GD20 is a cell-permeable, nucleotide-inactive-state-selective inhibitor of Gαs, with high selectivity over other G protein subfamilies. GD20 inhibits Gαs steady-state GTPase activity with IC50 of 1.15 μM.

(R)-70 is a 5-HT2AR partial agonists with EC50 of 110 nM, and shows 6.4-fold/51-fold selectivity over 5HT2BR/5HT2CR. (R)-70 has substantial brain permeability in mouse pharmacokinetic studies and dose not possess locomotor-stimulating or reinforcing activity.

(R)-69 is a 5-HT2AR partial agonists with EC50 of 41 nM, and shows 4.6-fold/29-fold selectivity over 5HT2BR/5HT2CR. (R)-69 has substantial brain permeability in mouse pharmacokinetic studies and dose not possess locomotor-stimulating or reinforcing activity.

UT-143 is a selective androgen receptor irreversible covalent antagonist and inhibits AR transactivation with IC50 of 150 nM. UT-143 covalently and selectively binds to C406 and C327 in the AF-1 region and inhibits PCa cell proliferation and tumor growth.

CPI-169 R is a novel and potent EZH2 inhibitor with IC50 <1 nM(inhibition of the catalytic activity of PRC2.

PL-SNS-032 conjugate 955 can potently degrade CDK9 in a ubiquitin-proteasome-dependent manner and is much more potent than SNS-032 against various tumor cells in vitro.

PABK (para-azidobenzyloxycarbonyl lysine) is a site-specific small molecule-activated amino acids which could be installed into proteins in the zebrafish embryo and enable fast and tunable activation of the function of several enzymes.

SRX 3305 is a potent, triple BTK/PI3K/BRD4 inhibitor with IC50 of 6.5 nM, 15 nM, and 4 nM toward BTK, PI3Kɑ and PI3Kδ respectively, inhibits BRD4 BD1 and BD2 with IC50 of 77 and 95 nM.SRX3305 showed enhanced binding to the drug-resistant C481S mutant of BTK compared to SRX-3262 (IC50=9 uM and 25 uM, respectively).SRX3305 displayed cytotoxicity aginst MCL cell lines JeKo-1, Mino, Granta with IC50 of 58 nM, 1 nM, 1.1 uM, respectively.SRX3305 inhibited cell vbiability of JeKo-1 BTK C481S and Mino BTK C481S mutant cell lines with IC50 of 1 uM and 47 nM, respectively, with minimally toxic to healthy donor PBMCs.SRX3305 showed improved efficacy in MCL and Ibrutinib-resistant MCL cells, SRX3305 impacted gene expression, perturbs the cell cycle and promotes apoptosis in MCL.

PRL295 is a small molecule Keap1-Nrf2 protein–protein interaction inhibitor.PRL295 binds to Keap1 in the cellular environment, disrupting its interaction with Nrf2, which leads to enhanced gene expression of the classical Nrf2 target NQO1 in cells and in vivo in the mouse liver.PRL-295 increases the thermostability of Keap1 in cell lysates and in live cells.PRL 295 decreased the levels of plasma alanine aminotransferase and aspartate aminotransferase upon acetaminophen-induced hepatic injury.

UHRF1 PHD inhibitor MLD4 is a specific compound that selectively inhibits the UHRF1-histone interaction (IC50=12.4 uM), targets the PHD finger of UHRF1, specifically disrupting histone H3 arginine 2 interactions with the PHD finger.UHRF1 PHD inhibitor MLD4 inhibited binding between H3K9me3(FAM) and UHRF1 with IC50 of 24-26 uM, displace UHRF1-histone H3 binding in cells.

NJH-2-075 is an alkyne-functionalized probe of EN523, retains binding to OTUB1 in vitro.

UHRF1 PHD inhibitor MLD5 is a specific compound that selectively inhibits the UHRF1-histone interaction (IC50=7.4 uM), targets the PHD finger of UHRF1, specifically disrupting histone H3 arginine 2 interactions with the PHD finger.UHRF1 PHD inhibitor MLD5 inhibited binding between H3K9me3(FAM) and UHRF1 with IC50 of 24-26 uM, displace UHRF1-histone H3 binding in cells.

BRD-K56819078 is a small-molecule senolytics and significantly decreases senescent cell burden and mRNA expression of senescence-associated genes in the kidneys of aged mices.

HHS-166 shows dose-dependent inhibition of arsenite-induced stress granule (SG) formation, and liganded G3BP1 Y40 in the NTF2 dimerization domain of this essential nucleating protein for SG regulation.

AHL-030 is a potent and selective EDC3-targeted ligands. AHL-030 is also an stress granules (SGs) enhancer and results in a 2-fold increase in SGs per arsenite-treated cell.

”Compound 53” (University of Texas Southwestern Medical Center) is a stimulator of interferon (IFN) genes (STING) agonist.

“compound 4e” (Chiesi Farmaceutici) is an inhaled p38α/β mitogen-activated protein kinase (MAPK) inhibitor being developed for lung inflammatory diseases.

“Compound 6” (Novartis) is a first-in-class YAP-TEAD protein-protein inhibitor. The TEAD transcription factor and its coactivator YAP and WWTR1/TAZ of the Hippo pathway are responsible for directly regulating the expression of genes involved in cell proliferation and organ size.

Overcoming FGFR mutation resistance and FGFR1-mediated hyperphosphatemia toxicity through isoform-selective FGFR2/3 inhibition. “Compound 29” is an ATP-competitive fibroblast growth factor receptor (FGFR) 2/3 inhibitor with subnanomolar potency.

compound 27, is a potent (13 nM) CNS-penetrant compound that reduces very long chain fatty acid (VLCFA) levels in the CNS, which are believed to be pathological in the rare disease adrenoleukodystrophy (ALD). The starting point came from an HTS on compounds from an internal collection.

“Compound 14d” (Shionogi & Co.) is a highly potent, dose-dependent adenosine monophosphate activated protein kinase (AMPK) activator being investigated for its blood-glucose-lowering effects.

AKB-9778 is a potent, selective inhibitor of vascular endothelial protein tyrosine phosphatase (VE-PTP) with IC50 of 17 pM.