Canagliflozin is a highly potent and selective SGLT2 inhibitor for CHO-hSGLT2, CHO-rSGLT2 and CHO-mSGLT2 with IC50 of 4.4 nM, 3.7 nM and 2 nM, respectively.

AS-252424 is a novel, potent and selective inhibitor of PI3Kγ with IC50 of 33 nM.

XL388 is a Novel Class of Highly Potent, Selective, ATP-Competitive, and Orally Bioavailable Inhibitors of the Mammalian Target of Rapamycin (mTOR).

NVP-BGT226 is a novel dual PI3K/mTOR inhibitor with IC50 of 1 nM.

Dasatinib is an orally bioavailable synthetic small molecule-inhibitor of SRC-family protein-tyrosine kinases.

Sunitinib Malate (Sutent, SU11248) is a multi-targeted RTK inhibitor targeting VEGFR2 (Flk-1) and PDGFRβ with IC50 of 80 nM and 2 nM, and also inhibits c-Kit.

Atazanavir is a HIV protease inhibitor with Ki of 2.66 nM.

FTY720 (Fingolimod, Gilenya) is a S1P antagonist with IC50 of 0.033 nM.

Cediranib (AZD2171) is a highly potent VEGFR2 inhibitor with IC50 of 0.5 nM, also inhibits Flt1/4 with IC50 of 5 nM/≤3 nM.

SB269970 is a potent and selective 5-HT7 receptor antagonist.

Sitaxentan sodium (TBC-11251) is a selective endothelin receptor-A antagonist with IC50 and Ki of 1.4 nM and 0.43 nM, respectively.

VX-745 is a potent and selective inhibitor of p38α MAPK and p38β MAPK with IC50 of 10 nM and 220 nM, respectively.

NVP-AEW541 is a potent inhibitor of IGF-1R with IC50 of 86 nM.

BMS-911543 is a potent and selective inhibitor of JAK2 with IC50 of 1.1 nM, approximately 350-, 75- and 65-fold selective to JAK1, JAK3 and TYK2, respectively.

HSP990 is an orally bioavailable inhibitor of human heat-shock protein 90 (Hsp90) with potential antineoplastic activity.

Methazolastone (Temozolomide, Temodar, Temodal) is a DNA damage inducer.

Docetaxel, an analog of taxol, is an inhibitor of depolymerisation of microtubules through binding to stabilized microtubules.

Bleomycin sulfate (Blenoxane) is a glycopeptide antibiotic and an anticancer agent for squamous cell carcinomas (SCC) with IC50 of 4 nM in UT-SCC-19A cells.

Dactinomycin (also known generically as Actinomycin D ) is the most significant member of actinomycines, which are a class of polypeptide antibiotics isolated from soil bacteria of the genus Streptomyces.

Fosaprepitant (MK-0517, L-758,298) is a water-soluble phosphoryl prodrug for Aprepitant which is a NK1 antagonist.

Vismodegib (formerly GDC-0449) is a hedgehog antagonist, is also an orally bioavailable small molecule with potential antineoplastic activity.

TW-37 is a novel nonpeptide inhibitor to recombinant Bcl-2, Bcl-xL and Mcl-1 with Ki of 0.29 μM, 1.11 μM and 0.26 μM, respectively.