Assay Detail
Binding
CHEMBL4733659
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of His-tagged BRD4 bromodomain 1 (unknown origin) using [Lys (5,8,12,16) Ac] H4(1-21) as substrate by fluorescence based assay
46
Total Activities
46
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 selective HDAC/BRD4 dual inhibitors as epigenetic probes.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 46 | 7.26 | 8.41 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4763504 | — | — | 1 | 8.41 |
| CHEMBL4747126 | — | — | 1 | 8.25 |
| CHEMBL4758435 | — | — | 1 | 8.11 |
| CHEMBL3581647 | BIRABRESIB | 2.0 | 1 | 8.04 |
| CHEMBL4800001 | — | — | 1 | 7.88 |
| CHEMBL4761044 | — | — | 1 | 7.87 |
| CHEMBL4776819 | — | — | 1 | 7.74 |
| CHEMBL4757853 | — | — | 1 | 7.70 |
| CHEMBL4777392 | — | — | 1 | 7.67 |
| CHEMBL4763062 | — | — | 1 | 7.65 |
| CHEMBL4780985 | — | — | 1 | 7.64 |
| CHEMBL4784336 | — | — | 1 | 7.58 |
| CHEMBL4755061 | — | — | 1 | 7.53 |
| CHEMBL4741981 | — | — | 1 | 7.52 |
| CHEMBL4753908 | — | — | 1 | 7.50 |
| CHEMBL4742103 | — | — | 1 | 7.50 |
| CHEMBL4798212 | — | — | 1 | 7.41 |
| CHEMBL4745135 | — | — | 1 | 7.39 |
| CHEMBL4793324 | — | — | 1 | 7.38 |
| CHEMBL4757963 | — | — | 1 | 7.36 |
| CHEMBL4745597 | — | — | 1 | 7.32 |
| CHEMBL4758664 | — | — | 1 | 7.29 |
| CHEMBL4749464 | — | — | 1 | 7.28 |
| CHEMBL4749756 | — | — | 1 | 7.27 |
| CHEMBL4758756 | — | — | 1 | 7.21 |
| CHEMBL4757429 | — | — | 1 | 7.21 |
| CHEMBL4761541 | — | — | 1 | 7.18 |
| CHEMBL4798570 | — | — | 1 | 7.14 |
| CHEMBL4788497 | — | — | 1 | 7.12 |
| CHEMBL4749433 | — | — | 1 | 7.07 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4763504 | — | IC50 | = | 3.9 | nM | 8.41 |
| CHEMBL4747126 | — | IC50 | = | 5.6 | nM | 8.25 |
| CHEMBL4758435 | — | IC50 | = | 7.7 | nM | 8.11 |
| CHEMBL3581647 | BIRABRESIB | IC50 | = | 9.2 | nM | 8.04 |
| CHEMBL4800001 | — | IC50 | = | 13.1 | nM | 7.88 |
| CHEMBL4761044 | — | IC50 | = | 13.4 | nM | 7.87 |
| CHEMBL4776819 | — | IC50 | = | 18.1 | nM | 7.74 |
| CHEMBL4757853 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL4777392 | — | IC50 | = | 21.4 | nM | 7.67 |
| CHEMBL4763062 | — | IC50 | = | 22.6 | nM | 7.65 |
| CHEMBL4780985 | — | IC50 | = | 22.8 | nM | 7.64 |
| CHEMBL4784336 | — | IC50 | = | 26.2 | nM | 7.58 |
| CHEMBL4755061 | — | IC50 | = | 29.5 | nM | 7.53 |
| CHEMBL4741981 | — | IC50 | = | 30.1 | nM | 7.52 |
| CHEMBL4742103 | — | IC50 | = | 31.7 | nM | 7.50 |
| CHEMBL4753908 | — | IC50 | = | 31.3 | nM | 7.50 |
| CHEMBL4798212 | — | IC50 | = | 38.6 | nM | 7.41 |
| CHEMBL4745135 | — | IC50 | = | 40.5 | nM | 7.39 |
| CHEMBL4793324 | — | IC50 | = | 42.1 | nM | 7.38 |
| CHEMBL4757963 | — | IC50 | = | 44.1 | nM | 7.36 |
| CHEMBL4745597 | — | IC50 | = | 47.8 | nM | 7.32 |
| CHEMBL4758664 | — | IC50 | = | 50.9 | nM | 7.29 |
| CHEMBL4749464 | — | IC50 | = | 52.8 | nM | 7.28 |
| CHEMBL4749756 | — | IC50 | = | 54.0 | nM | 7.27 |
| CHEMBL4757429 | — | IC50 | = | 61.0 | nM | 7.21 |
| CHEMBL4758756 | — | IC50 | = | 62.4 | nM | 7.21 |
| CHEMBL4761541 | — | IC50 | = | 65.5 | nM | 7.18 |
| CHEMBL4798570 | — | IC50 | = | 73.0 | nM | 7.14 |
| CHEMBL4788497 | — | IC50 | = | 76.7 | nM | 7.12 |
| CHEMBL4749433 | — | IC50 | = | 85.9 | nM | 7.07 |
| CHEMBL4749460 | — | IC50 | = | 101.6 | nM | 6.99 |
| CHEMBL4753402 | — | IC50 | = | 117.4 | nM | 6.93 |
| CHEMBL4778531 | — | IC50 | = | 142.0 | nM | 6.85 |
| CHEMBL4757283 | — | IC50 | = | 139.9 | nM | 6.85 |
| CHEMBL4798322 | — | IC50 | = | 146.0 | nM | 6.84 |
| CHEMBL4753930 | — | IC50 | = | 228.8 | nM | 6.64 |
| CHEMBL4781215 | — | IC50 | = | 252.0 | nM | 6.60 |
| CHEMBL4753842 | — | IC50 | = | 305.0 | nM | 6.52 |
| CHEMBL4297454 | ABBV-744 | IC50 | = | 327.5 | nM | 6.49 |
| CHEMBL4752600 | — | IC50 | = | 371.0 | nM | 6.43 |
| CHEMBL4794499 | — | IC50 | = | 368.7 | nM | 6.43 |
| CHEMBL4750537 | — | IC50 | = | 583.0 | nM | 6.23 |
| CHEMBL4743731 | — | IC50 | = | 823.0 | nM | 6.08 |
| CHEMBL98 | VORINOSTAT | IC50 | > | 10000.0 | nM | - |
| CHEMBL4778689 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL27759 | ENTINOSTAT | IC50 | > | 10000.0 | nM | - |