Assay Detail
Binding
CHEMBL5337543
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 and ATP addition and measured after 60 mins by ADP-Glo kinase assay
51
Total Activities
51
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
Discovery and optimization of dihydropteridone derivatives as novel PLK1 and BRD4 dual inhibitor for the treatment of cancer.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 51 | 8.79 | 9.77 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5417495 | — | — | 1 | 9.77 |
| CHEMBL5416208 | — | — | 1 | 9.70 |
| CHEMBL5422122 | — | — | 1 | 9.52 |
| CHEMBL5429440 | — | — | 1 | 9.52 |
| CHEMBL5419367 | — | — | 1 | 9.52 |
| CHEMBL5426964 | — | — | 1 | 9.52 |
| CHEMBL5427957 | — | — | 1 | 9.40 |
| CHEMBL5403473 | — | — | 1 | 9.38 |
| CHEMBL5410968 | — | — | 1 | 9.37 |
| CHEMBL5403358 | — | — | 1 | 9.30 |
| CHEMBL5418129 | — | — | 1 | 9.30 |
| CHEMBL5395480 | — | — | 1 | 9.30 |
| CHEMBL5401381 | — | — | 1 | 9.30 |
| CHEMBL5412127 | — | — | 1 | 9.29 |
| CHEMBL5421238 | — | — | 1 | 9.28 |
| CHEMBL5394764 | — | — | 1 | 9.22 |
| CHEMBL5437669 | — | — | 1 | 9.19 |
| CHEMBL5428087 | — | — | 1 | 9.15 |
| CHEMBL5438409 | — | — | 1 | 9.14 |
| CHEMBL1233528 | VOLASERTIB | 3.0 | 1 | 9.09 |
| CHEMBL513909 | BI-2536 | 2.0 | 1 | 9.05 |
| CHEMBL5409700 | — | — | 1 | 9.05 |
| CHEMBL5408776 | — | — | 1 | 9.03 |
| CHEMBL5398977 | — | — | 1 | 9.00 |
| CHEMBL5421723 | — | — | 1 | 8.90 |
| CHEMBL5409453 | — | — | 1 | 8.87 |
| CHEMBL5405036 | — | — | 1 | 8.80 |
| CHEMBL5440739 | — | — | 1 | 8.80 |
| CHEMBL5406467 | — | — | 1 | 8.70 |
| CHEMBL5415796 | — | — | 1 | 8.68 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5417495 | — | IC50 | = | 0.17 | nM | 9.77 |
| CHEMBL5416208 | — | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL5429440 | — | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL5419367 | — | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL5426964 | — | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL5422122 | — | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL5427957 | — | IC50 | = | 0.4 | nM | 9.40 |
| CHEMBL5403473 | — | IC50 | = | 0.42 | nM | 9.38 |
| CHEMBL5410968 | — | IC50 | = | 0.43 | nM | 9.37 |
| CHEMBL5403358 | — | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL5418129 | — | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL5395480 | — | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL5401381 | — | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL5412127 | — | IC50 | = | 0.51 | nM | 9.29 |
| CHEMBL5421238 | — | IC50 | = | 0.52 | nM | 9.28 |
| CHEMBL5394764 | — | IC50 | = | 0.6 | nM | 9.22 |
| CHEMBL5437669 | — | IC50 | = | 0.65 | nM | 9.19 |
| CHEMBL5428087 | — | IC50 | = | 0.7 | nM | 9.15 |
| CHEMBL5438409 | — | IC50 | = | 0.72 | nM | 9.14 |
| CHEMBL1233528 | VOLASERTIB | IC50 | = | 0.82 | nM | 9.09 |
| CHEMBL513909 | BI-2536 | IC50 | = | 0.9 | nM | 9.05 |
| CHEMBL5409700 | — | IC50 | = | 0.9 | nM | 9.05 |
| CHEMBL5408776 | — | IC50 | = | 0.94 | nM | 9.03 |
| CHEMBL5398977 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL5421723 | — | IC50 | = | 1.27 | nM | 8.90 |
| CHEMBL5409453 | — | IC50 | = | 1.34 | nM | 8.87 |
| CHEMBL5440739 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL5405036 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL5406467 | — | IC50 | = | 1.98 | nM | 8.70 |
| CHEMBL5415796 | — | IC50 | = | 2.09 | nM | 8.68 |
| CHEMBL5428017 | — | IC50 | = | 2.3 | nM | 8.64 |
| CHEMBL5402922 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL5437723 | — | IC50 | = | 3.12 | nM | 8.51 |
| CHEMBL5402431 | — | IC50 | = | 3.3 | nM | 8.48 |
| CHEMBL5415794 | — | IC50 | = | 3.6 | nM | 8.44 |
| CHEMBL5395241 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL5417454 | — | IC50 | = | 4.1 | nM | 8.39 |
| CHEMBL5430428 | — | IC50 | = | 4.1 | nM | 8.39 |
| CHEMBL5408013 | — | IC50 | = | 5.2 | nM | 8.28 |
| CHEMBL5437467 | — | IC50 | = | 5.3 | nM | 8.28 |
| CHEMBL5410310 | — | IC50 | = | 5.2 | nM | 8.28 |
| CHEMBL5402704 | — | IC50 | = | 6.5 | nM | 8.19 |
| CHEMBL5412529 | — | IC50 | = | 7.2 | nM | 8.14 |
| CHEMBL5434467 | — | IC50 | = | 7.8 | nM | 8.11 |
| CHEMBL5422930 | — | IC50 | = | 8.6 | nM | 8.07 |
| CHEMBL5418320 | — | IC50 | = | 8.6 | nM | 8.07 |
| CHEMBL5417441 | — | IC50 | = | 8.8 | nM | 8.06 |
| CHEMBL5408583 | — | IC50 | = | 8.9 | nM | 8.05 |
| CHEMBL5426693 | — | IC50 | = | 10.4 | nM | 7.98 |
| CHEMBL5400502 | — | IC50 | = | 10.9 | nM | 7.96 |