1644248-18-9

BMS-911172 is a potent and brain-penetrant, AP2-associated protein kinase 1 (AAK1)-selective inhibitor (IC50 = 12 and 51 nM in enzymes and cells, respectively). BMS-911172 was active in the formalin assay in the Chung mouse model (60 mg/kg s.c.) as well as in the chronic constriction injury-induced thermal hyperalgesia and mechanical allodynia rat model (60 mg/kg). PD marker assay in mice showed a dose-dependent inhibition of phosphorylation of AAK1 substrate mu-2 in the brain. There were no motor side effects at the doses tested. BMS-911172 may be useful for the treatment of neuropathic pain

BMS-911172 is an adaptor associated kinase 1 (AAK1 kinase) inhibitor (IC50 = 35 nM).

[1] Hartz RA, et al. Aryl amide kinase inhibitors. WO2015006100A1.