Assay Detail
Binding
CHEMBL4773000
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Inhibition of recombinant human full-length His-tagged Aurora B expressed in baculovirus expression system using 5-FAM-LRRASLG-CONH2 as substrate preincubated for 60 mins followed by substrate addition by microfluidic assay
32
Total Activities
32
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
Discovery of SP-96, the first non-ATP-competitive Aurora Kinase B inhibitor, for reduced myelosuppression.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 32 | 7.23 | 9.50 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4799738 | — | — | 1 | 9.50 |
| CHEMBL215152 | DEFOSBARASERTIB | 2.0 | 1 | 9.49 |
| CHEMBL4784002 | — | — | 1 | 9.47 |
| CHEMBL4799497 | — | — | 1 | 8.53 |
| CHEMBL3699142 | — | — | 1 | 8.52 |
| CHEMBL4796319 | — | — | 1 | 8.00 |
| CHEMBL4785614 | — | — | 1 | 7.82 |
| CHEMBL572878 | TOZASERTIB | 2.0 | 1 | 7.75 |
| CHEMBL4784119 | — | — | 1 | 7.64 |
| CHEMBL4796460 | — | — | 1 | 7.53 |
| CHEMBL4780095 | — | — | 1 | 7.52 |
| CHEMBL4776298 | — | — | 1 | 7.45 |
| CHEMBL4779701 | — | — | 1 | 7.21 |
| CHEMBL4789795 | — | — | 1 | 7.20 |
| CHEMBL4776505 | — | — | 1 | 7.14 |
| CHEMBL4788491 | — | — | 1 | 7.12 |
| CHEMBL4779005 | — | — | 1 | 7.04 |
| CHEMBL4794846 | — | — | 1 | 6.94 |
| CHEMBL4799187 | — | — | 1 | 6.85 |
| CHEMBL4789271 | — | — | 1 | 6.73 |
| CHEMBL4796509 | — | — | 1 | 6.71 |
| CHEMBL4776475 | — | — | 1 | 6.68 |
| CHEMBL4786894 | — | — | 1 | 6.65 |
| CHEMBL4781573 | — | — | 1 | 6.62 |
| CHEMBL514409 | HESPERADIN | — | 1 | 6.60 |
| CHEMBL4799236 | — | — | 1 | 6.51 |
| CHEMBL4789341 | — | — | 1 | 6.03 |
| CHEMBL4777770 | — | — | 1 | 6.03 |
| CHEMBL4785707 | — | — | 1 | 6.00 |
| CHEMBL4776476 | — | — | 1 | 5.67 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4799738 | — | IC50 | = | 0.316 | nM | 9.50 |
| CHEMBL215152 | DEFOSBARASERTIB | IC50 | = | 0.326 | nM | 9.49 |
| CHEMBL4784002 | — | IC50 | = | 0.336 | nM | 9.47 |
| CHEMBL4799497 | — | IC50 | = | 2.981 | nM | 8.53 |
| CHEMBL3699142 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL4796319 | — | IC50 | = | 9.968 | nM | 8.00 |
| CHEMBL4785614 | — | IC50 | = | 15.08 | nM | 7.82 |
| CHEMBL572878 | TOZASERTIB | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL4784119 | — | IC50 | = | 22.84 | nM | 7.64 |
| CHEMBL4796460 | — | IC50 | = | 29.82 | nM | 7.53 |
| CHEMBL4780095 | — | IC50 | = | 29.89 | nM | 7.52 |
| CHEMBL4776298 | — | IC50 | = | 35.3 | nM | 7.45 |
| CHEMBL4779701 | — | IC50 | = | 61.2 | nM | 7.21 |
| CHEMBL4789795 | — | IC50 | = | 63.07 | nM | 7.20 |
| CHEMBL4776505 | — | IC50 | = | 71.63 | nM | 7.14 |
| CHEMBL4788491 | — | IC50 | = | 75.87 | nM | 7.12 |
| CHEMBL4779005 | — | IC50 | = | 90.62 | nM | 7.04 |
| CHEMBL4794846 | — | IC50 | = | 116.0 | nM | 6.94 |
| CHEMBL4799187 | — | IC50 | = | 141.8 | nM | 6.85 |
| CHEMBL4789271 | — | IC50 | = | 185.3 | nM | 6.73 |
| CHEMBL4796509 | — | IC50 | = | 197.03 | nM | 6.71 |
| CHEMBL4776475 | — | IC50 | = | 209.53 | nM | 6.68 |
| CHEMBL4786894 | — | IC50 | = | 222.1 | nM | 6.65 |
| CHEMBL4781573 | — | IC50 | = | 238.45 | nM | 6.62 |
| CHEMBL514409 | HESPERADIN | IC50 | = | 250.0 | nM | 6.60 |
| CHEMBL4799236 | — | IC50 | = | 310.6 | nM | 6.51 |
| CHEMBL4789341 | — | IC50 | = | 944.2 | nM | 6.03 |
| CHEMBL4777770 | — | IC50 | = | 939.1 | nM | 6.03 |
| CHEMBL4785707 | — | IC50 | = | 1008.0 | nM | 6.00 |
| CHEMBL4776476 | — | IC50 | = | 2150.6 | nM | 5.67 |
| CHEMBL4794161 | — | IC50 | = | 6580.6 | nM | 5.18 |
| CHEMBL4778166 | — | IC50 | > | 15000.0 | nM | - |