DC8444Sabutoclax
Sabutoclax is a potent and effective Bcl-2 Family (Bcl-2, Bcl-XL, Mcl-1, Bfl-1) inhibitor with IC50s of 0.32 μM, 0.31 μM, 0.20 μM, and 0.62 μM, respectively.
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DC8444Sabutoclax is a potent and effective Bcl-2 Family (Bcl-2, Bcl-XL, Mcl-1, Bfl-1) inhibitor with IC50s of 0.32 μM, 0.31 μM, 0.20 μM, and 0.62 μM, respectively.
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DC8459Palovarotene is a nuclear retinoic acid receptor γ (RAR-γ) agonist.
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DC7419GNE-7915 is a potent, selective and brain-penetrant inhibitor of LRRK2 with an IC50 of 9 nM.
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DC22298AMG-510 is a specific covalent inhibitor of K-RAS(G12C) with potential antineoplastic activity. Upon oral administration, KRAS mutant-targeting AMG-510 selectively targets the KRAS p.G12C mutant, at either the DNA, RNA…
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DC7383The dissociation constant (KD) value of CH5424802 For ALK in an ATP-competitive manner is 2.4 nM. CH5424802 has substantial inhibitory potency against both native ALK and L1196M with Ki of 0.83 nM and 1.56 nM,…
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DC7431ISRIB (trans-isomer) is a potent inhibitor of PERK with an IC50 of 5 nM.
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DC7206R1530 is the multikinase inhibitor with potential antiangiogenesis and antineoplastic activities.R1530 is also a mitosis-angiogenesis inhibitor (MAI) that inhibits multiple receptor tyrosine kinases involved in…
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DC7365ATB-346 is a novel hydrogen sulphide-releasing derivative of naproxen with markedly reduced toxicity. IC50 value: Target: COX-2 ATB-346 suppressed gastric prostaglandin E(2) synthesis as effectively as naproxen, but…
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DC8052AZ-5104 is an active, demethylated metabolite of AZD 9291. AZ-5104 is an EGFR inhibitor with IC50s of 1, 6, 1, 25 and 7 nM for EGFRL858R/T790M, EGFRL858R, EGFRL861Q, EGFR and ErbB4, respectively.
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DC5184Epirubicin (hydrochloride) is a semisynthetic L-arabino derivative of doxorubicin, and an antineoplastic agent by inhibiting Topoisomerase.
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DC1025AT7519 Hydrochloride is a potent inhibitor of CDKs, with IC50s of 210, 47, 100, 13, 170, and <10 nM for CDK1, CDK2, CDK4 to CDK6, and CDK9, respectively.
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DC7720Lificiguat binds to the β subunit of soluble guanylyl cyclase(sGC) with Kd of 0.6-1.1 μM in the presence of CO.
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DC7603Bioymifi(DR5 Activator) is the first novel and potent small-molecule activatior of the TRAIL receptor DR5 in human cancer cells.
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DC4188Doxorubicin hydrochloride is a cytotoxic anthracycline antibiotic for the treatment of multiple cancers. The possible mechanisms by which doxorubicin acts in the cancer cell are intercalation into DNA and disruption of…
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DC7807SB 239063 is a potent and selective p38 MAPK inhibitor (IC50 = 44 nM for p38α). SB 239063 displays > 220-fold selectivity over ERK, JNK1 and other kinases; ~ 3-fold more selective than SB 203580. IC50 value: 44 nM (…
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DC1001Tacrolimus is a macrocyclic lactone with potent immunosuppressive properties. Tacrolimus binds to FK506 binding protein (FKBP) to form a complex and inhibits calcineurin phosphatase.
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DC2093Genistin is the major isoflavonoid of soybeans and soy products.
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DC7543Bromosporine is a broad spectrum inhibitor for bromodomains with IC50 of 0.41 μM, 0.29 μM, 0.122 μM and 0.017 μM for BRD2, BRD4, BRD9 and CECR2, respectively.IC50 value: 0.41/0.29/0.122/0.017 uM (BRD2/BRD4/BRD9/CECR2)…
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DC7387Clemizole hydrochloride is an H1 histamine receptor antagonist, is found to substantially inhibit HCV replication. The IC50 of Clemizole for RNA binding by NS4B is 24±1 nM, whereas its EC50 for viral replication is 8 µM.
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DC7503(Z)-SMI-4a is a selective ATP-competitive Pim-1 kinase inhibitor with an IC50 of 21 nM for Pim-1 compared to an IC50 of 100 nM for Pim-2 and with little or no activity against a panel of 50 other kinases tested.
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DC7708UNBS5162 is a pan-antagonist of CXCL chemokine expression, with anti-tumor activity.
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DC7332UNC1215 is a potent and selective chemical probe for the methyllysine (Kme) reading function of L3MBTL3 with Kd value of 120 nM.
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DC22211ALG1001 (Risuteganib, ALG-1001) is a first-in-class, RGD class oligopeptide that inhibits integrin receptors (αvβ3, αvβ5, and α5β1) associated with angiogenesis; ALG1001 inhibits an integrin-mediated pathway of the…
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DC5046CPI-203 is a novel potent, selective and cell permeable inhibitor of BET bromodomain, with an IC50 value of appr 37 nM (BRD4 α-screen assay).
