Zhao, Jichen published the artcileHighly Selective MERTK Inhibitors Achieved by a Single Methyl Group, HPLC of Formula: 1375301-91-9, the publication is Journal of Medicinal Chemistry (2018), 61(22), 10242-10254, database is CAplus and MEDLINE.
Although all kinases share the same ATP binding pocket, subtle differences in the residues that form the pocket differentiate individual kinases’ affinity for ATP competitive inhibitors. The authors have found that by introducing a single Me group, the selectivity of the MERTK inhibitors over another target, FLT3, was increased up to 1000-fold (compound I). Compound II was identified as an in vivo tool compound with subnanomolar activity against MERTK and 38-fold selectivity over FLT3 in vitro. The potency and selectivity of II for MERTK over FLT3 were confirmed in cell-based assays using human cancer cell lines. Compound II had favorable pharmacokinetic properties in mice. Phosphorylation of MERTK was decreased by 75% in bone marrow leukemia cells from mice treated with II compared to vehicle-treated mice.
Journal of Medicinal Chemistry published new progress about 1375301-91-9. 1375301-91-9 belongs to pyrimidines, auxiliary class Pyrimidine,Boronic acid and ester,Boronate Esters,Boronic acid and ester, name is 2-Cyclopropyl-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)pyrimidine, and the molecular formula is C5H6N2O2, HPLC of Formula: 1375301-91-9.
Referemce:
https://pubchem.ncbi.nlm.nih.gov/compound/Pyrimidine,
Pyrimidine – Wikipedia