“Ligand-gated Ion Channels”的搜索结果
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IFN-α and IFNAR interaction inhibitor
IFN alpha-IFNAR-IN-1 hydrochloride is a nonpeptidic, low-molecular-weight inhibitor of the interaction between IFN-α and IFNAR; inhibit MVA-induced IFN-α responses by BM-pDCs (IC50=2-8 uM).
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EGFR/T790M inhibitor
HS-10296 hydrochloride is an orally available and third-Generation inhibitor of epidermal growth factor receptor (EGFR)-activating mutations and T790M-resistant mutation with limited activity against wild-type EGFR.
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HCV RNA replication inhibitor
Sofosbuvir impurity A, an diastereoisomer of sofosbuvir, is the impurity of sofosbuvir. Sofosbuvir (PSI-7977) is an inhibitor of HCV RNA replication, demonstrates potent anti-hepatitis C virus activity.
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HCV RNA replication inhibitor
Sofosbuvir impurity C is the less active impurity of Sofosbuvir, Sofosbuvir is an active inhibitor of HCV RNA replication in the HCV replicon assay, demonstrates potent anti-hepatitis C virus (HCV) activity.
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HCV RNA replication inhibitor
PSI-7976 is the isomer of PSI-7977. PSI-7977 is an active inhibitor of HCV RNA replication in the HCV replicon assay, demonstrates potent anti-hepatitis C virus (HCV) activity.
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FASN inhibitor
HS-80 is an enantiomer of Fasnall, which is a selective fatty acid synthase (FASN) inhibitor. HS-80 is able to inhibit the incorporation of tritiated acetate into lipids with an IC50 of 7.13 μM.
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BET binding to histones inhibitor
(R)-BAY1238097 is the R-isomer with lower activity of BAY1238097. BAY1238097 is a potent and selective inhibitor of BET binding to histones and has strong anti-proliferative activity in different AML (acute myeloid leukemia) and MM (multiple myeloma) models through down-regulation of c-Myc levels and its downstream transcriptome.
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Tau and Aβ aggregation inhibitor
PE859 is a potent inhibitor of both tau and Aβ aggregation with IC50 values of 0.66 and 1.2 μM, respectively.
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RET inhibitor
cis-Pralsetinib (cis-BLU-667) is a highly potent and selective inhibitor of rearranged during transfection (RET), with IC50s ranging from 0.3 to 0.4 nM for WT RET and four enzyme variants (V804L, V804M, M918T, CCDC6-RET), and with broad, robust and anti-tumor activity against multiple RET-driven solid tumor types.
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Adenosine deaminase inhibitor
EHNA hydrochloride is a specific inhibitor of adenosine deaminase, prevents dAdo degradation and increases mitochondrial dATP levels in fibroblasts.
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indirect thrombin inhibitor
Odiparcil (SB-424323) is indirect thrombin inhibitor that exerts its anticoagulant effect through activation of antithrombin II (heparin cofactor II) .
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PTEF/CDK9 inhibitor
(-)-BAY-1251152 is an enanthiomer of BAY-1251152 with rotation (-). BAY-1251152 is a potent and highly selective PTEF/CDK9 inhibitor.
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CDK9 inhibitor
CDK9-IN-1 is a novel, selective CDK9 inhibitor for the treatment of HIV infection, with an IC50 of 39 nM for CDK9/CycT1, extracted from reference, compound 87.
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dihydropyrimidine dehydrogenase inhibitor
Eniluracil (5-Ethynyluracil), a uracil analogue and a mechanism-based irreversible inhibitor of dihydropyrimidine dehydrogenase (DPD), increases the oral bioavailability of 5-fluorouracil (5-FU) to 100%, facilitating uniform absorption and predictable toxicity.
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Complex I of oxidative phosphorylation inhibitor
IACS-10759 Hydrochloride is a potent inhibitor of complex I of oxidative phosphorylation (OXPHOS).
