DC7728EHop-016 is specific for Rac1 and Rac3 at concentrations of ≤5 μM. At higher concentrations, EHop-016 inhibits the close homolog Cdc42. In MDA-MB-435 cells that demonstrate high active levels of the Rac GEF Vav2,…
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DC7804Anacetrapib is a potent CETP inhibitor, with IC50s of 7.9±2.5 nM and 11.8±1.9 nM for rhCETP and C13S CETP mutant, respectively.
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DC7717kb-NB77-78 is an analogue of CID797718, but shows no PKD inhibitory activity[1].
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DC8735Sacubitril (AHU-377) hemicalcium salt is a potent NEP inhibitor with an IC50 of 5 nM. Sacubitril hemicalcium salt is a component of the heart failure medicine LCZ696.
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DCC4889Novel Sirtuin1 Activator, Down-Regulating Sclerostin and Rescuing Ovariectomy-Induced Bone Loss
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DC2089Retigabine is a novel anti-convulsant, enhances activation of KCNQ2/Q3 potassium channels.
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DC9313Sarpogrelate(MCI-9042) hydrochloride, a selective 5-HT2 antagonist, has been widely used as an anti-platelet agent for the treatment of PAD.Sarpogrelate is a drug which acts as an antagonist at the 5HT2A and 5-HT2B…
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DC8816ARS-853 is a selective, covalent KRASG12C inhibitor with an IC50 of 2.5 μM.
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DCAPI1390Atovaquone is a medication used to treat or prevent for pneumocystis pneumonia, toxoplasmosis, malaria, and babesia.Target: AntiparasiticAtovaquone (atavaquone) is a chemical compound that belongs to the class of…
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DC7362AT13148 is an orally active and ATP-competitive, multi-AGC kinase inhibitor with IC50s of 38 nM/402 nM/50 nM, 8 nM, 3 nM, and 6 nM/4 nM for Akt1/2/3, p70S6K, PKA, and ROCKI/II, respectively.
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DCAPI1199Lonidamine is an orally administered small molecule hexokinase inactivator.Target: OthersLonidamine is a derivative of indazole-3-carboxylic acid, which for a long time, has been known to inhibit aerobic glycolysis in…
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DC5199INCB018424 potently and selectively inhibits JAK2V617F-mediated signaling and proliferation in Ba/F3 cells and HEL cells. INCB018424 markedly increases apoptosis in a dose dependent manner in Ba/F3 cells. INCB018424…
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DC9854SAR407899 is a selective, potent and ATP-competitive ROCK inhibitor, with an IC50 of 135 nM for ROCK-2, and Kis of 36 nM and 41 nM for human and rat ROCK-2, respectively.
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DC8303GTS-21 dihydrochloride is a selective α7 nicotinic acetylcholine receptor agonist, has recently been established as a promising treatment for inflammation. Target: nAChRin vitro: GTS-21 is one of the most potent…
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DC7979CCG-1423 is a novel inhibitor of RhoA/C-mediated gene transcription that is capable of inhibiting invasion of PC-3 prostate cancer cells in a Matrigel model of metastasis.
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DC10461Autophinib is a potent autophagy inhibitor, which can inhibit autophagy induced by starvation or rapamycin by targeting the lipid kinase VPS34 with IC50s of 90, 40 and 19 nM, respectively.
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DCAPI1022Dofetilide(Tikosyn) is a class III antiarrhythmic agent.In patients with congestive heart failure and reduced left ventricular function, dofetilide was effective in converting atrial fibrillation, preventing its…
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DC7707LCZ696 is a dual angiotensin II receptor and neprilysin inhibitor.
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DC10704Asimadoline is a potent κ opioid receptor agonist with IC50s of 5.6 and 1.2 nM for guinea pig and human recombinant κ opioid receptor, respectively.
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DC7097Cebranopadol is an analgesic NOP and opioid receptor agonist with Kis/EC50s of 0.9 nM/13 nM, 0.7 nM/1.2 nM, 2.6 nM/17 nM, 18 nM/110 nM for human NOP, MOP, KOP and delta-opioid peptide (DOP) receptor, respectively.
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DC8406A 438079 (hydrochloride) is a potent, and selective P2X7 receptor antagonist with pIC50 of 6.9.
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DC10762Edonerpic maleate is a novel neurotrophic agent which can inhibit amyloid-β peptides (Aβ).
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DC9770NCB-0846 is an orally available TNIK inhibitor with an IC50 of 21 nM.
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DC8283PD 150606 is a selective, cell-permeable non-peptide calpain inhibitor (Ki values for ν and m-calpains are 0.21 and 0.37 μM respectively).
