Pyr01 is a targeted activator of cell kill (TACK) and shows more than 300-fold more potent than doravirine and also retains reverse transcriptase (RT) inhibition activity within about 3-fold of doravirine.

RLY-2608 is an oral allosteric pan-mutant isoform-selective PI3K伪 inhibitor that was discovered using MD modeling and cryo-EM to identify allosteric networks and opportunities for small molecules, followed by DEL screening.

FN1-8 is a novel, synthetic small molecule that efficiently interferes with Gli/TAF9 interaction and downregulate Gli/TAF9-dependent transcriptional activity (at 15 uM); inhibits non-canonical Gli activation and acts downstream of the canonical Hh pathway; suppresses cancer cell proliferation in vitro and inhibits tumor growth in vivo.

TNG260 is a CoREST-selective deacetylase inhibitor and shows 500-fold selectivity for the CoREST complex over the other HDAC1-containing complexes, NuRD and Sin3.

RMC-6291 is a potent covalent inhibitor of KRASG12C(ON) that forms a tri-complex within tumor cells between KRASG12C(ON) and cyclophilin A (CypA). RMC-6291 overcomes limitations of first-generation KRASG12C(OFF) inhibitors in preclinical models by directly targeting the active form of this important oncogenic driver.

LNP023 is a highly potent factor B (FB) inhibitor with an IC50 value of 10 nM. LNP023 shows direct, reversible, and high-affinity binding to human FB (KD=7.9 nM).