Assay Detail
Binding
CHEMBL4020217
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding affinity to human N-terminal His6-tagged BRD4 BD1-BD2 (K57 to K550 residues) after 1 hr using alexa-647 conjugated probe by TR-FRET assay
32
Total Activities
32
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 N-(4-(2,4-Difluorophenoxy)-3-(6-methyl-7-oxo-6,7-dihydro-1H-pyrrolo[2,3-c]pyridin-4-yl)phenyl)ethanesulfonamide (ABBV-075/Mivebresib), a Potent and Orally Available Bromodomain and Extraterminal Domain (BET) Family Bromodomain Inhibitor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 32 | 7.76 | 8.82 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3898684 | — | — | 1 | 8.82 |
| CHEMBL3987016 | MIVEBRESIB | 2.0 | 1 | 8.82 |
| CHEMBL3970220 | — | — | 1 | 8.62 |
| CHEMBL3898479 | — | — | 1 | 8.54 |
| CHEMBL3901761 | — | — | 1 | 8.51 |
| CHEMBL4098055 | — | — | 1 | 8.47 |
| CHEMBL3980661 | — | — | 1 | 8.44 |
| CHEMBL3948433 | — | — | 1 | 8.43 |
| CHEMBL3889757 | — | — | 1 | 8.39 |
| CHEMBL3904317 | — | — | 1 | 8.36 |
| CHEMBL3974260 | — | — | 1 | 8.35 |
| CHEMBL3973984 | — | — | 1 | 8.24 |
| CHEMBL3942897 | — | — | 1 | 8.20 |
| CHEMBL4060619 | — | — | 1 | 8.19 |
| CHEMBL4059602 | — | — | 1 | 8.05 |
| CHEMBL3933860 | — | — | 1 | 8.03 |
| CHEMBL3928793 | — | — | 1 | 8.01 |
| CHEMBL3933555 | — | — | 1 | 7.92 |
| CHEMBL3914893 | — | — | 1 | 7.85 |
| CHEMBL3911104 | — | — | 1 | 7.72 |
| CHEMBL4061028 | — | — | 1 | 7.58 |
| CHEMBL3919590 | — | — | 1 | 7.50 |
| CHEMBL3967185 | — | — | 1 | 7.50 |
| CHEMBL3963357 | — | — | 1 | 7.42 |
| CHEMBL3980983 | — | — | 1 | 7.32 |
| CHEMBL3926000 | — | — | 1 | 7.17 |
| CHEMBL3964603 | — | — | 1 | 7.17 |
| CHEMBL1957266 | — | — | 1 | 7.11 |
| CHEMBL4089203 | — | — | 1 | 6.37 |
| CHEMBL4088769 | — | — | 1 | 6.05 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3898684 | — | Ki | = | 1.5 | nM | 8.82 |
| CHEMBL3987016 | MIVEBRESIB | Ki | = | 1.5 | nM | 8.82 |
| CHEMBL3970220 | — | Ki | = | 2.4 | nM | 8.62 |
| CHEMBL3898479 | — | Ki | = | 2.9 | nM | 8.54 |
| CHEMBL3901761 | — | Ki | = | 3.1 | nM | 8.51 |
| CHEMBL4098055 | — | Ki | = | 3.4 | nM | 8.47 |
| CHEMBL3980661 | — | Ki | = | 3.6 | nM | 8.44 |
| CHEMBL3948433 | — | Ki | = | 3.7 | nM | 8.43 |
| CHEMBL3889757 | — | Ki | = | 4.1 | nM | 8.39 |
| CHEMBL3904317 | — | Ki | = | 4.4 | nM | 8.36 |
| CHEMBL3974260 | — | Ki | = | 4.5 | nM | 8.35 |
| CHEMBL3973984 | — | Ki | = | 5.8 | nM | 8.24 |
| CHEMBL3942897 | — | Ki | = | 6.3 | nM | 8.20 |
| CHEMBL4060619 | — | Ki | = | 6.4 | nM | 8.19 |
| CHEMBL4059602 | — | Ki | = | 9.0 | nM | 8.05 |
| CHEMBL3933860 | — | Ki | = | 9.4 | nM | 8.03 |
| CHEMBL3928793 | — | Ki | = | 9.8 | nM | 8.01 |
| CHEMBL3933555 | — | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL3914893 | — | Ki | = | 14.0 | nM | 7.85 |
| CHEMBL3911104 | — | Ki | = | 19.0 | nM | 7.72 |
| CHEMBL4061028 | — | Ki | = | 26.0 | nM | 7.58 |
| CHEMBL3919590 | — | Ki | = | 32.0 | nM | 7.50 |
| CHEMBL3967185 | — | Ki | = | 32.0 | nM | 7.50 |
| CHEMBL3963357 | — | Ki | = | 38.0 | nM | 7.42 |
| CHEMBL3980983 | — | Ki | = | 48.0 | nM | 7.32 |
| CHEMBL3926000 | — | Ki | = | 68.0 | nM | 7.17 |
| CHEMBL3964603 | — | Ki | = | 68.0 | nM | 7.17 |
| CHEMBL1957266 | — | Ki | = | 77.0 | nM | 7.11 |
| CHEMBL4089203 | — | Ki | = | 430.0 | nM | 6.37 |
| CHEMBL4088769 | — | Ki | = | 890.0 | nM | 6.05 |
| CHEMBL4082851 | — | Ki | = | 1700.0 | nM | 5.77 |
| CHEMBL4100828 | — | Ki | = | 3000.0 | nM | 5.52 |