Assay Detail
Binding
CHEMBL5045649
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of GST-ATAD2 BD (981 to 1108 residues) (unknown origin) expressed in Escherichia coli BL21 (DE3) and biotinylated tetra-acetylated histone H4 peptides as substrate incubated for 30 mins by TR-FRET assay
23
Total Activities
23
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
ATPase family AAA domain-containing protein 2 (CHEMBL2150837) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Discovery of a Potent and Selective ATAD2 Bromodomain Inhibitor with Antiproliferative Activity in Breast Cancer Models.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 23 | 6.21 | 8.20 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5079885 | — | — | 1 | 8.20 |
| CHEMBL5087319 | — | — | 1 | 7.80 |
| CHEMBL5090369 | — | — | 1 | 7.70 |
| CHEMBL5093862 | — | — | 1 | 7.70 |
| CHEMBL5077167 | — | — | 1 | 7.50 |
| CHEMBL5086059 | — | — | 1 | 7.40 |
| CHEMBL5086260 | — | — | 1 | 7.10 |
| CHEMBL5074983 | — | — | 1 | 6.70 |
| CHEMBL5084768 | — | — | 1 | 6.60 |
| CHEMBL5093167 | — | — | 1 | 6.40 |
| CHEMBL5083025 | — | — | 1 | 6.40 |
| CHEMBL5092181 | — | — | 1 | 6.40 |
| CHEMBL5083653 | — | — | 1 | 5.80 |
| CHEMBL5074478 | — | — | 1 | 5.50 |
| CHEMBL5090538 | — | — | 1 | 5.50 |
| CHEMBL5087156 | — | — | 1 | 5.30 |
| CHEMBL5075463 | — | — | 1 | 5.20 |
| CHEMBL5087174 | — | — | 1 | 4.90 |
| CHEMBL5074753 | — | — | 1 | 4.70 |
| CHEMBL5090410 | — | — | 1 | 4.70 |
| CHEMBL5083337 | — | — | 1 | 4.60 |
| CHEMBL5084439 | — | — | 1 | 4.50 |
| CHEMBL5077001 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5079885 | — | IC50 | = | 6.31 | nM | 8.20 |
| CHEMBL5087319 | — | IC50 | = | 15.85 | nM | 7.80 |
| CHEMBL5090369 | — | IC50 | = | 19.95 | nM | 7.70 |
| CHEMBL5093862 | — | IC50 | = | 19.95 | nM | 7.70 |
| CHEMBL5077167 | — | IC50 | = | 31.62 | nM | 7.50 |
| CHEMBL5086059 | — | IC50 | = | 39.81 | nM | 7.40 |
| CHEMBL5086260 | — | IC50 | = | 79.43 | nM | 7.10 |
| CHEMBL5074983 | — | IC50 | = | 199.53 | nM | 6.70 |
| CHEMBL5084768 | — | IC50 | = | 251.19 | nM | 6.60 |
| CHEMBL5093167 | — | IC50 | = | 398.11 | nM | 6.40 |
| CHEMBL5083025 | — | IC50 | = | 398.11 | nM | 6.40 |
| CHEMBL5092181 | — | IC50 | = | 398.11 | nM | 6.40 |
| CHEMBL5083653 | — | IC50 | = | 1584.89 | nM | 5.80 |
| CHEMBL5074478 | — | IC50 | = | 3162.28 | nM | 5.50 |
| CHEMBL5090538 | — | IC50 | = | 3162.28 | nM | 5.50 |
| CHEMBL5087156 | — | IC50 | = | 5011.87 | nM | 5.30 |
| CHEMBL5075463 | — | IC50 | = | 6309.57 | nM | 5.20 |
| CHEMBL5087174 | — | IC50 | = | 12589.25 | nM | 4.90 |
| CHEMBL5074753 | — | IC50 | = | 19952.62 | nM | 4.70 |
| CHEMBL5090410 | — | IC50 | = | 19952.62 | nM | 4.70 |
| CHEMBL5083337 | — | IC50 | = | 25118.86 | nM | 4.60 |
| CHEMBL5084439 | — | IC50 | = | 31622.78 | nM | 4.50 |
| CHEMBL5077001 | — | IC50 | > | 19952.62 | nM | - |