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Metabolism

Items 1-50 of 6503

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  1. A10707
    Pemetrexed disodium (Alimta)

    DHFR inhibitor

    Pemetrexed disodium is chemically similar to folic acid and is in the class of chemotherapy drugs called folate antimetabolites. It works by inhibiting three enzymes used in purine and pyrimidine synthesis?€?thymidylate synthase (TS), dihydrofolate reductase (DHFR), and glycinamide ribonucleotide formyltransferase.
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  2. A10435
    Gossypol

    dehydrogenase inhibitor

    Gossypol is a polyphenolic aldehyde that permeates cells and acts as an inhibitor for several dehydrogenase enzymes.
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  3. A11144
    TH-302 (Evofosfamide)
    TH-302 is a selectively targeting hypoxic regions of solid tumors hypoxia-activated prodrug.
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  4. A12652
    T0901317

    LXR/FXR agonist

    T0901317 is a potent and selective agonist for LXR and FXR, with EC50s of 50 nM and 5 μM, respectively
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  5. A14339
    U 73122

    Phospholipase C inhibitor

    U 73122 is a phospholipase C inhibitor. It inhibits agonist-induced platelet aggregation with IC50 values of 1-5 uM.
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  6. A13343
    Zinc Protoporphyrin

    HO-1 inhibitor

    Zinc Protoporphyrin (Zn(II)-protoporphyrin IX) is a competitive heme oxygenase-1 (HO-1) inhibitor, markedly attenuates the protective effects of Phloroglucinol (PG) against H2O2.
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  7. A14412
    ASP9521
    ASP9521 is a novel, selective, orally bioavailable inhibitor of 17??-hydroxysteroid dehydrogenase type 5 (17bHSD5, AKR1C3).
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  8. A10804
    Roflumilast

    PDE inhibitor

    Roflumilast acts as a selective, long-acting inhibitor of the enzyme PDE-4.
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  9. A11062
    Onalespib (AT13387)

    HSP90 Inhibitor

    AT13387 is a targeted inhibitor of Hsp90,inhibiting its chaperone function and promoting the degradation of oncogenic signaling proteins involved in tumor cell proliferation and survival.
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  10. A10809
    Rosiglitazone maleate

    PPAR agonist

    Rosiglitazone maleate, an antidiabetic drug, works as an insulin sensitizer, by binding to the PPAR receptors in fat cells and making the cells more responsive to insulin.
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  11. A13143
    Cilofexor

    FXR agonist

    Cilofexor (GS-9674) is a farnesoid X receptor (FXR) agonist.
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  12. A13247
    Ferrostatin-1 (Fer-1)

    ferroptosis inhibitor

    Ferrostatin-1 (Fer-1) is a potent and selective inhibitor of ferroptosis with EC50 of 60 nM.
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  13. A15554
    Epacadostat (INCB024360)

    IDO inhibitor

    Epacadostat is a potent and selective indoleamine 2,3-dioxygenase (IDO1) inhibitor with IC50 of 10 nM, Phase 2,
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  14. A10293
    Deferasirox

    Iron chelator

    Deferasirox is a rationally-designed oral iron chelator, also a cytochrome P450 3A4 inducer, Cytochrome P450 2C8 inhibitor, and Cytochrome P450 1A2 inhibitor.
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  15. A11928
    LCL-161

    Antagonist of IAPs inhibitor

    LCL161 is an orally bioavailable second mitochondrial-derived activator of caspases (SMAC) mimetic and inhibitor of IAP (Inhibitor of Apoptosis Protein) family of proteins, with potential antineoplastic activity.
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  16. A17323
    Valproic acid

    HDAC inhibitor

    Valproic acid is an HDAC inhibitor, with IC50 in the range of 0.5 and 2 mM, also inhibits HDAC1 (IC50, 400 μM), and induces proteasomal degradation of HDAC2; Valproic acid sodium salt is used in the treatment of epilepsy, bipolar disorder and prevention of migraine headaches.
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  17. A10082
    Apixaban (BMS-562247-01)

