Assay Detail
Binding
CHEMBL4843806
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of Alexa Fluor 647 labelled ligand from recombinant human N-terminal 6His-tagged BRD4-BD1 Y390A mutant (1 to 477 residue) expressed in Escherichia coli incubated for 30 mins by TR-FRET assay
33
Total Activities
33
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 a Novel Bromodomain and Extra Terminal Domain (BET) Protein Inhibitor, I-BET282E, Suitable for Clinical Progression.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 33 | 6.88 | 7.90 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4874801 | — | — | 1 | 7.90 |
| CHEMBL4874457 | — | — | 1 | 7.60 |
| CHEMBL2017291 | — | — | 1 | 7.60 |
| CHEMBL4862999 | — | — | 1 | 7.50 |
| CHEMBL4874356 | — | — | 1 | 7.50 |
| CHEMBL4853472 | — | — | 1 | 7.50 |
| CHEMBL4874790 | — | — | 1 | 7.50 |
| CHEMBL4861790 | — | — | 1 | 7.40 |
| CHEMBL4847186 | — | — | 1 | 7.40 |
| CHEMBL4878439 | — | — | 1 | 7.40 |
| CHEMBL4846393 | — | — | 1 | 7.40 |
| CHEMBL4862592 | — | — | 1 | 7.40 |
| CHEMBL4855128 | — | — | 1 | 7.20 |
| CHEMBL4861057 | — | — | 1 | 7.20 |
| CHEMBL4875479 | — | — | 1 | 7.10 |
| CHEMBL4855373 | — | — | 1 | 7.00 |
| CHEMBL4859880 | — | — | 1 | 7.00 |
| CHEMBL4849704 | — | — | 1 | 6.90 |
| CHEMBL4864056 | — | — | 1 | 6.90 |
| CHEMBL2017286 | — | — | 1 | 6.80 |
| CHEMBL4875886 | — | — | 1 | 6.80 |
| CHEMBL4869970 | — | — | 1 | 6.80 |
| CHEMBL4862100 | — | — | 1 | 6.70 |
| CHEMBL4877490 | — | — | 1 | 6.60 |
| CHEMBL4846391 | — | — | 1 | 6.20 |
| CHEMBL4873648 | — | — | 1 | 6.20 |
| CHEMBL4861667 | — | — | 1 | 6.20 |
| CHEMBL4861475 | — | — | 1 | 6.10 |
| CHEMBL4859354 | — | — | 1 | 6.10 |
| CHEMBL4859578 | — | — | 1 | 5.90 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4874801 | — | IC50 | = | 12.59 | nM | 7.90 |
| CHEMBL4874457 | — | IC50 | = | 25.12 | nM | 7.60 |
| CHEMBL2017291 | — | IC50 | = | 25.12 | nM | 7.60 |
| CHEMBL4862999 | — | IC50 | = | 31.62 | nM | 7.50 |
| CHEMBL4874356 | — | IC50 | = | 31.62 | nM | 7.50 |
| CHEMBL4853472 | — | IC50 | = | 31.62 | nM | 7.50 |
| CHEMBL4874790 | — | IC50 | = | 31.62 | nM | 7.50 |
| CHEMBL4861790 | — | IC50 | = | 39.81 | nM | 7.40 |
| CHEMBL4847186 | — | IC50 | = | 39.81 | nM | 7.40 |
| CHEMBL4878439 | — | IC50 | = | 39.81 | nM | 7.40 |
| CHEMBL4846393 | — | IC50 | = | 39.81 | nM | 7.40 |
| CHEMBL4862592 | — | IC50 | = | 39.81 | nM | 7.40 |
| CHEMBL4855128 | — | IC50 | = | 63.1 | nM | 7.20 |
| CHEMBL4861057 | — | IC50 | = | 63.1 | nM | 7.20 |
| CHEMBL4875479 | — | IC50 | = | 79.43 | nM | 7.10 |
| CHEMBL4859880 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL4855373 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL4849704 | — | IC50 | = | 125.89 | nM | 6.90 |
| CHEMBL4864056 | — | IC50 | = | 125.89 | nM | 6.90 |
| CHEMBL2017286 | — | IC50 | = | 158.49 | nM | 6.80 |
| CHEMBL4875886 | — | IC50 | = | 158.49 | nM | 6.80 |
| CHEMBL4869970 | — | IC50 | = | 158.49 | nM | 6.80 |
| CHEMBL4862100 | — | IC50 | = | 199.53 | nM | 6.70 |
| CHEMBL4877490 | — | IC50 | = | 251.19 | nM | 6.60 |
| CHEMBL4846391 | — | IC50 | = | 630.96 | nM | 6.20 |
| CHEMBL4861667 | — | IC50 | = | 630.96 | nM | 6.20 |
| CHEMBL4873648 | — | IC50 | = | 630.96 | nM | 6.20 |
| CHEMBL4861475 | — | IC50 | = | 794.33 | nM | 6.10 |
| CHEMBL4859354 | — | IC50 | = | 794.33 | nM | 6.10 |
| CHEMBL4859578 | — | IC50 | = | 1258.93 | nM | 5.90 |
| CHEMBL4869121 | — | IC50 | = | 1258.93 | nM | 5.90 |
| CHEMBL4871914 | — | IC50 | = | 1584.89 | nM | 5.80 |
| CHEMBL4864900 | — | IC50 | = | 1995.26 | nM | 5.70 |