Assay Detail
Binding
CHEMBL5228705
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human FLT3-ITD mutant preincubated with enzyme for 20 mins followed by [gamma-33P]ATP addition and measured after 120 mins by filter binding method
33
Total Activities
33
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 |
Target
Receptor-type tyrosine-protein kinase FLT3 (CHEMBL1974) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Discovery of a Potent FLT3 Inhibitor (LT-850-166) with the Capacity of Overcoming a Variety of FLT3 Mutations.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 33 | 8.30 | 9.15 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5289647 | — | — | 1 | 9.15 |
| CHEMBL5280424 | — | — | 1 | 9.07 |
| CHEMBL5275773 | — | — | 1 | 9.03 |
| CHEMBL5267748 | — | — | 1 | 9.03 |
| CHEMBL5288323 | — | — | 1 | 8.94 |
| CHEMBL4456471 | — | — | 1 | 8.87 |
| CHEMBL5273185 | — | — | 1 | 8.85 |
| CHEMBL4077071 | — | — | 1 | 8.77 |
| CHEMBL5198364 | — | — | 1 | 8.73 |
| CHEMBL5278798 | — | — | 1 | 8.69 |
| CHEMBL5287778 | — | — | 1 | 8.49 |
| CHEMBL5270580 | — | — | 1 | 8.45 |
| CHEMBL5279911 | — | — | 1 | 8.45 |
| CHEMBL5277795 | — | — | 1 | 8.43 |
| CHEMBL5270690 | — | — | 1 | 8.42 |
| CHEMBL5289832 | — | — | 1 | 8.41 |
| CHEMBL5277875 | — | — | 1 | 8.41 |
| CHEMBL5287986 | — | — | 1 | 8.34 |
| CHEMBL5290123 | — | — | 1 | 8.30 |
| CHEMBL5290855 | — | — | 1 | 8.30 |
| CHEMBL5270966 | — | — | 1 | 8.24 |
| CHEMBL5287938 | — | — | 1 | 8.12 |
| CHEMBL5286906 | — | — | 1 | 8.12 |
| CHEMBL5272321 | — | — | 1 | 8.08 |
| CHEMBL5280468 | — | — | 1 | 8.04 |
| CHEMBL5287861 | — | — | 1 | 7.99 |
| CHEMBL5273225 | — | — | 1 | 7.95 |
| CHEMBL5281795 | — | — | 1 | 7.89 |
| CHEMBL5266516 | — | — | 1 | 7.85 |
| CHEMBL5283600 | — | — | 1 | 7.79 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5289647 | — | IC50 | = | 0.7 | nM | 9.15 |
| CHEMBL5280424 | — | IC50 | = | 0.85 | nM | 9.07 |
| CHEMBL5275773 | — | IC50 | = | 0.94 | nM | 9.03 |
| CHEMBL5267748 | — | IC50 | = | 0.94 | nM | 9.03 |
| CHEMBL5288323 | — | IC50 | = | 1.14 | nM | 8.94 |
| CHEMBL4456471 | — | IC50 | = | 1.34 | nM | 8.87 |
| CHEMBL5273185 | — | IC50 | = | 1.42 | nM | 8.85 |
| CHEMBL4077071 | — | IC50 | = | 1.71 | nM | 8.77 |
| CHEMBL5198364 | — | IC50 | = | 1.84 | nM | 8.73 |
| CHEMBL5278798 | — | IC50 | = | 2.06 | nM | 8.69 |
| CHEMBL5287778 | — | IC50 | = | 3.22 | nM | 8.49 |
| CHEMBL5270580 | — | IC50 | = | 3.59 | nM | 8.45 |
| CHEMBL5279911 | — | IC50 | = | 3.58 | nM | 8.45 |
| CHEMBL5277795 | — | IC50 | = | 3.72 | nM | 8.43 |
| CHEMBL5270690 | — | IC50 | = | 3.77 | nM | 8.42 |
| CHEMBL5277875 | — | IC50 | = | 3.86 | nM | 8.41 |
| CHEMBL5289832 | — | IC50 | = | 3.88 | nM | 8.41 |
| CHEMBL5287986 | — | IC50 | = | 4.58 | nM | 8.34 |
| CHEMBL5290123 | — | IC50 | = | 4.96 | nM | 8.30 |
| CHEMBL5290855 | — | IC50 | = | 4.96 | nM | 8.30 |
| CHEMBL5270966 | — | IC50 | = | 5.73 | nM | 8.24 |
| CHEMBL5287938 | — | IC50 | = | 7.65 | nM | 8.12 |
| CHEMBL5286906 | — | IC50 | = | 7.59 | nM | 8.12 |
| CHEMBL5272321 | — | IC50 | = | 8.34 | nM | 8.08 |
| CHEMBL5280468 | — | IC50 | = | 9.06 | nM | 8.04 |
| CHEMBL5287861 | — | IC50 | = | 10.33 | nM | 7.99 |
| CHEMBL5273225 | — | IC50 | = | 11.13 | nM | 7.95 |
| CHEMBL5281795 | — | IC50 | = | 12.9 | nM | 7.89 |
| CHEMBL5266516 | — | IC50 | = | 14.06 | nM | 7.85 |
| CHEMBL5283600 | — | IC50 | = | 16.05 | nM | 7.79 |
| CHEMBL5276126 | — | IC50 | = | 23.7 | nM | 7.62 |
| CHEMBL5272638 | — | IC50 | = | 213.3 | nM | 6.67 |
| CHEMBL5280266 | — | IC50 | = | 397.3 | nM | 6.40 |