Assay Detail
Binding
CHEMBL1244696
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding affinity to FLT3 catalytic domain by KinomeScan kinase binding assay
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Target
Receptor-type tyrosine-protein kinase FLT3 (CHEMBL1974) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 7 | 8.25 | 9.33 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL535 | SUNITINIB | 4.0 | 1 | 9.33 |
| CHEMBL576982 | QUIZARTINIB | 4.0 | 1 | 8.80 |
| CHEMBL124660 | TANDUTINIB | 2.0 | 1 | 8.52 |
| CHEMBL603469 | LESTAURTINIB | 3.0 | 1 | 8.07 |
| CHEMBL608533 | MIDOSTAURIN | 4.0 | 1 | 7.96 |
| CHEMBL1336 | SORAFENIB | 4.0 | 1 | 7.89 |
| CHEMBL1240703 | CGP-52421 | — | 1 | 7.17 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL535 | SUNITINIB | Kd | = | 0.47 | nM | 9.33 |
| CHEMBL576982 | QUIZARTINIB | Kd | = | 1.6 | nM | 8.80 |
| CHEMBL124660 | TANDUTINIB | Kd | = | 3.0 | nM | 8.52 |
| CHEMBL603469 | LESTAURTINIB | Kd | = | 8.5 | nM | 8.07 |
| CHEMBL608533 | MIDOSTAURIN | Kd | = | 11.0 | nM | 7.96 |
| CHEMBL1336 | SORAFENIB | Kd | = | 13.0 | nM | 7.89 |
| CHEMBL1240703 | CGP-52421 | Kd | = | 68.0 | nM | 7.17 |