Metabolism

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  1. CYP3A Inhibitor

    Cobicistat is a potent inhibitor of cytochrome P450 3A enzymes, including the important CYP3A4 subtype. It also inhibits intestinal transport proteins, increasing the overall absorption of several HIV medications, including atazanavir, darunavir and tenofovir alafenamide fumarate.
  2. PDE4 Inhibitor

    Apremilast, a novel PDE4 inhibitor, inhibits spontaneous production of tumour necrosis factor-alpha from human rheumatoid synovial cells and ameliorates experimental arthritis.
  3. ACE inhibitor/Beta blocker

    Moxonidine is a new-generation centrally-acting antihypertensive drug. It may have a role when thiazides, beta-blockers, ACE inhibitors and calcium channel blockers are not appropriate or have failed to control blood pressure. In addition, it demonstrates favourable effects on parameters of the insulin resistance syndrome, apparently independent of blood pressure reduction.
  4. PDE-2 Inhibitor

    BAY 60-7550 is a potent PDE2 inhibitor with IC50 values of 2.0 nM (bovine) and 4.7 nM (human).
  5. Collagen proline hydroxylase inhibitor

    Collagen proline hydroxylase inhibitor is a collagen proline hydroxylase inhibitor.
  6. DGAT1 inhibitor

    T863 is an orally active, selective and potent DGAT1 (Acyl-CoA:diacylglycerol acyltransferase 1) inhibitor that interacts with the acyl-CoA binding site of DGAT1, and inhibits triacylglycerol synthesis in cells.
  7. PC-PLC inhibitor

    D609 is a selective competitive phosphatidyl choline-specific phospholipase C (PC-PLC) inhibitor (Ki = 6.4 μM); antiviral and antitumor agent.
  8. CETP inhibitor

    Evacetrapib (LY2484595) is a potent and selective inhibitor of CETP with IC50 of 5.5 nM, elevates HDL cholesterol without increases in aldosterone or blood pressure. Phase 3.
  9. SGK1 inhibitor

    EMD638683 R-Form is the R-form of EMD638683. EMD638683 is a highly selective SGK1 inhibitor with IC50 of 3 μM.
  10. SGK1 inhibitor

    EMD638683 S-Form is the S-form of EMD638683. EMD638683 is a highly selective SGK1 inhibitor with IC50 of 3 μM.
  11. Hsp90 inhibitor

    Ganetespib is a potent, synthetic, small molecule inhibitor of Hsp90, a chaperone protein that is essential to the function of certain other proteins that drive the growth, proliferation, and survival of many different types of cancer.
  12. SCD inhibitor

    MK-8245 is a Liver-Targeted Stearoyl-CoA Desaturase (SCD) Inhibitor. MK-8245 is useful for the Treatment of Diabetes and Dyslipidemia.
  13. TPH inhibitor

    LX-1031 is a potent, orally available tryptophan 5-hydroxylase (TPH) inhibitor that reduces serotonin (5-HT) synthesis peripherally.
  14. factor Xa inhibitor

    Otamixaban(FXV 673) is an intravenous direct factor Xa inhibitor.
  15. DHFR inhibitor

    Pralatrexate is an antifolate (a folate analogue metabolic inhibitor) designed to accumulate preferentially in cancer cells.
  16. DGAT1 Inhibitor

    PF-04620110 is an orally active, selective and potent diglyceride acyltransferase-1 (DGAT1) inhibitor with IC50 of 19 nM.
  17. Autotaxin inhibitor

    PF-8380 is a potent and specific autotaxin inhibitor with an IC50 value of 2.8 nM.
  18. PDE-9 inhibitor

    PDE-9 inhibitor is useful for neurodegenerative diseases.
  19. Adenosine deaminase inhibitor

    Pentostatin is an irreversible inhibitor of adenosine deaminase (Ki = 2.5 pM).
  20. PC-PLC inhibitor

    SPK-601 (LMV-601) is an inhibitor of the phosphatidylcholine-specific phospholipase C (PC-PLC). SPK-601 also can be used as an antimicrobial agent.
  21. PDE1 inhibitor

    Vinpocetine is a Ca2+-calmodulin-dependent phosphodiesterase I (PDE1) inhibitor.
  22. Carbonic anhydrase inhibitor

