PHD-1-IN-1 is an orally active and potent HIF prolylhydroxylase domain-1 (PHD-1) inhibitor with an IC50 of 0.034 μM. PHD-1-IN-1 has a unique monodentate binding interaction with the active site Fe2+ ion and induces the formation of an “Arg367-out” pocket.IC50 & Target: IC50: 0.034 μM (PHD-1)In Vivo: PHD-1-IN-1 (compound 17; 3 mg/kg of p.o. or 0.5 mg/kg of i.v.) has a Cmax of 0.8 μM, a AUC of 176 ng?h/mL, Kp,uu of 1.11 and B/P of 0.95.