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Assay Detail

CHEMBL833531

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Binding
Inhibitory activity against DNA-dependent protein kinase (DNA-PK) at 0.5 uM
10
Total Activities
10
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

DNA-dependent protein kinase catalytic subunit (CHEMBL3142)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Identification of a highly potent and selective DNA-dependent protein kinase (DNA-PK) inhibitor (NU7441) by screening of chromenone libraries.
Leahy JJ, Golding BT, Griffin RJ, Hardcastle IR, Richardson C, Rigoreau L, Smith GC.
Bioorg Med Chem Lett (2004) 14 : 6083 -6087
PubMed 15546735 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 10 6.49 7.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL188678 1 7.70
CHEMBL186048 1 7.40
CHEMBL435507 1 6.72
CHEMBL360183 1 6.52
CHEMBL189552 1 6.22
CHEMBL362729 1 6.16
CHEMBL187562 1 6.10
CHEMBL362521 1 6.10
CHEMBL363755 1 6.05
CHEMBL367315 1 5.89

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL188678 IC50 = 20.0 nM 7.70
CHEMBL186048 IC50 = 40.0 nM 7.40
CHEMBL435507 IC50 = 190.0 nM 6.72
CHEMBL360183 IC50 = 300.0 nM 6.52
CHEMBL189552 IC50 = 600.0 nM 6.22
CHEMBL362729 IC50 = 700.0 nM 6.16
CHEMBL187562 IC50 = 800.0 nM 6.10
CHEMBL362521 IC50 = 800.0 nM 6.10
CHEMBL363755 IC50 = 900.0 nM 6.05
CHEMBL367315 IC50 = 1300.0 nM 5.89