SMAP (DT-061, DT061) is an orally bioavailable small molecule activator of PP2A, inhibits KRAS-driven tumor growth.

An irreversible, dual EGFR/HER2 inhibitor with IC50 of 0.5/0.4/10/14 nM for wt EGFR/EGFR L858R/EGFR L858R+T790M/HER2 respectively.

A potent, selective inhibitor of phosphodiesterases PDE4 with IC50 of 3 nM, 130 nM and 240 nM for PDE4A, PDE4B, and PDE4D, respectively.

WZ8040 is a potent, mutant-selective, irreversible EGFRT790M inhibitor, does not inhibit ERBB2 phosphorylation (T798I) and is 100-fold less potent against wild-type EGFR.

A non-peptide, centrally-penetrant and selective agonist of GHSR with appetite-enhancing and anabolic effects.

An aminoglycoside antibiotic similar in structure to gentamicin B1.

BMS-599626 (AC480) is a selective and efficacious inhibitor of HER1 and HER2 with IC50 of 20 nM and 30 nM, respectively.

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.