Metabolism

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  1. PDE3 inhibitor

    SDZ-MKS 492 (MKS 492) is a selective type III isozyme inhibitor of cyclic nucleotide phosphodiesterase, effective in allergic bronchoconstriction and platelet activating factor (PAF) or LTB4-induced inflammatory reactions in animals.
  2. APT-2 inhibitor

    ML349 is a potent and specific acyl protein thioesterase 2 (APT-2) inhibitor with a Ki of 120 nM. ML349 is also an inhibitor of LYPLA2 with an IC50 of 144 nM.
  3. CYP3A4 enzyme inhibitor

    Bergaptol is a hydroxylated psoralen that acts as a potent inhibitors of debenzylation activity of CYP3A4 enzyme with an IC50 value of 24.92 uM. Recent studies suggest that it may have antiproliferative and anticancer properties.
  4. δ6 desaturase inhibitor

    Selective δ6 desaturase inhibitor (IC50 = 0.2 μM in vitro).
  5. Carbonic anhydrase inhbitor

    Indisulam (E7070) is a carbonic anhydrase inhbitor, is also a novel synthetic sulfon-amide that targets the G1 phase of the cell cycle.
  6. FPTase inhibitor

    Lonafarnib (SCH 66336) is a selectively FPTase inhibitor for H-ras, K-ras-4B and N-ras with IC50 of 1.9 nM, 5.2 nM and 2.8 nM, respectively.
  7. FTase inhibitor

    FTI 276 is an inhibitor that inhibits farnesyltransferase (FTase) (IC50 = 0.5 nM). Inhibits H-Ras and K-Ras processing in whole cells (IC50 values are 0.1 and 10 μM respectively) and disrupts constitutive H-Ras-specific actvation of MAPK. Causes significant antiproliferative effects in human malignant glioma cells and many other tumor cell lines.
  8. GAPDH inhibitor

    CGP 3466B maleate is an orally active glyceraldehyde-3-phosphate dehydrogenase (GAPDH) inhibitor.
  9. HSP70 Inhibitor

    Occupies mortalin-2 (mot-2), a member of the Hsp70 family, at its p53 binding site and enables p53 translocation to the nucleus. Selectively cytotoxic; causes growth arrest of cancer cells in culture. Also inhibits telomerase activity and cross-links F-actin.
  10. dual FAAH/MAGL inhibitor

    JZL195 is a selective and efficacious dual FAAH/MAGL inhibitor with IC50 of 13 nM and 19 nM for mouse brain FAAH and MAGL respectively.
  11. FAAH inhibitor

    JNJ 1661010 is a selective and reversible inhibitor of fatty acid amide hydrolase (FAAH) (IC50 = 12nM).
  12. Dihydroorotate Dehydrogenase Inhibitor

    Brequinar is an inhibitor of dihydroorotate dehydrogenase, an enzyme that is required for de novo pyrimidine biosynthesis.
  13. 5-LPO inhibitor

    ICI 211965 (ZM-211965) is a selective and orally potent 5-Lipoxygenase (5-LPO) inhibitor.
  14. DGAT1 inhibitor

    Pradigastat (LCQ-908) is a diacylglycerol acyltransferase 1 (DGAT1) inhibitor.
  15. Cathepsin K inhibitor

    L-873724 is a potent, orally bioavailable, selective and reversible non-basic cathepsin K inhibitor.
  16. squalene synthetase inhibitor

    YM-53601 free base is a squalene synthetase inhibitor which suppresses lipogenic biosynthesis and lipid secretion in rodents.
  17. NAMPT inhibitor

    CHS-828 is a potent inhibitor of NAD+ biosynthesis enzyme NAMPT with IC50 <25 nM.
  18. FXa Inhibitor

    Betrixaban is an anticoagulant drug which acts as a direct factor Xa inhibitor. It is potent, orally active and highly selective for factor Xa, being selected from a group of similar compounds for its low hERG affinity.
  19. CYP3A4 inhibitor

    PF 4981517 is a potent and selective inhibitor of CYP3A4 (IC50 values are 0.03, 17 and 70 μM for CYP3A4, CYP3A5 and CYP3A7 respectively).
  20. PDE 3/4 inhibitor

    Zardaverine is a phosphodiesterase inhibitor, selective for PDE3 and 4 (IC50 values are 0.5 and 0.8 uM respectively).
  21. platelet PDE inhibitor

    Ro 15-2041 is a selective platelet phosphodiesterase inhibitor with antithrombotic properties.
  22. CRM1 inhibitor

    KPT-330 inhibitor of CRM1 (XPO1)-mediated nuclear export has selective anti-leukaemic activity in preclinical models of T-cell acute lymphoblastic leukaemia and acute myeloid leukaemia.
  23. Mitochondrial respiratory chain inhibitor

    Sulfosuccinimidyl oleate (Sulfo-N-succinimidyl oleate) is a long chain fatty acid that inhibits fatty acid transport into cells. Sulfosuccinimidyl oleate is a potent and irreversible inhibitor of mitochondrial respiratory chain.
  24. DGAT2 inhibitor

    PF-06424439 is an oral, potent and selective imidazopyridine diacylglycerol acyltransferase 2 (DGAT2) inhibitor with an IC50 of 14 nM.
  25. PDE5 inhibitor

    Avanafil is a PDE5 Inhibitor for the Treatment of Erectile Dysfunction
  26. CYP17 inhibitor

