Assay Detail
Binding
CHEMBL5162525
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of C-terminal His6-tagged BRD3 BD2 (unknown origin) using H-YSGRGK(Ac)GGK(Ac)GLGK(Ac)-GGAK(Ac)RHRK-Biotin-OH as substrate incubated for 1 hrs by HTRF assay
4
Total Activities
4
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 |
Publication
Structure-Based Discovery and Optimization of Furo[3,2-<i>c</i>]pyridin-4(5<i>H</i>)-one Derivatives as Potent and Second Bromodomain (BD2)-Selective Bromo and Extra Terminal Domain (BET) Inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 4 | 8.39 | 9.06 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4297454 | ABBV-744 | 1.0 | 1 | 9.06 |
| CHEMBL1957266 | — | — | 1 | 8.31 |
| CHEMBL5206088 | — | — | 1 | 8.28 |
| CHEMBL5204783 | — | — | 1 | 7.89 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4297454 | ABBV-744 | IC50 | = | 0.88 | nM | 9.06 |
| CHEMBL1957266 | — | IC50 | = | 4.87 | nM | 8.31 |
| CHEMBL5206088 | — | IC50 | = | 5.31 | nM | 8.28 |
| CHEMBL5204783 | — | IC50 | = | 12.81 | nM | 7.89 |