OSU-03012 is a potent inhibitor of recombinant PDK-1 with IC50 of 5 μM and 2-fold increase in potency over OSU-02067.

BX795 is a potent and selective dual inhibitor of TBK1/PDK1 with IC50s of 2 nM/6 nM respectively, also inhibit Aurora B and IκB kinase ε (IKKε).

BX-912 is a selective inhibitor of 3-Phosphoinositide-dependent Kinase-1 (PDK1) with IC50 of 12 nM, showing > 10 fold selectivity over PKA, PKC, C-Kit, EGFR etc.

PHT-427 is dual inhibitor of Akt and PDPK1 with Ki of 2.7 μM and 5.2 μM, respectively, targeting PH domains of Akt and PDPK1.

GSK2334470 is a PDK1 inhibitor with IC50 of ~10 nM, with no activity at other close related AGC-kinases.