Assay Detail
Binding
CHEMBL5123484
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Inhibition of human recombinant His-tagged FLT3 kinase domain (564 to 958 residues) expressed in baculovirus expression system incubated for 30 mins in presence of ATP by HTRF analysis
30
Total Activities
30
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 indirubin-3'-aminooxy-acetamide derivatives as potent and selective FLT3/D835Y mutant kinase inhibitors for acute myeloid leukemia.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 30 | 8.83 | 9.59 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5195819 | — | — | 1 | 9.59 |
| CHEMBL5188834 | — | — | 1 | 9.57 |
| CHEMBL5201185 | — | — | 1 | 9.54 |
| CHEMBL5188978 | — | — | 1 | 9.54 |
| CHEMBL5170345 | — | — | 1 | 9.19 |
| CHEMBL5209537 | — | — | 1 | 9.17 |
| CHEMBL5186291 | — | — | 1 | 9.10 |
| CHEMBL5170760 | — | — | 1 | 9.10 |
| CHEMBL1623035 | — | — | 1 | 9.06 |
| CHEMBL5202926 | — | — | 1 | 9.03 |
| CHEMBL5199328 | — | — | 1 | 8.93 |
| CHEMBL5186183 | — | — | 1 | 8.93 |
| CHEMBL5185448 | — | — | 1 | 8.91 |
| CHEMBL5195070 | — | — | 1 | 8.89 |
| CHEMBL5172103 | — | — | 1 | 8.85 |
| CHEMBL5173987 | — | — | 1 | 8.79 |
| CHEMBL5169874 | — | — | 1 | 8.78 |
| CHEMBL5181917 | — | — | 1 | 8.74 |
| CHEMBL5195353 | — | — | 1 | 8.70 |
| CHEMBL5181019 | — | — | 1 | 8.70 |
| CHEMBL5182954 | — | — | 1 | 8.68 |
| CHEMBL5202099 | — | — | 1 | 8.60 |
| CHEMBL5169937 | — | — | 1 | 8.58 |
| CHEMBL5201194 | — | — | 1 | 8.48 |
| CHEMBL5200813 | — | — | 1 | 8.44 |
| CHEMBL5196786 | — | — | 1 | 8.30 |
| CHEMBL5182860 | — | — | 1 | 8.14 |
| CHEMBL5192189 | — | — | 1 | 7.82 |
| CHEMBL5182679 | — | — | 1 | 7.80 |
| CHEMBL5191315 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5195819 | — | IC50 | = | 0.26 | nM | 9.59 |
| CHEMBL5188834 | — | IC50 | = | 0.27 | nM | 9.57 |
| CHEMBL5201185 | — | IC50 | = | 0.29 | nM | 9.54 |
| CHEMBL5188978 | — | IC50 | = | 0.29 | nM | 9.54 |
| CHEMBL5170345 | — | IC50 | = | 0.64 | nM | 9.19 |
| CHEMBL5209537 | — | IC50 | = | 0.67 | nM | 9.17 |
| CHEMBL5186291 | — | IC50 | = | 0.79 | nM | 9.10 |
| CHEMBL5170760 | — | IC50 | = | 0.8 | nM | 9.10 |
| CHEMBL1623035 | — | IC50 | = | 0.88 | nM | 9.06 |
| CHEMBL5202926 | — | IC50 | = | 0.93 | nM | 9.03 |
| CHEMBL5199328 | — | IC50 | = | 1.17 | nM | 8.93 |
| CHEMBL5186183 | — | IC50 | = | 1.18 | nM | 8.93 |
| CHEMBL5185448 | — | IC50 | = | 1.23 | nM | 8.91 |
| CHEMBL5195070 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL5172103 | — | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL5173987 | — | IC50 | = | 1.63 | nM | 8.79 |
| CHEMBL5169874 | — | IC50 | = | 1.66 | nM | 8.78 |
| CHEMBL5181917 | — | IC50 | = | 1.82 | nM | 8.74 |
| CHEMBL5195353 | — | IC50 | = | 2.02 | nM | 8.70 |
| CHEMBL5181019 | — | IC50 | = | 2.01 | nM | 8.70 |
| CHEMBL5182954 | — | IC50 | = | 2.07 | nM | 8.68 |
| CHEMBL5202099 | — | IC50 | = | 2.54 | nM | 8.60 |
| CHEMBL5169937 | — | IC50 | = | 2.62 | nM | 8.58 |
| CHEMBL5201194 | — | IC50 | = | 3.29 | nM | 8.48 |
| CHEMBL5200813 | — | IC50 | = | 3.65 | nM | 8.44 |
| CHEMBL5196786 | — | IC50 | = | 4.95 | nM | 8.30 |
| CHEMBL5182860 | — | IC50 | = | 7.31 | nM | 8.14 |
| CHEMBL5192189 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL5182679 | — | IC50 | = | 15.8 | nM | 7.80 |
| CHEMBL5191315 | — | IC50 | > | 50.0 | nM | - |