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.
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