Assay Detail
Binding
CHEMBL3705425
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Enzyme Inhibtion Assay: To determine Aurora B activity of representative compounds of the invention, Active Aurora B enzyme (recombinant residues 1-344) and INCENP (recombinant GST fusion protein (Upstate)) were incubated in wells of a 384 well plate with biotinylted histone H3 peptide residues 1-21 (Upstate), 1 mM ATP, and various concentrations of inhibitors in a HEPES buffer, pH 7.4 containing MgCl2, sodium othrovanadate, and Triton X-100. After 1 hour, the reaction was stopped with EDTA and anti-phospho-histone H3 Europium Cryptate (Cis-Bio) and SA-APC (Phycolink, Prozyme) were added to detect the phosphopeptide. The amount of phosphorylation was determined by the time-resolved fluorescence ratio of signals at 665 nm and 615 nm.
6
Total Activities
5
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
Thieno[3,2-C]pyridine kinase inhibitors with improved CYP safety profile
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 6 | 7.94 | 8.17 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1980297 | ILORASERTIB | 2.0 | 2 | 8.17 |
| CHEMBL1969102 | — | — | 1 | 8.07 |
| CHEMBL3646210 | — | — | 1 | 7.95 |
| CHEMBL2004290 | — | — | 1 | 7.83 |
| CHEMBL3646211 | — | — | 1 | 7.54 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1980297 | ILORASERTIB | IC50 | = | 6.73 | nM | 8.17 |
| CHEMBL1980297 | ILORASERTIB | IC50 | = | 7.87 | nM | 8.10 |
| CHEMBL1969102 | — | IC50 | = | 8.44 | nM | 8.07 |
| CHEMBL3646210 | — | IC50 | = | 11.21 | nM | 7.95 |
| CHEMBL2004290 | — | IC50 | = | 14.84 | nM | 7.83 |
| CHEMBL3646211 | — | IC50 | = | 28.93 | nM | 7.54 |