Assay Detail
Binding
CHEMBL5045659
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of Halo-tagged Histone H3.3 from Nanoluc-ATAD2 BD (962 to 1119 residues) (unknown origin) transfected in human HCT116 cells incubated for 18 hrs in presence of efflux inhibitor elacridar by NanoBRET assay
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HCT-116 |
| 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 | 4 | 6.50 | 7.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5079885 | — | — | 1 | 7.00 |
| CHEMBL4206758 | — | — | 1 | 6.60 |
| CHEMBL5090369 | — | — | 1 | 6.30 |
| CHEMBL5086260 | — | — | 1 | 6.10 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5079885 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL4206758 | — | IC50 | = | 251.19 | nM | 6.60 |
| CHEMBL5090369 | — | IC50 | = | 501.19 | nM | 6.30 |
| CHEMBL5086260 | — | IC50 | = | 794.33 | nM | 6.10 |