AGI5198 1355326-35-0 AGI-5198 is the first highly potent and selective inhibitor of IDH1 R132H/R132C mutants with IC50 of 0.07 μM/0.16 μM.

ABT-199 1257044-40-8 ABT-199 is a Bcl-2-selective inhibitor with Ki of 0.01 nM in cell-free assays, 4800-fold more selective versus Bcl-xL and Bcl-w, and no activity to Mcl-1. Phase 3.

TAE-226 761437-28-9 TAE226 (NVP-TAE226) is a potent FAK inhibitor with IC50 of 5.5 nM and modestly potent to Pyk2, ~10- to 100-fold less potent against InsR, IGF-1R, ALK, and c-Met.

LY2157299 700874-72-2 LY2157299 is a potent TGFβ receptor I (TβRI) inhibitor with IC50 of 56 nM. Phase 2.

WZ811 55778-02-4 WZ811 is a novel small molecular and potency CXCR4 antagonist with EC50 of 0.3 nM.

RG108 48208-26-0 RG108 is an inhibitor of DNA methyltransferase with IC50 of 115 nM, does not cause trapping of covalent enzymes.

Ki-16425 355025-24-0 Ki-16425 is a competitive, potent and reversible antagonist to LPA1, LPA2 and LPA3 with Ki of 0.34 μM, 6.5 μM and 0.93 μM, respectively, shows no activity at LPA4, LPA5, LPA6.

TSU-68 252916-29-3 TSU-68 has greatest potency against PDGFR autophosphorylation with Ki of 8 nM, but also strongly inhibits Flk-1 and FGFR1 trans-phosphorylation