Ontology highlight
ABSTRACT:
SUBMITTER: Feng Y
PROVIDER: S-EPMC7812606 | biostudies-literature | 2021 Jan
REPOSITORIES: biostudies-literature
ACS medicinal chemistry letters 20201213 1
Potent JNK3 isoform selective inhibitors were developed from a thiophenyl-pyrazolourea scaffold. Through structure activity relationship (SAR) studies utilizing enzymatic and cell-based assays, and in vitro and in vivo drug metabolism and pharmacokinetic (DMPK) studies, potent and highly selective JNK3 inhibitors with oral bioavailability and brain penetrant capability were developed. Inhibitor <b>17</b> was a potent and isoform selective JNK3 inhibitor (IC<sub>50</sub> = 35 nM), had significant ...[more]