
CHEMBL223381 1 -
CHEMBL223775 1 -
CHEMBL222525 1 -
CHEMBL222577 1 -
CHEMBL223437 1 -
CHEMBL222544 1 -
CHEMBL225608 1 -
CHEMBL225609 1 -
CHEMBL389267 1 -
CHEMBL223382 1 -
CHEMBL223041 1 -
CHEMBL222745 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL222102 KU-55933 IC50 = 13.0 nM 7.89
CHEMBL373979 IC50 = 3200.0 nM 5.50
CHEMBL374930 IC50 = 4300.0 nM 5.37
CHEMBL223980 IC50 = 10000.0 nM 5.00
CHEMBL222545 IC50 = 18000.0 nM 4.75
CHEMBL221459 IC50 = 28500.0 nM 4.54
CHEMBL223436 IC50 > 10000.0 nM -
CHEMBL222180 IC50 > 100000.0 nM -
CHEMBL225796 IC50 > 100000.0 nM -
CHEMBL221412 IC50 > 100000.0 nM -
CHEMBL222766 IC50 > 100000.0 nM -
CHEMBL222765 IC50 > 10000.0 nM -
CHEMBL223034 IC50 > 10000.0 nM -
CHEMBL222179 IC50 > 100000.0 nM -
CHEMBL221565 IC50 > 10000.0 nM -
CHEMBL223559 IC50 > 10000.0 nM -
CHEMBL223610 IC50 > 10000.0 nM -
CHEMBL225273 IC50 > 10000.0 nM -
CHEMBL224782 IC50 > 100000.0 nM -
CHEMBL426894 IC50 > 10000.0 nM -
CHEMBL222815 IC50 > 100000.0 nM -
CHEMBL222181 IC50 > 10000.0 nM -
CHEMBL373526 IC50 > 10000.0 nM -
CHEMBL222577 IC50 > 10000.0 nM -
CHEMBL222745 IC50 > 10000.0 nM -
CHEMBL223041 IC50 > 10000.0 nM -
CHEMBL223382 IC50 > 100000.0 nM -
CHEMBL389267 IC50 > 10000.0 nM -
CHEMBL225609 IC50 > 10000.0 nM -
CHEMBL225608 IC50 > 100000.0 nM -
CHEMBL222544 IC50 > 10000.0 nM -
CHEMBL223437 IC50 > 10000.0 nM -
CHEMBL375346 IC50 > 100000.0 nM -
CHEMBL222525 IC50 > 10000.0 nM -
CHEMBL223775 IC50 > 10000.0 nM -
CHEMBL223381 IC50 > 10000.0 nM -
CHEMBL374133 IC50 > 10000.0 nM -
CHEMBL374290 IC50 > 100000.0 nM -
CHEMBL373699 IC50 > 100000.0 nM -
CHEMBL223667 IC50 > 10000.0 nM -