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DC8276Apilimod(STA 5326) mesylate is a potent IL-12/IL-23 inhibitor, IL-12 production in cultures of IFN-γ/LPS–stimulated human PBMCs is strongly inhibited by STA-5326 with an IC50 of 10 nM.
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DC7539AK-1 is a potent, specific and cell-permeable SIRT2 inhibitor.
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DC8095CNV1014802(GSK-1014802) Hcl is a novel small molecule state-dependent sodium channel blocker; Nav1.7 sodium channel inhibitor.IC50 value: Target: sodium channel blockerLike lamotrigine, both GSK2 and GSK3 were able to…
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DC8608Nintedanib esylate (BIBF 1120 esylate) is a potent triple angiokinase inhibitor for VEGFR1/2/3, FGFR1/2/3 and PDGFRα/β with IC50s of 34 nM/13 nM/13 nM, 69 nM/37 nM/108 nM and 59 nM/65 nM, respectively.
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DC7381CGP 57380 is a cell-permeable pyrazolo-pyrimidine compound that acts as a selective inhibitor of Mnk1 with IC50 of 2.2 μM, but has no inhibitory activity against p38, JNK1, ERK1/2, PKC, or Src-like kinases.
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DC8463NVP-TNKS656 is a highly potent, selective, and orally active TNKS2 inhibitor with IC50 of 6 nM, and is > 300 fold selectivity against PARP1 and PARP2.
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DC31421Givinostat or gavinostat, aslo known as ITF2357, is a potent and orally active histone deacetylase inhibitor with potential anti-inflammatory, anti-angiogenic, and antineoplastic activities. It is a hydroxamate used in…
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DC9604Desogestrel(Org-2969) is a third-generation 19-nortestosterone derivative progestogen; is contained in many oral contraceptive preparations, both combined (COCs) to ethinyl-estradiol (EE) or alone in a progestin-only…
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DC9879AZD8835 is a potent and selective inhibitor of PI3Kα and PI3Kδ with IC50s of 6.2 and 5.7 nM, respectively.
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DC9708GDC-0084 is a brain penetrant inhibitor of PI3K and mTOR, with Kis of 2 nM, 46 nM, 3 nM, 10 nM and 70 nM for PI3Kα PI3Kβ, PI3Kδ, PI3Kγ and mTOR, respectively.
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DC9859GAL-021 a new intravenous BKCa-channel blocker.
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DC9983E7449 is a potent PARP1 and PARP2 inhibitor and also inhibits TNKS1 and TNKS2, with IC50s of 2.0, 1.0, ∼50 and ∼50 nM for PARP1, PARP2, TNKS1 and TNKS2, respectively, using 32P-NAD+ as substrate.
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DC11398Edicotinib(JNJ-40346527)is a small molecule and orally available inhibitor of colony-stimulating factor-1 receptor (CSF1R; FMS) with potential antineoplastic activity. FMS tyrosine kinase inhibitor JNJ-40346527 blocks…
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DC7951BPTES is an allosteric and selective glutaminase inhibitor with an IC50 of 0.16 μM.
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DC7691PF 1022A is a N-methylated cyclooctadepsipeptides (CODPs) with strong anthelmintic properties; acts as an ionophore.PF 1022A showed strong anthelmintic activities against Ascaridia galli in chickens [1]. PF1022A is a…
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DC9858CPI-455 is a specific KDM5 inhibitor.
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DC8941Aclidinium Bromide(LAS 34273; LAS-W 330) is a long-acting, inhaled muscarinic antagonist as a maintenance treatment for chronic obstructive pulmonary disease (COPD).
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DC8785TC-O 9311 is a potent orphan G protein-coupled receptor 139 (GPR139) agonist with an EC50 of 39 nM[1].
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DC5146RN486 is a selective Btk inhibitor with an IC50 Value of 4.0 nM.
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DC3169PF-562271 is a potent ATP-competitive, reversible inhibitor of FAK and Pyk2 kinase, with an IC50 of 1.5 nM and 13 nM, respectively.
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DC23052(-)-Securinine is plant-derived alkaloid and also a GABAA receptor antagonist.
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DC74021IBS007125 is a small molecule inhibitor of c-Maf, inhibits multiple myeloma proliferation by targeting cMaf transcriptional activity.
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DC10171Hispidulin is a natural flavone with a broad spectrum of biological activities. Hispidulin is a Pim-1 inhibitor with an IC50 of 2.71 μM.
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DC7882S0859, an N-cyanosulphonamide compound, reversibly inhibit NBC-mediated pH(i) recovery (K (i)=1.7 microM, full inhibition at approximately 30 microM).NBCNa(+)-coupled HCO(3)(-) transporters (NBCs) mediate the transport…
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