DC26112A novel reactivator of wild-type and mutant p53, shows a p53-dependent anti-proliferative activity in human wt and mut p53R280K-expressing tumor cells; enhances p53 transcriptional activity and restores wt-like DNA…
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DC31068Tivozanib is an orally available, selective VEGFR inhibitor with IC50 values of 0.21, 0.16, and 0.24 nM for VEGFR1, VEGFR2, and VEGFR3, respectively.
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DC5034MK-8245 is a liver-targeting inhibitor of stearoyl-CoA desaturase (SCD) with IC50 of 1 nM for human SCD1 and 3 nM for both rat SCD1 and mouse SCD1, with anti-diabetic and anti-dyslipidemic efficacy.
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DC23990N-Desethyl Sunitinib is a metabolite of sunitinib. Sunitinib is a potent, ATP-competitive VEGFR, PDGFRβ and KIT inhibitor with Ki values of 2, 9, 17, 8 and 4 nM for VEGFR -1, -2, -3, PDGFRβ and KIT, respectively.
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DC9682ML264 is an antitumor agent that potently and selectively inhibits Krüppel-like factor five (KLF5) expression.
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DC83888-Bromo-cAMP sodium salt (8-Br-Camp sodium salt), a cyclic AMP analog, is an activator of cyclic AMP-dependent protein kinase (PKA)[1].
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DC12626MitoBloCK-11 (MB-11) is a s mall molecule inhibitor of mitochondrial protein import possibly acts through transport protein Seo1, but not Tom70 or Tom20; inhibits precursor proteins that contain hydrophobic segments,…
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DC9137(S)-Timolol maleate, is a potent non-selective β-adrenergic receptor antagonist (Ki values are 1.97 and 2.0 nM for β1 and β2 receptor subtypes respectively).(S)-Timolol, 50% bioavailability following oral…
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DC31174Doxorubicin free base, also called doxorubicin, is an anthracycline antibiotic with antineoplastic activity. Approved API for cancer therapeutic use is doxorubicin HCl. Doxorubicin, isolated from the bacterium…
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DC23507FC131 TFA is a CXCR4 antagonist that inhibits the binding of [125I]-SDF-1 to CXCR4 with an IC50 value of 4.5 nM. FC131 TFA has anti-HIV activity.
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DCAPI1413For the detailed information of pioglitazone hydrochloride, the solubility of pioglitazone hydrochloride in water, the solubility of pioglitazone hydrochloride in DMSO, the solubility of pioglitazone hydrochloride in…
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DC8285Acotiamide monohydrochloride trihydrate is an orally active and first-in-class gastroprokinetic agent for the treatment of functional dyspepsia. Acotiamide monohydrochloride trihydrate enhances acetylcholine released…
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DC9619Nafamostat mesylate, a synthetic serine protease inhibitor, is an anticoagulant.Target: Serine ProteaseTranilast (FUT-175) is an antiallergic drug for bronchial asthma. It has been used for the treatment of allergic…
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DC11641Cridanimod is a small-molecule immunomodulator and interferon inducer[1]. Cridanimod is a potent progesterone receptor (PR) activator mediated through induction of IFNα and IFNβ expression[2].
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DC21072Voxilaprevir (GS-9857) is a fluorinated macrocyclic hepatitis C virus (HCV) nonstructural protein (NS) 3/4A protease inhibitor with potent in vitro antiviral activity against genotypes 1-6 HCV and broad coverage of…
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DC26224CTOP is a potent and highly selective μ-opioid receptor antagonist. CTOP antagonizes the acute morphine-induced analgesic effect and hypermotility. CTOP enhances extracellular dopamine levels in the nucleus accumbens.…
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DC21644SHP504 is a distinct, allosteric site 2 SHP2 inhibitor with IC50 of 21 uM (SHP2 1-525), and selective over the phosphatase domain (SHP2 PTP IC50>100 uM).downregulates DUSP6 mRNA, a downstream MAPK pathway marker, in…
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DC7333UNC1999 is a SAM-competitive, potent and selective inhibitor of EZH1/2 with IC50s of 10 nM and 45 nM, repectively.
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DC5889Fludarabine(NSC 118218), a DNA synthesis inhibitor, is a chemotherapy drug used in the treatment of hematological malignancies.Fludarabine or fludarabine ph osphate (Fludara) is a chemotherapy drug used in the…
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DC39048Zamicastat is a concentration-dependent dual P-gp and BCRP inhibitor with IC50 values of 73.8±7.2 μM and 17.0±2.7 μM, respectively.
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DC12045HS-1371 is a potent and ATP-competitive RIP3 inhibitor with an IC50 of 20.8 nM[1].
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DC7699VTP-27999 is an alkyl amine Renin inhibitor; VTP-27999 is useful for Hypertension and End-Organ Diseases.
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DC7793K-Ras(G12C) inhibitor 12 is a K-Ras(G12C) inhibitor, the half-maximum effective concentration (EC50) for K-Ras(G12C) inhibitor 12 in H1792 cells is 0.32 μM.Binding of K-Ras(G12C) inhibitor 12 to K-Ras(G12C) disrupts…
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DC39204GNF4877 is a potent DYRK1A and GSK3β inhibitor with IC50s of 6 nM and 16 nM, respectively, which leads to blockade of nuclear factor of activated T-cells (NFATc) nuclear export and increased β-cell proliferation (EC50…
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DC39203JWG-071 is the first reported kinase-selective chemical probe for ERK5. JWG-071 improves ERK5 activity and BRD4 selectivity. JWG-071 will be a much-needed chemical probe for deconvoluting ERK5 and BRD4 pharmacology[1].
