Assay Detail
Binding
CHEMBL4403932
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of DNA-PK in human A549 cells assessed as reduction in irradiation-induced autophosphorylation at S2056 residue preincubated for 1 hr followed by 8 Gy irradiation and measured after 1 hr by ELISA
18
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | A549 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
DNA-dependent protein kinase catalytic subunit (CHEMBL3142) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
The Discovery of 7-Methyl-2-[(7-methyl[1,2,4]triazolo[1,5-<i>a</i>]pyridin-6-yl)amino]-9-(tetrahydro-2<i>H</i>-pyran-4-yl)-7,9-dihydro-8<i>H</i>-purin-8-one (AZD7648), a Potent and Selective DNA-Dependent Protein Kinase (DNA-PK) Inhibitor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 18 | 6.77 | 7.60 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4560221 | — | — | 1 | 7.60 |
| CHEMBL4555040 | — | — | 1 | 7.50 |
| CHEMBL4450232 | — | — | 1 | 7.30 |
| CHEMBL4447991 | — | — | 1 | 7.30 |
| CHEMBL4474647 | — | — | 1 | 7.30 |
| CHEMBL4513701 | — | — | 1 | 7.20 |
| CHEMBL4439259 | AZD-7648 | 1.0 | 2 | 7.04 |
| CHEMBL4581254 | — | — | 1 | 6.90 |
| CHEMBL4474502 | — | — | 1 | 6.90 |
| CHEMBL4459057 | — | — | 1 | 6.80 |
| CHEMBL4449235 | — | — | 1 | 6.60 |
| CHEMBL4553941 | — | — | 1 | 6.60 |
| CHEMBL4483014 | — | — | 1 | 6.50 |
| CHEMBL4438672 | — | — | 1 | 6.40 |
| CHEMBL4466619 | — | — | 1 | 5.90 |
| CHEMBL4529390 | — | — | 1 | 5.70 |
| CHEMBL4456514 | — | — | 1 | 5.30 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4560221 | — | IC50 | = | 25.12 | nM | 7.60 |
| CHEMBL4555040 | — | IC50 | = | 31.62 | nM | 7.50 |
| CHEMBL4450232 | — | IC50 | = | 50.12 | nM | 7.30 |
| CHEMBL4447991 | — | IC50 | = | 50.12 | nM | 7.30 |
| CHEMBL4474647 | — | IC50 | = | 50.12 | nM | 7.30 |
| CHEMBL4513701 | — | IC50 | = | 63.1 | nM | 7.20 |
| CHEMBL4439259 | AZD-7648 | IC50 | = | 91.0 | nM | 7.04 |
| CHEMBL4439259 | AZD-7648 | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL4581254 | — | IC50 | = | 125.89 | nM | 6.90 |
| CHEMBL4474502 | — | IC50 | = | 125.89 | nM | 6.90 |
| CHEMBL4459057 | — | IC50 | = | 158.49 | nM | 6.80 |
| CHEMBL4553941 | — | IC50 | = | 251.19 | nM | 6.60 |
| CHEMBL4449235 | — | IC50 | = | 251.19 | nM | 6.60 |
| CHEMBL4483014 | — | IC50 | = | 316.23 | nM | 6.50 |
| CHEMBL4438672 | — | IC50 | = | 398.11 | nM | 6.40 |
| CHEMBL4466619 | — | IC50 | = | 1258.93 | nM | 5.90 |
| CHEMBL4529390 | — | IC50 | = | 1995.26 | nM | 5.70 |
| CHEMBL4456514 | — | IC50 | = | 5011.87 | nM | 5.30 |