Assay Detail
Binding
CHEMBL3610436
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Binding affinity to BRD4 (unknown origin) expressed in Escherichia coli BL21 after 1 hr by proprietary competition assay
18
Total Activities
18
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
BRD4 Structure-Activity Relationships of Dual PLK1 Kinase/BRD4 Bromodomain Inhibitor BI-2536.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 18 | 6.82 | 8.06 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3609308 | — | — | 1 | 8.06 |
| CHEMBL3609314 | — | — | 1 | 7.57 |
| CHEMBL3609312 | — | — | 1 | 7.54 |
| CHEMBL3609310 | — | — | 1 | 7.43 |
| CHEMBL3609311 | — | — | 1 | 7.34 |
| CHEMBL3609305 | — | — | 1 | 7.27 |
| CHEMBL513909 | BI-2536 | 2.0 | 1 | 7.25 |
| CHEMBL3609309 | — | — | 1 | 7.22 |
| CHEMBL3609313 | — | — | 1 | 7.00 |
| CHEMBL3609315 | — | — | 1 | 7.00 |
| CHEMBL3609300 | — | — | 1 | 6.33 |
| CHEMBL3609307 | — | — | 1 | 6.01 |
| CHEMBL3609304 | — | — | 1 | 5.85 |
| CHEMBL3609301 | — | — | 1 | 5.35 |
| CHEMBL3609299 | — | — | 1 | 5.10 |
| CHEMBL3609306 | — | — | 1 | - |
| CHEMBL3609303 | — | — | 1 | - |
| CHEMBL3609302 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3609308 | — | Ki | = | 8.7 | nM | 8.06 |
| CHEMBL3609314 | — | Ki | = | 27.0 | nM | 7.57 |
| CHEMBL3609312 | — | Ki | = | 29.0 | nM | 7.54 |
| CHEMBL3609310 | — | Ki | = | 37.0 | nM | 7.43 |
| CHEMBL3609311 | — | Ki | = | 46.0 | nM | 7.34 |
| CHEMBL3609305 | — | Ki | = | 54.0 | nM | 7.27 |
| CHEMBL513909 | BI-2536 | Ki | = | 56.0 | nM | 7.25 |
| CHEMBL3609309 | — | Ki | = | 60.0 | nM | 7.22 |
| CHEMBL3609313 | — | Ki | = | 100.0 | nM | 7.00 |
| CHEMBL3609315 | — | Ki | = | 99.0 | nM | 7.00 |
| CHEMBL3609300 | — | Ki | = | 470.0 | nM | 6.33 |
| CHEMBL3609307 | — | Ki | = | 970.0 | nM | 6.01 |
| CHEMBL3609304 | — | Ki | = | 1400.0 | nM | 5.85 |
| CHEMBL3609301 | — | Ki | = | 4500.0 | nM | 5.35 |
| CHEMBL3609299 | — | Ki | = | 7950.0 | nM | 5.10 |
| CHEMBL3609306 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL3609303 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL3609302 | — | Ki | > | 10000.0 | nM | - |