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DC9186Lercanidipine hydrochloride is a calcium channel blocker of the dihydropyridine class.Lercanidipine is a calcium channel blocker of the dihydropyridine class, which works by relaxing and opening the blood vessels…
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DC26220VKGILS-NH2 is a reversed amino acid sequence control peptide for SLIGKV-NH2 (protease-activated receptor 2 (PAR2) agonist). VKGILS-NH2 has no effect on DNA synthesis in cells[1][2].
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DC22627Trametinib DMSO solvate is a potent MEK inhibitor that specifically inhibits MEK1/2, with an IC50 value of about 2 nM.
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DC41134Thalidomide-5-OH is the Thalidomide-based cereblon ligand used in the recruitment of CRBN protein. Thalidomide-5-OH can be connected to the ligand for protein by a linker to form PROTACs[1].
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DC8901Azilsartan medoxomil(TAK 491) is an orally administered angiotensin II receptor type 1 antagonist with IC50 of 0.62 nM, which used in the treatment of adults with essential hypertension.
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DC65648LY3437943 is a triple agonist peptide of the glucagon receptor (GCGR), glucosedependent insulinotropic polypeptide receptor (GIPR), and glucagon-like peptide-1 receptor (GLP-1R). LY3437943 inhibits for human GCGR,…
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DC23302Disarib is a novel BCL2-specific inhibitor that binds predominantly to the BH1 domain, demonstrates strong affinity to BCL2, but not to other antiapoptotic BCL2 family members(BCL-xL, BCL2A1 etc.); is a novel BCL2…
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DC9103Rabeprazole sodium(LY307640 sodium) is an antiulcer drug in the class of proton pump inhibitors.Rabeprazole belongs to a class of antisecretory compounds (substituted benzimidazole proton-pump inhibitors) that do not…
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DC22243TAS0728 is a potent, selective, oral active, irreversible and covalent-binding HER2 inhibitor, binds to HER2 at C805, inhibits its kinase activity, with an IC50 of 13 nM. TAS0728 shows IC50s of 4.9, 8.5, 31, 65, 33,…
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DC9162Ranolazine(RS-43285) is an antianginal agent with antiarrhythmic properties that achieves its effects via a novel mechanism of action (inhibition of the late phase of the inward sodium current), without affecting heart…
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DC10633AD80, a multikinase inhibitor, inhibits RET, RAF,SRCand S6K, with greatly reduced mTOR activity.
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DC10064GSK-F1 is a potent inhibitor of PI4KA. It has markedly better pharmacokinetic properties in vivo with respects to GSK-A1 (SYN-1219). GSK-F1 does not cross the blood-brain barrier. Phosphatidylinositol 4-kinase type…
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DC22635SPDP is a short-chain crosslinker for amine-to-sulfhydryl conjugation via NHS-ester and pyridyldithiol reactive groups that form cleavable (reducible) disulfide bonds with cysteine sulfhydryls. equal amounts of…
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DC32374β-nicotinamide mononucleotide is an intermediate in NAD+ biosynthesis produced from nicotinamide (NAM) and phosphoribosyl pyrophosphate (PRPP) by nicotinamide phosphoribosyl transferase enzyme.
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DC73618NUCC-0200590 is a small-molecule inhibitor of the TRIP8b-HCN interaction with IC50 of 7.0 uM in AlphaScreen assays, effectively disrupts the TRIP8b-HCN interaction in vitro and in vivo.
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DC5062Abemaciclib (LY2835219) (methanesulfonate) is a selective CDK4/6 inhibitor with IC50s of 2 nM and 10 nM for CDK4 and CDK6, respectively.
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DC39201NMDAR/TRPM4 inhibitor 8 (Compound 8) is a neuroprotective NMDAR-TRPM4 interaction interface inhibitor but spare the critical healthy NMDAR function.
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DC11162MID-1 is an inhibitor of MG53-IRS-1 (Mitsugumin 53-Insulin Receptor Substrate-1) interaction. MID-1 disrupts molecular association of MG53 with IRS-1 and abolishes MG53-induced IRS-1 ubiquitination and degradation in…
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DC28247Aripiprazole lauroxil, an N-acyloxymethyl prodrug of aripiprazole, is a Long-acting injectable (LAI) typical antipsychotic for schizophrenia. Aripiprazole lauroxil is cleaved by body’s enzyme esterase to…
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DC26175F-15599 is a highly selective G-protein biased 5-HT1A receptor agonist, with Ki of 3.4 nM.
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DC8391SAG (hydrochloride) is a potent Smo receptor agonist, and activates the Hedgehog signaling pathway, with a Kd of 59 nM.
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DC11871MMV019313 (MMV 019313, MMV-019313) is a potent, specific malaria bifunctional farnesyl/geranylgeranyl diphosphate synthase (FPPS/GGPPS) inhibitor with IC50 of 330 nM; shows no activity against human FPPS or GGPPS (>200…
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DC39022BAY 2416964 is a 2-heteroaryl-3-oxo-2,3-dihydropyridazine-4-carboxamide compound and an aryl hydrocarbon receptor (AHR) antagonist extracted from patent WO2018146010A1, example 192, has an IC50 of 341 nM. AHR…
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