Assay Detail
Binding
CHEMBL2390016
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant GST tagged Aurora A kinase (123 to 401) (unknown origin) transfected in insect sf9 cells after 90 mins by wallac counting analysis
35
Total Activities
35
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
Discovery of 3-phenyl-1H-5-pyrazolylamine derivatives containing a urea pharmacophore as potent and efficacious inhibitors of FMS-like tyrosine kinase-3 (FLT3).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 35 | 6.56 | 7.33 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2386792 | — | — | 1 | 7.33 |
| CHEMBL2386789 | — | — | 1 | 7.28 |
| CHEMBL2386818 | — | — | 1 | 7.19 |
| CHEMBL2386795 | — | — | 1 | 7.16 |
| CHEMBL2386796 | — | — | 1 | 7.14 |
| CHEMBL2386807 | — | — | 1 | 7.01 |
| CHEMBL2386788 | — | — | 1 | 6.92 |
| CHEMBL2386806 | — | — | 1 | 6.92 |
| CHEMBL2386793 | — | — | 1 | 6.80 |
| CHEMBL2386794 | — | — | 1 | 6.80 |
| CHEMBL2386790 | — | — | 1 | 6.60 |
| CHEMBL2386817 | — | — | 1 | 6.52 |
| CHEMBL2386805 | — | — | 1 | 6.50 |
| CHEMBL2386812 | — | — | 1 | 6.48 |
| CHEMBL1807392 | — | — | 1 | 6.47 |
| CHEMBL2386808 | — | — | 1 | 6.31 |
| CHEMBL2386804 | — | — | 1 | 6.30 |
| CHEMBL2386791 | — | — | 1 | 6.22 |
| CHEMBL2386816 | — | — | 1 | 6.21 |
| CHEMBL2386809 | — | — | 1 | 6.15 |
| CHEMBL223360 | LINIFANIB | 3.0 | 1 | 6.12 |
| CHEMBL2386797 | — | — | 1 | 6.12 |
| CHEMBL2386810 | — | — | 1 | 6.10 |
| CHEMBL2386801 | — | — | 1 | 6.03 |
| CHEMBL1336 | SORAFENIB | 4.0 | 1 | 5.42 |
| CHEMBL2386803 | — | — | 1 | - |
| CHEMBL2386802 | — | — | 1 | - |
| CHEMBL2386800 | — | — | 1 | - |
| CHEMBL2386799 | — | — | 1 | - |
| CHEMBL2105709 | QUIZARTINIB DIHYDROCHLORIDE | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2386792 | — | IC50 | = | 47.0 | nM | 7.33 |
| CHEMBL2386789 | — | IC50 | = | 53.0 | nM | 7.28 |
| CHEMBL2386818 | — | IC50 | = | 65.0 | nM | 7.19 |
| CHEMBL2386795 | — | IC50 | = | 69.0 | nM | 7.16 |
| CHEMBL2386796 | — | IC50 | = | 73.0 | nM | 7.14 |
| CHEMBL2386807 | — | IC50 | = | 98.0 | nM | 7.01 |
| CHEMBL2386788 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL2386806 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL2386793 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL2386794 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL2386790 | — | IC50 | = | 250.0 | nM | 6.60 |
| CHEMBL2386817 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL2386805 | — | IC50 | = | 320.0 | nM | 6.50 |
| CHEMBL2386812 | — | IC50 | = | 330.0 | nM | 6.48 |
| CHEMBL1807392 | — | IC50 | = | 340.0 | nM | 6.47 |
| CHEMBL2386808 | — | IC50 | = | 490.0 | nM | 6.31 |
| CHEMBL2386804 | — | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL2386791 | — | IC50 | = | 600.0 | nM | 6.22 |
| CHEMBL2386816 | — | IC50 | = | 610.0 | nM | 6.21 |
| CHEMBL2386809 | — | IC50 | = | 710.0 | nM | 6.15 |
| CHEMBL223360 | LINIFANIB | IC50 | = | 760.0 | nM | 6.12 |
| CHEMBL2386797 | — | IC50 | = | 760.0 | nM | 6.12 |
| CHEMBL2386810 | — | IC50 | = | 790.0 | nM | 6.10 |
| CHEMBL2386801 | — | IC50 | = | 940.0 | nM | 6.03 |
| CHEMBL1336 | SORAFENIB | IC50 | = | 3800.0 | nM | 5.42 |
| CHEMBL2386798 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL2063324 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL2386813 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL2386814 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL2386815 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL2105709 | QUIZARTINIB DIHYDROCHLORIDE | IC50 | > | 10000.0 | nM | - |
| CHEMBL2386799 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL2386800 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL2386802 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL2386803 | — | IC50 | > | 1000.0 | nM | - |