Assay Detail
Binding
CHEMBL2187905
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Binding affinity to human BRD2 assessed as inhibition of Alexa Fluor 488 binding after 60 mins by fluorescence anisotropic analysis
15
Total Activities
15
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
Identification of a novel series of BET family bromodomain inhibitors: binding mode and profile of I-BET151 (GSK1210151A).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 15 | 5.90 | 6.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2017288 | — | — | 1 | 6.40 |
| CHEMBL2017291 | — | — | 1 | 6.30 |
| CHEMBL2017285 | — | — | 1 | 6.30 |
| CHEMBL2017283 | — | — | 1 | 6.30 |
| CHEMBL2017273 | — | — | 1 | 6.30 |
| CHEMBL2017269 | — | — | 1 | 6.10 |
| CHEMBL2017281 | — | — | 1 | 6.00 |
| CHEMBL2181820 | — | — | 1 | 5.80 |
| CHEMBL2017286 | — | — | 1 | 5.80 |
| CHEMBL2181818 | — | — | 1 | 5.80 |
| CHEMBL2017289 | — | — | 1 | 5.70 |
| CHEMBL2017277 | — | — | 1 | 5.70 |
| CHEMBL2017282 | — | — | 1 | 5.60 |
| CHEMBL2181819 | — | — | 1 | 5.50 |
| CHEMBL2017264 | — | — | 1 | 4.90 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2017288 | — | IC50 | = | 398.11 | nM | 6.40 |
| CHEMBL2017291 | — | IC50 | = | 501.19 | nM | 6.30 |
| CHEMBL2017285 | — | IC50 | = | 501.19 | nM | 6.30 |
| CHEMBL2017283 | — | IC50 | = | 501.19 | nM | 6.30 |
| CHEMBL2017273 | — | IC50 | = | 501.19 | nM | 6.30 |
| CHEMBL2017269 | — | IC50 | = | 794.33 | nM | 6.10 |
| CHEMBL2017281 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL2181820 | — | IC50 | = | 1584.89 | nM | 5.80 |
| CHEMBL2017286 | — | IC50 | = | 1584.89 | nM | 5.80 |
| CHEMBL2181818 | — | IC50 | = | 1584.89 | nM | 5.80 |
| CHEMBL2017289 | — | IC50 | = | 1995.26 | nM | 5.70 |
| CHEMBL2017277 | — | IC50 | = | 1995.26 | nM | 5.70 |
| CHEMBL2017282 | — | IC50 | = | 2511.89 | nM | 5.60 |
| CHEMBL2181819 | — | IC50 | = | 3162.28 | nM | 5.50 |
| CHEMBL2017264 | — | IC50 | = | 12589.25 | nM | 4.90 |