Talabostat mesilate(PT-100; Val-boroPro) is an orally active, specific inhibitor of dipeptidyl peptidases(IC50=1 nM for DPP4), including tumor-associated fibroblast activation protein.

TP-0903 is a a high-affinity Axl inhibitor with IC50 of 27 nM.

Voxtalisib (SAR245409, XL765) is a dual inhibitor of mTOR/PI3K, mostly for p110γ with IC50 of 9 nM; also inhibits DNA-PK and mTOR.

ZSTK474 is a potent pan-class I PI3K inhibitor with IC50 of 37 nM.

Theliatinib (HMPL-309) is a novel small molecule, EGFR tyrosine kinase inhibitor with potential antineoplastic and anti-angiogenesis activities.

GLPG0187 is a small molecule integrin receptor antagonist (IRA) with potential antineoplastic activity.

TAS-120 is a highly potent and selective irreversible FGFR inhibitor, effective in tumors harboring various FGFR gene abnormalities.

BIBX 1382 is a potent, selective inhibitor of EGFR tyrosine kinase (IC50 = 3 nM); displays > 1000-fold lower potency against ErbB2 (IC50 = 3.4 μM) and a range of other related tyrosine kinases (IC50 > 10 μM).

RO4987655(CH-4987655) is an orally active small molecule, targeting mitogen-activated protein kinase kinase 1 (MAP2K1/MEK1 IC50=5.2 nM), with potential antineoplastic activity.