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Assay Detail

CHEMBL2423447

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Binding
Inhibition of DNA-PK (unknown origin)
2
Total Activities
2
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

1-substituted (Dibenzo[b,d]thiophen-4-yl)-2-morpholino-4H-chromen-4-ones endowed with dual DNA-PK/PI3-K inhibitory activity.
Cano C, Saravanan K, Bailey C, Bardos J, Curtin NJ, Frigerio M, Golding BT, Hardcastle IR, Hummersone MG, Menear KA, Newell DR, Richardson CJ, Shea K, Smith GC, Thommes P, Ting A, Griffin RJ.
J Med Chem (2013) 56 : 6386 -6401
PubMed 23855836 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 6.63 7.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL188678 1 7.40
CHEMBL98350 LY-294002 -1.0 1 5.85

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL188678 IC50 = 40.0 nM 7.40
CHEMBL98350 LY-294002 IC50 = 1400.0 nM 5.85