DC7904CTX-0294885 is a novel broad-spectrum kinase inhibitor. CTx-0294885 exhibits inhibitory activity against a broad range of kinases in vitro. Use of a quantitative proteomics approach confirmed the selectivity of…
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DC7477PAC-1 is an activator of procaspase-3 induces apoptosis in cancer cells with EC50 of 2.08 μM.
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DC2012Bedaquiline is a diarylquinoline antibiotic that inhibits mycobacterial ATP synthase.
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DC7293SGI-1027 is a DNA methyltransferase (DNMT) inhibitor, with IC50s of 7.5 μM, 8 μM, and 12.5 μM for DNMT3B, DNMT3A, and DNMT1 with poly(dI-dC) as substrate.
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DC7165NSI-189 is a nootropic and neurogenic research chemical derived from nicotinamide and pyrazine.
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DC8710Tranylcypromine HCl is an inhibitor of monoamine oxidase (MAO) and prostacyclin synthase, potently suppresses the enzymatic activity of Lysine-Specific Demethylase 1 (LSD1) (IC50 <2 μM for BHC110/LSD1).
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DC7437JIB-04 is a pan-selective Jumonji histone demethylase inihibitor with IC50s of 230, 340, 855, 445, 435, 1100, and 290 nM for JARID1A, JMJD2E, JMJD3, JMJD2A, JMJD2B, JMJD2C, and JMJD2D, respectively.
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DC7900Lomitapide (AEGR-733; BMS-201038) is a potent inhibitor of microsomal triglyceride-transfer protein (MTP) with an IC50 of 8 nM in vitro.
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DC4101Apatinib is a highly selective VEGFR2 inhibitor with an IC50 of 1 nM. Apatinib also potently suppresses the activities of Ret, c-Kit and c-Src with IC50s of 13, 429 and 530 nM, respectively.
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DC60864D927 is a molecular glue and promotes glucose uptake in the absence of insulin. D927 also increases the affinity of RAS binding to PI3Kα by ~500-fold. In vivo, D927 mimicks the effects of insulin and rapidly lowers…
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DC7045A-769662 is a potent, reversible AMPK activator with EC50 of 0.8 μM.
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DC10768IT-901 is an orally active and potent NF-κB subunit c-Rel inhibitor with an IC50 of 0.1 µM, 3 μM for NF-κB DNA binding and c-Rel DNA binding, respectively. IT-901, a bioactive naphthalenethiobarbiturate derivative, has…
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DC10034GLPG0187 is a broad spectrum integrin receptor antagonist with antitumor activity; inhibits αvβ1-integrin with an IC50 of 1.3 nM.
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DC2005Ataluren (PTC124) is an orally available CFTR-G542X nonsense allele inhibitor.
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DC3170Cediranib maleate (AZD-2171 maleate) is a highly potent, orally available VEGFR tyrosine kinase inhibitor with IC50s of <1, <3, 5, 5, 36, 2 nM for Flt1, KDR, Flt4, PDGFRα, PDGFRβ, c-Kit, respectively.
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DC7082Belinostat inhibits the growth of tumor cells (A2780, HCT116, HT29, WIL, CALU-3, MCF7, PC3 and HS852) with IC50 from 0.2-0.66 μM. PD101 shows low activity in A2780/cp70 and 2780AD cells, which are cisplatin and…
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DC5882IC50 Value: 4 nM [1]Target: microtubule
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DC7066Binimetinib (MEK162) is an oral and selective MEK1/2 inhibitor with an IC50 of 12 nM.
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DC5105Favipiravir is a novel viral RNA polymerase inhibitor, it is phosphoribosylated by cellular enzymes to its active form, Favipiravir-ribofuranosyl-5′-triphosphate (RTP). Favipiravir-RTP inhibits the influenza viral…
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DC7424HPGDS inhibitor 1 is a novel and selective Hematopoietic Prostaglandin D Synthase (HPGDS) inhibitor with an IC50 Value of 0.7 nM.IC50 Value: 0.7 nM [1]Target: HPGDSHPGDS inhibitor 1 was elected for further profiling…
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DC7850OF-1 is a selective BRPF1B and BRPF2 bromodomain inhibitor with Kd values of 100 nM/500 nM for BRPF1B/BRPF2; 39-fold selectivity over BRD4.
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DC7116Lenvatinib is an oral, multi-targeted tyrosine kinase inhibitor with IC50s of 4 and 5.2 nM for VEGFR2(KDR) and VEGFR3(Flt-4), respectively. Lenvatinib is less potent against VEGFR1/Flt-1 and shows approximately 10-fold…
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DC9641NSC348884 is a nucleophosmin inhibitor disrupts oligomer formation and induces apoptosis, inhibits cell proliferation at an IC50 of 1.7-4.0 μM in distinct cancer cell lines.