    Factor Xa inhibitor

    Apixaban is an anticoagulant for the prevention of venous thromboembolism and venous thromboembolic events.
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  18. A14317
    Edoxaban (tosylate Monohydrate)

    Factor Xa inhibitor

    Edoxaban is a selective factor Xa inhibitor with Ki of 0.561 nM
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  19. A10741
    (E/Z)-Polydatin ((E/Z)-Piceid)

    PLA inhibitor

    Polydatin protects cerebral cells from ischemic damages via improvement of microcirculation and inhibition of platelet aggregation. In addition, polydatin inhibits ICAM-1 expression in endothelial cells stimulated by lipopolysaccharide; it also attenuates adhesion between white blood cells and endothelial cells.
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  20. A18420
    IDH1 Inhibitor 2

    IDH1 inhibitor

    DH1 Inhibitor 2 is a potent IDH1 inhibitor via a direct covalent modification of His315, with an IC50 of 110 nM.
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  21. A11402
    Ganetespib (STA-9090)

    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.
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  22. A11186
    Turofexorate isopropyl (WAY-362450)

    FXR agonist

    WAY-362450 is a highly potent, selective, and orally bioavailable farnesoid X receptor (FXR) agonist (EC50: 4 nM, eff=149%).

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  23. A11141
    GW4064

    FXR agonist

    GW4064 is a selective, non-steroidal farnesoid X receptor (FXR) agonist (EC50 = 15 nM).
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  24. A14325
    LP-533401

    Tph1 inhibitor

    LP-533401 is a small molecule inhibitor of Tph1.
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  25. A15865
    RSL3

    Ferroptosis inhibitor

    RSL3 is a ferroptosis activator in a VDAC-independent manner,exhibiting selectivity for tumor cells bearing oncogenic RAS.
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  26. A12769
    Zofenopril calcium

    ACE inhibitor

    Zofenopril calcium is an angiotensin-converting enzyme ACE inhibitor.
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  27. A13309
    GSK-650394

    SGK1 inhibitor

    GSK 650394 is a glucocorticoid- and serum-regulated kinase 1 (SGK1) inhibitor which displays antiproliferative properties against the LNCaP prostate carcinoma cell line.
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  28. A12105
    Punicalagin

    Carbonic anhydrase inhibitor

    Punicalagin is an ellagitannin, a type of phenolic compounds. It is a highly active carbonic anhydrase inhibitor.
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  29. A10454
    Hordenine

    MAO-B inhibitor

    Hordenine is a phenethylamine alkaloid with antibacterial and antibiotic properties.
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  30. A10216
    Cilomilast (SB-207499)

    PDE-4 inhibitor

    Cilomilast is orally active and acts as a selective Phosphodiesterase-4 inhibitor with antiinflammatory effects that target bronchoconstriction, mucus hypersecretion, and airway remodeling associated with COPD.
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  31. A11019
    Ibudilast (KC-404)

    PDE Inhibitor

    Ibudilast, a pharmacologic phosphodiesterase inhibitor, prevents human immunodeficiency Virus-1 Tat-Mediated activation of microglial cells.
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  32. A11981
    Troglitazone

    PPARγ agonist

    Troglitazone is a selective PPARγ receptor agonist (EC50 values are 780 and 555 nM at murine and human PPARγ receptors respectively).
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  33. A18765
    3-Methyluridine
    3-Methyluridine is a modified nucleoside of cellular RNA.
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  34. A13502
    Z-FL-COCHO (LY3000328)

    Cathepsin S inhibitor

    Z-FL-COCHO (LY3000328) is a novel Cathepsin S inhibitor.

