Assay Detail
Binding
CHEMBL3591211
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of I-BET762 from 6His-Thr-BRD4 (1 to 477) BD1 (unknown origin) harboring BD2 Y390A mutant after 30 mins by TR-FRET analysis
34
Total Activities
30
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
Structure-Based Optimization of Naphthyridones into Potent ATAD2 Bromodomain Inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 34 | 5.04 | 6.20 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3590391 | — | — | 1 | 6.20 |
| CHEMBL3590389 | — | — | 1 | 5.80 |
| CHEMBL3590405 | — | — | 2 | 5.40 |
| CHEMBL3590388 | — | — | 2 | 5.40 |
| CHEMBL3590397 | — | — | 1 | 5.30 |
| CHEMBL3590404 | — | — | 1 | 5.30 |
| CHEMBL3590399 | — | — | 1 | 5.20 |
| CHEMBL3590380 | — | — | 1 | 5.20 |
| CHEMBL3590396 | — | — | 2 | 5.20 |
| CHEMBL3590402 | — | — | 1 | 5.20 |
| CHEMBL3590401 | — | — | 1 | 5.20 |
| CHEMBL3590385 | — | — | 1 | 5.10 |
| CHEMBL3590384 | — | — | 1 | 5.10 |
| CHEMBL3590382 | — | — | 1 | 5.00 |
| CHEMBL3590407 | — | — | 1 | 5.00 |
| CHEMBL3590381 | — | — | 1 | 5.00 |
| CHEMBL3590403 | — | — | 1 | 5.00 |
| CHEMBL3590394 | — | — | 2 | 5.00 |
| CHEMBL3590392 | — | — | 1 | 5.00 |
| CHEMBL3590387 | — | — | 1 | 4.90 |
| CHEMBL3590398 | — | — | 1 | 4.90 |
| CHEMBL3590395 | — | — | 1 | 4.90 |
| CHEMBL3590393 | — | — | 1 | 4.90 |
| CHEMBL3590390 | — | — | 1 | 4.90 |
| CHEMBL3590383 | — | — | 1 | 4.80 |
| CHEMBL3590406 | — | — | 1 | 4.60 |
| CHEMBL3590400 | — | — | 1 | 4.60 |
| CHEMBL3590379 | — | — | 1 | 4.60 |
| CHEMBL3590386 | — | — | 1 | 4.30 |
| CHEMBL3590408 | — | — | 1 | 4.10 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3590391 | — | IC50 | = | 630.96 | nM | 6.20 |
| CHEMBL3590389 | — | IC50 | = | 1584.89 | nM | 5.80 |
| CHEMBL3590405 | — | IC50 | = | 3981.07 | nM | 5.40 |
| CHEMBL3590405 | — | IC50 | = | 3981.07 | nM | 5.40 |
| CHEMBL3590388 | — | IC50 | = | 3981.07 | nM | 5.40 |
| CHEMBL3590388 | — | IC50 | = | 5011.87 | nM | 5.30 |
| CHEMBL3590397 | — | IC50 | = | 5011.87 | nM | 5.30 |
| CHEMBL3590404 | — | IC50 | = | 5011.87 | nM | 5.30 |
| CHEMBL3590399 | — | IC50 | = | 6309.57 | nM | 5.20 |
| CHEMBL3590380 | — | IC50 | = | 6309.57 | nM | 5.20 |
| CHEMBL3590396 | — | IC50 | = | 6309.57 | nM | 5.20 |
| CHEMBL3590401 | — | IC50 | = | 6309.57 | nM | 5.20 |
| CHEMBL3590402 | — | IC50 | = | 6309.57 | nM | 5.20 |
| CHEMBL3590385 | — | IC50 | = | 7943.28 | nM | 5.10 |
| CHEMBL3590384 | — | IC50 | = | 7943.28 | nM | 5.10 |
| CHEMBL3590394 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL3590403 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL3590381 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL3590407 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL3590382 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL3590392 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL3590396 | — | IC50 | = | 12589.25 | nM | 4.90 |
| CHEMBL3590398 | — | IC50 | = | 12589.25 | nM | 4.90 |
| CHEMBL3590387 | — | IC50 | = | 12589.25 | nM | 4.90 |
| CHEMBL3590395 | — | IC50 | = | 12589.25 | nM | 4.90 |
| CHEMBL3590393 | — | IC50 | = | 12589.25 | nM | 4.90 |
| CHEMBL3590390 | — | IC50 | = | 12589.25 | nM | 4.90 |
| CHEMBL3590394 | — | IC50 | = | 15848.93 | nM | 4.80 |
| CHEMBL3590383 | — | IC50 | = | 15848.93 | nM | 4.80 |
| CHEMBL3590406 | — | IC50 | = | 25118.86 | nM | 4.60 |
| CHEMBL3590400 | — | IC50 | = | 25118.86 | nM | 4.60 |
| CHEMBL3590379 | — | IC50 | = | 25118.86 | nM | 4.60 |
| CHEMBL3590386 | — | IC50 | = | 50118.72 | nM | 4.30 |
| CHEMBL3590408 | — | IC50 | = | 79432.82 | nM | 4.10 |