Metabolism

Items 1051-1100 of 5815

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  1. androgen receptor/CYP17A1 dual inhibitor

    ODM-204 is novel nonsteroidal dual inhibitor of both androgen receptor and CYP17A1 enzyme, with IC50s of 80 nM and 22 nM, respectively.

  2. DGAT1 inhibitor

    GSK2973980A is a potent and selective Acyl-CoA:diacylglycerol acyltransferase 1 (DGAT1) inhibitor with an IC50 of 3 nM.
  3. acetylhydrolase inhibtor

    Acetylhydrolase-IN-1 is a 1-Alkyl-2-acetylglycerophosphocholine esterase (Alkylacetyl-GPC: acetylhydrolase) inhibtor.
  4. endothelial lipase inhibitor

    Endothelial lipase inhibitor-1 is a potent endothelial lipase inhibitor with an IC50 of 49 nM.
  5. IDH1 inhibitor

    IDH1 Inhibitor 1 is a potent, orally bioavailable, brain-penetrant and selective mutant IDH1 inhibitor with IC50s of 0.021 μM, 0.045 μM, and 2.52 μM for IDH1R132H, IDH1R132C, and IDH1WT, respectively. Anticancer activity.
  6. FASN inhibitor

    FASN-IN-1 is a fatty acid synthase (FASN) inhibitor extracted from patent WO2015134790A1, compound 56.
  7. Human RARβ2 receptor agonist

    AC-55649 is a potent, highly isoform-selective agonist of human RARβ2 receptor, with a pEC50 of 6.9.
  8. ACC inhibitor

    ND-646 is an orally bioavailable and steric inhibitor of acetyl-CoA carboxylase (ACC) with IC50s of 3.5 nM and 4.1 nM for recombinant hACC1 and hACC2, respectively.
  9. PPARα/ PPARγ1 agonist

    Imiglitazar (TAK559) is a potent and dual human PPARα and PPARγ1 agonist with EC50 values of 67 and 31 nM.
  10. PPARα/PPARγ dual agonist

    LJ570 is a PPARα/PPARγ dual agonist with EC50s of 1.05 and 0.12 μM, respectively.
  11. Ferroptosis inhibitor

    UAMC-3203 is a potent and selective Ferroptosis inhibitor with an IC50 of 12 nM.
  12. Fosfructose (Diphosphofructose;Esafosfan;FDP) is a cytoprotective natural sugar phosphate for the potential treatment of cardiovascular ischemia, sickle cell anemia and asthma.
  13. PKM2 inhibitor

    PKM2-IN-1 is a pyruvate kinase M2 (PKM2) inhibitor with an IC50 of 2.95 μM.
  14. PPARδ agonist

    PPARδ agonist is a PPARδ agonist extracted from patent US20180071304, compound example 10.
  15. Hsp90-Cdc37 interaction disruptors

    Hsp90-Cdc37-IN-1 is an Hsp90-Cdc37 interaction disruptors that inhibit cell migration and reverse drug resistance, with an IC50 of 140 nM.
  16. PDE2A inhibitor

    PF-05085727 is a potent, selective and brain penetrant Phosphodiesterase 2A (PDE2A) inhibitor with an IC50 of 2 nM.
  17. CS-722 Free base is a synthesized centrally acting muscle relaxant, and has a muscle relaxant activity and depressant effectson the spinal reflex.
  18. Cathepsin S inhibitor

    MIV-247 is a selective cathepsin S inhibitor with Kis of 2.1, 4.2 and 7.5 nM for human, mouse and cynomolgus monkey cathepsin S, respectively.
  19. ATX inhibitor

    ATX inhibitor 1 is a potent ATX (IC50=1.23 nM, FS-3 and 2.18 nM, bis-pNPP) inhibitor.
  20. SCD inhibitor

    T-3764518 is a novel and potent stearoyl coenzyme A desaturase (SCD) inhibitor with an IC50 of 4.7 nM.
  21. PCSK9 inhibitor

    SBC-110736 is a proprotein convertase subtilisin kexin type 9 (PCSK9) inhibitor extracted from patent WO2014150395A1, Figure 1.
  22. PDE5 inhibitor

    ER21355 is an inhibitor of phosphodiesterase 5 (PDE5), used for treatment of prostatic diseases.
  23. vitamin B1 antagonist

    Oxythiamine, an antimetabolite and a vitamin B1 antagonist, is a well-known thiamine antagonist and inhibitor of transketolase.
  24. Mito-TEMPO is a mitochondria-targeted superoxide dismutase mimetic with superoxide and alkyl radical scavenging properties.
  25. ACE inhibitor

    Rentiapril is an orally active angiotensin converting enzyme (ACE) inhibitor with antihypertensive activity.
  26. FAAH inhibitor

    FAAH-IN-1 is a fatty acid amide hydrolase (FAAH) inhibitor, with IC50s of 145 nM and 650 nM for rat and human FAAH, respectively.
  27. LOXL2 inhibitor