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DC7695Defactinib is a novel FAK inhibitor with potential antiangiogenic and antineoplastic activities.
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DC7991Clozapine N-oxide (CNO) is a major metabolite of the anti-psychotic drug clozapine. Clozapine N-oxide is a agonist for the chemogenetic Designer Receptors Exclusively Activated by Designer Drug (DREADD) system.
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DC7493SB1317 is a potent inhibitor of CDK2, JAK2, and FLT3 for the treatment of cancer, with IC50 of 13, 73, and 56 nM for CDK2, JAK2 and FLT3, respectively.
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DC7443Kobe0065 is a novel and effective inhibitor of Ras-Raf interaction, competitively inhibiting the binding of H-Ras·GTP to c-Raf-1 RBD with a Ki value of 46±13 μM.
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DC5028IWP-2 is an inhibitor of Wnt processing and secretion with IC50 of 27 nM.
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DC7212NMS-873 is a potent, selective allosteric VCP/p97 inhibitor with IC50 value of 30 nM.
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DC7996BAY 87-2243 is a highly potent and selective hypoxia-inducible factor-1 (HIF-1) inhibitor.
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DC7927EPZ011989 is a potent, selective orally bioavailable EZH2 inhibitor with Ki < 3 nM for EZH2 wt and EZH2 Y646; 15-fold selectivity over EZH1 and >3000-fold selectivity over other HMTase.IC50 value: < 3 nM ( Ki for wt…
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DC7100CFTR(inh)-172 is a potent and selective blocker of the CFTR chloride channel; reversibly inhibited CFTR short-circuit current in less than 2 minutes with a Ki of 300 nM.
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DC10621Amenamevir is a helicase-primase inhibitor which has potent antiviral activity against HSVs with an EC50 of 14 ng/mL.
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DC7246SR-3677 is a potent and selective ROCK-II inhibitor with an IC50 of ~3 nM.
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DC7453LEE011, as dual CDK4/CDK6 inhibitor, significantly inhibits the growth of 12 of 17 neuroblastoma cell lines with mean IC50 of 307 nM. The growth inhibition of neuroblastoma cell lines is primarily cytostatic and is…
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DC9841Fostamatinib (R788), a prodrug of the active metabolite R406, is a potent Syk inhibitor with IC50 of 41 nM.
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DC6902Thiazovivin is a potent ROCK inhibitor, which can protect human embryonic stem cells.
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DC7257PYR-41 is a specific and cell permeable inhibitor of ubiquitin-activating enzyme E1 with an IC50 of < 10 μM, with no or little activity at E2.
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DC4230Ruxolitinib is a potent and selective JAK1/2 inhibitor with IC50s of 3.3 nM and 2.8 nM in cell-free assays, and has 130-fold selectivity for JAK1/2 over JAK3.
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DC12021(+)-JQ1 PA is a derivative of the Bromodomain and extra-terminal (BET) inhibitor JQ1, with an IC50 of 10.4 nM.
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DC7540AK-7 is a selective cell- and brain-permeable SIRT2 inhibitor, with an IC50 of 15.5 μM.
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DC10796Prexasertib (LY2606368) is a potent, selective and ATP-competitive checkpoint kinase 1 (Chk1) inhibitor, with an IC50 and a Ki of <1 nM and 0.9 nM, respectively.
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DC9948SNX-5422 (PF-04929113), a prodrug of SNX-2112, is an orally active Hsp90 inhibitor, with a Kd of 41 nM, and also induces Her-2 degradation, with an IC50 of 37 nM.
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DC5149Dabrafenib is an ATP-competitive inhibitor of Raf with IC50s of 5 nM and 0.6 nM for C-Raf and B-RafV600E, respectively.
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DC9251RS102895 hydrochloride is a potent CCR2 antagonist, with an IC50 of 360 nM, and shows no effect on CCR1.
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DC10844Aftin-4 is an Amyloid-β42 (Aβ42) inducer.
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DC1054GDC-0941 (Pictilisib) is a potent inhibitor of PI3Kα/δ with an IC50 of 3 nM, with modest selectivity against p110β (11-fold) and p110γ (25-fold).
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DC7343YM-201636 is a potent and selective PIKfyve inhibitor with an IC50 of 33 nM. YM-201636 also inhibits p110α with IC50 of 3.3 μM.
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