Membrane Transporters-Ion Channels

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  1. VDAC1/Apoptosis inhibitor

    NSC 15364 is an inhibitor of VDAC1 oligomerization and apoptosis.
  2. glutamine transporter ASCT2 inhibitor

    GPNA hydrochloride is a well known substrate of the enzyme γ-glutamyltransferase (GGT). GPNA hydrochloride is a specific glutamine (Gln) transporter ASCT2 inhibitor.
  3. gastric H+/K+ ATPase inhibitor

    Soraprazan is a reversible, and fast-acting inhibitor of gastric H+/K+ ATPase.
  4. Proton Pump inhibitor

    Linaprazan (AZD0865) inhibits gastric H+,K+-ATPase by K+-competitive binding. (IC50: 1.0 ± 0.2 μM) It is a acid-suppressing agents with rapid onset of action and potent acid inhibition.
  5. BCRP inhibitor

    (S)-ML753286 is a breast cancer resistance protein (BCRP) inhibitor with an IC50 of 0.6 μM on BCRP efflux transporter.
  6. SGLT1/SGLT2 inhibitor

    LX2761 is chemically stable and potent inhibitor against sodium-dependent glucose cotransporter 1 (SGLT1) and SGLT2 in vitro with IC50s of 2.2 nM and 2.7nM for hSGLT1 and hSGLT2, but displays specific SGLT1 inhibition in the gastrointestinal (GI) tract.
  7. TRPM8 inhibitor

    BCTC is a potent and specific inhibitor of transient receptor potential cation channel subfamily M member 8 (TRPM8) in prostate cancer (PCa) DU145 cells.
  8. CFTR inhibitor

    (R)-BPO-27 is a potent CFTR inhibitor with an IC50 of 4 nM.
  9. Na+-dependent glutamate transporter inhibitor

    MPDC is a potent and competitive inhibitor of the Na+-dependent high-affinity glutamate transporter in forebrain synaptosomes.
  10. TRPC6 inhibitor

    SAR7334 is a potent and specific TRPC6 inhibitor, inhibiting TRPC6 currents with IC50 of 7.9 nM.
  11. BTS

    Myosin S1 ATPase Inhibitor

    BTS is a potent inhibitor of Ca2+-stimulated myosin S1 ATPase (IC50 ~ 5 μM) and reversibly blocks the gliding motility.
  12. KCC2 inhibitor

    VU 0240551 is a small molecule inhibitor of the neuronal K-Cl cotransporter, KCC2 (IC50 = 560 nM for K+ uptake assay in KCC2-overexpressing cells).
  13. gastric H+/K+-ATPase inhibitor

    Tegoprazan, a potassium-competitive acid blocker, is a potent, oral active and highly selective inhibitor of gastric H+/K+-ATPase that could control gastric acid secretion and motility, with IC50 values ranging from 0.29-0.52 μM for porcine, canine, and human H+/K+-ATPases in vitro.
  14. Calcium Channel Inhibitor

    Gabapentin enacarbil (XP-13512) is a prodrug for the anticonvulsant and analgesic drug gabapentin.
  15. Potassium Channel inhibitor

    Azimilide(NE-10064) is a class III antiarrhythmic compound, inhibits I(Ks) and I(Kr) in guinea-pig cardiac myocytes and I(Ks) (minK) channels expressed in Xenopus oocytes.
  16. IBAT inhibitor

    Elobixibat is a potent ileal bile acid transporter (IBAT) inhibitor with IC50 values of 0.53 ?? 0.17 nM, 0.13 ?? 0.03 nM, and 5.8 ?? 1.6 nM for human IBAT, mouse IBAT, and canine IBAT.
  17. 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.
  18. ROMK inhibitor

    MK-7145 is a ROMK inhibitor, with an IC50 of 0.045 μM.
  19. dual NE/DA transporter inhibitor

