| DC72983 |
ZINC20451377
Featured
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ZINC20451377 is a small molecule that binds to hepatitis B surface antigen (HBsAg) with high affinity (Kd=65.3 nM), reduces HBsAg levels and HBV virion secretion in cell culture model for HBV. |
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| DC72995 |
ING-1466
Featured
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ING-1466 is an orally active entry inhibitor of influenza A viruses (IAVs) with EC50 of 0.18 uM against IAV H1N1 (PR8-NS1-Gluc), binds to hemagglutinin (HA) and blocks HA-mediated viral infection. |
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| DC72999 |
CK-2-63
Featured
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CK-2-63 is a potent first-in-class M. tuberculosis cytochrome bd (cyt bd) inhibitor, demonstrates growth suppression of M. tuberculosis H37Rv with IC50 of 3.7 uM. |
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| DC73064 |
NACE2i
Featured
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NACE2i is a cell permeable, specific and selective peptide inhibitor of nuclear ACE2, inhibits binding between IMP1α and ACE2 and SARS-CoV-2 viral replication.
NACE2i specifically targets nuclear ACE2 and not other nuclear proteins targeted by the importin pathway.
NACE2i has no impact on ACE2 enzymatic activity.
NACE2i prevents inflammation and macrophage infiltration, and increases NK cell infiltration in bronchioles.
NACE2i treatment increases the levels of the active histone mark, H3K27ac, restores host translation in infected hamster bronchiolar cells, and leads to an enrichment in methylated ACE2 in hamster bronchioles and lung macrophages.
NACE2i has a dual mode of action: suppressing the lethal inflammation in severe COVID-19 and inhibiting viral replication by restoring host translation of anti-viral cytokines. |
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| DC73066 |
NBCoV2
Featured
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NBCoV2 is a highly potent small molecule viral fusion inhibitor with potential pan-Coronavirus activity (SARS-CoV IC50=13.8 nM, SARS-CoV-2 IC50=22.8 nM, MERS-CoV IC50=77 nM, cell-based single-cycle assays).
NBCoV2 also has potent antiviral activity against all mutant pseudoviruses carrying single-, double-, or triple-mutations featured in the B.1.1.7 UK, B.1.351 RSA, and B.1.617.2 Delta variants (IC50=30-80 nM).
NBCoV2 completely preventing the induction of any virus-induced CPE (IC100=1.25 uM, SARS-CoV-2 (US_WA-1/2020)).
NBCoV2 bind to the S2 subdomain of the SARS-CoV-2 trimer, thus, inhibits the fusion of CoVs with the cell membran, and is specific for the SARS-CoV-2 S protein. |
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| DC73073 |
SB27012
Featured
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SB27012 (SB 27012) is a small molecule PPI inhibitor of the Spike RBD-ACE2 interaction (IC50=7.7 uM in ELISA assays), binds ACE2 (Kd=210 nM) without affecting ACE2 enzymatic activity. |
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| DC73117 |
BAY 1892005
Featured
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BAY 1892005 is a small molecule that modulate mutant p53 condensation and nuclear accumulation, binds covalently to mutant p53R175H and p53Y220C and shows stabilization of p53WT and p53Y220C, exhibits anti-proliferative activity in a set of cell lines wit |
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| DC73134 |
GNE-684
Featured
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GNE-684 is a potent, cross-species, specific RIP1 kinase (RIPK1) inhibitor with IC50 of 21, 189 and 691 nM for human, mouse and rat RIP1, respectively. |
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| DC73145 |
FX2149
Featured
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FX2149 (FX 2149) is a potent, BBB permeable inhibitor of LRRK2 GTP binding activity with IC90 of 10 nM, reduces PD-linked mutant LRRK2 variants (G2019S and R1441C) that bound with GTP. |
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| DC73146 |
MK-1468
Featured
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MK-1468 is a potent, selective, brain-penetrant LRRK2 inhibitor with IC50 of 0.4 nM (G2019S LRRK2), potently inhibits the phosphorylation of LRRK2 serine 935 (pSer935) in hPBMCs with IC50 of 2.8 nM. |
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| DC73152 |
SW118150
Featured
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SW120619 is a specific small molecule inhibitor of WNK3 kinase with IC50 of 0.7 uM, weakly inhibits WNK1 and WNK2 with IC50 of 2.3 and 16.8 uM, respectively. |
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| DC73159 |
ML315
Featured
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ML315 is a small molecule inhibitor of the cdc2-like (Clk) and dual specificity tyrosine phosphorylation-regulated (Dyrk) kinases with IC50 of 68, 231, >10,000, 68, 282 and 1156 nM for CLK1/2/3/4 and DYRK1/2, respectively. |
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| DC73160 |
MW01
Featured
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MW01 is a specific inhibitor for DNA damage-induced NF-κB activity, inhibits CLK2 and CLK4 with IC50 of 360 and 14.1 nM, does not inhibit CLK3. |
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| DC73170 |
GFH009
Featured
