Assay Detail
Binding
CHEMBL5534404
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human DNA-PK incubated for 30 mins in presence of Mg/ATP by HTRF method
69
Total Activities
69
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
Discovery, Optimization, and Evaluation of Potent and Selective DNA-PK Inhibitors in Combination with Chemotherapy or Radiotherapy for the Treatment of Malignancies.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 69 | 8.62 | 10.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5563688 | — | — | 1 | 10.00 |
| CHEMBL5566630 | — | — | 1 | 10.00 |
| CHEMBL5591635 | — | — | 1 | 9.70 |
| CHEMBL5595209 | — | — | 1 | 9.40 |
| CHEMBL5571078 | — | — | 1 | 9.40 |
| CHEMBL5579677 | — | — | 1 | 9.40 |
| CHEMBL5565603 | — | — | 1 | 9.15 |
| CHEMBL5572811 | — | — | 1 | 9.10 |
| CHEMBL5579700 | — | — | 1 | 9.10 |
| CHEMBL5563776 | — | — | 1 | 9.05 |
| CHEMBL5570412 | — | — | 1 | 9.00 |
| CHEMBL5572936 | — | — | 1 | 9.00 |
| CHEMBL5572260 | — | — | 1 | 9.00 |
| CHEMBL5563712 | — | — | 1 | 9.00 |
| CHEMBL5569108 | — | — | 1 | 9.00 |
| CHEMBL4439259 | AZD-7648 | 1.0 | 1 | 9.00 |
| CHEMBL5575123 | — | — | 1 | 9.00 |
| CHEMBL5592744 | — | — | 1 | 8.70 |
| CHEMBL5566668 | — | — | 1 | 8.70 |
| CHEMBL5571620 | — | — | 1 | 8.52 |
| CHEMBL5571138 | — | — | 1 | 8.52 |
| CHEMBL5591387 | — | — | 1 | 8.40 |
| CHEMBL5565467 | — | — | 1 | 8.30 |
| CHEMBL5574317 | — | — | 1 | 8.30 |
| CHEMBL5564989 | — | — | 1 | 8.28 |
| CHEMBL5572732 | — | — | 1 | 8.22 |
| CHEMBL5572444 | — | — | 1 | 8.22 |
| CHEMBL5592925 | — | — | 1 | 8.22 |
| CHEMBL5569624 | — | — | 1 | 8.22 |
| CHEMBL5567517 | — | — | 1 | 8.10 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5563688 | — | IC50 | = | 0.1 | nM | 10.00 |
| CHEMBL5566630 | — | IC50 | = | 0.1 | nM | 10.00 |
| CHEMBL5591635 | — | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL5595209 | — | IC50 | = | 0.4 | nM | 9.40 |
| CHEMBL5571078 | — | IC50 | = | 0.4 | nM | 9.40 |
| CHEMBL5579677 | — | IC50 | = | 0.4 | nM | 9.40 |
| CHEMBL5565603 | — | IC50 | = | 0.7 | nM | 9.15 |
| CHEMBL5572811 | — | IC50 | = | 0.8 | nM | 9.10 |
| CHEMBL5579700 | — | IC50 | = | 0.8 | nM | 9.10 |
| CHEMBL5563776 | — | IC50 | = | 0.9 | nM | 9.05 |
| CHEMBL5575123 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL5572936 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL5570412 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL5572260 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL5563712 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL5569108 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL4439259 | AZD-7648 | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL5592744 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL5566668 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL5571620 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL5571138 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL5591387 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL5565467 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL5574317 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL5564989 | — | IC50 | = | 5.3 | nM | 8.28 |
| CHEMBL5572732 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL5569624 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL5572444 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL5592925 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL5567517 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL5595206 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL5572075 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL5564999 | — | IC50 | = | 9.6 | nM | 8.02 |
| CHEMBL5571804 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL5563030 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL5595128 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL5571528 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL5595223 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL5575061 | — | IC50 | = | 161.0 | nM | 6.79 |
| CHEMBL5564480 | — | IC50 | - | — | - | |
| CHEMBL5566583 | — | IC50 | - | — | - | |
| CHEMBL5569734 | — | IC50 | = | -3.2 | nM | - |
| CHEMBL5575226 | — | IC50 | - | — | - | |
| CHEMBL5569185 | — | IC50 | - | — | - | |
| CHEMBL5572712 | — | IC50 | - | — | - | |
| CHEMBL5571811 | — | IC50 | = | -7.0 | nM | - |
| CHEMBL5594448 | — | IC50 | - | — | - | |
| CHEMBL5568679 | — | IC50 | - | — | - | |
| CHEMBL5574660 | — | IC50 | - | — | - | |
| CHEMBL5563944 | — | IC50 | - | — | - |