Assay Detail
Binding
CHEMBL4194886
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Binding affinity to BRD4 in human H1299 cells stably expressing E2 and HPV16-LCR luciferase reporter incubated for 24 hrs by Bright-Glo luciferase reporter gene assay based BRD4 engagement assay
28
Total Activities
28
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 and optimization of novel constrained pyrrolopyridone BET family inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 28 | 7.66 | 8.82 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4212498 | — | — | 1 | 8.82 |
| CHEMBL4208129 | — | — | 1 | 8.77 |
| CHEMBL4213481 | — | — | 1 | 8.64 |
| CHEMBL4215988 | — | — | 1 | 8.60 |
| CHEMBL4217457 | — | — | 1 | 8.44 |
| CHEMBL4208136 | — | — | 1 | 8.43 |
| CHEMBL4213045 | — | — | 1 | 8.39 |
| CHEMBL4218411 | — | — | 1 | 8.37 |
| CHEMBL4212062 | — | — | 1 | 8.34 |
| CHEMBL4204316 | — | — | 1 | 8.19 |
| CHEMBL4217818 | — | — | 1 | 8.05 |
| CHEMBL4214501 | — | — | 1 | 7.75 |
| CHEMBL3987016 | MIVEBRESIB | 2.0 | 1 | 7.70 |
| CHEMBL3978817 | — | — | 1 | 7.70 |
| CHEMBL4202833 | — | — | 1 | 7.68 |
| CHEMBL4210131 | — | — | 1 | 7.64 |
| CHEMBL4215043 | — | — | 1 | 7.64 |
| CHEMBL4202497 | — | — | 1 | 7.55 |
| CHEMBL4203764 | — | — | 1 | 7.51 |
| CHEMBL4206058 | — | — | 1 | 7.50 |
| CHEMBL4208643 | — | — | 1 | 7.32 |
| CHEMBL3903195 | — | — | 1 | 7.24 |
| CHEMBL4217560 | — | — | 1 | 7.02 |
| CHEMBL4215025 | — | — | 1 | 6.82 |
| CHEMBL4207708 | — | — | 1 | 6.72 |
| CHEMBL4207179 | — | — | 1 | 6.70 |
| CHEMBL3904546 | — | — | 1 | 5.72 |
| CHEMBL4203377 | — | — | 1 | 5.30 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4212498 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL4208129 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL4213481 | — | IC50 | = | 2.3 | nM | 8.64 |
| CHEMBL4215988 | — | IC50 | = | 2.5 | nM | 8.60 |
| CHEMBL4217457 | — | IC50 | = | 3.6 | nM | 8.44 |
| CHEMBL4208136 | — | IC50 | = | 3.7 | nM | 8.43 |
| CHEMBL4213045 | — | IC50 | = | 4.1 | nM | 8.39 |
| CHEMBL4218411 | — | IC50 | = | 4.3 | nM | 8.37 |
| CHEMBL4212062 | — | IC50 | = | 4.6 | nM | 8.34 |
| CHEMBL4204316 | — | IC50 | = | 6.5 | nM | 8.19 |
| CHEMBL4217818 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL4214501 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL3987016 | MIVEBRESIB | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL3978817 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL4202833 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL4210131 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL4215043 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL4202497 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL4203764 | — | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL4206058 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL4208643 | — | IC50 | = | 48.0 | nM | 7.32 |
| CHEMBL3903195 | — | IC50 | = | 58.0 | nM | 7.24 |
| CHEMBL4217560 | — | IC50 | = | 95.0 | nM | 7.02 |
| CHEMBL4215025 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL4207708 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL4207179 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL3904546 | — | IC50 | = | 1900.0 | nM | 5.72 |
| CHEMBL4203377 | — | IC50 | = | 5000.0 | nM | 5.30 |