||BI-167107 is a β-Arrestin-Biased D2R Agonist. Targeting the D2R mediated activation of β-arrestin-2 might therefore be a valuable approach for the design of novel antiparkinsonian drugs.
||SB-204990 is the prodrug of the potent ATP citrate-lyase inhibitor SB-201076. SB-204990, when administered orally to rats, was absorbed into the systemic circulation, pharmacologically relevant concentrations of SB-201076 were recovered in the liver. SB-204990 (25 mg/kg per day) also decreased plasma cholesterol levels (by up to 23%) and triglyceride levels (by up to 38%) in the dog, preferentially decreasing low-density lipoprotein compared with high-density lipoprotein cholesterol levels. SB-204990 is an important enzyme in controlling substrate supply for lipid synthesis de novo and a potential enzyme target for hypolipidaemic intervention.
||BAY-545 is a potent and selective antagonist of the A2B adenosine receptor
||NTN21277, also known as Gefitinib-based PROTAC 3 is a VHL-recruiting PROTAC that induces the degradation of EGFR and EGFR mutants with DC50 of 11.7 nM and 22.3 nM for HCC827 cell (Exon 19 del) and H3255 cell (L858R).
||AZD-3409 is a potent prenyl transferase inhibitor. AZD-3409 showed higher potency than lonafarnib. The mean IC(50) for cytotoxicity of AZD3409 was 510 in MEF cells, 10,600 in A549 cells and 6,170 in MCF7 cells, respectively. In these cells, the IC(50) for FTase activity of AZD3409 ranged from 3.0 to 14.2 nM and of lonafarnib from 0.26 to 31.3 nM. AZD3409 inhibits farnesylation to a higher extent than geranylgeranylation. Both inhibition of farnesylation and geranylgeranylation could not be correlated to the antiproliferative activity of the drug. AZD3409 might be active in gefitinib-resistant breast carcinoma.
||EW-7197 Hydrochloride is a highly potent, selective, and orally bioavailable inhibitor of TGF-β type 1 receptor kinase.
||GSK3532795, also known as BMS-955176, is a potent, orally active, second-generation HIV-1 maturation inhibitor (MI) that advanced through phase IIb clinical trials. GSK3532795 combines broad coverage of polymorphic viruses (EC50 <15 nM toward a panel of common polymorphisms representative of 96.5% HIV-1 subtype B virus) with a favorable pharmacokinetic profile in preclinical species.
||TAS-120 is an orally bioavailable inhibitor of the fibroblast growth factor receptor (FGFR) with potential antineoplastic activity. FGFR inhibitor TAS-120 selectively and irreversibly binds to and inhibits FGFR, which may result in the inhibition of both the FGFR-mediated signal transduction pathway and tumor cell proliferation, and increased cell death in FGFR-overexpressing tumor cells. FGFR is a receptor tyrosine kinase essential to tumor cell proliferation, differentiation and survival and its expression is upregulated in many tumor cell types.
||SB-423562 is a calcium-sensing receptor antagonist potentially for the treatment of autosomal dominant hypocalcemia
||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.