Assay Detail
Binding
CHEMBL2433086
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Inhibition of His-FLAG-tagged BRD4 binding domain1 (unknown origin) binding to H4-TetraAc-biotin peptide after 20 mins by AlphaLISA
25
Total Activities
25
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, Design, and Optimization of Isoxazole Azepine BET Inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 25 | 6.67 | 7.75 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2017291 | — | — | 1 | 7.75 |
| CHEMBL1957266 | — | — | 1 | 7.62 |
| CHEMBL2431090 | — | — | 1 | 7.58 |
| CHEMBL2431078 | — | — | 1 | 7.54 |
| CHEMBL2431079 | — | — | 1 | 7.48 |
| CHEMBL2431091 | — | — | 1 | 7.44 |
| CHEMBL2431080 | — | — | 1 | 7.38 |
| CHEMBL2431082 | — | — | 1 | 7.14 |
| CHEMBL2431081 | — | — | 1 | 7.14 |
| CHEMBL2431076 | — | — | 1 | 7.13 |
| CHEMBL2431093 | — | — | 1 | 7.07 |
| CHEMBL1232461 | MOLIBRESIB | 2.0 | 1 | 6.92 |
| CHEMBL2431094 | — | — | 1 | 6.72 |
| CHEMBL2431074 | — | — | 1 | 6.72 |
| CHEMBL2431073 | — | — | 1 | 6.70 |
| CHEMBL2431077 | — | — | 1 | 6.60 |
| CHEMBL2431075 | — | — | 1 | 6.60 |
| CHEMBL2431089 | — | — | 1 | 6.54 |
| CHEMBL2431085 | — | — | 1 | 6.52 |
| CHEMBL2431086 | — | — | 1 | 5.96 |
| CHEMBL2431092 | — | — | 1 | 5.68 |
| CHEMBL2431083 | — | — | 1 | 5.60 |
| CHEMBL2431084 | — | — | 1 | 5.24 |
| CHEMBL2431087 | — | — | 1 | 5.21 |
| CHEMBL2431088 | — | — | 1 | 4.48 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2017291 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL1957266 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL2431090 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL2431078 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL2431079 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL2431091 | — | IC50 | = | 36.0 | nM | 7.44 |
| CHEMBL2431080 | — | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL2431082 | — | IC50 | = | 73.0 | nM | 7.14 |
| CHEMBL2431081 | — | IC50 | = | 72.0 | nM | 7.14 |
| CHEMBL2431076 | — | IC50 | = | 74.0 | nM | 7.13 |
| CHEMBL2431093 | — | IC50 | = | 86.0 | nM | 7.07 |
| CHEMBL1232461 | MOLIBRESIB | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL2431094 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL2431074 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL2431073 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL2431077 | — | IC50 | = | 250.0 | nM | 6.60 |
| CHEMBL2431075 | — | IC50 | = | 250.0 | nM | 6.60 |
| CHEMBL2431089 | — | IC50 | = | 290.0 | nM | 6.54 |
| CHEMBL2431085 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL2431086 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL2431092 | — | IC50 | = | 2100.0 | nM | 5.68 |
| CHEMBL2431083 | — | IC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL2431084 | — | IC50 | = | 5700.0 | nM | 5.24 |
| CHEMBL2431087 | — | IC50 | = | 6200.0 | nM | 5.21 |
| CHEMBL2431088 | — | IC50 | = | 33000.0 | nM | 4.48 |