Assay Detail
Binding
CHEMBL3380433
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Inhibition of Aurora B (unknown origin) using HLRRASLG substrate
34
Total Activities
34
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
Novel acylureidoindolin-2-one derivatives as dual Aurora B/FLT3 inhibitors for the treatment of acute myeloid leukemia.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 34 | 8.15 | 9.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL215152 | DEFOSBARASERTIB | 2.0 | 1 | 9.52 |
| CHEMBL3329684 | — | — | 1 | 9.40 |
| CHEMBL3329669 | — | — | 1 | 8.92 |
| CHEMBL3329673 | — | — | 1 | 8.89 |
| CHEMBL3329670 | — | — | 1 | 8.82 |
| CHEMBL3329675 | — | — | 1 | 8.82 |
| CHEMBL3329668 | — | — | 1 | 8.74 |
| CHEMBL388978 | STAUROSPORINE | — | 1 | 8.74 |
| CHEMBL3329664 | — | — | 1 | 8.72 |
| CHEMBL3329672 | — | — | 1 | 8.64 |
| CHEMBL3329674 | — | — | 1 | 8.52 |
| CHEMBL3329671 | — | — | 1 | 8.52 |
| CHEMBL3329655 | — | — | 1 | 8.28 |
| CHEMBL3329658 | — | — | 1 | 8.19 |
| CHEMBL3329656 | — | — | 1 | 8.19 |
| CHEMBL3329683 | — | — | 1 | 8.12 |
| CHEMBL3329657 | — | — | 1 | 8.11 |
| CHEMBL3329682 | — | — | 1 | 7.98 |
| CHEMBL3329652 | — | — | 1 | 7.83 |
| CHEMBL3329660 | — | — | 1 | 7.82 |
| CHEMBL3329681 | — | — | 1 | 7.79 |
| CHEMBL3329680 | — | — | 1 | 7.78 |
| CHEMBL3329661 | — | — | 1 | 7.74 |
| CHEMBL3329679 | — | — | 1 | 7.74 |
| CHEMBL3361346 | — | — | 1 | 7.67 |
| CHEMBL3329662 | — | — | 1 | 7.53 |
| CHEMBL3329678 | — | — | 1 | 7.51 |
| CHEMBL3329659 | — | — | 1 | 7.39 |
| CHEMBL3329665 | — | — | 1 | 7.26 |
| CHEMBL3329663 | — | — | 1 | 6.80 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL215152 | DEFOSBARASERTIB | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL3329684 | — | IC50 | = | 0.4 | nM | 9.40 |
| CHEMBL3329669 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL3329673 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL3329670 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL3329675 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL3329668 | — | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL388978 | STAUROSPORINE | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL3329664 | — | IC50 | = | 1.9 | nM | 8.72 |
| CHEMBL3329672 | — | IC50 | = | 2.3 | nM | 8.64 |
| CHEMBL3329674 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL3329671 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL3329655 | — | IC50 | = | 5.3 | nM | 8.28 |
| CHEMBL3329658 | — | IC50 | = | 6.5 | nM | 8.19 |
| CHEMBL3329656 | — | IC50 | = | 6.5 | nM | 8.19 |
| CHEMBL3329683 | — | IC50 | = | 7.6 | nM | 8.12 |
| CHEMBL3329657 | — | IC50 | = | 7.7 | nM | 8.11 |
| CHEMBL3329682 | — | IC50 | = | 10.5 | nM | 7.98 |
| CHEMBL3329652 | — | IC50 | = | 14.9 | nM | 7.83 |
| CHEMBL3329660 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL3329681 | — | IC50 | = | 16.4 | nM | 7.79 |
| CHEMBL3329680 | — | IC50 | = | 16.8 | nM | 7.78 |
| CHEMBL3329661 | — | IC50 | = | 18.4 | nM | 7.74 |
| CHEMBL3329679 | — | IC50 | = | 18.4 | nM | 7.74 |
| CHEMBL3361346 | — | IC50 | = | 21.5 | nM | 7.67 |
| CHEMBL3329662 | — | IC50 | = | 29.8 | nM | 7.53 |
| CHEMBL3329678 | — | IC50 | = | 30.6 | nM | 7.51 |
| CHEMBL3329659 | — | IC50 | = | 40.9 | nM | 7.39 |
| CHEMBL3329665 | — | IC50 | = | 55.5 | nM | 7.26 |
| CHEMBL3329663 | — | IC50 | = | 158.7 | nM | 6.80 |
| CHEMBL3329677 | — | IC50 | = | 217.9 | nM | 6.66 |
| CHEMBL3329676 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL3329666 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL3329667 | — | IC50 | > | 1000.0 | nM | - |