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Assay Detail

CHEMBL3377243

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

Binding
Inhibition of human DNA-PK by non-radiometric ADP-Glo assay
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Class II but Not Second Class-Prospects for the Development of Class II PI3K Inhibitors.
Mountford SJ, Zheng Z, Sundaram K, Jennings IG, Hamilton JR, Thompson PE.
ACS Med Chem Lett (2015) 6 : 3 -6
PubMed 25589915 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 6.95 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL573339 PI-103 1 8.70
CHEMBL1241857 1 7.89
CHEMBL1229535 1 7.19
CHEMBL3218571 1 5.82
CHEMBL2216870 IDELALISIB 4.0 1 5.17

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL573339 PI-103 IC50 = 2.0 nM 8.70
CHEMBL1241857 IC50 = 13.0 nM 7.89
CHEMBL1229535 IC50 = 64.0 nM 7.19
CHEMBL3218571 IC50 = 1500.0 nM 5.82
CHEMBL2216870 IDELALISIB IC50 = 6700.0 nM 5.17