Assay Detail
Binding
CHEMBL5216112
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Inhibition of BRD4 (unknown origin) expressed in Escherichia coli BL21 (DE3) using [Lys(Ac)5/8/12/16]-histone H4 (1 to 21residues)-GGK as substrate incubated for 30 mins by TR-FRET assay
24
Total Activities
24
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
Discovery of Novel BRD4 Ligand Scaffolds by Automated Navigation of the Fragment Chemical Space.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 24 | 3.96 | 4.58 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5218482 | — | — | 1 | 4.58 |
| CHEMBL5219547 | — | — | 1 | 4.52 |
| CHEMBL197512 | — | — | 1 | 4.14 |
| CHEMBL5220412 | — | — | 1 | 4.10 |
| CHEMBL5220338 | — | — | 1 | 4.07 |
| CHEMBL2431088 | — | — | 1 | 4.04 |
| CHEMBL5220563 | — | — | 1 | 3.72 |
| CHEMBL5218934 | — | — | 1 | 3.31 |
| CHEMBL5219925 | — | — | 1 | 3.19 |
| CHEMBL5219301 | — | — | 1 | - |
| CHEMBL5220571 | — | — | 1 | - |
| CHEMBL5220909 | — | — | 1 | - |
| CHEMBL5220081 | — | — | 1 | - |
| CHEMBL1536867 | — | — | 1 | - |
| CHEMBL5219185 | — | — | 1 | - |
| CHEMBL5220065 | — | — | 1 | - |
| CHEMBL5218493 | — | — | 1 | - |
| CHEMBL5219610 | — | — | 1 | - |
| CHEMBL5218610 | — | — | 1 | - |
| CHEMBL5219368 | — | — | 1 | - |
| CHEMBL5219549 | — | — | 1 | - |
| CHEMBL5219295 | — | — | 1 | - |
| CHEMBL5220722 | — | — | 1 | - |
| CHEMBL4470721 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5218482 | — | IC50 | = | 26000.0 | nM | 4.58 |
| CHEMBL5219547 | — | IC50 | = | 30000.0 | nM | 4.52 |
| CHEMBL197512 | — | IC50 | = | 72000.0 | nM | 4.14 |
| CHEMBL5220412 | — | IC50 | = | 79000.0 | nM | 4.10 |
| CHEMBL5220338 | — | IC50 | = | 86000.0 | nM | 4.07 |
| CHEMBL2431088 | — | IC50 | = | 91000.0 | nM | 4.04 |
| CHEMBL5220563 | — | IC50 | = | 191000.0 | nM | 3.72 |
| CHEMBL5218934 | — | IC50 | = | 491000.0 | nM | 3.31 |
| CHEMBL5219925 | — | IC50 | = | 644000.0 | nM | 3.19 |
| CHEMBL5219301 | — | IC50 | - | — | - | |
| CHEMBL5220571 | — | IC50 | - | — | - | |
| CHEMBL5220909 | — | IC50 | - | — | - | |
| CHEMBL5220081 | — | IC50 | - | — | - | |
| CHEMBL1536867 | — | IC50 | - | — | - | |
| CHEMBL5219185 | — | IC50 | - | — | - | |
| CHEMBL5220065 | — | IC50 | - | — | - | |
| CHEMBL5218493 | — | IC50 | - | — | - | |
| CHEMBL5219610 | — | IC50 | - | — | - | |
| CHEMBL5218610 | — | IC50 | - | — | - | |
| CHEMBL5219368 | — | IC50 | - | — | - | |
| CHEMBL5219549 | — | IC50 | - | — | - | |
| CHEMBL5219295 | — | IC50 | - | — | - | |
| CHEMBL5220722 | — | IC50 | - | — | - | |
| CHEMBL4470721 | — | IC50 | - | — | - |