Assay Detail
Binding
CHEMBL4194884
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Binding affinity to His-tagged BRD4 bromodomain 1 to 2 (K57 to K550 amino acids) (unknown origin) using Alexa647-labeled BET-inhibitor as fluorescent probe by bromodomain TR-FRET binding 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 |
|---|---|---|---|
| Ki | 28 | 7.94 | 9.21 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4208129 | — | — | 1 | 9.21 |
| CHEMBL4217457 | — | — | 1 | 9.06 |
| CHEMBL4212498 | — | — | 1 | 9.06 |
| CHEMBL3987016 | MIVEBRESIB | 2.0 | 1 | 8.82 |
| CHEMBL4214501 | — | — | 1 | 8.57 |
| CHEMBL4204316 | — | — | 1 | 8.57 |
| CHEMBL4213481 | — | — | 1 | 8.54 |
| CHEMBL4215988 | — | — | 1 | 8.48 |
| CHEMBL4213045 | — | — | 1 | 8.39 |
| CHEMBL4206058 | — | — | 1 | 8.36 |
| CHEMBL4208136 | — | — | 1 | 8.33 |
| CHEMBL4218411 | — | — | 1 | 8.32 |
| CHEMBL4202833 | — | — | 1 | 8.15 |
| CHEMBL4217818 | — | — | 1 | 8.14 |
| CHEMBL4203764 | — | — | 1 | 8.11 |
| CHEMBL4212062 | — | — | 1 | 8.08 |
| CHEMBL4210131 | — | — | 1 | 7.92 |
| CHEMBL3978817 | — | — | 1 | 7.89 |
| CHEMBL4215043 | — | — | 1 | 7.80 |
| CHEMBL4208643 | — | — | 1 | 7.77 |
| CHEMBL4202497 | — | — | 1 | 7.58 |
| CHEMBL4217560 | — | — | 1 | 7.37 |
| CHEMBL3903195 | — | — | 1 | 7.16 |
| CHEMBL4215025 | — | — | 1 | 7.10 |
| CHEMBL4207708 | — | — | 1 | 6.75 |
| CHEMBL4207179 | — | — | 1 | 6.66 |
| CHEMBL3904546 | — | — | 1 | 6.17 |
| CHEMBL4203377 | — | — | 1 | 5.82 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4208129 | — | Ki | = | 0.62 | nM | 9.21 |
| CHEMBL4217457 | — | Ki | = | 0.87 | nM | 9.06 |
| CHEMBL4212498 | — | Ki | = | 0.87 | nM | 9.06 |
| CHEMBL3987016 | MIVEBRESIB | Ki | = | 1.5 | nM | 8.82 |
| CHEMBL4214501 | — | Ki | = | 2.7 | nM | 8.57 |
| CHEMBL4204316 | — | Ki | = | 2.7 | nM | 8.57 |
| CHEMBL4213481 | — | Ki | = | 2.9 | nM | 8.54 |
| CHEMBL4215988 | — | Ki | = | 3.3 | nM | 8.48 |
| CHEMBL4213045 | — | Ki | = | 4.1 | nM | 8.39 |
| CHEMBL4206058 | — | Ki | = | 4.4 | nM | 8.36 |
| CHEMBL4208136 | — | Ki | = | 4.7 | nM | 8.33 |
| CHEMBL4218411 | — | Ki | = | 4.8 | nM | 8.32 |
| CHEMBL4202833 | — | Ki | = | 7.1 | nM | 8.15 |
| CHEMBL4217818 | — | Ki | = | 7.3 | nM | 8.14 |
| CHEMBL4203764 | — | Ki | = | 7.7 | nM | 8.11 |
| CHEMBL4212062 | — | Ki | = | 8.4 | nM | 8.08 |
| CHEMBL4210131 | — | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL3978817 | — | Ki | = | 13.0 | nM | 7.89 |
| CHEMBL4215043 | — | Ki | = | 16.0 | nM | 7.80 |
| CHEMBL4208643 | — | Ki | = | 17.0 | nM | 7.77 |
| CHEMBL4202497 | — | Ki | = | 26.0 | nM | 7.58 |
| CHEMBL4217560 | — | Ki | = | 43.0 | nM | 7.37 |
| CHEMBL3903195 | — | Ki | = | 69.0 | nM | 7.16 |
| CHEMBL4215025 | — | Ki | = | 80.0 | nM | 7.10 |
| CHEMBL4207708 | — | Ki | = | 180.0 | nM | 6.75 |
| CHEMBL4207179 | — | Ki | = | 220.0 | nM | 6.66 |
| CHEMBL3904546 | — | Ki | = | 680.0 | nM | 6.17 |
| CHEMBL4203377 | — | Ki | = | 1500.0 | nM | 5.82 |