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Assay Detail

CHEMBL3767086

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

Binding
Inhibition of human DNA-PK using EPPLSQEAFADLWKK as substrate by HTRF assay
17
Total Activities
17
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

Synthesis, structure elucidation, DNA-PK and PI3K and anti-cancer activity of 8- and 6-aryl-substituted-1-3-benzoxazines.
Morrison R, Al-Rawi JM, Jennings IG, Thompson PE, Angove MJ.
Eur J Med Chem (2016) 110 : 326 -339
PubMed 26854431 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 17 5.34 7.47

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3764883 1 7.47
CHEMBL3763392 1 6.57
CHEMBL98350 LY-294002 -1.0 1 6.52
CHEMBL3763722 1 6.25
CHEMBL3763878 1 5.67
CHEMBL3765110 1 5.24
CHEMBL3763764 1 5.22
CHEMBL3764119 1 5.15
CHEMBL3763707 1 5.05
CHEMBL3765574 1 5.01
CHEMBL3765105 1 5.00
CHEMBL3763897 1 4.96
CHEMBL3764880 1 4.91
CHEMBL3763205 1 4.80
CHEMBL3765457 1 4.69
CHEMBL3765681 1 4.20
CHEMBL3765523 1 4.11

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3764883 IC50 = 34.0 nM 7.47
CHEMBL3763392 IC50 = 269.0 nM 6.57
CHEMBL98350 LY-294002 IC50 = 300.0 nM 6.52
CHEMBL3763722 IC50 = 564.0 nM 6.25
CHEMBL3763878 IC50 = 2120.0 nM 5.67
CHEMBL3765110 IC50 = 5770.0 nM 5.24
CHEMBL3763764 IC50 = 6050.0 nM 5.22
CHEMBL3764119 IC50 = 7120.0 nM 5.15
CHEMBL3763707 IC50 = 8810.0 nM 5.05
CHEMBL3765574 IC50 = 9800.0 nM 5.01
CHEMBL3765105 IC50 = 9940.0 nM 5.00
CHEMBL3763897 IC50 = 10900.0 nM 4.96
CHEMBL3764880 IC50 = 12300.0 nM 4.91
CHEMBL3763205 IC50 = 15700.0 nM 4.80
CHEMBL3765457 IC50 = 20300.0 nM 4.69
CHEMBL3765681 IC50 = 63500.0 nM 4.20
CHEMBL3765523 IC50 = 78400.0 nM 4.11