Pirmagrel is the selective thromboxane synthetase inhibitor. The compound was well tolerated by all subjects without evidence of any adverse reactions. Serum thromboxane B2 levels (the stable metabolic product of thromboxane A2) were significantly reduced after administration of the compound, with the maximal effect of a 99 per cent reduction occurring at 0.5 and 1 hour after administration. Bleeding times showed a slight increase 2 hours after administration of the compound. Pirmagrel was able to completely prevent the increase in serum thromboxane B2 following allergen challenge in asthmatic patients; while it caused a very small reduction in the early response to allergen, there was no effect on the late response or on airway hyperresponsiveness. Pirmagrel was developed for the treatment of ischemic heart disorders and thrombosis. However, this development was discontinued.

Metazamide is an imidazolone derivative exerting analgesic properties. It affects glucose utilization and activity of glucose-6-phosphate dehydrogenase, isocitrate dehydrogenase and malate dehydrogenase in rat erythrocytes.

XAV-939 was discovered as a selectively inhibitor of Wnt/β-catenin-mediated transcription through tankyrase1/2 inhibition, regulates axin levels and does not affect CRE, NF-κB or TGF-β. Wnt/b-catenin pathway has been implicated in many cancers.

NVP-TNKS656 was identified as an orally active selective tankyrase 2 (TNKS2) inhibitor, which is also antagonist of Wnt pathway activity. On animal models for Colorectal Cancer was shown, that NVP-TNKS656 reduces nuclear β-catenin, reverts such resistance, and represses tumor growth.

PEAQX (NVP-AAM 077) is a potent and orally active NMDA antagonist with a 15-fold preference for human NMDA receptors with the 1A/2A(IC50=270 nM), rather than 1A/2B (29,600 nM). Animals treated with PCP or PEAQX on PN7, PN9, and PN11 showed a sensitized locomotor response to PCP challenge on PN28-PN35. PEAQX induced social suppression in rats.

AAL993 (ZK260253) is a potent and selective VEGF receptor kinase (VEGF-R) tyrosine kinase inhibitor (VEGFR2), which binds to an inactive conformation of the protein. In addition, AAL993 possesses dual functions, including suppression of HIF-1 alpha expression through ERK inhibition without affecting Akt phosphorylation.

AST-487 is an inhibitor of RET (IC50 = 0.88 uM), FLT3 (Ki = 0.52 uM), KDR (IC50 = 0.17 uM), c-Abl (IC50 = 0.02 uM), and c-Kit (IC50 = 0.5 uM). AST-487 has potent and selective antiproliferative effects 7 on primary AML patient cells and cell lines expressing FLT3-ITD or FLT3 kinase domain point mutants. AST-487, which selectively targets mutant FLT3 protein kinase activity, is also shown to override PKC412 resistance in vitro, and has significant antileukemic activity in an in vivo model of FLT3-ITD(+) leukemia. Finally, the combination of NVP-AST487 with standard chemotherapeutic agents leads to enhanced inhibition of proliferation of mutant FLT3-expressing cells. AST-487 displays high selectivity and potency toward FLT3 as a molecular target, and could potentially be used to override drug resistance in AML.

NVP-ADW742 is a novel small weight molecular inhibitor of insulin-like growth factor-1 receptor (IGF-IR), which is investigated for treatment of different types of cancers.

AEW-541 is a pyrrolo[2,3-d]pyrimidine derivative small molecular weight kinase inhibitor of the IGF-IR IGF-1R/InsR with IC50 of 150 nM/140 nM in cell-free assays, greater potency and selectivity for IGF-1R in a cell-based assay. In vivo, this orally bioavailable compound inhibits IGF-IR signaling in tumor xenografts and significantly reduces the growth of IGF-IR-driven fibrosarcomas. AEW-541 represents a class of selective, small molecule IGF-IR kinase inhibitors with proven in vivo antitumor activity and potential therapeutic application.