    CYP17-IN-1 (compound 9c) is a potent and orally active CYP17 inhibitor against rat and human CYP17 with IC50s of 15.8 and 20.1 nM.
  27. PDE5 inhibitor

    Sildenafil, one of the selective phosphodiesterase-5 (PDE5) inhibitors(IC50= 5.22 nM), is considered the best treatment for erectile dysfunction.
  28. HSP90 inhibitor

    Debio 0932 is a novel heat shock protein 90 (HSP90) inhibitor with strong affinity for HSP90 alpha/beta, high oral bioavailability and potent anti-proliferative activity against a broad range of cancer cell lines (with a mean IC50 of 220 nmol/L), including many non-small cell lung cancer (NSCLC) cell lines which are resistant to standard-of-care (SOC) agents.
  29. DHFR inhibitor

    Pemetrexed is a novel antifolate with multiple targets
  30. MAGL Inhibitor

    JZL184 is a potent and selective monoacylglycerol lipase (MAGL) inhibitor. Blocks hydrolysis of the endocannabinoid 2-arachidonyl glycerol (2-AG) in vivo in the mouse brain (IC50 = 8 nM).
  31. PDE-4-D inhibitor

    CP671305 is a potent, orally active, selective inhibitor of phosphodiesterase-4-D, and possesses high activities.
  32. HSF1 activation inhibitor

    Rocaglamide (Rocaglamide A) is isolated from the genus Aglaia and can be used to treat coughs, injuries, asthma and inflammatory skin diseases. Rocaglamide is a potent inhibitor of NF-κB activation in T-cells. Rocaglamide is a potent and selective heat shock factor 1 (HSF1) activation inhibitor with an IC50 of ~50 nM. Rocaglamide inhibits the function of the translation initiation factor eIF4A. Rocaglamide also has anticancer properties in leukemia.
  33. ACE inhibitor

    Zofenopril calcium is an angiotensin-converting enzyme ACE inhibitor.
  34. PDE4 inhibitor?€?

    AN2728 is a topically administered, boron-containing, anti-inflammatory compound that inhibits PDE4 activity and thereby suppresses the release of TNFalpha, IL-12, IL-23 and other cytokines
  35. Hydroxylase Inhibitor

    Ro 61-8048 is a potent and competitive kynurenine 3-hydroxylase inhibitor (Ki = 4.8 nM, IC50 = 37 nM).
  36. HSP90 Inhibitor

    HSP990 is an orally bioavailable inhibitor of human heat-shock protein 90 (Hsp90) with potential antineoplastic activity.
  37. factor Xa inhibitor

    Razaxaban is a selective, potent, and orally bioavailable inhibitor of coagulation factor Xa.
  38. factor Xa inhibitor

    Letaxaban, also known as TAK-442, is a potent, selective, and orally active factor Xa inhibitor, which is a tetrahydropyrimidin-2(1H)-one derivative. TAK-442 inhibited endogenous FXa activity in platelet-poor human [half-maximal inhibitory concentration (IC(50)): 53 nM, TAK-442] and rat (IC(50): 32 nM, TAK-442) plasma.
  39. COX/5-LOX inhibitor

    Tepoxalin is a dual cyclooxygenase/5-lipoxygenase inhibitor of arachidonic acid metabolism with potent anti-inflammatory activity and a favorable gastrointestinal profile
  40. IDH1 inhibitor

    AGI-5198, also know as IDH-C35, is the a very potent and selective mutant IDH1 inhibitor that was shown to potential anticancer activity.
  41. IDH2 R140Q inhibitor

    AGI-6780 is a potent, selective inhibitor of mutant IDH2 with an IC50 value of 23 nM.
  42. PDE inhibitor

    Forskolin is a cell-permeable diterpenoid that possesses anti-hypertensive, positive inotropic, and adenylyl cyclase activating properties.
  43. IDH1 R132H inhibitor

    IDH-C227 is a potent and selective IDH1 R132H inhibitor.
  44. MAO-A inhibitor

    Salsolidine is a tetrahydroisoquinoline alkaloid, acts as a stereoselective competitive MAO A inhibitor.
  45. PDE9A inhibitor

    BI-409306 is a potent and selective PDE9A inhibitor, with an IC50 of 52 nM.
  46. CRM1 Inhibitor

    KPT185 is a selective CRM1 inhibitor. KPT-185 significantly inhibits leukemia cell proliferation with IC50 ranging from 100 nM to 500 nM, and induces cell-cycle arrest and apoptosis of AML cell lines and primary AML blasts.
  47. HIF inhibitor

    BAY 87-2243, a highly potent and selective inhibitor of hypoxia-induced gene activation has antitumor activities by inhibition of mitochondrial complex I.
  48. IDO1 inhibitor

    INCB024360 is an orally available hydroxyamidine and inhibitor of indoleamine 2,3-dioxygenase (IDO1), with potential immunomodulating and antineoplastic activities.
  49. PDE2A inhibitor

    PF-05180999 is a phosphodiesterase 2A (PDE2A) inhibitor, with an IC50 of 1.6 nM.
  50. oxidative phosphorylation inhibitor

    Gboxin is an oxidative phosphorylation inhibitor that targets glioblastoma. Gboxin inhibits the activity of F0F1 ATP synthase. Antitumour activity.

Items 151-200 of 756

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