Assay Detail
Binding
CHEMBL827974
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of DNA dependent protein kinase isolated from HeLa cells
84
Total Activities
83
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HeLa |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Target
DNA-dependent protein kinase catalytic subunit (CHEMBL3142) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Selective benzopyranone and pyrimido[2,1-a]isoquinolin-4-one inhibitors of DNA-dependent protein kinase: synthesis, structure-activity studies, and radiosensitization of a human tumor cell line in vitro.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 84 | 5.57 | 6.72 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL435507 | — | — | 1 | 6.72 |
| CHEMBL104468 | — | — | 1 | 6.64 |
| CHEMBL176233 | — | — | 1 | 6.58 |
| CHEMBL179242 | — | — | 1 | 6.55 |
| CHEMBL179108 | — | — | 1 | 6.44 |
| CHEMBL175883 | — | — | 1 | 6.41 |
| CHEMBL175459 | — | — | 1 | 6.02 |
| CHEMBL97024 | — | — | 1 | 5.92 |
| CHEMBL367315 | — | — | 1 | 5.90 |
| CHEMBL367537 | — | — | 1 | 5.90 |
| CHEMBL360038 | — | — | 1 | 5.86 |
| CHEMBL98350 | LY-294002 | -1.0 | 2 | 5.83 |
| CHEMBL175944 | — | — | 1 | 5.79 |
| CHEMBL179635 | — | — | 1 | 5.78 |
| CHEMBL179168 | — | — | 1 | 5.77 |
| CHEMBL175510 | — | — | 1 | 5.76 |
| CHEMBL178969 | — | — | 1 | 5.72 |
| CHEMBL177938 | — | — | 1 | 5.72 |
| CHEMBL367141 | — | — | 1 | 5.70 |
| CHEMBL179043 | — | — | 1 | 5.70 |
| CHEMBL369146 | — | — | 1 | 5.65 |
| CHEMBL361530 | — | — | 1 | 5.55 |
| CHEMBL435542 | — | — | 1 | 5.50 |
| CHEMBL179591 | — | — | 1 | 5.49 |
| CHEMBL177279 | — | — | 1 | 5.49 |
| CHEMBL176436 | — | — | 1 | 5.49 |
| CHEMBL176280 | — | — | 1 | 5.45 |
| CHEMBL367468 | — | — | 1 | 5.42 |
| CHEMBL179412 | — | — | 1 | 5.38 |
| CHEMBL176064 | — | — | 1 | 5.33 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL435507 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL104468 | — | IC50 | = | 230.0 | nM | 6.64 |
| CHEMBL176233 | — | IC50 | = | 260.0 | nM | 6.58 |
| CHEMBL179242 | — | IC50 | = | 280.0 | nM | 6.55 |
| CHEMBL179108 | — | IC50 | = | 360.0 | nM | 6.44 |
| CHEMBL175883 | — | IC50 | = | 390.0 | nM | 6.41 |
| CHEMBL175459 | — | IC50 | = | 950.0 | nM | 6.02 |
| CHEMBL97024 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL367537 | — | IC50 | = | 1250.0 | nM | 5.90 |
| CHEMBL367315 | — | IC50 | = | 1260.0 | nM | 5.90 |
| CHEMBL360038 | — | IC50 | = | 1380.0 | nM | 5.86 |
| CHEMBL98350 | LY-294002 | IC50 | = | 1470.0 | nM | 5.83 |
| CHEMBL98350 | LY-294002 | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL175944 | — | IC50 | = | 1610.0 | nM | 5.79 |
| CHEMBL179635 | — | IC50 | = | 1650.0 | nM | 5.78 |
| CHEMBL179168 | — | IC50 | = | 1690.0 | nM | 5.77 |
| CHEMBL175510 | — | IC50 | = | 1750.0 | nM | 5.76 |
| CHEMBL177938 | — | IC50 | = | 1920.0 | nM | 5.72 |
| CHEMBL178969 | — | IC50 | = | 1900.0 | nM | 5.72 |
| CHEMBL367141 | — | IC50 | = | 2010.0 | nM | 5.70 |
| CHEMBL179043 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL369146 | — | IC50 | = | 2240.0 | nM | 5.65 |
| CHEMBL361530 | — | IC50 | = | 2810.0 | nM | 5.55 |
| CHEMBL435542 | — | IC50 | = | 3190.0 | nM | 5.50 |
| CHEMBL176436 | — | IC50 | = | 3250.0 | nM | 5.49 |
| CHEMBL179591 | — | IC50 | = | 3270.0 | nM | 5.49 |
| CHEMBL177279 | — | IC50 | = | 3240.0 | nM | 5.49 |
| CHEMBL176280 | — | IC50 | = | 3520.0 | nM | 5.45 |
| CHEMBL367468 | — | IC50 | = | 3810.0 | nM | 5.42 |
| CHEMBL179412 | — | IC50 | = | 4140.0 | nM | 5.38 |
| CHEMBL176064 | — | IC50 | = | 4670.0 | nM | 5.33 |
| CHEMBL367262 | — | IC50 | = | 4820.0 | nM | 5.32 |
| CHEMBL283196 | ALPHA-NAPHTHOFLAVONE | IC50 | = | 4980.0 | nM | 5.30 |
| CHEMBL179640 | — | IC50 | = | 5150.0 | nM | 5.29 |
| CHEMBL361588 | — | IC50 | = | 5350.0 | nM | 5.27 |
| CHEMBL433802 | — | IC50 | = | 5710.0 | nM | 5.24 |
| CHEMBL436080 | — | IC50 | = | 5710.0 | nM | 5.24 |
| CHEMBL179914 | — | IC50 | = | 6170.0 | nM | 5.21 |
| CHEMBL180023 | — | IC50 | = | 6490.0 | nM | 5.19 |
| CHEMBL179641 | — | IC50 | = | 6660.0 | nM | 5.18 |
| CHEMBL179002 | — | IC50 | = | 6680.0 | nM | 5.17 |
| CHEMBL176193 | — | IC50 | = | 6710.0 | nM | 5.17 |
| CHEMBL179276 | — | IC50 | = | 7700.0 | nM | 5.11 |
| CHEMBL369452 | — | IC50 | = | 8050.0 | nM | 5.09 |
| CHEMBL361608 | — | IC50 | = | 8590.0 | nM | 5.07 |
| CHEMBL177997 | — | IC50 | = | 8460.0 | nM | 5.07 |
| CHEMBL176114 | — | IC50 | = | 8810.0 | nM | 5.05 |
| CHEMBL175892 | — | IC50 | = | 9270.0 | nM | 5.03 |
| CHEMBL180529 | — | IC50 | = | 10470.0 | nM | 4.98 |
| CHEMBL176325 | — | IC50 | = | 10940.0 | nM | 4.96 |