Assay Detail
Binding
CHEMBL1244930
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Binding affinity to PKN1
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 |
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 | 7.43 | 8.28 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL603469 | LESTAURTINIB | 3.0 | 1 | 8.28 |
| CHEMBL608533 | MIDOSTAURIN | 4.0 | 1 | 8.03 |
| CHEMBL1240703 | CGP-52421 | — | 1 | 7.24 |
| CHEMBL535 | SUNITINIB | 4.0 | 1 | 6.15 |
| CHEMBL124660 | TANDUTINIB | 2.0 | 1 | - |
| CHEMBL576982 | QUIZARTINIB | 4.0 | 1 | - |
| CHEMBL1336 | SORAFENIB | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL603469 | LESTAURTINIB | Kd | = | 5.3 | nM | 8.28 |
| CHEMBL608533 | MIDOSTAURIN | Kd | = | 9.3 | nM | 8.03 |
| CHEMBL1240703 | CGP-52421 | Kd | = | 57.0 | nM | 7.24 |
| CHEMBL535 | SUNITINIB | Kd | = | 710.0 | nM | 6.15 |
| CHEMBL124660 | TANDUTINIB | Kd | > | 10000.0 | nM | - |
| CHEMBL576982 | QUIZARTINIB | Kd | > | 10000.0 | nM | - |
| CHEMBL1336 | SORAFENIB | Kd | > | 10000.0 | nM | - |