Assay Detail
Binding
CHEMBL5547050
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human full-length DNA-PK using EPPLSQEAFADLWKK as substrate incubated for 60 mins in presence of ATP by ADP-Glo kinase assay
16
Total Activities
16
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
Discovery of Novel Heterotricyclic Compounds as DNA-Dependent Protein Kinase (DNA-PK) Inhibitors with Enhanced Chemosensitivity, Oral Bioavailability, and the Ability to Potentiate Cancer Immunotherapy.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 16 | 8.23 | 9.96 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5570653 | — | — | 1 | 9.96 |
| CHEMBL5575934 | — | — | 1 | 9.46 |
| CHEMBL5573665 | — | — | 1 | 9.21 |
| CHEMBL5191459 | — | — | 1 | 9.10 |
| CHEMBL4439259 | AZD-7648 | 1.0 | 1 | 8.92 |
| CHEMBL5566235 | — | — | 1 | 8.44 |
| CHEMBL5575262 | — | — | 1 | 8.25 |
| CHEMBL5594841 | — | — | 1 | 8.08 |
| CHEMBL5574154 | — | — | 1 | 8.05 |
| CHEMBL5573849 | — | — | 1 | 7.82 |
| CHEMBL5573920 | — | — | 1 | 7.67 |
| CHEMBL5573858 | — | — | 1 | 7.58 |
| CHEMBL5574170 | — | — | 1 | 7.53 |
| CHEMBL5570510 | — | — | 1 | 7.29 |
| CHEMBL5575434 | — | — | 1 | 7.20 |
| CHEMBL5575062 | — | — | 1 | 7.15 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5570653 | — | IC50 | = | 0.11 | nM | 9.96 |
| CHEMBL5575934 | — | IC50 | = | 0.35 | nM | 9.46 |
| CHEMBL5573665 | — | IC50 | = | 0.62 | nM | 9.21 |
| CHEMBL5191459 | — | IC50 | = | 0.8 | nM | 9.10 |
| CHEMBL4439259 | AZD-7648 | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL5566235 | — | IC50 | = | 3.6 | nM | 8.44 |
| CHEMBL5575262 | — | IC50 | = | 5.6 | nM | 8.25 |
| CHEMBL5594841 | — | IC50 | = | 8.4 | nM | 8.08 |
| CHEMBL5574154 | — | IC50 | = | 8.9 | nM | 8.05 |
| CHEMBL5573849 | — | IC50 | = | 15.3 | nM | 7.82 |
| CHEMBL5573920 | — | IC50 | = | 21.4 | nM | 7.67 |
| CHEMBL5573858 | — | IC50 | = | 26.1 | nM | 7.58 |
| CHEMBL5574170 | — | IC50 | = | 29.4 | nM | 7.53 |
| CHEMBL5570510 | — | IC50 | = | 51.8 | nM | 7.29 |
| CHEMBL5575434 | — | IC50 | = | 62.8 | nM | 7.20 |
| CHEMBL5575062 | — | IC50 | = | 71.5 | nM | 7.15 |