Assay Detail
Binding
CHEMBL931996
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Inhibition of Aurora A kinase
7
Total Activities
7
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Publication
Aurora kinase A inhibitors: identification, SAR exploration and molecular modeling of 6,7-dihydro-4H-pyrazolo-[1,5-a]pyrrolo[3,4-d]pyrimidine-5,8-dione scaffold.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 5 | 4.95 | 5.25 |
| Ki | 2 | 8.56 | 9.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL572878 | TOZASERTIB | 2.0 | 1 | 9.22 |
| CHEMBL402548 | DANUSERTIB | 2.0 | 1 | 7.89 |
| CHEMBL402349 | — | — | 1 | 5.25 |
| CHEMBL271894 | — | — | 1 | 5.10 |
| CHEMBL1589017 | — | — | 1 | 4.82 |
| CHEMBL439417 | — | — | 1 | 4.82 |
| CHEMBL255808 | — | — | 1 | 4.74 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL572878 | TOZASERTIB | Ki | = | 0.6 | nM | 9.22 |
| CHEMBL402548 | DANUSERTIB | Ki | = | 13.0 | nM | 7.89 |
| CHEMBL402349 | — | IC50 | = | 5600.0 | nM | 5.25 |
| CHEMBL271894 | — | IC50 | = | 8000.0 | nM | 5.10 |
| CHEMBL1589017 | — | IC50 | = | 15100.0 | nM | 4.82 |
| CHEMBL439417 | — | IC50 | = | 15200.0 | nM | 4.82 |
| CHEMBL255808 | — | IC50 | = | 18300.0 | nM | 4.74 |