Assay Detail
Binding
CHEMBL4821758
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Inhibition of BRD4-BD1 (unknown origin) preincubated for 15 mins followed by substrate addition and measured after 1 hr
20
Total Activities
20
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 3,5-dimethylisoxazole derivatives as novel, potent inhibitors for bromodomain and extraterminal domain (BET) family.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 20 | 7.71 | 8.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4850099 | — | — | 1 | 8.52 |
| CHEMBL4873148 | — | — | 1 | 8.51 |
| CHEMBL4867171 | — | — | 1 | 8.25 |
| CHEMBL4865930 | — | — | 1 | 8.06 |
| CHEMBL4863343 | — | — | 1 | 8.04 |
| CHEMBL4875215 | — | — | 1 | 7.92 |
| CHEMBL4867208 | — | — | 1 | 7.89 |
| CHEMBL4860249 | — | — | 1 | 7.43 |
| CHEMBL1957266 | — | — | 1 | 7.38 |
| CHEMBL4637198 | — | — | 1 | 7.28 |
| CHEMBL4859501 | — | — | 1 | 7.26 |
| CHEMBL4875647 | — | — | 1 | 7.24 |
| CHEMBL4878278 | — | — | 1 | 7.13 |
| CHEMBL4857203 | — | — | 1 | 6.98 |
| CHEMBL4851529 | — | — | 1 | - |
| CHEMBL4877162 | — | — | 1 | - |
| CHEMBL4865463 | — | — | 1 | - |
| CHEMBL4858249 | — | — | 1 | - |
| CHEMBL4848587 | — | — | 1 | - |
| CHEMBL4859291 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4850099 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL4873148 | — | IC50 | = | 3.1 | nM | 8.51 |
| CHEMBL4867171 | — | IC50 | = | 5.6 | nM | 8.25 |
| CHEMBL4865930 | — | IC50 | = | 8.8 | nM | 8.06 |
| CHEMBL4863343 | — | IC50 | = | 9.2 | nM | 8.04 |
| CHEMBL4875215 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL4867208 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL4860249 | — | IC50 | = | 37.0 | nM | 7.43 |
| CHEMBL1957266 | — | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL4637198 | — | IC50 | = | 53.0 | nM | 7.28 |
| CHEMBL4859501 | — | IC50 | = | 55.0 | nM | 7.26 |
| CHEMBL4875647 | — | IC50 | = | 58.0 | nM | 7.24 |
| CHEMBL4878278 | — | IC50 | = | 74.0 | nM | 7.13 |
| CHEMBL4857203 | — | IC50 | = | 105.0 | nM | 6.98 |
| CHEMBL4851529 | — | IC50 | - | — | - | |
| CHEMBL4877162 | — | IC50 | - | — | - | |
| CHEMBL4865463 | — | IC50 | - | — | - | |
| CHEMBL4858249 | — | IC50 | - | — | - | |
| CHEMBL4848587 | — | IC50 | - | — | - | |
| CHEMBL4859291 | — | IC50 | - | — | - |