Compound Detail
CHEMBL3989516
FOSTAMATINIB DISODIUM 💊 Approved Drug
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💊 Approved Drug
COc1cc(Nc2ncc(F)c(Nc3ccc4c(n3)N(COP(=O)([O-])[O-])C(=O)C(C)(C)O4)n2)cc(OC)c1OC.O.O.O.O.O.O.[Na+].[Na+]
Basic Information
| ChEMBL ID | CHEMBL3989516 |
| Name | FOSTAMATINIB DISODIUM |
| Phase | Approved |
| Structure Type | MOL |
| InChI Key | ZQGJCHHKJNSPMS-UHFFFAOYSA-L |
| Therapeutic | ✓ Yes |
| Parent Compound | CHEMBL2103830 |
| Active Moiety | CHEMBL475251 |
3
Targets
3
Activities
2
Assay Types
0
PK Parameters
18
Publications
14
Known Names
7
Indications
1
Mechanisms
Molecular Properties
580.5
MW (Da)
3.09
ALogP
12
HBA
4
HBD
186.7
PSA (Ų)
0.26
QED
2
Ro5 Violations
10
Rot. Bonds
Drug Information
| Molecule Type | Small molecule |
| First Approval | 2018 |
| Availability | Prescription |
| Chirality | Achiral |
Mechanism of Action
| Mechanism | Action Type | Target | Direct | Efficacy |
|---|---|---|---|---|
| Tyrosine-protein kinase SYK inhibitor | INHIBITOR | Tyrosine-protein kinase SYK | ✓ | ✓ |
Indications
Purpura, Thrombocytopenic, Idiopathic Thrombocytopenia Anemia, Hemolytic, Autoimmune Arthritis, Rheumatoid Glomerulonephritis, IGA Lupus Erythematosus, Systemic Lymphoma
Activity Summary
IC50 2 meas. best 7.77
Kd 1 meas. best 7.16
Target Activity Profile
| Target | Type | Best pChEMBL | Mean pChEMBL | Best (nM) | # Data |
|---|---|---|---|---|---|
| Tyrosine-protein kinase SYK CHEMBL2599 | IC50 | 7.77 | 7.77 | 17.0 | 1 |
| Vascular endothelial growth factor receptor 2 CHEMBL279 | Kd | 7.16 | 7.16 | 70.0 | 1 |
| Ramos CHEMBL614629 | IC50 | 6.57 | 6.57 | 267.0 | 1 |
Activity Data Samples
Top measurements by pChEMBL value
| Target | Type | Rel. | Value | Units | pChEMBL | Assay | PubMed |
|---|---|---|---|---|---|---|---|
| Tyrosine-protein kinase SYK | IC50 | = | 17.0 | nM | 7.77 | Inhibition of human recombinant spleen tyrosine kinase (360 to 635 amino acid re... | 23151054 |
| Vascular endothelial growth factor receptor 2 | Kd | = | 70.0 | nM | 7.16 | Inhibition of vascular endothelial growth factor receptor 2 | 23151054 |
| Ramos | IC50 | = | 267.0 | nM | 6.57 | Cytotoxicity against human Ramos cells | 23151054 |
Literature References
| PubMed | DOI | Target Context | # Activities |
|---|---|---|---|
| - | 10.6019/CHEMBL5724709 | HEK-293T | 2 |
| - | 10.6019/CHEMBL5724709 | U2OS | 2 |
| - | 10.6019/CHEMBL5724709 | Fibroblast | 2 |
| - | 10.6019/CHEMBL5724796 | Cyclin-dependent kinase 2 | 1 |
| - | 10.6019/CHEMBL5724796 | Bromodomain-containing protein 4 | 1 |
| - | 10.6019/CHEMBL5724796 | Transcription intermediary factor 1-alpha | 1 |
| - | 10.6019/CHEMBL5724796 | Peregrin | 1 |
| - | 10.6019/CHEMBL5724796 | Fibroblast growth factor receptor 2 | 1 |
| - | 10.6019/CHEMBL5724796 | Tyrosine-protein kinase ABL1 | 1 |
| - | 10.6019/CHEMBL5724796 | Aurora kinase A | 1 |
| - | 10.6019/CHEMBL5724796 | Mitogen-activated protein kinase 1 | 1 |
| - | 10.6019/CHEMBL5724796 | Glycogen synthase kinase-3 beta | 1 |
| 23151054 | 10.1021/jm301367c | Vascular endothelial growth factor receptor 2 | 1 |
| - | 10.6019/CHEMBL5724796 | Casein kinase I isoform delta | 1 |
| 23151054 | 10.1021/jm301367c | Tyrosine-protein kinase SYK | 1 |
| 23151054 | 10.1021/jm301367c | Ramos | 1 |
| 23151054 | 10.1021/jm301367c | No relevant target | 1 |
| 23151054 | 10.1021/jm301367c | ADMET | 1 |
Data from ChEMBL 36 via Core Engine