    Tioxolone is an anti-acne preparation.
  23. Monoamine oxidase inhibitor

    Rasagiline is an irreversible inhibitor of monoamine oxidase used as a monotherapy in early Parkinson's disease or as an adjunct therapy in more advanced cases. It is selective for MAO type B over type A by a factor of fourteen.
  24. ACE inhibitor

    Cilazapril is a pyridazine angiotensin-converting enzyme inhibitor (ACE inhibitor) used for the treatment of hypertension and congestive heart failure.
  25. ACE inhibitor

    Fosinopril is an angiotensin converting enzyme (ACE) inhibitor used for the treatment of hypertension and some types of chronic heart failure.
  26. ACE inhibitor

    Temocapril is an ACE inhibitor.
  27. Carbonic anhydrase inhibitor

    Brinzolamide is a carbonic anhydrase inhibitor.
  28. Hsp90/SRC/COX-2 Inhibitor

    Radicicol is a potent inhibitor of Hsp90, SRC, and Cox-2
  29. MAO-B Inhibitor

    SL-251188, an oxazolidinone derivative, was characterized in baboons as a radioligand for the in vivo visualization of MAO-B using positron emission tomography (PET).
  30. Serotonin synthesis inhibitor

    LX 1606 is an orally bioavailable, small-molecule, tryptophan hydroxylase (TPH) inhibitor with potential antiserotonergic activity.
  31. Dehydrogenase Inhibitor

    CPI-613 is a racemic mixture of the enantiomers of a synthetic alpha-lipoic lipoic acid analogue with potential chemopreventive and antineoplastic activities.
  32. HMG-CoA reductase inhibitor

    Atorvastatin (Lipitor) is an inhibitor of HMG-CoA reductase used as a cholesterol-lowering medication that blocks the production of cholesterol.
  33. HMG-CoA reductase inhibitor

    Lovastatin is an inhibitor of HMG-CoA reductase with IC50 of 3.4 nM, used for lowering cholesterol (hypolipidemic agent).
  34. MAO Inhibitor

    Moclobemide is a reversible and selective inhibitor of monoamine oxidase A (MAO-A).
  35. HMG-CoA reductase inhibitor

    Pravastatin sodium is a water-soluble, competitive inhibitor of 3-hydroxy-3-methyl coenzyme A (HMG-CoA) reductase. Potently blocks cholesterol synthesis in vivo (Ki~ 1 nM) and displays cardioprotective properties.
  36. FAAH inhibitor

    LY 2183240 acts both as a potent inhibitor of the reuptake of the endocannabinoid anandamide, and as an inhibitor of fatty acid amide hydrolase (FAAH), the primary enzyme responsible for degrading anandamide.
  37. IACS-10759 is a potent inhibitor of complex I of oxidative phosphorylation (OXPHOS).
  38. Carbonic anhydrase inhibitor

    Punicalagin is an ellagitannin, a type of phenolic compounds. It is a highly active carbonic anhydrase inhibitor.
  39. Carbonic anhydrase inhibitor

    Punicalin is a highly active carbonic anhydrase inhibitor.
  40. PTEN Inhibitor

    Shikonin, a component of chinese herbal medicine, inhibits chemokine receptor function and suppresses human immunodeficiency virus type 1.
  41. HMG-CoA reductase inhibitor

    Swertiamarin has shown potential as antiatherogenic agent by inhibiting HMG-CoA reductase activity in high cholesterol fed rats.
  42. dual inhibitor of thrombin and factor Xa

    RWJ-445167 (3DP-10017) is a dual inhibitor of thrombin and factor Xa with Ki of 4.0 nM and 230 nM, respectively, exhibiting potent antithrombotic activity.
  43. MAO-A inhibitor

    CX-157 is a reversible inhibitor of monoamine oxidase-A (MAO-A) with an EC50 of 19.3?ng/mL.
  44. PDE4 inhibitor

    AN3199 is a PDE4 inhibitor with IC50 of 94.5 nM.
  45. LDHA inhibitor

    GNE-140 racemate is a racemate mixture of (R)-GNE-140 and (S)-GNE-140. (R)-GNE-140 is a potent lactate dehydrogenase A (LDHA) inhibitor.
  46. ACCA inhibitor

    TOFA (RMI14514;MDL14514) is an allosteric inhibitor of acetyl-CoA carboxylase-α (ACCA ).
  47. 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.
  48. 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.
  49. 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.
  50. δ6 desaturase inhibitor

    Selective δ6 desaturase inhibitor (IC50 = 0.2 μM in vitro).

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