Assay Detail
Binding
CHEMBL4020283
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of BRD4 in human H1299 cells assessed as decrease in HPV LCR-E2-EP400-mediated transcriptional repression after 24 hrs by Bright-Glo luciferase reporter gene 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 |
|---|---|---|---|
| EC50 | 32 | 7.09 | 8.09 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3898684 | — | — | 1 | 8.09 |
| CHEMBL3970220 | — | — | 1 | 7.96 |
| CHEMBL4098055 | — | — | 1 | 7.77 |
| CHEMBL3948433 | — | — | 1 | 7.75 |
| CHEMBL3933555 | — | — | 1 | 7.72 |
| CHEMBL3987016 | MIVEBRESIB | 2.0 | 1 | 7.70 |
| CHEMBL3911104 | — | — | 1 | 7.70 |
| CHEMBL3974260 | — | — | 1 | 7.68 |
| CHEMBL3904317 | — | — | 1 | 7.66 |
| CHEMBL3928793 | — | — | 1 | 7.58 |
| CHEMBL3901761 | — | — | 1 | 7.46 |
| CHEMBL3980661 | — | — | 1 | 7.41 |
| CHEMBL3898479 | — | — | 1 | 7.37 |
| CHEMBL3933860 | — | — | 1 | 7.32 |
| CHEMBL3973984 | — | — | 1 | 7.30 |
| CHEMBL4059602 | — | — | 1 | 7.19 |
| CHEMBL3942897 | — | — | 1 | 7.17 |
| CHEMBL3919590 | — | — | 1 | 7.16 |
| CHEMBL3914893 | — | — | 1 | 7.15 |
| CHEMBL4060619 | — | — | 1 | 7.12 |
| CHEMBL3963357 | — | — | 1 | 7.10 |
| CHEMBL3889757 | — | — | 1 | 7.06 |
| CHEMBL3926000 | — | — | 1 | 7.05 |
| CHEMBL3964603 | — | — | 1 | 6.92 |
| CHEMBL1957266 | — | — | 1 | 6.82 |
| CHEMBL3967185 | — | — | 1 | 6.77 |
| CHEMBL4061028 | — | — | 1 | 6.57 |
| CHEMBL3980983 | — | — | 1 | 6.32 |
| CHEMBL4089203 | — | — | 1 | 6.06 |
| CHEMBL4082851 | — | — | 1 | 5.64 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3898684 | — | EC50 | = | 8.1 | nM | 8.09 |
| CHEMBL3970220 | — | EC50 | = | 11.0 | nM | 7.96 |
| CHEMBL4098055 | — | EC50 | = | 17.0 | nM | 7.77 |
| CHEMBL3948433 | — | EC50 | = | 18.0 | nM | 7.75 |
| CHEMBL3933555 | — | EC50 | = | 19.0 | nM | 7.72 |
| CHEMBL3987016 | MIVEBRESIB | EC50 | = | 20.0 | nM | 7.70 |
| CHEMBL3911104 | — | EC50 | = | 20.0 | nM | 7.70 |
| CHEMBL3974260 | — | EC50 | = | 21.0 | nM | 7.68 |
| CHEMBL3904317 | — | EC50 | = | 22.0 | nM | 7.66 |
| CHEMBL3928793 | — | EC50 | = | 26.0 | nM | 7.58 |
| CHEMBL3901761 | — | EC50 | = | 35.0 | nM | 7.46 |
| CHEMBL3980661 | — | EC50 | = | 39.0 | nM | 7.41 |
| CHEMBL3898479 | — | EC50 | = | 43.0 | nM | 7.37 |
| CHEMBL3933860 | — | EC50 | = | 48.0 | nM | 7.32 |
| CHEMBL3973984 | — | EC50 | = | 50.0 | nM | 7.30 |
| CHEMBL4059602 | — | EC50 | = | 65.0 | nM | 7.19 |
| CHEMBL3942897 | — | EC50 | = | 67.0 | nM | 7.17 |
| CHEMBL3919590 | — | EC50 | = | 70.0 | nM | 7.16 |
| CHEMBL3914893 | — | EC50 | = | 71.0 | nM | 7.15 |
| CHEMBL4060619 | — | EC50 | = | 76.0 | nM | 7.12 |
| CHEMBL3963357 | — | EC50 | = | 79.0 | nM | 7.10 |
| CHEMBL3889757 | — | EC50 | = | 88.0 | nM | 7.06 |
| CHEMBL3926000 | — | EC50 | = | 90.0 | nM | 7.05 |
| CHEMBL3964603 | — | EC50 | = | 120.0 | nM | 6.92 |
| CHEMBL1957266 | — | EC50 | = | 153.0 | nM | 6.82 |
| CHEMBL3967185 | — | EC50 | = | 170.0 | nM | 6.77 |
| CHEMBL4061028 | — | EC50 | = | 270.0 | nM | 6.57 |
| CHEMBL3980983 | — | EC50 | = | 480.0 | nM | 6.32 |
| CHEMBL4089203 | — | EC50 | = | 880.0 | nM | 6.06 |
| CHEMBL4082851 | — | EC50 | = | 2300.0 | nM | 5.64 |
| CHEMBL4088769 | — | EC50 | = | 4100.0 | nM | 5.39 |
| CHEMBL4100828 | — | EC50 | = | 8500.0 | nM | 5.07 |