    PAT-1251 is a potent, selective and oral Lysyl Oxidase-Like 2 (LOXL2) inhibitor.
  28. pan HDAC inhibitor

    Tefinostat (CHR-2845) is a monocyte/macrophage-targeted pan HDAC inhibitor, cleaved into active acid CHR-2847 by the intracellular esterase human carboxylesterase-1 (hCE-1). Anti-monocytoid lineage leukaemias activity.
  29. aspartyl-tRNA synthetase inhibitor

    Asp-AMS, an analogue of aspartyl-adenylate, is an aspartyl-tRNA synthetase inhibitor and also a strong competitive inhibitor of the mitochondrial enzyme.
  30. ACDase inhibitor

    LCL521 is an acid ceramidase (ACDase) inhibitor. LCL521 also inhibits the lysosomal acid sphingomyelinase (ASMase).
  31. FASN inhibitor

    HS-79 is an enantiomer of Fasnall, which is a selective fatty acid synthase (FASN) inhibitor. HS-79 is able to inhibit the incorporation of tritiated acetate into lipids with an IC50 of 1.57 μM.
  32. PDE3 inhibitor

    LAS-31180 is an inhibitor of phosphodiesterase 3, with positive inotropic and vasodilator properties.
  33. DGAT1 inhibitor

    Diacylglycerol acyltransferase inhibitor-1 is a diacylglycerol acyltransferase (DGAT1) inhibitor.
  34. LDHA inhibitor

    GSK2837808A is a potent and selective lactate dehydrogenase A (LDHA) inhibitor with IC50s of 1.9 and 14 nM for LDHA and LDHB, respectively.
  35. GCase inhibitor

    Conduritol B epoxide is an irreversible covalently bound acid β-glucosidase (GCase) inhibitor.
  36. PDE1 inhibitor

    PDE1-IN-2 is an inhibitor of PDE1 extracted from patent WO2016/55618 A1, example 31; has IC50 values of 6, 140 and 164 nM for PDE1C, PDE1B and PDE1A, respectvely.
  37. PDE5 inhibitor

    MY-5445 is a specific phosphodiesterase type 5 (PDE5) inhibitor.
  38. Nrf2 activator

    TBHQ (tert-Butylhydroquinone) is a widely used Nrf2 activator, protects against Doxorubicin (DOX)-induced cardiotoxicity through activation of Nrf2.
  39. CYP3A inducer

    CDD3506 is used for elevating high density lipoprotein cholesterol (HDL) by inducing hepatic cytochrome P450IIIA (CYP3A) activity.
  40. CYP3A inducer

    CDD3505 is used for elevating high density lipoprotein cholesterol (HDL) by inducing hepatic cytochrome P450IIIA (CYP3A) activity.
  41. PDE-4 inhibitor

    Roflumilast Impurity E is the impurity of Roflumilast. Roflumilast(Daliresp) is a drug which acts as a selective and long-acting inhibitor of the enzyme PDE-4 with an IC50 value of 0.8 nM.
  42. sEH inhibitor

    TTPU is a soluble epoxide hydrolase (sEH) inhibitor with IC50 values of 37 and 3.7 nM for monkey and human sEH, respectively.
  43. CYP1B1 inhibitor

    DMU2139 is a potent and specific CYP1B1 inhibitor, with IC50s of 9 nM and 795 nM for CYP1B1 and CYP1A1, respectively.
  44. RARα agonist

    AGN 194078 is a selective RARα agonist with a Kd and EC50 of 3 and 112 nM, respectively.
  45. CYP1B1 inhibitor

    DMU2105 is a potent and specific CYP1B1 inhibitor, with IC50s of 10 nM and 742 nM for CYP1B1 and CYP1A1, respectively.
  46. PDE inhibitor

    Revizinone is a novel selective phosphodiesterase (PDE) inhibitor with IC50 values on this enzyme to 0.036 microM.
  47. LXRβ agonist

    LXRβ agonist-2 is a highly potent and β-selective liver X receptor (LXRβ) agonist with EC50 of 7 nM, displays 28.5-fold selectivity over LXRα (EC50=200 nM) and used in the treatment of atherosclerosis.
  48. NAMPT inhibitor

    LB-60-OF61 is a NAMPT inhibitor and is a cytotoxic compound with a selectivity towards MYC overexpressing cell lines.
  49. GCN2 inhibitor

    GCN2-IN-1 (A-92) is a potent general control nonderepressible 2 kinase (GCN2) inhibitor with an IC50 of <0.3 μM in the enzyme assay and an IC50 of 0.3-3 μM in the cell assay.
  50. ABHD6 inhibitor

    JZP-430 is a potent, highly selective, irreversible inhibitor of α/β-hydrolase domain 6 (ABHD6) with an IC50 of 44 nM, exhibits ~230-fold selectivity over fatty acid amide hydrolase (FAAH) and lysosomal acid lipase (LAL).

Items 1051-1100 of 5815

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