Fig. 39. Top: Development of IDO1 inhibitors.86,175aHuman whole blood assay. bLog P = Alog P98.44cRat hepatocytes, in vitro unbound clearance. dIn vivo PK study performed in rat. eNot determined. Bottom: Overlay of IDO1-bound structures of 93 (magenta; PDB code: 6WJY) and related aryl-linked bisamide (cyan; PDB code: 6V52) illustrating the utility of BCP as an isostere of a phenyl spacer. Water molecules are shown as spheres; hydrogen bonds are shown as pale blue dashed lines.
