Assay Detail
Binding
CHEMBL664848
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In vitro inhibition of DNA-dependent protein kinase(DNA-PK) from HeLa (human carcinoma) cells.
22
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Cell Type | HeLa |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Target
DNA-dependent protein kinase catalytic subunit (CHEMBL3142) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
2,6-disubstituted pyran-4-one and thiopyran-4-one inhibitors of DNA-Dependent protein kinase (DNA-PK).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 22 | 6.33 | 6.75 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL105612 | — | — | 1 | 6.75 |
| CHEMBL105678 | — | — | 1 | 6.72 |
| CHEMBL319261 | — | — | 1 | 6.66 |
| CHEMBL104468 | — | — | 1 | 6.64 |
| CHEMBL104682 | — | — | 1 | 6.58 |
| CHEMBL321784 | — | — | 1 | 6.55 |
| CHEMBL102581 | — | — | 1 | 6.48 |
| CHEMBL105521 | — | — | 1 | 6.46 |
| CHEMBL104450 | — | — | 1 | 6.46 |
| CHEMBL105256 | — | — | 1 | 6.42 |
| CHEMBL102529 | — | — | 1 | 6.32 |
| CHEMBL319909 | — | — | 1 | 6.28 |
| CHEMBL323136 | — | — | 1 | 6.28 |
| CHEMBL106543 | — | — | 1 | 6.27 |
| CHEMBL316769 | — | — | 1 | 6.17 |
| CHEMBL276746 | — | — | 1 | 6.14 |
| CHEMBL323145 | — | — | 1 | 6.10 |
| CHEMBL431228 | — | — | 1 | 6.08 |
| CHEMBL104644 | — | — | 1 | 6.04 |
| CHEMBL102396 | — | — | 1 | 6.04 |
| CHEMBL105613 | — | — | 1 | 5.96 |
| CHEMBL98350 | LY-294002 | -1.0 | 1 | 5.85 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL105612 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL105678 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL319261 | — | IC50 | = | 220.0 | nM | 6.66 |
| CHEMBL104468 | — | IC50 | = | 230.0 | nM | 6.64 |
| CHEMBL104682 | — | IC50 | = | 260.0 | nM | 6.58 |
| CHEMBL321784 | — | IC50 | = | 280.0 | nM | 6.55 |
| CHEMBL102581 | — | IC50 | = | 330.0 | nM | 6.48 |
| CHEMBL105521 | — | IC50 | = | 350.0 | nM | 6.46 |
| CHEMBL104450 | — | IC50 | = | 350.0 | nM | 6.46 |
| CHEMBL105256 | — | IC50 | = | 380.0 | nM | 6.42 |
| CHEMBL102529 | — | IC50 | = | 480.0 | nM | 6.32 |
| CHEMBL319909 | — | IC50 | = | 530.0 | nM | 6.28 |
| CHEMBL323136 | — | IC50 | = | 530.0 | nM | 6.28 |
| CHEMBL106543 | — | IC50 | = | 540.0 | nM | 6.27 |
| CHEMBL316769 | — | IC50 | = | 680.0 | nM | 6.17 |
| CHEMBL276746 | — | IC50 | = | 720.0 | nM | 6.14 |
| CHEMBL323145 | — | IC50 | = | 800.0 | nM | 6.10 |
| CHEMBL431228 | — | IC50 | = | 840.0 | nM | 6.08 |
| CHEMBL104644 | — | IC50 | = | 920.0 | nM | 6.04 |
| CHEMBL102396 | — | IC50 | = | 920.0 | nM | 6.04 |
| CHEMBL105613 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL98350 | LY-294002 | IC50 | = | 1400.0 | nM | 5.85 |