Assay Detail
Binding
CHEMBL3610437
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding affinity to PLK1 (unknown origin) expressed in HEK293 cells 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 |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Serine/threonine-protein kinase PLK1 (CHEMBL3024) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
BRD4 Structure-Activity Relationships of Dual PLK1 Kinase/BRD4 Bromodomain Inhibitor BI-2536.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 18 | 8.65 | 9.66 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL513909 | BI-2536 | 2.0 | 1 | 9.66 |
| CHEMBL3609305 | — | — | 1 | 9.38 |
| CHEMBL3609310 | — | — | 1 | 9.28 |
| CHEMBL3609314 | — | — | 1 | 9.08 |
| CHEMBL3609300 | — | — | 1 | 9.04 |
| CHEMBL3609306 | — | — | 1 | 8.38 |
| CHEMBL3609308 | — | — | 1 | 8.24 |
| CHEMBL3609307 | — | — | 1 | 8.16 |
| CHEMBL3609315 | — | — | 1 | 6.62 |
| CHEMBL3609299 | — | — | 1 | - |
| CHEMBL3609301 | — | — | 1 | - |
| CHEMBL3609313 | — | — | 1 | - |
| CHEMBL3609312 | — | — | 1 | - |
| CHEMBL3609311 | — | — | 1 | - |
| CHEMBL3609302 | — | — | 1 | - |
| CHEMBL3609309 | — | — | 1 | - |
| CHEMBL3609303 | — | — | 1 | - |
| CHEMBL3609304 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL513909 | BI-2536 | Ki | = | 0.22 | nM | 9.66 |
| CHEMBL3609305 | — | Ki | = | 0.42 | nM | 9.38 |
| CHEMBL3609310 | — | Ki | = | 0.52 | nM | 9.28 |
| CHEMBL3609314 | — | Ki | = | 0.84 | nM | 9.08 |
| CHEMBL3609300 | — | Ki | = | 0.91 | nM | 9.04 |
| CHEMBL3609306 | — | Ki | = | 4.2 | nM | 8.38 |
| CHEMBL3609308 | — | Ki | = | 5.8 | nM | 8.24 |
| CHEMBL3609307 | — | Ki | = | 6.95 | nM | 8.16 |
| CHEMBL3609315 | — | Ki | = | 240.0 | nM | 6.62 |
| CHEMBL3609299 | — | Ki | - | — | - | |
| CHEMBL3609301 | — | Ki | - | — | - | |
| CHEMBL3609313 | — | Ki | - | — | - | |
| CHEMBL3609312 | — | Ki | - | — | - | |
| CHEMBL3609311 | — | Ki | - | — | - | |
| CHEMBL3609302 | — | Ki | - | — | - | |
| CHEMBL3609309 | — | Ki | - | — | - | |
| CHEMBL3609303 | — | Ki | - | — | - | |
| CHEMBL3609304 | — | Ki | - | — | - |