Assay Detail
Binding
CHEMBL2344827
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of FLT3-ITD mutant in human MV4-11 cells assessed as decrease in cell viability after 72 hrs by MTT assay
34
Total Activities
34
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | MV4-11 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Receptor-type tyrosine-protein kinase FLT3 (CHEMBL1974) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Structure-activity relationship studies of pyrazolo[3,4-d]pyrimidine derivatives leading to the discovery of a novel multikinase inhibitor that potently inhibits FLT3 and VEGFR2 and evaluation of its activity against acute myeloid leukemia in vitro and in vivo.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 34 | 6.79 | 8.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2331570 | — | — | 1 | 8.40 |
| CHEMBL2332840 | — | — | 1 | 8.40 |
| CHEMBL2332849 | — | — | 1 | 8.30 |
| CHEMBL1336 | SORAFENIB | 4.0 | 1 | 8.15 |
| CHEMBL2332867 | — | — | 1 | 7.96 |
| CHEMBL2332870 | — | — | 1 | 7.77 |
| CHEMBL2332871 | — | — | 1 | 7.75 |
| CHEMBL2332846 | — | — | 1 | 7.70 |
| CHEMBL2332848 | — | — | 1 | 7.43 |
| CHEMBL2332869 | — | — | 1 | 7.27 |
| CHEMBL2332868 | — | — | 1 | 7.23 |
| CHEMBL2332851 | — | — | 1 | 7.10 |
| CHEMBL2332847 | — | — | 1 | 7.08 |
| CHEMBL2332866 | — | — | 1 | 7.05 |
| CHEMBL2332865 | — | — | 1 | 7.02 |
| CHEMBL2332844 | — | — | 1 | 6.58 |
| CHEMBL2332860 | — | — | 1 | 6.50 |
| CHEMBL2332864 | — | — | 1 | 6.44 |
| CHEMBL2332861 | — | — | 1 | 6.35 |
| CHEMBL2332862 | — | — | 1 | 5.97 |
| CHEMBL2332842 | — | — | 1 | 5.91 |
| CHEMBL2332863 | — | — | 1 | 5.86 |
| CHEMBL2332850 | — | — | 1 | 5.80 |
| CHEMBL2332841 | — | — | 1 | 5.78 |
| CHEMBL2332843 | — | — | 1 | 5.77 |
| CHEMBL2332845 | — | — | 1 | 5.69 |
| CHEMBL2332852 | — | — | 1 | 5.34 |
| CHEMBL2332856 | — | — | 1 | 5.15 |
| CHEMBL2332853 | — | — | 1 | 5.11 |
| CHEMBL2332854 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2331570 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL2332840 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL2332849 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL1336 | SORAFENIB | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL2332867 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL2332870 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL2332871 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL2332846 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL2332848 | — | IC50 | = | 37.0 | nM | 7.43 |
| CHEMBL2332869 | — | IC50 | = | 54.0 | nM | 7.27 |
| CHEMBL2332868 | — | IC50 | = | 59.0 | nM | 7.23 |
| CHEMBL2332851 | — | IC50 | = | 79.0 | nM | 7.10 |
| CHEMBL2332847 | — | IC50 | = | 83.0 | nM | 7.08 |
| CHEMBL2332866 | — | IC50 | = | 90.0 | nM | 7.05 |
| CHEMBL2332865 | — | IC50 | = | 96.0 | nM | 7.02 |
| CHEMBL2332844 | — | IC50 | = | 260.0 | nM | 6.58 |
| CHEMBL2332860 | — | IC50 | = | 320.0 | nM | 6.50 |
| CHEMBL2332864 | — | IC50 | = | 363.0 | nM | 6.44 |
| CHEMBL2332861 | — | IC50 | = | 449.0 | nM | 6.35 |
| CHEMBL2332862 | — | IC50 | = | 1074.0 | nM | 5.97 |
| CHEMBL2332842 | — | IC50 | = | 1240.0 | nM | 5.91 |
| CHEMBL2332863 | — | IC50 | = | 1371.0 | nM | 5.86 |
| CHEMBL2332850 | — | IC50 | = | 1590.0 | nM | 5.80 |
| CHEMBL2332841 | — | IC50 | = | 1650.0 | nM | 5.78 |
| CHEMBL2332843 | — | IC50 | = | 1690.0 | nM | 5.77 |
| CHEMBL2332845 | — | IC50 | = | 2050.0 | nM | 5.69 |
| CHEMBL2332852 | — | IC50 | = | 4530.0 | nM | 5.34 |
| CHEMBL2332856 | — | IC50 | = | 7070.0 | nM | 5.15 |
| CHEMBL2332853 | — | IC50 | = | 7820.0 | nM | 5.11 |
| CHEMBL2332854 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL2332855 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL2332857 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL2332858 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL2332859 | — | IC50 | > | 10000.0 | nM | - |