Assay Detail
Binding
CHEMBL1244978
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding affinity to SIK
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
Serine/threonine-protein kinase SIK1 (CHEMBL6082) ↗| 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 | 6.64 | 7.18 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1240703 | CGP-52421 | — | 1 | 7.18 |
| CHEMBL603469 | LESTAURTINIB | 3.0 | 1 | 7.09 |
| CHEMBL608533 | MIDOSTAURIN | 4.0 | 1 | 6.80 |
| CHEMBL535 | SUNITINIB | 4.0 | 1 | 5.50 |
| CHEMBL124660 | TANDUTINIB | 2.0 | 1 | - |
| CHEMBL576982 | QUIZARTINIB | 4.0 | 1 | - |
| CHEMBL1336 | SORAFENIB | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1240703 | CGP-52421 | Kd | = | 66.0 | nM | 7.18 |
| CHEMBL603469 | LESTAURTINIB | Kd | = | 82.0 | nM | 7.09 |
| CHEMBL608533 | MIDOSTAURIN | Kd | = | 160.0 | nM | 6.80 |
| CHEMBL535 | SUNITINIB | Kd | = | 3200.0 | nM | 5.50 |
| CHEMBL124660 | TANDUTINIB | Kd | > | 10000.0 | nM | - |
| CHEMBL576982 | QUIZARTINIB | Kd | > | 10000.0 | nM | - |
| CHEMBL1336 | SORAFENIB | Kd | > | 10000.0 | nM | - |