Assay Detail
Binding
CHEMBL5528692
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of FLT3 (unknown origin) by bioluminescent ADP-Glo assay
6
Total Activities
6
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
An imidazo[1,2-a]pyridine-pyridine derivative potently inhibits FLT3-ITD and FLT3-ITD secondary mutants, including gilteritinib-resistant FLT3-ITD/F691L.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 6 | 7.56 | 8.18 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5595005 | — | — | 1 | 8.18 |
| CHEMBL5575586 | — | — | 1 | 8.10 |
| CHEMBL3301622 | GILTERITINIB | 4.0 | 1 | 7.97 |
| CHEMBL5569052 | — | — | 1 | 7.02 |
| CHEMBL5562812 | — | — | 1 | 6.54 |
| CHEMBL24828 | VANDETANIB | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5595005 | — | IC50 | = | 6.63 | nM | 8.18 |
| CHEMBL5575586 | — | IC50 | = | 7.94 | nM | 8.10 |
| CHEMBL3301622 | GILTERITINIB | IC50 | = | 10.59 | nM | 7.97 |
| CHEMBL5569052 | — | IC50 | = | 94.58 | nM | 7.02 |
| CHEMBL5562812 | — | IC50 | = | 288.0 | nM | 6.54 |
| CHEMBL24828 | VANDETANIB | IC50 | > | 1000.0 | nM | - |