Assay Detail
Binding
CHEMBL4403931
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human HeLa cell-derived full length DNA-PK catalytic subunit using fluorescein-EPPLSQEAFADLWKK as substrate preincubated for 30 mins followed by substrate addition and measured after 40 mins TR-FRET assay
21
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HeLa |
| 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 | 21 | 8.81 | 10.10 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4447991 | — | — | 1 | 10.10 |
| CHEMBL4560221 | — | — | 1 | 9.80 |
| CHEMBL4450232 | — | — | 1 | 9.70 |
| CHEMBL4553941 | — | — | 1 | 9.60 |
| CHEMBL4555040 | — | — | 1 | 9.50 |
| CHEMBL4581254 | — | — | 1 | 9.50 |
| CHEMBL4513701 | — | — | 1 | 9.40 |
| CHEMBL4474647 | — | — | 1 | 9.40 |
| CHEMBL4439259 | AZD-7648 | 1.0 | 2 | 9.22 |
| CHEMBL4459057 | — | — | 1 | 8.70 |
| CHEMBL4438672 | — | — | 1 | 8.60 |
| CHEMBL4474502 | — | — | 1 | 8.50 |
| CHEMBL4529390 | — | — | 1 | 8.30 |
| CHEMBL4483014 | — | — | 1 | 8.30 |
| CHEMBL4586576 | — | — | 1 | 8.20 |
| CHEMBL4552812 | — | — | 1 | 8.10 |
| CHEMBL4466619 | — | — | 1 | 8.00 |
| CHEMBL4449235 | — | — | 1 | 8.00 |
| CHEMBL4450430 | — | — | 1 | 7.90 |
| CHEMBL4456514 | — | — | 1 | 6.90 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4447991 | — | IC50 | = | 0.07943 | nM | 10.10 |
| CHEMBL4560221 | — | IC50 | = | 0.1585 | nM | 9.80 |
| CHEMBL4450232 | — | IC50 | = | 0.1995 | nM | 9.70 |
| CHEMBL4553941 | — | IC50 | = | 0.2512 | nM | 9.60 |
| CHEMBL4555040 | — | IC50 | = | 0.3162 | nM | 9.50 |
| CHEMBL4581254 | — | IC50 | = | 0.3162 | nM | 9.50 |
| CHEMBL4513701 | — | IC50 | = | 0.3981 | nM | 9.40 |
| CHEMBL4474647 | — | IC50 | = | 0.3981 | nM | 9.40 |
| CHEMBL4439259 | AZD-7648 | IC50 | = | 0.6 | nM | 9.22 |
| CHEMBL4439259 | AZD-7648 | IC50 | = | 0.631 | nM | 9.20 |
| CHEMBL4459057 | — | IC50 | = | 1.995 | nM | 8.70 |
| CHEMBL4438672 | — | IC50 | = | 2.512 | nM | 8.60 |
| CHEMBL4474502 | — | IC50 | = | 3.162 | nM | 8.50 |
| CHEMBL4529390 | — | IC50 | = | 5.012 | nM | 8.30 |
| CHEMBL4483014 | — | IC50 | = | 5.012 | nM | 8.30 |
| CHEMBL4586576 | — | IC50 | = | 6.31 | nM | 8.20 |
| CHEMBL4552812 | — | IC50 | = | 7.943 | nM | 8.10 |
| CHEMBL4466619 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL4449235 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL4450430 | — | IC50 | = | 12.59 | nM | 7.90 |
| CHEMBL4456514 | — | IC50 | = | 125.89 | nM | 6.90 |