Assay Detail
Binding
CHEMBL858719
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Inhibitory activity against DNA-dependent protein kinase receptor
162
Total Activities
138
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Target
DNA-dependent protein kinase catalytic subunit (CHEMBL3142) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Discovery of potent chromen-4-one inhibitors of the DNA-dependent protein kinase (DNA-PK) using a small-molecule library approach.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 139 | 5.74 | 7.70 |
| Ki | 23 | 9.19 | 9.19 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL188678 | — | — | 2 | 9.19 |
| CHEMBL198750 | — | — | 1 | 7.64 |
| CHEMBL186048 | — | — | 1 | 7.40 |
| CHEMBL104468 | — | — | 1 | 6.64 |
| CHEMBL198675 | — | — | 1 | 6.60 |
| CHEMBL360183 | — | — | 1 | 6.52 |
| CHEMBL198482 | — | — | 1 | 6.46 |
| CHEMBL95298 | — | — | 1 | 6.42 |
| CHEMBL175883 | — | — | 1 | 6.40 |
| CHEMBL197004 | — | — | 1 | 6.36 |
| CHEMBL197379 | — | — | 1 | 6.36 |
| CHEMBL197536 | — | — | 1 | 6.35 |
| CHEMBL427194 | — | — | 1 | 6.33 |
| CHEMBL198576 | — | — | 1 | 6.31 |
| CHEMBL199577 | — | — | 1 | 6.30 |
| CHEMBL372143 | — | — | 2 | 6.25 |
| CHEMBL189552 | — | — | 1 | 6.22 |
| CHEMBL362729 | — | — | 1 | 6.16 |
| CHEMBL371947 | — | — | 1 | 6.16 |
| CHEMBL201988 | — | — | 1 | 6.15 |
| CHEMBL276746 | — | — | 1 | 6.14 |
| CHEMBL187562 | — | — | 1 | 6.10 |
| CHEMBL362521 | — | — | 1 | 6.10 |
| CHEMBL196870 | — | — | 1 | 6.10 |
| CHEMBL198138 | — | — | 1 | 6.10 |
| CHEMBL372627 | — | — | 1 | 6.08 |
| CHEMBL363755 | — | — | 1 | 6.05 |
| CHEMBL372830 | — | — | 1 | 6.03 |
| CHEMBL197218 | — | — | 1 | 6.00 |
| CHEMBL105613 | — | — | 1 | 5.96 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL188678 | — | Ki | = | 0.65 | nM | 9.19 |
| CHEMBL188678 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL198750 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL186048 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL104468 | — | IC50 | = | 230.0 | nM | 6.64 |
| CHEMBL198675 | — | IC50 | = | 250.0 | nM | 6.60 |
| CHEMBL360183 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL198482 | — | IC50 | = | 350.0 | nM | 6.46 |
| CHEMBL95298 | — | IC50 | = | 380.0 | nM | 6.42 |
| CHEMBL175883 | — | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL197004 | — | IC50 | = | 440.0 | nM | 6.36 |
| CHEMBL197379 | — | IC50 | = | 440.0 | nM | 6.36 |
| CHEMBL197536 | — | IC50 | = | 450.0 | nM | 6.35 |
| CHEMBL427194 | — | IC50 | = | 470.0 | nM | 6.33 |
| CHEMBL198576 | — | IC50 | = | 490.0 | nM | 6.31 |
| CHEMBL199577 | — | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL372143 | — | IC50 | = | 560.0 | nM | 6.25 |
| CHEMBL189552 | — | IC50 | = | 600.0 | nM | 6.22 |
| CHEMBL371947 | — | IC50 | = | 690.0 | nM | 6.16 |
| CHEMBL362729 | — | IC50 | = | 700.0 | nM | 6.16 |
| CHEMBL201988 | — | IC50 | = | 710.0 | nM | 6.15 |
| CHEMBL276746 | — | IC50 | = | 720.0 | nM | 6.14 |
| CHEMBL198138 | — | IC50 | = | 790.0 | nM | 6.10 |
| CHEMBL362521 | — | IC50 | = | 800.0 | nM | 6.10 |
| CHEMBL187562 | — | IC50 | = | 800.0 | nM | 6.10 |
| CHEMBL196870 | — | IC50 | = | 800.0 | nM | 6.10 |
| CHEMBL372627 | — | IC50 | = | 840.0 | nM | 6.08 |
| CHEMBL363755 | — | IC50 | = | 900.0 | nM | 6.05 |
| CHEMBL372830 | — | IC50 | = | 940.0 | nM | 6.03 |
| CHEMBL197218 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL105613 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL372633 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL198898 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL200685 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL426099 | — | IC50 | = | 1320.0 | nM | 5.88 |
| CHEMBL360038 | — | IC50 | = | 1380.0 | nM | 5.86 |
| CHEMBL200201 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL98350 | LY-294002 | IC50 | = | 1470.0 | nM | 5.83 |
| CHEMBL198476 | — | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL198944 | — | IC50 | = | 1680.0 | nM | 5.78 |
| CHEMBL199165 | — | IC50 | = | 1920.0 | nM | 5.72 |
| CHEMBL371468 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL372143 | — | IC50 | = | 2020.0 | nM | 5.70 |
| CHEMBL197391 | — | IC50 | = | 2300.0 | nM | 5.64 |
| CHEMBL200733 | — | IC50 | = | 2400.0 | nM | 5.62 |
| CHEMBL197487 | — | IC50 | = | 2530.0 | nM | 5.60 |
| CHEMBL200517 | — | IC50 | = | 2600.0 | nM | 5.58 |
| CHEMBL200567 | — | IC50 | = | 2600.0 | nM | 5.58 |
| CHEMBL383376 | — | IC50 | = | 2700.0 | nM | 5.57 |
| CHEMBL369990 | — | IC50 | = | 2800.0 | nM | 5.55 |