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Assay Detail

CHEMBL916755

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Binding
Inhibition of DNA-PK in HeLa cell nuclear extracts
ChEMBL ↗
111
Total Activities
111
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

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

Target

DNA-dependent protein kinase catalytic subunit (CHEMBL3142) ↗
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 88 5.85 6.80
Inhibition 23 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL105678 — — 1 6.80
CHEMBL102581 — — 1 6.80
CHEMBL105612 — — 1 6.75
CHEMBL319261 — — 1 6.66
CHEMBL104682 — — 1 6.58
CHEMBL321784 — — 1 6.55
CHEMBL105256 — — 1 6.51
CHEMBL105521 — — 1 6.46
CHEMBL224092 — — 1 6.41
CHEMBL222745 — — 1 6.40
CHEMBL222821 — — 1 6.33
CHEMBL102529 — — 1 6.32
CHEMBL374290 — — 1 6.30
CHEMBL323136 — — 1 6.28
CHEMBL221410 — — 1 6.28
CHEMBL106543 — — 1 6.27
CHEMBL222544 — — 1 6.22
CHEMBL276746 — — 1 6.19
CHEMBL316769 — — 1 6.17
CHEMBL222820 — — 1 6.17
CHEMBL323145 — — 1 6.16
CHEMBL319909 — — 1 6.16
CHEMBL426894 — — 1 6.10
CHEMBL222545 — — 1 6.10
CHEMBL431228 — — 1 6.08
CHEMBL223041 — — 1 6.05
CHEMBL104644 — — 1 6.04
CHEMBL225796 — — 1 6.04
CHEMBL221412 — — 1 6.00
CHEMBL222815 — — 1 6.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL102581 — IC50 = 160.0 nM 6.80
CHEMBL105678 — IC50 = 160.0 nM 6.80
CHEMBL105612 — IC50 = 180.0 nM 6.75
CHEMBL319261 — IC50 = 220.0 nM 6.66
CHEMBL104682 — IC50 = 260.0 nM 6.58
CHEMBL321784 — IC50 = 280.0 nM 6.55
CHEMBL105256 — IC50 = 310.0 nM 6.51
CHEMBL105521 — IC50 = 350.0 nM 6.46
CHEMBL224092 — IC50 = 390.0 nM 6.41
CHEMBL222745 — IC50 = 400.0 nM 6.40
CHEMBL222821 — IC50 = 470.0 nM 6.33
CHEMBL102529 — IC50 = 480.0 nM 6.32
CHEMBL374290 — IC50 = 500.0 nM 6.30
CHEMBL221410 — IC50 = 530.0 nM 6.28
CHEMBL323136 — IC50 = 530.0 nM 6.28
CHEMBL106543 — IC50 = 540.0 nM 6.27
CHEMBL222544 — IC50 = 600.0 nM 6.22
CHEMBL276746 — IC50 = 650.0 nM 6.19
CHEMBL316769 — IC50 = 680.0 nM 6.17
CHEMBL222820 — IC50 = 680.0 nM 6.17
CHEMBL323145 — IC50 = 700.0 nM 6.16
CHEMBL319909 — IC50 = 690.0 nM 6.16
CHEMBL222545 — IC50 = 800.0 nM 6.10
CHEMBL426894 — IC50 = 800.0 nM 6.10
CHEMBL431228 — IC50 = 840.0 nM 6.08
CHEMBL223041 — IC50 = 900.0 nM 6.05
CHEMBL104644 — IC50 = 920.0 nM 6.04
CHEMBL225796 — IC50 = 910.0 nM 6.04
CHEMBL223775 — IC50 = 1000.0 nM 6.00
CHEMBL222815 — IC50 = 1000.0 nM 6.00
CHEMBL221412 — IC50 = 1000.0 nM 6.00
CHEMBL224827 — IC50 = 1060.0 nM 5.97
CHEMBL223667 — IC50 = 1100.0 nM 5.96
CHEMBL374133 — IC50 = 1100.0 nM 5.96
CHEMBL102396 — IC50 = 1100.0 nM 5.96
CHEMBL373979 — IC50 = 1200.0 nM 5.92
CHEMBL367537 — IC50 = 1250.0 nM 5.90
CHEMBL225609 — IC50 = 1300.0 nM 5.89
CHEMBL223980 — IC50 = 1300.0 nM 5.89
CHEMBL389267 — IC50 = 1300.0 nM 5.89
CHEMBL105613 — IC50 = 1300.0 nM 5.89
CHEMBL223381 — IC50 = 1600.0 nM 5.80
CHEMBL222179 — IC50 = 1800.0 nM 5.75
CHEMBL222102 KU-55933 IC50 = 1800.0 nM 5.75
CHEMBL221409 — IC50 = 1800.0 nM 5.75
CHEMBL375210 — IC50 = 1900.0 nM 5.72
CHEMBL221403 — IC50 = 2100.0 nM 5.68
CHEMBL225608 — IC50 = 2300.0 nM 5.64
CHEMBL222765 — IC50 = 2500.0 nM 5.60
CHEMBL223437 — IC50 = 2500.0 nM 5.60