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DC10495KAI407 is a potent non-8-aminoquinoline compound that kills Plasmodium cynomolgi early dormant liver stage parasites in vitro. KAI407 showed an activity profile similar to that of primaquine (PQ), efficiently killing…
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DC3110Fimepinostat (CUDC-907) potently inhibits class I PI3Ks as well as classes I and II HDAC enzymes with an IC50 of 19/54/39 nM and 1.7/5.0/1.8/2.8 nM for PI3Kα/PI3Kβ/PI3Kδ and HDAC1/HDAC2/HDAC3/HDAC10 , respectively.
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DC6315GSK2636771 is a potent, selective and oral inhibitor of PI3Kβ with a Ki of 0.89 nM and an IC50 of 5.2 nM, showing 900-fold selectivity over p110α and p110γ, and 10-fold selectivity over p110δ isoforms.
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DC7548Nexturastat A is a potent and selective HDAC6 inhibitor with IC50 of 5 nM; no inhibition on other HDAC forms.Nexturastat A displayed low micromolar activity compared to the low nanomolar activity against HDAC6.…
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DC7215NSC-405020 is a novel small molecule inhibitor of MT1-MMP that specifically targets PEX domain rather than the catalytic domain of MT1-MMP with IC50 >100 μM and does not inhibit the catalytic activity of MT1-MMP or…
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DC1082ZM-306416 (CB 676475) is a potent inhibitor of VEGFR with IC50s of 0.1 and 2 μM for KDR and Flt, respectively. ZM-306416 is also a EGFR inhibitor with an IC50 of <10 nM.
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DC7307TAK-632 is a potent pan-RAF inhibitor with IC50 of 1.4, 2.4 and 8.3 nM for CRAF, BRAFV600E, BRAFWT, respectively.
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DC7535Y-320 is a new phenylpyrazoleanilide immunomodulator; inhibits IL-17 production by CD4 T cells stimulated with IL-15 with IC50 values of 20 to 60 nM.Y-320 inhibited IL-17 production by CD4 T cells stimulated with IL-15…
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DC7483PPQ-102 is a potent CFTR inhibitor which can completely inhibited CFTR chloride current with IC50 of ~90 nM.
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DC7252PR-619 is a broad-range DUB inhibitor with EC50 of 3.93, 4.9, 6.86, 7.2, and 8.61 μM for USP4, USP8, USP7, USP2, and USP5, respectively.
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DC5181XL-765, also known as SAR245409, is a PI3K/mTOR dual kinase inhibitor XL765 is an orally bioavailable small molecule targeting the phosphatidylinositol 3 kinase (PI3K) and mammalian target of rapamycin (mTOR) kinases…
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DC9246PJ34 is a potent specific inhibitor of PARPl/2 with IC50 of 110 nM and 86 nM, respectively.
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DC7042GSK126 is a potent, highly selective inhibitor of EZH2 methyltransferase with an IC50 of 9.9 nM.
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DC10799SSR240612 is a potent, and orally active specific non-peptide bradykinin B1 receptor antagonist, with Kis of 0.48 nM and 0.73 nM for B1 kinin receptors of human fibroblast MRC5 and HEK cells expressing human B1…
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DC10710Skp2 Inhibitor C1(SKPin C1) is a specific small molecule inhibitor of Skp2-mediated p27 degradation, selectively inhibited Skp2-mediated p27 degradation by reducing p27 binding through key compound-receptor…
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DC7451LDN193189 potently inhibits BMP4-mediated Smad1, Smad5 and Smad8 activation with IC50 of 5 nM, and efficiently inhibits transcriptional activity of the BMP type I receptors ALK2 and ALK3 with IC50 of 5 nM and 30 nM,…
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DC60152SHIN-2 is a novel SHMT inhibitor, increasing survival in NOTCH1-driven mouse primary T-ALL in vivo
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DC7092BX795 is a potent and selective PDK1 inhibitor with an IC50 of 6 nM, showing 50-fold selectivity over PKA, PKC, c-Kit, GSK3β etc.
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DC7309TAK-960 is an orally available, selective inhibitor of polo-like kinase 1 (PLK1), with an IC50 of 0.8 nM at 10 μM ATP; TAK-960 also shows inhibitory activities against PLK2 and PLK3, with IC50s of 16.9 and 50.2 nM,…
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DC7137GLPG0634 is a selective JAK1 inhibitor with IC50 of 10 nM, 28 nM, 810 nM, and 116 nM for JAK1, JAK2, JAK3, and TYK2, respectively.
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DC7731Emapunil(AC-5216;XBD-173) is a translocator protein[TSPO (18 kDa)] ligand.IC50 value:Target: TSPO ligandXBD173 enhanced gamma-aminobutyric acid-mediated neurotransmission and counteracted induced panic attacks in…
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DC7185Erismodegib diphosphate (LDE225 diphosphate) is a potent and selective Smo antagonist with IC50 of 1.3 nM and 2.5 nM for mouse and human Smo in binding assay, respectively.
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DC7331UNC0638 selectively inhibits G9a and GLP histone methyltransferase activity with IC50s of less than 15 nM and 19 nM, respectively.
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DC7374BIX-01294 is an inhibitor of G9a Histone Methyltransferase with IC50 of 1.9 μM.
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