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Synonyms: CGP 57148 | Gleevec® | Glivec® | STI571
imatinib is an approved drug (FDA & EMA (2001))
Compound class: Synthetic organic
Comment: Imatinib is a Type-2 kinase inhibitor. Its main inhibitory activity is against ABL kinase, but it has significant action at secondary targets including platelet-derived growth factor receptor (PDGFR) and stem cell growth factor receptor (KIT).
Coronavirus: imatinib is reported to block Spike protein-induced SARS-CoV and MERS-CoV fusion in vitro , potentially by blocking Abl2 at the endosomal membrane and disrupting the actin dynamics that are required for virus-host fusion . It will be informative to determine if this holds true for SARS-CoV-2, and whether re-purposing of imatinib and/or newer Abl kinase inhibitors (dasatinib, bosutinib, ponatinib, nilotinib) could be a viable strategy against COVID-19. This approach would likely to be most effective during the early stage of infection.
Ligand Activity Visualisation Charts
These 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.✖
View more information in the IUPHAR Pharmacology Education Project: imatinib
|Compound class||Synthetic organic|
|Approved drug?||Yes (FDA & EMA (2001))|
|WHO Essential Medicine||WHO Essential Medicines List (EML) (23rd List, 2023). Access PDF version.
Click to view more information about the WHO Model Lists of Essential Medicines.
|International Nonproprietary Names|
|CGP 57148 | Gleevec® | Glivec® | STI571|
|Reactome Reaction||R-HSA-9669854, R-HSA-9674430, R-HSA-9674095, R-HSA-9669900, R-HSA-9669859, R-HSA-9674397|
|CAS Registry No.||152459-95-5|
|GtoPdb PubChem SID||178102314|
|RCSB PDB Ligand||STI|
|Search Google for chemical match using the InChIKey||KTUFNOKKBVMGRW-UHFFFAOYSA-N|
|Search Google for chemicals with the same backbone||KTUFNOKKBVMGRW|
|Search PubMed clinical trials||imatinib|
|Search PubMed titles||imatinib|
|Search PubMed titles/abstracts||imatinib|
|SynPHARM||78741 (in complex with ABL proto-oncogene 1, non-receptor tyrosine kinase)|
|UniChem Compound Search for chemical match using the InChIKey||KTUFNOKKBVMGRW-UHFFFAOYSA-N|
|UniChem Connectivity Search for chemical match using the InChIKey||KTUFNOKKBVMGRW-UHFFFAOYSA-N|