Assay Detail
Binding
CHEMBL3705783
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Biochemical Assay: The inhibitory activity of putative kinase inhibitors and the potency of selected compounds were determined using a trans-phosphorylation assay.Specific peptide or protein substrates are trans-phosphorylated by their specific serine-threonine or tyrosine kinase, in the presence of ATP traced with 33P-gamma-ATP, and in the presence of their own optimal buffer and cofactors.At the end of the phosphorylation reaction, more than 98% cold ATP and radioactive ATP is captured by an excess of the ion exchange dowex resin; the resin then settles down to the bottom of the reaction plate by gravity.Supernatant, containing the phosphorylated substrate, is subsequently withdrawn and transferred into a counting plate, then evaluated by beta-counting.Reagents/Assay Conditions i. Dowex Resin Preparation500 g of wet resin (SIGMA, custom prepared resin DOWEX 1x8 200-400 mesh, 2.5 Kg) are weighed out and diluted to 2 L in 150 mM sodium formate, pH 3.00.The resin is allowed to settle down.
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 |
Target
Serine/threonine-protein kinase PLK1 (CHEMBL3024) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Substituted pyrazolo-quinazoline derivatives, process for their preparation and their use as kinase inhibitors
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 15 | 8.15 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1793896 | — | — | 1 | 9.00 |
| CHEMBL1272140 | — | — | 1 | 9.00 |
| CHEMBL1271644 | — | — | 1 | 8.70 |
| CHEMBL1738758 | ONVANSERTIB | 2.0 | 1 | 8.52 |
| CHEMBL3652222 | — | — | 1 | 8.30 |
| CHEMBL1793892 | — | — | 1 | 8.30 |
| CHEMBL3652224 | — | — | 1 | 8.15 |
| CHEMBL1774327 | — | — | 1 | 8.10 |
| CHEMBL1094408 | NMS-1286937 | — | 1 | 8.00 |
| CHEMBL3652219 | — | — | 1 | 8.00 |
| CHEMBL1793895 | — | — | 1 | 7.89 |
| CHEMBL1094477 | — | — | 1 | 7.85 |
| CHEMBL3652221 | — | — | 1 | 7.58 |
| CHEMBL3652220 | — | — | 1 | 7.58 |
| CHEMBL3652223 | — | — | 1 | 7.34 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1793896 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL1272140 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL1271644 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL1738758 | ONVANSERTIB | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL3652222 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL1793892 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL3652224 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL1774327 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL1094408 | NMS-1286937 | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL3652219 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL1793895 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL1094477 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL3652221 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL3652220 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL3652223 | — | IC50 | = | 46.0 | nM | 7.34 |