||GSK547 is a highly selective and potent inhibitor of RIP1 kinase that targets RIP1 in vivo
||OSI-027 is an orally bioavailable mammalian target of rapamycin (mTOR) kinase inhibitor with potential antineoplastic activity. mTOR kinase inhibitor OSI-027 binds to and inhibits both the raptor-mTOR (TOR complex 1 or TORC1) and the rictor-mTOR (TOR complex 2 or TORC2) complexes of mTOR, which may result in tumor cell apoptosis and a decrease in tumor cell proliferation. mTOR is a serine/threonine kinase that is upregulated in some tumors and plays an important role downstream in the PI3K/Akt/mTOR signaling pathway. Check for active clinical trials or closed clinical trials using this agent. (NCI Thesaurus).
||BAY-293 is a potent SOS1 inhibitor that blocks RAS activation via disruption of the RAS-SOS1 interaction. BAY-293) selectively inhibits the KRAS-SOS1 interaction with an IC50 of 21 nM and is a valuable chemical probe for future investigations.
||AMG-510 is a potent KRAS G12C covalent inhibitor. AMG-510 selectively targets the KRAS p.G12C mutant, at either the DNA, RNA or protein level, and prevents, through an as of yet not elucidated manner, expression of and/or tumor cell signaling through the KRAS p.G12C mutant. This may inhibit growth in KRAS p.G12C-expressing tumor cells
|| BI-3812 is a potent inhibitor of the interaction of the BTB/POZ domain of BCL6 with several co-repressors. It acts by inhibiting the BCL6::Co-repressor complex formation.
||Selpercatinib is a tyrosine kinase inhibitor with antineoplastic properties
||Olutasidenib is a potent, selective inhibitor of mutant Isocitrate dehydrogenase (IDH)1 for the treatment of acute myeloid leukemia
||MB-07811, also known as MB-07344, is a thyroid hormone receptor beta (TRB) agonist potentially for the treatment of hyperlipidemia. The prodrug [MB07811] of a novel phosphonate-containing thyroid hormone receptor agonist [MB07344] is the first application of the HepDirect liver-targeting approach to a non-nucleotide agent.
||R-268712 is a specific inhibitor of activin receptor-like kinase 5 (ALK5). It is also an orally active transforming growth factor-β type I receptor inhibitor.
||AZD7507 is a potent and selective CSF-1R inhibitor (32 nM cell activity), AZD7507 is considered a promising compound as it retained the desired potency and oral pharmacokinetic properties of AZ683. Moreover, in a telemetry study in dogs given a single oral dose, there was no cardiovascular toxicity, no elevation of troponin related to the treatment, and no alteration in the ECG.
||GDC-0077 is an orally available PI3K inhibitor with potential antineoplastic activity.
||BI1744 is a long acting β2-adrenoceptor agonist with an EC50 of 1.4±0.08 nM.
||Parathyroid hormone (PTH) is essential for calcium homeostasis and its action is mediated by the PTH type 1 receptor (PTHR1), a class B G-protein-coupled receptor. Hypoparathyroidism and osteoporosis can be treated with PTH injections; however, no orally effective PTH analogue is available.
||Baloxavir is an anti-influenza agent extracted from patent WO 2017104691 A1.
||BLU-667 is a potent and selective inhibitor of RET mutations, fusions, and predicted resistant mutants. RET fusions are key drivers of multiple cancers, including lung and thyroid cancer, and our research suggests that RET also plays a key role in some colon and breast cancers. By simultaneously targeting the primary driver and predicted resistant mutants that render cancer cells insensitive to treatment with currently approved drugs,
||Mirogabalin, also known as DS-5565, is an α2δ-1 ligand being developed for pain associated with diabetic peripheral neuropathy, fibromyalgia, and postherpetic neuralgia. It has shown promising results in Phase II clinical trials for the treatment of diabetic peripheral neuropathic pain.
||Resmetirom, or MGL-3196, shows outstanding safety in a rat heart model and is efficacious in a preclinical model at doses that showed no impact on the central thyroid axis.
||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.
||Ertugliflozin, also known as also known as PF-04971729, is a potent and selective inhibitor of the sodium-dependent glucose cotransporter 2 and clinical candidate for the treatment of type 2 diabetes mellitus.