Assay Detail
Binding
CHEMBL5361509
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of PLK1 (unknown origin) preincubated for 10 mins followed by substrate addition measured after 60 mins in presence of ATP by ADP-Glo assay
35
Total Activities
35
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 |
Target
Serine/threonine-protein kinase PLK1 (CHEMBL3024) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Design, synthesis, and biological evaluation of novel dihydropteridone derivatives possessing oxadiazoles moiety as potent inhibitors of PLK1.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 35 | 9.33 | 9.74 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5423881 | — | — | 1 | 9.74 |
| CHEMBL5419732 | — | — | 1 | 9.72 |
| CHEMBL5433401 | — | — | 1 | 9.64 |
| CHEMBL5438707 | — | — | 1 | 9.64 |
| CHEMBL5415945 | — | — | 1 | 9.59 |
| CHEMBL5421113 | — | — | 1 | 9.52 |
| CHEMBL5435085 | — | — | 1 | 9.49 |
| CHEMBL5429110 | — | — | 1 | 9.48 |
| CHEMBL5438696 | — | — | 1 | 9.47 |
| CHEMBL5398211 | — | — | 1 | 9.43 |
| CHEMBL5396078 | — | — | 1 | 9.41 |
| CHEMBL5437785 | — | — | 1 | 9.40 |
| CHEMBL5426743 | — | — | 1 | 9.38 |
| CHEMBL5402308 | — | — | 1 | 9.38 |
| CHEMBL5394854 | — | — | 1 | 9.36 |
| CHEMBL5430344 | — | — | 1 | 9.35 |
| CHEMBL5435649 | — | — | 1 | 9.30 |
| CHEMBL5433215 | — | — | 1 | 9.30 |
| CHEMBL513909 | BI-2536 | 2.0 | 1 | 9.29 |
| CHEMBL5430202 | — | — | 1 | 9.28 |
| CHEMBL5426933 | — | — | 1 | 9.28 |
| CHEMBL5416239 | — | — | 1 | 9.28 |
| CHEMBL5401755 | — | — | 1 | 9.26 |
| CHEMBL5440471 | — | — | 1 | 9.26 |
| CHEMBL5434561 | — | — | 1 | 9.22 |
| CHEMBL5399905 | — | — | 1 | 9.21 |
| CHEMBL5395023 | — | — | 1 | 9.21 |
| CHEMBL5400707 | — | — | 1 | 9.20 |
| CHEMBL5439937 | — | — | 1 | 9.19 |
| CHEMBL5403446 | — | — | 1 | 9.16 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5423881 | — | IC50 | = | 0.18 | nM | 9.74 |
| CHEMBL5419732 | — | IC50 | = | 0.19 | nM | 9.72 |
| CHEMBL5433401 | — | IC50 | = | 0.23 | nM | 9.64 |
| CHEMBL5438707 | — | IC50 | = | 0.23 | nM | 9.64 |
| CHEMBL5415945 | — | IC50 | = | 0.26 | nM | 9.59 |
| CHEMBL5421113 | — | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL5435085 | — | IC50 | = | 0.32 | nM | 9.49 |
| CHEMBL5429110 | — | IC50 | = | 0.33 | nM | 9.48 |
| CHEMBL5438696 | — | IC50 | = | 0.34 | nM | 9.47 |
| CHEMBL5398211 | — | IC50 | = | 0.37 | nM | 9.43 |
| CHEMBL5396078 | — | IC50 | = | 0.39 | nM | 9.41 |
| CHEMBL5437785 | — | IC50 | = | 0.4 | nM | 9.40 |
| CHEMBL5426743 | — | IC50 | = | 0.42 | nM | 9.38 |
| CHEMBL5402308 | — | IC50 | = | 0.42 | nM | 9.38 |
| CHEMBL5394854 | — | IC50 | = | 0.44 | nM | 9.36 |
| CHEMBL5430344 | — | IC50 | = | 0.45 | nM | 9.35 |
| CHEMBL5433215 | — | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL5435649 | — | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL513909 | BI-2536 | IC50 | = | 0.51 | nM | 9.29 |
| CHEMBL5430202 | — | IC50 | = | 0.53 | nM | 9.28 |
| CHEMBL5426933 | — | IC50 | = | 0.53 | nM | 9.28 |
| CHEMBL5416239 | — | IC50 | = | 0.53 | nM | 9.28 |
| CHEMBL5401755 | — | IC50 | = | 0.55 | nM | 9.26 |
| CHEMBL5440471 | — | IC50 | = | 0.55 | nM | 9.26 |
| CHEMBL5434561 | — | IC50 | = | 0.6 | nM | 9.22 |
| CHEMBL5395023 | — | IC50 | = | 0.62 | nM | 9.21 |
| CHEMBL5399905 | — | IC50 | = | 0.62 | nM | 9.21 |
| CHEMBL5400707 | — | IC50 | = | 0.63 | nM | 9.20 |
| CHEMBL5439937 | — | IC50 | = | 0.64 | nM | 9.19 |
| CHEMBL5403446 | — | IC50 | = | 0.69 | nM | 9.16 |
| CHEMBL5426079 | — | IC50 | = | 0.76 | nM | 9.12 |
| CHEMBL5412655 | — | IC50 | = | 0.79 | nM | 9.10 |
| CHEMBL5405803 | — | IC50 | = | 0.91 | nM | 9.04 |
| CHEMBL5423798 | — | IC50 | = | 1.02 | nM | 8.99 |
| CHEMBL5404388 | — | IC50 | = | 1.07 | nM | 8.97 |