Assay Detail
Binding
CHEMBL3595191
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Inhibition of recombinant GST-tagged Aurora-A kinase domain (S123 to S401) (unknown origin) expressed in insect Sf9 cells using tetra(LRRASLG) peptide as substrate after 90 mins by Kinase-Glo assay
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | Sf9 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Identification of a potent 5-phenyl-thiazol-2-ylamine-based inhibitor of FLT3 with activity against drug resistance-conferring point mutations.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 17 | 7.04 | 7.60 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3593296 | — | — | 1 | 7.60 |
| CHEMBL3593290 | — | — | 1 | 7.50 |
| CHEMBL3593292 | — | — | 1 | 7.44 |
| CHEMBL3593291 | — | — | 1 | 7.42 |
| CHEMBL3593289 | — | — | 1 | 7.42 |
| CHEMBL3593288 | — | — | 1 | 7.39 |
| CHEMBL3593293 | — | — | 1 | 7.37 |
| CHEMBL3593287 | — | — | 1 | 7.25 |
| CHEMBL608533 | MIDOSTAURIN | 4.0 | 1 | 7.10 |
| CHEMBL3593285 | — | — | 1 | 7.02 |
| CHEMBL3593295 | — | — | 1 | 6.85 |
| CHEMBL3593284 | — | — | 1 | 6.82 |
| CHEMBL3593286 | — | — | 1 | 6.57 |
| CHEMBL3593294 | — | — | 1 | 6.50 |
| CHEMBL1336 | SORAFENIB | 4.0 | 1 | 5.42 |
| CHEMBL576982 | QUIZARTINIB | 4.0 | 1 | - |
| CHEMBL3593283 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3593296 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL3593290 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL3593292 | — | IC50 | = | 36.0 | nM | 7.44 |
| CHEMBL3593291 | — | IC50 | = | 38.0 | nM | 7.42 |
| CHEMBL3593289 | — | IC50 | = | 38.0 | nM | 7.42 |
| CHEMBL3593288 | — | IC50 | = | 41.0 | nM | 7.39 |
| CHEMBL3593293 | — | IC50 | = | 43.0 | nM | 7.37 |
| CHEMBL3593287 | — | IC50 | = | 56.0 | nM | 7.25 |
| CHEMBL608533 | MIDOSTAURIN | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL3593285 | — | IC50 | = | 95.0 | nM | 7.02 |
| CHEMBL3593295 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL3593284 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL3593286 | — | IC50 | = | 270.0 | nM | 6.57 |
| CHEMBL3593294 | — | IC50 | = | 320.0 | nM | 6.50 |
| CHEMBL1336 | SORAFENIB | IC50 | = | 3800.0 | nM | 5.42 |
| CHEMBL576982 | QUIZARTINIB | IC50 | > | 10000.0 | nM | - |
| CHEMBL3593283 | — | IC50 | > | 10000.0 | nM | - |