||ABBV-744 is a BDII-selective BET bromodomain inhibitor that is being investigated to treat AML and metastic castration-resistant prostate cancer.
||IACS-010759 or IACS-10759 is a potent and selective Oxidative Phosphorylation Inhibitor (IC50 < 10 nM) with potential antineoplastic activity.
||ARS-1620 is a prodrug designed from ARS-853, which is a potent and selective S-IIP G12C inhibitor.
||ARS-1323 is a novel inhibitor of mutant K-ras G12C extracted from patent WO 2015054572 A1. IC50 & Target: K-Ras G12C
||ARS-1630 is the R-conformational atropisomer of ARS-1620, 1,000-fold less potent than ARS-1620 (1.2 ± 0.6 M-1s-1) and thus acts as a unique inactive control compound.
||Derazantinib, also known as ARQ-087, is an orally bioavailable inhibitor of the fibroblast growth factor receptor (FGFR) with potential antineoplastic activity.
||BGB-324; Bemcentinib; R428
||BGB-324, also known as R428 or Bemcentinib, is a selective small molecule inhibitor of Axl kinase, which showed activity to blocks tumor spread and prolongs survival in models of metastatic breast cancer.
||Ciforadenant; CPI-444; V81444
||CPI-444 is a potent and selective inhibitor of A2A receptor (A2AR) induces antitumor responses.
||E7046 is an orally bioavailable and specific EP4 antagonist, with IC50 of 13.5 nM and Ki of 23.14 nM, exhibiting anti-tumor activities.
||ND-630 is an acetyl-CoA carboxylase (ACC) inhibitor; inhibits human ACC1 and ACC2 with IC50 values of 2.1 and 6.1 nM, respectively.
||ND-646 is an orally bioavailable and steric inhibitor of acetyl-CoA carboxylase (ACC) with IC50s of 3.5 nM and 4.1 nM for recombinant hACC1 and hACC2, respectively.
||BLU-554 is a fibroblast growth factor receptor 4 (FGFR4) inhibitor potentially for the treatment of hepatocellular carcinoma and cholangiocarcinoma.
||IPI549 is a potent and selective PI3Kγ Inhibitor with an IC50 of 16 nM.
||EED226 is a potent, selective, and orally bioavailable embryonic ectoderm development (EED) inhibitor with an IC50 of 22 nM.
||GLPG0187 is a broad spectrum integrin receptor antagonist with antitumor activity; inhibits αvβ1-integrin with an IC50 of 1.3 nM.
||H3B-6527 (H3 Biomedicine) is a highly selective FGFR4 inhibitor with potent antitumour activity in FGF19 amplified cell lines and mice.
||FGF-401 is an inhibitor of FGFR4 extracted from patent WO2015059668A1, compound example 83; has an IC50 of 1.9 nM.
||EED inhibitor-1 is an EED inhibitor extracted from patent US20160176882 A1, compound example 2; has IC50s of 59, 89, 26 nM in EED Alphascreen binding, LC-MS and ELISA assay.
||BLU-285 is a potent and selective exon 17 mutant KIT kinase inhibitor with IC50 of 0.27 nM for KIT D816V.
||Evofosfamide, also known as TH-302, is a hypoxia-activated prodrug consisting of a 2-nitroimidazole phosphoramidate conjugate with potential antineoplastic activity.
||GDC-0326 is a potent and selective inhibitor of α-Isoform of Phosphoinositide 3-Kinase (PI3Kalpha inhibitor). GDC-0326 achieves a very high level of selectivity over other kinases. GDC-0326 has low plasma CL in human.
||OTS964 is an inhibitor of lymphokine-activated killer T cell-originated protein kinase (TOPK; IC50 = 28 nM). It specifically blocks cytokinesis, leading to apoptosis, in a broad range of cancer cells. OTS964 induces apoptosis of human lung cancer cells in mouse xenografts.
||GSK461364 dose-dependently halts cell cycling in diverse proliferating cancer cell lines and, at higher doses, triggers apoptosis. It appears to be more effective against p53-deficient tumors and is able to cross the blood-brain barrier. GSK461364 is effective in vivo, inducing tumor growth inhibition or growth delay in xenograft models in mice.