Assay Detail
Binding
CHEMBL5505637
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human DNA-PK using EPPLSQEAFADLWK as substrate in presence of ATP by kinase hotspot assay
95
Total Activities
95
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
Identification of 6-Anilino Imidazo[4,5-<i>c</i>]pyridin-2-ones as Selective DNA-Dependent Protein Kinase Inhibitors and Their Application as Radiosensitizers.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 95 | 6.70 | 9.44 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4297629 | NEDISERTIB | 1.0 | 1 | 9.44 |
| CHEMBL1879463 | DACTOLISIB | 3.0 | 1 | 9.10 |
| CHEMBL5559388 | — | — | 1 | 8.67 |
| CHEMBL4439259 | AZD-7648 | 1.0 | 1 | 8.60 |
| CHEMBL5527881 | — | — | 1 | 8.36 |
| CHEMBL5559285 | — | — | 1 | 8.31 |
| CHEMBL5517961 | — | — | 1 | 8.25 |
| CHEMBL5532026 | — | — | 1 | 8.21 |
| CHEMBL5556014 | — | — | 1 | 8.19 |
| CHEMBL5558866 | — | — | 1 | 8.15 |
| CHEMBL5542587 | — | — | 1 | 8.15 |
| CHEMBL5555639 | — | — | 1 | 8.14 |
| CHEMBL5523360 | — | — | 1 | 8.13 |
| CHEMBL5555573 | — | — | 1 | 8.12 |
| CHEMBL5542350 | — | — | 1 | 8.10 |
| CHEMBL5512590 | — | — | 1 | 7.75 |
| CHEMBL5542711 | — | — | 1 | 7.65 |
| CHEMBL5557396 | — | — | 1 | 7.53 |
| CHEMBL5558337 | — | — | 1 | 7.50 |
| CHEMBL5527866 | — | — | 1 | 7.40 |
| CHEMBL5531947 | — | — | 1 | 7.40 |
| CHEMBL5559345 | — | — | 1 | 7.39 |
| CHEMBL5517925 | — | — | 1 | 7.37 |
| CHEMBL5542141 | — | — | 1 | 7.28 |
| CHEMBL5532291 | — | — | 1 | 7.20 |
| CHEMBL5549794 | — | — | 1 | 7.14 |
| CHEMBL5523377 | — | — | 1 | 7.14 |
| CHEMBL5559046 | — | — | 1 | 7.12 |
| CHEMBL5543038 | — | — | 1 | 7.11 |
| CHEMBL5559461 | — | — | 1 | 7.03 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4297629 | NEDISERTIB | IC50 | = | 0.36 | nM | 9.44 |
| CHEMBL1879463 | DACTOLISIB | IC50 | = | 0.8 | nM | 9.10 |
| CHEMBL5559388 | — | IC50 | = | 2.12 | nM | 8.67 |
| CHEMBL4439259 | AZD-7648 | IC50 | = | 2.53 | nM | 8.60 |
| CHEMBL5527881 | — | IC50 | = | 4.4 | nM | 8.36 |
| CHEMBL5559285 | — | IC50 | = | 4.85 | nM | 8.31 |
| CHEMBL5517961 | — | IC50 | = | 5.6 | nM | 8.25 |
| CHEMBL5532026 | — | IC50 | = | 6.2 | nM | 8.21 |
| CHEMBL5556014 | — | IC50 | = | 6.5 | nM | 8.19 |
| CHEMBL5558866 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL5542587 | — | IC50 | = | 7.1 | nM | 8.15 |
| CHEMBL5555639 | — | IC50 | = | 7.27 | nM | 8.14 |
| CHEMBL5523360 | — | IC50 | = | 7.35 | nM | 8.13 |
| CHEMBL5555573 | — | IC50 | = | 7.54 | nM | 8.12 |
| CHEMBL5542350 | — | IC50 | = | 7.95 | nM | 8.10 |
| CHEMBL5512590 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL5542711 | — | IC50 | = | 22.4 | nM | 7.65 |
| CHEMBL5557396 | — | IC50 | = | 29.8 | nM | 7.53 |
| CHEMBL5558337 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL5527866 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL5531947 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL5559345 | — | IC50 | = | 40.4 | nM | 7.39 |
| CHEMBL5517925 | — | IC50 | = | 43.0 | nM | 7.37 |
| CHEMBL5542141 | — | IC50 | = | 53.0 | nM | 7.28 |
| CHEMBL5532291 | — | IC50 | = | 62.8 | nM | 7.20 |
| CHEMBL5549794 | — | IC50 | = | 72.8 | nM | 7.14 |
| CHEMBL5523377 | — | IC50 | = | 72.8 | nM | 7.14 |
| CHEMBL5559046 | — | IC50 | = | 75.0 | nM | 7.12 |
| CHEMBL5543038 | — | IC50 | = | 77.0 | nM | 7.11 |
| CHEMBL5559461 | — | IC50 | = | 94.0 | nM | 7.03 |
| CHEMBL5557807 | — | IC50 | = | 97.0 | nM | 7.01 |
| CHEMBL5523471 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL5559203 | — | IC50 | = | 108.0 | nM | 6.97 |
| CHEMBL5542179 | — | IC50 | = | 138.0 | nM | 6.86 |
| CHEMBL5556556 | — | IC50 | = | 138.0 | nM | 6.86 |
| CHEMBL5523582 | — | IC50 | = | 137.0 | nM | 6.86 |
| CHEMBL5532012 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL5542181 | — | IC50 | = | 147.0 | nM | 6.83 |
| CHEMBL5532346 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL5523472 | — | IC50 | = | 157.0 | nM | 6.80 |
| CHEMBL5559035 | — | IC50 | = | 185.0 | nM | 6.73 |
| CHEMBL5555900 | — | IC50 | = | 201.0 | nM | 6.70 |
| CHEMBL5527864 | — | IC50 | = | 245.0 | nM | 6.61 |
| CHEMBL5542754 | — | IC50 | = | 282.0 | nM | 6.55 |
| CHEMBL5555371 | — | IC50 | = | 284.0 | nM | 6.55 |
| CHEMBL5542841 | — | IC50 | = | 411.0 | nM | 6.39 |
| CHEMBL5518133 | — | IC50 | = | 565.0 | nM | 6.25 |
| CHEMBL5512574 | — | IC50 | = | 625.0 | nM | 6.20 |
| CHEMBL5518025 | — | IC50 | = | 1060.0 | nM | 5.97 |
| CHEMBL5558154 | — | IC50 | = | 1090.0 | nM | 5.96 |