Assay Detail
Binding
CHEMBL4331530
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of BRD4 BD1 (unknown origin) using biotin labelled NeC: SGRG-K(Ac)-GG-K(Ac)-GLG-K(Ac)-GGA-K(Ac)-RHRKVGG-K as substrate preincubated for 15 mins followed by substrate addition measured after 30 mins by alpha screen assay
65
Total Activities
65
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
Rational design of 5-((1H-imidazol-1-yl)methyl)quinolin-8-ol derivatives as novel bromodomain-containing protein 4 inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 65 | 6.42 | 7.34 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4514822 | — | — | 1 | 7.34 |
| CHEMBL4443068 | — | — | 1 | 7.27 |
| CHEMBL4553865 | — | — | 1 | 7.21 |
| CHEMBL4590925 | — | — | 1 | 7.17 |
| CHEMBL4467977 | — | — | 1 | 7.17 |
| CHEMBL4470331 | — | — | 1 | 7.16 |
| CHEMBL4469389 | — | — | 1 | 7.16 |
| CHEMBL4448093 | — | — | 1 | 7.14 |
| CHEMBL4563906 | — | — | 1 | 7.12 |
| CHEMBL4514104 | — | — | 1 | 7.09 |
| CHEMBL4440666 | — | — | 1 | 7.04 |
| CHEMBL4543026 | — | — | 1 | 7.02 |
| CHEMBL1361699 | — | — | 1 | 7.00 |
| CHEMBL4518465 | — | — | 1 | 6.97 |
| CHEMBL4567741 | — | — | 1 | 6.81 |
| CHEMBL4582810 | — | — | 1 | 6.75 |
| CHEMBL4548295 | — | — | 1 | 6.54 |
| CHEMBL2094437 | — | — | 1 | 6.47 |
| CHEMBL4442513 | — | — | 1 | 6.43 |
| CHEMBL4454149 | — | — | 1 | 6.17 |
| CHEMBL2325745 | — | — | 1 | 6.13 |
| CHEMBL1454910 | NITROXOLINE | 4.0 | 1 | 6.01 |
| CHEMBL2094361 | — | — | 1 | 6.00 |
| CHEMBL4070621 | — | — | 1 | 5.68 |
| CHEMBL1452711 | — | — | 1 | 5.68 |
| CHEMBL4456255 | — | — | 1 | 5.52 |
| CHEMBL2094636 | — | — | 1 | 5.37 |
| CHEMBL4535610 | — | — | 1 | 5.33 |
| CHEMBL1481742 | — | — | 1 | 5.32 |
| CHEMBL2325491 | — | — | 1 | 5.32 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4514822 | — | IC50 | = | 46.0 | nM | 7.34 |
| CHEMBL4443068 | — | IC50 | = | 54.0 | nM | 7.27 |
| CHEMBL4553865 | — | IC50 | = | 61.0 | nM | 7.21 |
| CHEMBL4590925 | — | IC50 | = | 68.0 | nM | 7.17 |
| CHEMBL4467977 | — | IC50 | = | 67.0 | nM | 7.17 |
| CHEMBL4470331 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL4469389 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL4448093 | — | IC50 | = | 73.0 | nM | 7.14 |
| CHEMBL4563906 | — | IC50 | = | 76.0 | nM | 7.12 |
| CHEMBL4514104 | — | IC50 | = | 82.0 | nM | 7.09 |
| CHEMBL4440666 | — | IC50 | = | 92.0 | nM | 7.04 |
| CHEMBL4543026 | — | IC50 | = | 95.0 | nM | 7.02 |
| CHEMBL1361699 | — | IC50 | = | 101.0 | nM | 7.00 |
| CHEMBL4518465 | — | IC50 | = | 107.0 | nM | 6.97 |
| CHEMBL4567741 | — | IC50 | = | 155.0 | nM | 6.81 |
| CHEMBL4582810 | — | IC50 | = | 176.0 | nM | 6.75 |
| CHEMBL4548295 | — | IC50 | = | 292.0 | nM | 6.54 |
| CHEMBL2094437 | — | IC50 | = | 337.0 | nM | 6.47 |
| CHEMBL4442513 | — | IC50 | = | 370.0 | nM | 6.43 |
| CHEMBL4454149 | — | IC50 | = | 670.0 | nM | 6.17 |
| CHEMBL2325745 | — | IC50 | = | 738.0 | nM | 6.13 |
| CHEMBL1454910 | NITROXOLINE | IC50 | = | 980.0 | nM | 6.01 |
| CHEMBL2094361 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL4070621 | — | IC50 | = | 2103.0 | nM | 5.68 |
| CHEMBL1452711 | — | IC50 | = | 2100.0 | nM | 5.68 |
| CHEMBL4456255 | — | IC50 | = | 3000.0 | nM | 5.52 |
| CHEMBL2094636 | — | IC50 | = | 4300.0 | nM | 5.37 |
| CHEMBL4535610 | — | IC50 | = | 4700.0 | nM | 5.33 |
| CHEMBL1481742 | — | IC50 | = | 4800.0 | nM | 5.32 |
| CHEMBL2325491 | — | IC50 | = | 4800.0 | nM | 5.32 |
| CHEMBL3197024 | — | IC50 | = | 5200.0 | nM | 5.28 |
| CHEMBL1497792 | — | IC50 | = | 18000.0 | nM | 4.75 |
| CHEMBL4554140 | — | IC50 | - | — | - | |
| CHEMBL1864229 | — | IC50 | - | — | - | |
| CHEMBL4517822 | — | IC50 | - | — | - | |
| CHEMBL4582148 | — | IC50 | - | — | - | |
| CHEMBL4483004 | — | IC50 | - | — | - | |
| CHEMBL2094568 | — | IC50 | - | — | - | |
| CHEMBL4453099 | — | IC50 | - | — | - | |
| CHEMBL3192241 | — | IC50 | - | — | - | |
| CHEMBL4521981 | — | IC50 | - | — | - | |
| CHEMBL4468600 | — | IC50 | - | — | - | |
| CHEMBL2094734 | — | IC50 | - | — | - | |
| CHEMBL4527583 | — | IC50 | - | — | - | |
| CHEMBL4457455 | — | IC50 | - | — | - | |
| CHEMBL578741 | — | IC50 | - | — | - | |
| CHEMBL4462834 | — | IC50 | - | — | - | |
| CHEMBL1889634 | — | IC50 | - | — | - | |
| CHEMBL1900969 | — | IC50 | - | — | - | |
| CHEMBL1897930 | — | IC50 | - | — | - |