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Hsp90 inhibitor
SNX-5422 Mesylate (PF-04929113 Mesylate), 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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RhoA subfamily Rho GTPases inhibitor
Rhosin is a potent, specific RhoA subfamily Rho GTPases inhibitor, which specifically binds to RhoA to inhibit RhoA-GEF interaction with a Kd of ~ 0.4 uM, and does not interact with Cdc42 or Rac1, nor the GEF, LARG. Rhosin induces cell apoptosis.
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DCN1-UBC12 interaction inhibitor
WS-383 is a potent, selective and reversible inhibitor of DCN1-UBC12 interaction, with an IC50 of 11 nM. WS-383 inhibits Cul3/1 neddylation, induces accumulation of p21, p27 and NRF2.
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PD-1/PD-L1 interaction inhibitor
BMS-1166 hydrochloride is a potent PD-1/PD-L1 interaction inhibitor with an IC50 of 1.4 nM. BMS-1166 antagonizes the inhibitory effect of PD-1/PD-L1 immune checkpoint on T cell activation.
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FAK inhibitor
Y15 is a potent and specific inhibitor of focal adhesion kinase (FAK) that inhibits its autophosphorylation activity, decreases the viability of cancer cells, and blocks tumor growth.
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RSV replication inhibitor
RSV604 is a novel inhibitor of respiratory syncytial virus replication(EC50=0.86 uM); a putative RSV nucleoprotein(N) inhibitor in phase 2 clinical trials.
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BACE-1 inhibitor
β-Secretase Inhibitor IV is a potent, cell-active BACE-1 inhibitor with IC50s of 15.6 and 16.3nM under BACE-1 concentrations of 2 nM and 100 pM, respectively.
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uricase inhibitor
Potassium oxonate is an inhibitor of uricase, inhibits the phosphorylation of 5-FU to 5-fluorouridine-5'-monophosphate catalyzed by pyrimidine phosphoribosyl-transferase in a different manner from allopurinol in cell-free extracts and intact cells in vitro.
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FAAH inhibitor
PF 750 is a selective and covalent fatty acid amide hydrolase (FAAH) inhibitor, with IC50s varied from 16.2-595 nM in different pre-incubation times. Covalently modifies the enzyme??s active site serine nucleophile.
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tubulin polymerization inhibitor
McMMAF is a protective group-conjugated MMAF. MMAF is a potent tubulin polymerization inhibitor.
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PDE-5 inhibitor
Mirodenafil(SK3530) is a phosphodiesterase type 5 (PDE-5) inhibitor developed for the treatment of erectile dysfunction.
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β-tubulin polymerization inhibitor
Valecobulin (CKD516) is a valine prodrug of (S516) and a vascular disrupting agent (VDA). Valecobulin is a potent β-tubulin polymerization inhibitor with marked antitumor activity against murine and human solid tumors.
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KMO inhibitor
UPF-648 is a potent kynurenine 3-monooxygenase (KMO) inhibitor; exhibits highly active at 1 uM (81 ?? 10% KMO inhibition); ineffective at blocking KAT activity.
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tubulin polymerization inhibitor
Soblidotin (Auristatin PE) is a novel synthetic Dolastatin 10 derivative and inhibitor of tubulin polymerization.
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glutathione analog inhibitor
Ezatiostat hydrochloride (TER199;TLK199 hydrochloride) is a glutathione analog inhibitor of glutathione S-transferase P1-1 (GSTP1-1).
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Cdc34 ubiquitin-conjugating enzyme inhibitor
CC0651 is an allosteric inhibitor of the human Cdc34 ubiquitin-conjugating enzyme. CC0651 potently (IC50=1.72 μM) inhibits the ubiquitination of p27Kip1, as confirmed by dose-response analysis.
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PAK1 inhibitor
IPA-3 is a selective non-ATP competitive PAK1 inhibitor with IC50 of 2.5 μM, and shows no inhibition to group II PAKs (PAKs 4-6).
