Screening chelating inhibitors of HIF-prolyl hydroxylase domain 2 (PHD2) and factor inhibiting HIF (FIH)

► Bidentate chelators were screened as inhibitors of FIH and PHD2. ► EPR of (CuII)-substituted enzymes showed active-site binding of chelators. ► Hydroxypyrones and catechols were moderately selective inhibitors.