Assay Detail
Binding
CHEMBL4839369
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of DNA-PK in human HT-144 cells assessed as reduction in gammaH2AX phosphorylation incubated for 30 mins by fluorescence assay
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HT-144 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
DNA-dependent protein kinase catalytic subunit (CHEMBL3142) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
BAY-8400: A Novel Potent and Selective DNA-PK Inhibitor which Shows Synergistic Efficacy in Combination with Targeted Alpha Therapies.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 9 | 6.96 | 7.36 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4871998 | — | — | 1 | 7.36 |
| CHEMBL4849035 | — | — | 1 | 7.33 |
| CHEMBL4850640 | — | — | 1 | 7.28 |
| CHEMBL4860779 | — | — | 1 | 7.22 |
| CHEMBL4851439 | — | — | 1 | 7.16 |
| CHEMBL4860129 | — | — | 1 | 7.04 |
| CHEMBL4873263 | — | — | 1 | 7.01 |
| CHEMBL4875626 | — | — | 1 | 6.30 |
| CHEMBL4867528 | — | — | 1 | 5.95 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4871998 | — | IC50 | = | 44.0 | nM | 7.36 |
| CHEMBL4849035 | — | IC50 | = | 47.0 | nM | 7.33 |
| CHEMBL4850640 | — | IC50 | = | 53.0 | nM | 7.28 |
| CHEMBL4860779 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL4851439 | — | IC50 | = | 69.0 | nM | 7.16 |
| CHEMBL4860129 | — | IC50 | = | 92.0 | nM | 7.04 |
| CHEMBL4873263 | — | IC50 | = | 98.0 | nM | 7.01 |
| CHEMBL4875626 | — | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL4867528 | — | IC50 | = | 1130.0 | nM | 5.95 |