VVD-214 (RO7589831) is a synthetic lethal allosteric inhibitor of WRN helicase. VD-214 covalently engages cysteine 727 of WRN in a nucleotide cooperative manner and inhibits ATP hydrolysis and helicase activity, resulting in widespread double-stranded DNA breaks, nuclear swelling, and cell death in MSI-high, but not microsatellite stable cells.

ABBV-303 is a novel c-Met targeted multispecific NK cell engager. ABBV-303 binding to NKG2D and CD16a results in redirection of both innate (NK cells) and adaptive (CD8+ T cells) immune cells to lyse c-Met expressing tumor cells.

A-1155463 is a highly potent and selective BCL-XL inhibitor.

LUNA18 is an 11-mer cyclic peptide inhibitor for the intracellular tough target RAS with Kd (KRAS/G12D) of 0.043 nM and cellular IC50 of 1.4 nM (AsPC-1). LUNA18 orally and dose-dependently exhibits potent anti-cancer activities in a mouse xenograft model. LUNA18 shows 21–47% oral bioavailability in animals such as mouse, rat, monkey, and dog and notably does not require special formulations.

Selective serotonin reuptake inhibitor

5-HT2 receptor agonist, inhibiting TNF-α-mediated proinflammatory signaling cascades and inflammation via 5-HT2A receptor activation and preventing the development of, and inflammation associated with, acute allergic asthma

Novel Covalent Inhibitor of Ca -Bound S100B

Promising therapeutic tool for AMPH-induced addiction, reducing the oxidative stress, attenuating evoked (MA and heat HA) and spontaneous pain (FST) phenotypes, and all phases of morphine-induced behavioral locomotor sensitization in mice

Estrogen receptor α (ERα) ligand as potent antiestrogen; Metabolite of tamoxifen

Novel anti-thrombosis agent, orally inhibiting venous thrombosis and arterial thrombosis in vivo, showing no bleeding risk

Novel lysophosphatidic acid receptor 3 (LPA3) agonist

Orphan nuclear receptor DAF-12 ligand, inhibiting the dauer-promoting activity of DAF-12

Novel water-sensitive probe, demonstrating superior sensitivity for detecting modulation of water microsolvation, structural conformation during oligomer formation and 5FUrd binding to both wild type and mutant SOD1

Building Block

Negative control for RSL3

Potent antagonist of GluN2B-NMDA receptors (Ki = 5.8 nM), inhibiting ion flux in two-electrode voltage clamp experiments (IC50 = 223 nM)

Novel prodrug of the sigma (σ) ligand haloperidol metabolite II conjugated with the histone deacetylase (HDAC) inhibitor valproic acid, demonstrating antiangiogenic activity

Novel profluorescent RAMOSUS3 (RMS3) probe with strigolactone-like bioactivity

Potent and selective 5-HT2 serotonin receptor agonist

Inhibitor of ADP-induced platelet aggregation; anti-thrombotic

Novel potassium channel opener

Novel angiogenesis inhibitor, regulating endothelial cell fate and angiogenesis

Novel probe for mycobacterial and fungal carbonic anhydrase

Catecholamine-depleting agent, actively against the 3 major monoamines in the CNS

Novel potent anti-malarial agent against multiple resistant strains of P. falciparum in vitro and show no cytotoxicity to mammalian cells

Folate-PEG2-amine is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.

Folate-PEG3-amine is a cleavable 3 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs).

A potent and selective Adenosine receptor A2A agonist

Seletalisib (UCB5857) is potent and selective PI3Kδ inhibitor with an IC50 of 12 nM.

A highly potent, selective and orally bioavailable trace amine-associated receptor 1 (TRRA1) full agonist with EC50 of 18 nM, >500-fold selectivity over human adrenergic α2A receptor.