References: |
GSK3179106 (GSK-3179106, GSK 3179106) is a potent, selective, first-in-class and gut-restricted with IC50 of 0.4 and 11 nM in the biochemical assay and cellular assay respectively, 273-fold selectivity over KDR; possesses good kinase selectivity, only 26 out of a set of >300 recombinant kinases were found to be inhibited at 1 uM; GSK3179106 dosed orally at 10 mg/kg for 3.5 days BID reduced the visceromotor response to colorectal distension in comparison to rats given an acetic acid enema and dosed with
vehicle, GSK3179106 has been developed for the treatment of IBS in a clinical setting. |