Metabolism

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Items 2401-2450 of 2992

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  1. irreversible inhibitor of succinate dehydrogenase

    3-Nitropropanoic acid (β-Nitropropionic acid) is an irreversible inhibitor of succinate dehydrogenase. 3-Nitropropanoic acid exhibits potent antimycobacterial activity with a MIC value of 3.3 μM.
  2. 11β-HSD1 inhibitor

    BI-187004, also known as VTP-34072, is an 11β-hydroxysteroid dehydrogenase 1 inhibitor.
  3. human cathepsin L inhibitor

    Oxocarbazate, also known as CID23631927, is an inhibitor of human cathepsin L.
  4. HSF1 inhibitor

    DTHIB is a direct and selective heat shock factor 1 (HSF1) inhibitor with a Kd of 160 nM.
  5. Cholesterol 24-hydroxylase (CH24H) inhibitor

    Soticlestat, also known as TAK 935 and OV935, is an inhibitor of the enzyme cholesterol 24-hydroxylase (CH24H).
  6. 12-Lipoxygenase (12-LOX) inhibitor

    CAY10698 is an inhibitor of 12-LO with an IC50 value of 5.1 μM.

  7. TLR7/9 inhibitor

    E6446 is an inhibitor os Toll-like receptor (TLR)7 and 9 signaling.
  8. FAAH-4 inhibitor

    WWL-154 is an inhibitor of serine hydrolase (SH) and fatty acid amide hydrolase FAAH-4.
  9. 11β-HSD1 inhibitor

    BI-135585 is a potent and selective 11β-HSD1 inhibitor.
  10. IDO1 inhibitor

    Navoximod, also known as IDO-IN-7 and NLG-1488, is an indoleamine 2,3-dioxygenase (IDO) inhibitor.
  11. Farnesyltransferase inhibitor

    CP-609754, also known as CP-609,754, LNK 754 and OSI 754, is a potent farnesyltransferase inhibitor with potential anticancer activity.
  12. PDE inhibitor

    ICI 153110 is an orally active phosphodiesterase inhibitor with both vasodilating and inotropic properties which is designed for the treatment of congestive cardiac failure.
  13. uPA system inhibitor

    UKI-1 is a novel synthetic inhibitor of the urokinase-type plasminogen activator system.
  14. NOS inhibitor

    SDMA (Symmetric dimethylarginine) is an endogenous inhibitor of nitric oxide (NO) synthase activity.
  15. IDO inhibitor

    IDO-IN-1 is a potent indoleamine 2,3-dioxygenase (IDO) inhibitor with an IC50 of 59 nM.
  16. FAAH inhibitor

    FAAH-IN-2 (O-Desmorpholinopropyl Gefitinib) is a potent FAAH(fatty acid amide hydrolase) inhibitor extracted from Patent WO/2008/100977A2.
  17. NF-κB inhibitor

    Cyclo(his-pro) (Cyclo(histidyl-proline)) is an orally active cyclic dipeptide structurally related to tyreotropin-releasing hormone. Cyclo(his-pro) could inhibit NF-κB nuclear accumulation.
  18. TPH1 Inhibitor

    Rodatristat ethyl (KAR5585) is a first-in-class oral tryptophan hydroxylase 1 (TPH1) Inhibitor with nanomolar in vitro potency. Rodatristat ethyl reduces the level of 5-HT and significantly reduces pulmonary arterial hypertension (PAH).
  19. hexokinase II inhibitor

    3-Bromopyruvic acid is a hexokinase II inhibitor, is an effective antitumor agent on the hepatoma cells.
  20. GMP inhibitor

    3-Methylxanthine, a xanthine derivative, is a cyclic guanosine monophosphate (GMP) inhibitor, with an IC50 of 920 μM on guinea-pig isolated trachealis muscle.
  21. PDE10A inhibitor

    Mardepodect (PF-2545920) is a potent, orally active and selective PDE10A inhibitor with an IC50 of 0.37 nM, with >1000-fold selectivity over other PDEs. Mardepodect can cross the blood-brain barrier.
  22. recombinant human sEH inhibitor

    GSK2256294A is a potent, reversible, tight binding inhibitor of isolated recombinant human sEH (soluble epoxide hydrolase) (IC50 = 27 pM; t1/2 = 121 min) and displays potent inhibition against the rat (IC50 = 61 pM) and murine (IC50 = 189 pM) orthologs of sEH.
  23. COX-2/5-LO inhibitor

    S-2474 is an inhibitor of COX-2 and 5-lipoxygenase (5-LO), with IC50s of 11 nM and 27 μM for COX-2 and COX-1 in human intact cells, and used as a nonsteroidal anti-inflammatory drug.
  24. PDE3 inhibitor

    NSP-805 is a potent and selective inhibitor of guinea pig cardiac phosphodiesterase 3 (PDE3), and a cardiotonic agent with vasodilator properties.
  25. IDH1 mutant inhibitor

    GSK864 is an isocitrate dehydrogenase 1 (IDH1) mutant inhibitor; inhibits IDH1 mutants R132C, R132H, and R132G with IC50 values of 8.8, 15.2 and 16.6 nM.
  26. SAH

    METTL3-14 inhibitor

    SAH is an amino acid derivative and a modulartor in several metabolic pathways. It is an intermediate in the synthesis of cysteine and adenosine. SAH is an inhibitor for METTL3-METTL14 heterodimer complex (METTL3-14) with an IC50 of 0.9 ?M.
  27. MAGL inhibitor