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GFH009 is a potent, selective CDK9 inhibitor, inhibits the activity of the CDK9/cyclin T1 regulatory complex of P-TEFb. |
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| DC73188 |
QBS10072S
Featured
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QBS10072S is a novel dual-function, BBB permeable chemotherapeutic agent with alkylating moiety and a selective large neutral amino acid transporter 1 (LAT1, SLC7A5) substrate, shows excellent BBB penetration and promising efficacy in vitro (U251 cell IC5 |
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| DC73189 |
H3B-960
Featured
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H3B-960 is a potent, selective and covalent inhibitor of Werner syndrome protein (WRN) helicase activity with IC50 of 60 nM. |
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| DC73191 |
HRO761
Featured
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HRO761 is a potent, selective, allosteric WRN inhibitor with IC50 of 100 nM (ATPase assay) and GI50 of 40 nM (SW48 cells), respectively. HRO761 binds at the interface of the D1 and D2 helicase domains, locking WRN in an inactive conformation. |
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| DC73203 |
DI-87
Featured
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DI-87 ((R)-DI-87) is a highly potent, specific, orally bioavailable deoxycytidine kinase (dCK) inhibitor with IC50 of 3.15 nM. |
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| DC73210 |
TH7528
Featured
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TH7528 is a SAMHD1 inhibitor with IC50 of 4.5 μM/2.8 μM/2.6 μM against dGTP/Cl-F-ara-ATP/ara-CTP, respectively. |
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| DC73219 |
Allopole
Featured
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Allopole is the first allosteric, specfic and cell-permeable inhibitor of the noncatalytic polo-box domain (PBD) of PLK1 (Polo-like kinase 1), Allopole is the prodrug of Allopole-A. |
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| DC73236 |
GSK3335103
Featured
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GSK3335103 is a highly potent and orally bioavailable nonpeptidic αvβ6 integrin inhibitor with pIC50 of 8.0. GSK3335103 shows high desirable oral pharmacokinetic profiles in rat, dog, and minipig, with low to moderate clearance, moderate volumes of distributio, high to complete oral bioavailabilities and high solubility in all physiological media. |
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| DC73241 |
AM-1882
Featured
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AM-1882 (AM1882) is a potent, selective mitotic kinesin KIF18A inhibitor with IC50 of 230 nM in kinesin-8 microtubule (MT)-ATPase motor assays. |
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| DC73242 |
AM-9022
Featured
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AM-9022 (AM9022) is a potent, selective and orally active mitotic kinesin KIF18A inhibitor with IC50 of 47 nM in kinesin-8 microtubule (MT)-ATPase motor assays. |
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| DC73247 |
FiVe1
Featured
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FiVe1 is a vimentin binding small molecule that promotes vimentin disorganization and phosphorylation during metaphase, causes mitotic catastrophe, multinucleation, and the loss of stemness in cancer cells. |
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| DC73285 |
GSK3482364
Featured
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GSK-3484862 is a non-covalent inhibitor for DNA methyltransferase (Dnmt1). GSK-3484862 induces DNA hypomethylation to against cancer. GSK-3484862 mediates dramatic demethylation in murine embryonic stem cells with minimal non-specific toxicity. |
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| DC73305 |
TYA-018
Featured
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TYA-018 (TYA018) is a potent, isoform-selective inhibitor of HDAC6 with IC50 of 10 nM, inhibits tubulin acetylation (Ac-Tubulin) with EC50 of 120 nM in cell-based assay in induced pluripotent stem cell-derived cardiomyocytes (iPSC-CMs). |
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| DC73322 |
DP308
Featured
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DP308 is a novel and effective 53BP1 tandem Tudor domain (TTD) inhibitor, disrupts the binding between 53BP1 and H4K20me2 peptide with IC50 of 1.69 uM. |
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| DC73330 |
IHMT-337
Featured
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IHMT-337 (IHMT337) is a potent, highly selective and irreversible EZH2 inhibitor, specifically inhibits the methylation at H3K27. |
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| DC73350 |
JYQ-42
Featured
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JYQ-42 is a potent, selective SIRT6 allosteric inhibitor, effectively inhibits SIRT6 deacetylation with IC50 of 2.33 uM, inhibits the deacetylation activity of SIRT6 in pancreatic cancer cell lines. |
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| DC73375 |
QAF-805
Featured
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QAF-805 (QAF805) is a potent, dual adenosine-A2B receptor and adenosine-A3 receptor antagonist with Ki of 3.4 nM (A2B). |
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