Synonyms: ASP-2215 | ASP2215 | Xospata®
gilteritinib is an approved drug (FDA (2018), EMA (2019))
Compound class:
Synthetic organic
Comment: Gilteritinib is an orally bioavailable inhibitor of the receptor tyrosine kinases (RTKs) FMS-related tyrosine kinase 3 (FLT3), AXL and anaplastic lymphoma kinase (ALK) [4], with clinical antineoplastic activity. Gilteritinib inhibits the activity of FLT3-activating mutations which are one of the most common genetic alterations in acute myeloid leukemia (AML).
SARS-CoV-2: AXL is a kinase upstream of p38 MAP kinases. p38 activity has been reported to be upregulated following SARS-CoV-2 infection of host cells in vitro, and gilteritinib produces an antiviral effect (IC50= 807 nM) [1]. Ligand Activity Visualisation ChartsThese are box plot that provide a unique visualisation, summarising all the activity data for a ligand taken from ChEMBL and GtoPdb across multiple targets and species. Click on a plot to see the median, interquartile range, low and high data points. A value of zero indicates that no data are available. A separate chart is created for each target, and where possible the algorithm tries to merge ChEMBL and GtoPdb targets by matching them on name and UniProt accession, for each available species. However, please note that inconsistency in naming of targets may lead to data for the same target being reported across multiple charts. ✖ |
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Classification | |
Compound class | Synthetic organic |
Approved drug? | Yes (FDA (2018), EMA (2019)) |
IUPAC Name |
6-ethyl-3-[3-methoxy-4-[4-(4-methylpiperazin-1-yl)piperidin-1-yl]anilino]-5-(oxan-4-ylamino)pyrazine-2-carboxamide |
International Nonproprietary Names | |
INN number | INN |
10048 | gilteritinib |
Synonyms |
ASP-2215 | ASP2215 | Xospata® |
Database Links | |
Specialist databases | |
Reactome Drug | R-ALL-9695700 |
Reactome Reaction | R-HSA-9702508, R-HSA-9695828, R-HSA-9702589 |
Other databases | |
CAS Registry No. | 1254053-43-4 (source: PubChem) |
ChEMBL Ligand | CHEMBL3301622 |
DrugCentral Ligand | 5306 |
GtoPdb PubChem SID | 252827366 |
PubChem CID | 49803313 |
RCSB PDB Ligand | C6F |
Search Google for chemical match using the InChIKey | GYQYAJJFPNQOOW-UHFFFAOYSA-N |
Search Google for chemicals with the same backbone | GYQYAJJFPNQOOW |
Search PubMed clinical trials | gilteritinib |
Search PubMed titles | gilteritinib |
Search PubMed titles/abstracts | gilteritinib |
UniChem Compound Search for chemical match using the InChIKey | GYQYAJJFPNQOOW-UHFFFAOYSA-N |
UniChem Connectivity Search for chemical match using the InChIKey | GYQYAJJFPNQOOW-UHFFFAOYSA-N |