Compound Detail
CHEMBL2105709
QUIZARTINIB DIHYDROCHLORIDE 💊 Approved Drug
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💊 Approved Drug
CC(C)(C)c1cc(NC(=O)Nc2ccc(-c3cn4c(n3)sc3cc(OCCN5CCOCC5)ccc34)cc2)no1.Cl.Cl
Basic Information
| ChEMBL ID | CHEMBL2105709 |
| Name | QUIZARTINIB DIHYDROCHLORIDE |
| Phase | Approved |
| Structure Type | MOL |
| InChI Key | DHYPGRVMIOATAE-UHFFFAOYSA-N |
| Therapeutic | ✓ Yes |
| Parent Compound | CHEMBL576982 |
| Active Moiety | CHEMBL576982 |
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
8
Publications
10
Known Names
4
Indications
1
Mechanisms
Molecular Properties
560.7
MW (Da)
5.86
ALogP
9
HBA
2
HBD
106.2
PSA (Ų)
0.26
QED
2
Ro5 Violations
7
Rot. Bonds
Drug Information
| Molecule Type | Small molecule |
| First Approval | 2023 |
| Availability | Prescription |
| Chirality | Achiral |
Mechanism of Action
| Mechanism | Action Type | Target | Direct | Efficacy |
|---|---|---|---|---|
| Tyrosine-protein kinase receptor FLT3 inhibitor | INHIBITOR | Receptor-type tyrosine-protein kinase FLT3 | ✓ | ✓ |
Indications
Leukemia, Myeloid Leukemia, Myeloid, Acute Myelodysplastic Syndromes Precursor Cell Lymphoblastic Leukemia-Lymphoma
Drug Warnings
Black Box Warning
cardiotoxicity
Activity Summary
IC50 2 meas. best 7.16
Target Activity Profile
| Target | Type | Best pChEMBL | Mean pChEMBL | Best (nM) | # Data |
|---|---|---|---|---|---|
| Receptor-type tyrosine-protein kinase FLT3 CHEMBL1974 | IC50 | 7.16 | 7.16 | 69.0 | 1 |
| Vascular endothelial growth factor receptor 2 CHEMBL279 | IC50 | 6.37 | 6.37 | 430.0 | 1 |
Activity Data Samples
Top measurements by pChEMBL value
| Target | Type | Rel. | Value | Units | pChEMBL | Assay | PubMed |
|---|---|---|---|---|---|---|---|
| Receptor-type tyrosine-protein kinase FLT3 | IC50 | = | 69.0 | nM | 7.16 | Inhibition of wild type GST tagged FLT3 kinase (567 to 993) (unknown origin) tra... | 23618709 |
| Vascular endothelial growth factor receptor 2 | IC50 | = | 430.0 | nM | 6.37 | Inhibition of recombinant GST tagged VEGFR2 (789 to 1356) (unknown origin) trans... | 23618709 |
Literature References
| PubMed | DOI | Target Context | # Activities |
|---|---|---|---|
| 23618709 | 10.1016/j.bmc.2013.03.083 | U-937 | 1 |
| 23618709 | 10.1016/j.bmc.2013.03.083 | K562 | 1 |
| 23618709 | 10.1016/j.bmc.2013.03.083 | NON-PROTEIN TARGET | 1 |
| 23618709 | 10.1016/j.bmc.2013.03.083 | MV4-11 | 1 |
| 23618709 | 10.1016/j.bmc.2013.03.083 | MOLM-13 | 1 |
| 23618709 | 10.1016/j.bmc.2013.03.083 | Aurora kinase A | 1 |
| 23618709 | 10.1016/j.bmc.2013.03.083 | Vascular endothelial growth factor receptor 2 | 1 |
| 23618709 | 10.1016/j.bmc.2013.03.083 | Receptor-type tyrosine-protein kinase FLT3 | 1 |
Data from ChEMBL 36 via Core Engine