Ontology highlight
ABSTRACT:
SUBMITTER: Tan L
PROVIDER: S-EPMC4292808 | biostudies-literature | 2015 Jan
REPOSITORIES: biostudies-literature
Journal of medicinal chemistry 20140730 1
We developed a pharmacophore model for type II inhibitors that was used to guide the construction of a library of kinase inhibitors. Kinome-wide selectivity profiling of the library resulted in the identification of a series of 4-substituted 1H-pyrrolo[2,3-b]pyridines that exhibited potent inhibitory activity against two mitogen-activated protein kinases (MAPKs), TAK1 (MAP3K7) and MAP4K2, as well as pharmacologically well interrogated kinases such as p38α (MAPK14) and ABL. Further investigation ...[more]