     
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  35. A11768
    Radicicol

    Hsp90/SRC/COX-2 Inhibitor

    Radicicol is a potent inhibitor of Hsp90, SRC, and Cox-2
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  36. A11820
    Prostaglandin E1 (PGE1)
    Prostaglandin E1 (PGE1) is the theoretical cyclooxygenase metabolite of dihomo-γ-linolenic acid (DGLA), but it is virtually undetectable in the plasma of normal humans or other animals. The IC50 of PGE1 for the inhibition of ADP-induced human platelet aggregation is 40 nM.
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  37. A13617
    FP-Biotin
    FP-Biotin is a biotinylated organophosphorus agent. It could be useful for identifying proteins that react with organophosphorus toxicants (OP).
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  38. A18874
    HSP27 inhibitor J2

    HSP27 inhibitor

    HSP27 inhibitor J2 (J2) is a HSP27 inhibitor, which significantly induces abnormal HSP27 dimer formation and inhibits a production of HSP27 giant polymers, thereby having an effect of inhibiting a chaperone function of the HSP27 and reducing a cell protection function thereof.
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  39. A11074
    PF-04929113 (SNX-5422)

    Hsp90 inhibitor

    PF-04929113 (SNX-5422) is orally bioavailable heat shock protein 90 (Hsp90) inhibitor.
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  40. A13998
    DMOG

    HIF-PH inhibitor

    DMOG is a cell permeable, competitive inhibitor of HIF-PH. It acts to stabilize HIF-1α expression at normal oxygen tensions in cultured cells, at concentrations between 0.1 and 1 mM.
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  41. A10660
    NVP-BEP800

    HSP90 Inhibitor

    NVP-BEP800 is a novel, fully synthetic, orally bioavailable inhibitor that binds to the NH2-terminal ATP-binding pocket of Hsp90.
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  42. A11195
    KW-2478

    HSP90 inhibitor

    KW-2478 is an agent that targets the human heat-shock protein 90 (Hsp90) with potential antineoplastic activity.

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  43. A13743
    Atorvastatin

    HMG-CoA reductase inhibitor

    Atorvastatin is an HMG-CoA reductase inhibitor (IC50 = 154 nM) that is effective in treating hypercholesterolemia and certain dyslipidemias.
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  44. A15860
    17-Hydroxyprogesterone

    Steroid Hormone

    17-Hydroxyprogesterone is an endogenous progestogen as well as chemical intermediate in the biosynthesis of other steroid hormones, including the corticosteroids and the androgens and the estrogens.
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  45. A10396
    Fludarabine (Fludara)

    STAT inhibitor

    Fludarabine or fludarabine phosphate (Fludara) is a chemotherapy drug used in the treatment of hematological malignancies (cancers of blood cells such as leukemias and lymphomas) .Fludarabine inhibits DNA synthesis by interfering with ribonucleotide reductase and DNA polymerase. It is active against both dividing and resting cells.
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  46. A10225
    Clarithromycin

    cytochrome P4503A4 inhibitor

    Clarithromycin is a macrolide antibiotic. It prevents bacteria from growing by interfering with their protein synthesis.
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  47. A11397
    Evacetrapib (LY2484595)

    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.
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  48. A16283
    Imeglimin hydrochloride

    oxidative phosphorylation blocker

    Imeglimin is the first in a new tetrahydrotriazine-containing class of oral antidiabetic agents, the glimins. It has been shown to act on the liver, muscle and pancreatic ??-cells to uniquely target the key defects of type 2 diabetes.
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  49. A11172
    Nepicastat HCl

    DBH inhibitor

    Nepicastat hydrochloride is an inhibitor of dopamine beta-hydroxylase, an enzyme that catalyzes the conversion of dopamine to norepinephrine.

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  50. A10292
    Decitabine

    DNA Methyltransferase Inhibitors

    Decitabine is a hypomethylating agent.It hypomethylates DNA by inhibiting DNA methyltransferase.
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  1. Inhibitor 2992items
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  5. Modulator 8items
  6. Blocker 2items
  7. Degrader 1item
  8. Inducer 10items
  9. Substrate 6items
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  1. STK 8items
  2. WNK 2items
  3. DCLK 1item
  4. GCN 3items
  5. GAK 2items
  6. SRPK 3items
  7. PASK 1item
  8. BUB1 4items
  9. Tyk2 1item