Assay Detail
Binding
CHEMBL5045652
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of GST-ATAD2 BD (951 to 1132 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
22
Total Activities
22
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 | 22 | 6.19 | 8.15 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5079885 | — | — | 1 | 8.15 |
| CHEMBL5087319 | — | — | 1 | 7.85 |
| CHEMBL5093862 | — | — | 1 | 7.70 |
| CHEMBL5090369 | — | — | 1 | 7.66 |
| CHEMBL5086059 | — | — | 1 | 7.39 |
| CHEMBL5086260 | — | — | 1 | 7.11 |
| CHEMBL5074983 | — | — | 1 | 6.68 |
| CHEMBL5084768 | — | — | 1 | 6.55 |
| CHEMBL5077167 | — | — | 1 | 6.52 |
| CHEMBL5092181 | — | — | 1 | 6.43 |
| CHEMBL5083025 | — | — | 1 | 6.38 |
| CHEMBL5093167 | — | — | 1 | 6.36 |
| CHEMBL5083653 | — | — | 1 | 5.83 |
| CHEMBL5090538 | — | — | 1 | 5.45 |
| CHEMBL5087156 | — | — | 1 | 5.31 |
| CHEMBL5075463 | — | — | 1 | 5.22 |
| CHEMBL5087174 | — | — | 1 | 4.93 |
| CHEMBL5090410 | — | — | 1 | 4.70 |
| CHEMBL5074753 | — | — | 1 | 4.67 |
| CHEMBL5083337 | — | — | 1 | 4.58 |
| CHEMBL5084439 | — | — | 1 | 4.46 |
| CHEMBL5077001 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5079885 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL5087319 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL5093862 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL5090369 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL5086059 | — | IC50 | = | 41.0 | nM | 7.39 |
| CHEMBL5086260 | — | IC50 | = | 78.0 | nM | 7.11 |
| CHEMBL5074983 | — | IC50 | = | 210.0 | nM | 6.68 |
| CHEMBL5084768 | — | IC50 | = | 280.0 | nM | 6.55 |
| CHEMBL5077167 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL5092181 | — | IC50 | = | 370.0 | nM | 6.43 |
| CHEMBL5083025 | — | IC50 | = | 420.0 | nM | 6.38 |
| CHEMBL5093167 | — | IC50 | = | 440.0 | nM | 6.36 |
| CHEMBL5083653 | — | IC50 | = | 1480.0 | nM | 5.83 |
| CHEMBL5090538 | — | IC50 | = | 3560.0 | nM | 5.45 |
| CHEMBL5087156 | — | IC50 | = | 4880.0 | nM | 5.31 |
| CHEMBL5075463 | — | IC50 | = | 6080.0 | nM | 5.22 |
| CHEMBL5087174 | — | IC50 | = | 11800.0 | nM | 4.93 |
| CHEMBL5090410 | — | IC50 | = | 20200.0 | nM | 4.70 |
| CHEMBL5074753 | — | IC50 | = | 21200.0 | nM | 4.67 |
| CHEMBL5083337 | — | IC50 | = | 26300.0 | nM | 4.58 |
| CHEMBL5084439 | — | IC50 | = | 34300.0 | nM | 4.46 |
| CHEMBL5077001 | — | IC50 | > | 20000.0 | nM | - |