Assay Detail
Binding
CHEMBL3767086
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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.
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 |