    KML29 is a potent and selective MAGL inhibitor with IC50 = 5.9, 15, and 43 nM in human, mouse, and rat brain proteomes, respectively.
  28. IDO inhibitor

    IDO-IN-2 is an IDO inhibitor extracted from patent WO/2015031295 A1, compound example 1, has IC50 values of 0.068 μM in HeLa cell and 0.16 μM in HEK293 cell.
  29. IDO-1 inhibitor

    PF-06840003 is a highly selective orally bioavailable IDO-1 inhibitor with IC50s of 0.41 μM, 0.59 μM, and 1.5 μM for hIDO-1, dIDO-1, and mIDO-1, respectively.
  30. PTP1B/IKK-βinhibitor and dual PPARα and PPARβ agonist

    Ertiprotafib is an inhibitor of PTP1B, IkB kinase β (IKK-β), and a dual PPARα and PPARβ agonist, with an IC50 of 1.6 μM for PTP1B, 400 nM for IKK-β, an EC50 of ~1 μM for PPARα/PPARβ.
  31. SCD inhibitor

    GSK1940029 (SCD inhibitor 1) is a stearoyl-coa desaturase (SCD) inhibitor extracted from patent WO/2009060053 A1, compound example 16.
  32. FASN inhibitor

    Desoxyrhaponticin is a stilbene glycoside from the Tibetan nutritional food Rheum tanguticum Maxim. Desoxyrhaponticin is a Fatty acid synthase (FAS) inhibitor, and has apoptotic effect on human cancer cells.
  33. CYP51 inhibitor

    Oteseconazole (VT-1161) is an orally active anti-fungal agent, potently binds to and inhibits Candida albicans CYP51 (Kd, <39 nM), shows no obvious effect on human CYP51.
  34. ACC inhibitor

    Olumacostat glasaretil is a small molecule inhibitor of acetyl coenzyme A carboxylase (ACC).
  35. SREBP inhibitor

    Nicodicosapent is a fatty acid niacin conjugate that is also an inhibitor of the sterol regulatory element binding protein (SREBP), a key regulator of cholesterol metabolism proteins such as PCSK9, HMG-CoA reductase, ATP citrate lyase, and NPC1L1.
  36. PFT inhibitor

    FTI-276 is a protein farnesyl transferase (PFT) inhibitor with IC50s of 0.9 and 0.5 nM for Plasmodium falciparum and human.
  37. phospholipase A2 inhibitor

    Varespladib methyl (A-002; LY333013) is a selective inhibitor of group II secretory phospholipase A2 (PLA2).
  38. IDO inhibitor

    IDO-IN-3 is a potent indoleamine 2,3-dioxygenase (IDO) inhibitor with an IC50 of 290 nM.
  39. LDHA inhibitor

    FX-11 (LDHA Inhibitor FX11) is a potent lactate dehydrogenase A (LDHA) inhibitor with an IC50 of 23.3 μM for HeLa cell??a Ki value of 8 μM.
  40. SREBP inhibitor

    FGH10019 is a novel sterol regulatory element-binding protein (SREBP) inhibitor with IC50 of 1 μM.
  41. DAF-9 cytochrome P450 inhibitor

    Dafadine-A, an analog of dafadine, is a novel inhibitor of DAF-9 cytochrome P450 in the nematode Caenorhabditis elegans; also inhibits the mammalian ortholog of DAF-9(CYP27A1).
  42. SGK-1 inhibitor

    SGK1-IN-1 is a highly active and selective inhibitor of SGK-1, with an IC50 of 1 nM.
  43. Farnesyl transferase inhibitor

    BMS-214662 is a potent and selective farnesyl transferase inhibitor with potent antitumor activity with an IC50 of 1.35 nM.
  44. SCD1 inhibitor

    MF-438 is a potent and orally bioavailable stearoyl-CoA desaturase 1 (SCD1) inhibitor with an EC50 of 2.3 nM for rSCD1.
  45. nuclear export receptor CRM1 inhibitor

    Leptomycin B (CI 940; LMB) is a potent inhibitor of the nuclear export of proteins. Leptomycin B inactivates CRM1/exportin 1 by covalent modification at a cysteine residue. Leptomycin B is a potent antifungal antibiotic blocking the eukaryotic cell cycle.
  46. HSP90α/HSP90β inhibitor

    TAS-116 is an oral bioavailable, ATP-competitive, highly specific HSP90α/HSP90β inhibitor (Kis of 34.7 nM and 21.3 nM, respectively) without inhibiting other HSP90 family proteins such as GRP94. TAS-116 demonstrates less ocular toxicity.
  47. CYP17 lyase inhibitor

    Seviteronel (VT-464) is a potent CYP17 lyase inhibitor(h-Lyase IC50=69 nM) that demonstrated both exceptional in vitro lyase/hydroxylase selectivity (~10-fold) and oral activity in a hamster model of androgen biosynthesis inhibition.
  48. ACC inhibitor

    Firsocostat (ND-630; GS-0976; NDI-010976) is an acetyl-CoA carboxylase (ACC) inhibitor; inhibits human ACC1 and ACC2 with IC50 values of 2.1 and 6.1 nM, respectively.
  49. CYP3A4/5 inhibitor and substrate

    Veledimex is an oral activator ligand for a proprietary gene therapy promoter system, and a moderate inhibitor of and substrate for CYP3A4/5.
  50. ACE/NEP inhibitor

    Omapatrilat is a dual inhibitor of the metalloproteases ACE and NEP with Ki values of 0.64 and 0.45 nM, respectively.

Items 2401-2450 of 2992

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