DNL343 is a potent, selective, and brain-penetrant eukaryotic translation initiation factor 2B (eIF2B) activator with ATF4 IC50 of 9.8 nM.

LY3473329 (Muvalaplin) is a potent, multivalent disruptor of lipoprotein(a) (Lp(a)). LY3473329-HCl binds to apolipoprotein KIV8 selectively with a potency of 22 nM and inhibits the formation of Lp(a) particles in vitro with IC50 of 0.09 nM.

NX-5948,be also known as BTK-IN-24,is an oral BTK degrader.

Suzetrigine is a SCN10A blocker. The SCN10A is associated with the onset of pain due to peripheral neuropathy. Suzetrigine functions as an analgesic.

BMS-986172 is a highly Potent MGAT2 Inhibitor that Achieved Targeted Efficacious Exposures at a L BMS-986172 showed on-target- and mechanism-based pharmacology. Moreover, its favorable pharmacokinetic (PK) profile and the lack of species variability in the glucuronidation potential resulted in a greater confidence level in the projection of a low dose for achieving targeted efficacious exposures in humans. Consistent with these projections.

Encaleret, also known as JIT-305, is an oral calcium-sensing receptor (CaSR) antagonist, for the treatment of osteoporosis.

PF-07202954 is a DGAT2 Inhibitor (IC50 = 10 nM) with Longer Predicted Half-Life.

NT-0796 is a Brain-Penetrant and Highly Potent. NLRP3 Inflammasome Inhibitor (IC50 = 0.32 nM) for Neuroinflammatory Disorders.

STM3006 is a highly potent, selective and orally active METTL3 inhibitor. STM3006 can be used for the research of acute myeloid leukaemia (AML).

Zosurabalpin (RG6006) is a class of tethered macrocyclic peptide (MCP) antibiotic. Zosurabalpin (RG6006), effectively treats highly drug-resistant contemporary isolates of CRAB (carbapenem-resistant acinetobacter baumannii) both in vitro and in mouse models of infection, overcoming existing antibiotic resistance mechanisms.

NC-TNP (noncationic thiourea lipids nanoparticles) could compress mRNA by strong hydrogen bonds interaction between thiourea groups of NC-TNP and the phosphate groups of mRNA. NC-TNP could escape the recycling pathway to inhibit the egress of internalized nanoparticles from the intracellular compartment to the extracellular milieu. NC-TNP-encapsulated mRNA shows higher gene transfection efficiency in vitro and in vivo than mRNA-LNP formulation. NC-TNP also shows spleen targeting delivery ability with higher accumulation ratio (spleen/liver), compared with traditional LNP.

TAK-994 is an oral, selective OX2R agonist developed by Takeda for the treatment of narcolepsy type 1 (with cataplexy) and type 2 (without cataplexy). The molecule follows Takeda’s previous clinical molecule, TAK-925 (danavorexton), which was the first OX2R agonist to be tested in people with NT1 but had poor oral bioavailability and was administered intravenously in the clinic.

RAS Inhibitor A122 - This oral tri-complex RAS(MULTI)(ON) inhibitor is a relative from a patent application of the currently undisclosed RMC-6236, which is currently in Phase I/Ib clinical trials for solid tumors. The RAS(MULTI) series was identified via SBDD based on extensive knowledge of RAS tricomplex inhibitors such as G12C tricomplex inhibitor, RMC-6291.

KIO-301 – A photoswitchable HCN channel blocker with positive initial results from a Phase I/II for retinitis pigmentosa and choroideremia study that is being developed by KIORA Therapeutics.

Ebio1 is a potent and subtype-selective activator for the voltage-gated potassium channel KCNQ2 with EC50 of 247.3 nM. Ebio1 engages the KCNQ2 activation by generating an extended channel gate with a larger conductance at the saturating voltage (+50 mV).

PS-13 precursor 19 is the precursor of PS-13. PS13 is a highly potent COX-1 inhibitor (IC50=1 nM) and 1,000 times more selective for COX-1 than COX-2 (7).

PS13 is a highly potent COX-1 inhibitor (IC50=1 nM) and 1,000 times more selective for COX-1 than COX-2 (7). In non-human primates, 11C-PS13 showed selective binding to COX-1 over COX-2 in most major organs including the spleen, gastrointestinal tract, kidneys, and brain.

SK-575 is a Highly Potent and Efficacious Proteolysis-Targeting Chimera Degrader of PARP1 for Treating Cancers. SK-575 potently inhibits the growth of cancer cells bearing BRCA1/2 mutations and induces potent and specific degradation of PARP1 in various human cancer cells even at low picomolar concentrations. SK-575 achieves durable tumor growth inhibition in mice when used as a single agent or in combination with cytotoxic agents, such as temozolomide and cisplatin.

NP3-562 is a potent, orally bioavailable, tricyclic NLRP3 inhibitor with IC50 of 0.26 μM in the FP binding assay. NP3-562 demonstrates excellent potency in human whole blood and full inhibition of IL-1β release in a mouse acute peritonitis model.

TL 13-27 is a negative control for TL 12-186. Demonstrates no kinase degradation in vitro.