Thiophene-Pyrazolourea Derivatives as Potent, Orally Bioavailable, and Isoform-Selective JNK3 Inhibitors
Yangbo Feng, HaJeung Park, Luke A. Bauer, Jae Cheon Ryu, Sung Ok Yoon
Abstract
in human JNK3 were solved at 1.84 Å, which showed that these JNK3 isoform selective inhibitors bound to the ATP pocket, had interactions in both hydrophobic pocket-I and hydrophobic pocket-II.
Topics & Concepts
BioavailabilityChemistryPharmacologyIn vivoMicrosomePharmacokineticsGene isoformEnzymeKinaseBiochemistryIC50Lead compoundIn vitroBiologyGeneBiotechnologyMelanoma and MAPK PathwaysCytokine Signaling Pathways and InteractionsProtein Tyrosine Phosphatases