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VEGFR inhibitor
AG-13958 (AG-013958), a potent VEGFR tyrosine kinase inhibitor, is used for treatment of choroidal neovascularization associated with age-related macular degeneration (AMD).
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HO inhibitor
Tin(IV) mesoporphyrin IX dichloride (Stannsoporfin) is a heme oxygenase (HO) inhibitor being developed for the prevention of hyperbilirubinemia in infants at risk of developing jaundice, extracted from patent WO2011103196A1.
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EGFR inhibitor
Mutant EGFR inhibitor is a potent and selective mutant EGFR inhibitor extracted from patent WO 2013014448 A1; inhibits EGFRL858R, EGFRExon 19 deletion and EGFRT790M.
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Aβ-aggregation inhibitor
MDR-1339 (DWK-1339) is an orally active and blood-brain-barrier-permeable Aβ-aggregation inhibitor, used in the research of Alzheimer's disease.
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aldose reductase inhibitor
Risarestat (CT-112), an aldose reductase inhibitor, is developed for the treatment of diabetic complications
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p38 MAPK inhibitor
FR 167653 free base, an orally active and selective p38 MAPK inhibitor, is a potent suppressor of TNF-α and IL-1β production via specific inhibition of p38 MAPK activity.
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MET inhibitor
SAR125844 is a potent, highly selective, reversible and ATP-competitive MET receptor tyrosine kinase (RTK) inhibitor, with an IC50 of 4.2 nM. Shows inhibition of MET autophosphorylation in cell-based assays.
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FabI enzyme inhibitor
MUT056399 (Fab-001) is a highly potent inhibitor of the FabI enzyme of both S. aureus and E. coli with 50% inhibitory concentration IC50s of 12 nM and 58 nM, respectively.
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platelet aggregation inhibitor
N6-(4-Hydroxybenzyl)adenosine is a inhibitor of platelet aggregation induced in vitro by collagen and their activity range was demonstrated (IC50: 6.77-141 μM).
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angiotensin-converting enzyme inhibitor
Lisinopril (MK-521) is angiotensin-converting enzyme inhibitor, used in treatment of hypertension, congestive heart failure, and heart attacks.
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insect chitinase and N- acetyl hexosaminidase inhibitor
Chitinase-IN-2 is a insect chitinase and N- acetyl hexosaminidase inhibitor and pesticide; 50 μM/20 μM compound concentration's inhibitory percentage are 98%/92% for chitinase/N- acetyl-hexosaminidase respectively.
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tubulin polymerization inhibitor
BNC105 is a tubulin polymerization inhibitor with potent antiproliferative and tumor vascular disrupting properties.
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Smo inhibitor
LEQ506 is a second-generation inhibitor of smoothened (Smo) with IC50s of 2 and 4 nM in human and mouse, respectively.
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TrioN inhibitor
ITX3 is a specific and nontoxic inhibitor of the TrioN (N-terminal GEF domain of the multidomain Trio protein) with IC50 of 76 uM; inhibits TrioN-stimulated RhoG exchange in vitro.
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NF-κB inhibitor
DMAPT (Dimethylamino Parthenolide), a water soluble analogue of Parthenolide (PTL), is an oral active NF-κB inhibitor, with a LD50 of 1.7 μM for cell population in AML cells. Has potential anti-cancer and anti-metastatic effect.
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HIF1α inhibitor
EL102 is a inhibitor of HIF1α , Which can inhibit tubulin polymerisation and decreased microtubule stability.
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anti-HIV-1 inhibitor
D77 is anti-HIV-1 inhibitor targeting the interaction between integrase and cellular LEDGF/p75.
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miR-210 inhibitor
Targapremir-210 is a potent miR-210 inhibitor with an IC50 of 200 nM in MDA-MB-231 cells. Targapremir-210 binds to the Dicer site of the miR-210 hairpin precursor. This interaction inhibits production of the mature miRNA.
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