pralsetinib
Ligand Summary
Pralsetinib is a kinase inhibitor of wild-type RET and oncogenic RET fusions (CCDC6-RET) and mutations (RET V804L, RET V804M and RET M918T) with half maximal inhibitory concentrations (IC50s) less than 0.5 nM. In purified enzyme assays, pralsetinib inhibited DDR1, TRKC, FLT3, JAK1-2, TRKA, VEGFR2, PDGFRb, and FGFR1 at higher concentrations that were still clinically achievable at Cmax. In cellular assays, pralsetinib inhibited RET at approximately 14-, 40-, and 12-fold lower concentrations than VEGFR2, FGFR2, and JAK2, respectively.
UNII: 1WPE73O1WV
PubChem: 129073603
Guide to Pharmacology: 10033
ChEMBL: CHEMBL4582651
DrugCentral: 5412
LyCHI: 3VU8UASRKXFR
Target Activities
4 Activities
Items per page:
10
1 – 4 of 4
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
---|---|---|---|---|---|---|
IC50 | ||||||
IC50 | ||||||
IC50 | INHIBITOR | |||||
IC50 | INHIBITOR | |||||