    Centanafadine is dual norepinephrine (NE)/dopamine (DA) transporter inhibitor, also inhibits serotonin transporter, with IC50s of 6 nM, 38 nM and 83 nM for human NE, DA and serotonin transporter , respectively.
  20. URAT1 inhibitor

    Verinurad (RDEA3170) is a highly potent and specific URAT1 inhibitor with an IC50 of 25 nM.
  21. Nav1.7 inhibitor

    Nav1.7 inhibitor is a potent Nav1.7 inhibitor.
  22. calcium channel inhibitor

    Bay-K-8644 (R)-(+)- is a calcium channel inhibitor. Bay-K-8644 (R)-(+)- inhibits Ba2+ currents (IBa) (IC50=975 nM).
  23. P-glycoprotein inhibitor

    Encequidar (HM30181; HM30181A) is a potent and selective inhibitor of P-glycoprotein.
  24. Serotonin reuptake inhibitor (SSRI)

    Escitalopram is a selective serotonin reuptake inhibitor (SSRI) with Ki of 0.89 nM.
  25. Sodium Channel Nav1.7 inhibitor

    Funapide (TV 45070; XEN402) is a potent Sodium Channel Nav1.7 inhibitor.
  26. H+/K+-ATPase inhibitor

    Picoprazole is a specific inhibitor of H+/K+-ATPase with IC50 of 3.1??0.4 μM.
  27. NHE1 inhibitor

    BI-9627 is a sodium-hydrogen exchanger isoform 1 (NHE1) inhibitor with an EC50 of 31 nM.
  28. hERG potassium channel inhibitor

    Cisapride(R 51619) is a nonselective 5-HT4 receptor agonist, it is also a potent hERG potassium channel inhibitor.
  29. potassium channel inhibitor

    VU591 is a potent, selective renal outer medullary potassium channel (ROMK or Kir1.1) inhibitor, with an IC50 of 0.24 μM.
  30. HCN channels inhibitor

    Zatebradine (UL-FS-49 (free base); UL-FS-49CL (free base)) is a potent inhibitor of hyperpolarization-activated cyclic nucleotide-gated (HCN) channels with an IC50 value of 1.96 ?M.
  31. TRPP3 channel inhibitor

    EIPA hydrochloride (L593754 hydrochloride) is a TRPP3 channel inhibitor with an IC50 of 10.5 μM. EIPA also inhibits Na+/H+-exchanger (NHE) and macropinocytosis.
  32. TRPC6 inhibitor

    DS88790512 is a potent, selective, and orally bioavailable TRPC6 inhibitor with an IC50 of 11 nM.
  33. CRM1 inhibitor

    CBS9106 (SL-801) is a reversible oral CRM1 inhibitor with CRM1 degrading and antitumor activities.
  34. NaV1.7 inhibitor

    GNE-131 is a potent and selective inhibitor of human sodium channel NaV1.7, with an IC50 of 3 nM.
  35. NCX inhibitor

    SN 6 is a selective Na+/Ca2+ exchanger (NCX) inhibitor, and inhibits 45Ca2+ uptake by NCX1, NCX2, and NCX3, with IC50s of 2.9, 16, and 8.6 μM, respectively.
  36. serotonin-norepinephrine reuptake inhibitor

    Nitroxazepine is a tricyclic antidepressant (TCA) for the treatment of depression. Nitroxazepine acts as a serotonin-norepinephrine reuptake inhibitor.
  37. MRP1/Pgp inhibitor

    Reversan (CBLC4H10) is a potent and nontoxic multidrug resistance-associated protein 1 (MRP1) and P-glycoprotein (Pgp) inhibitor.
  38. GLT-1/EAAT2 reuptake inhibitor

    WAY-213613 is a potent, selective nonsubstrate reuptake inhibitor of GLT-1/EAAT2 with IC50 of 85 nM EAAT2.
  39. ROMK inhibitor

    VU591 hydrochloride is a potent, selective renal outer medullary potassium channel (ROMK or Kir1.1) inhibitor, with an IC50 of 0.24 μM.
  40. SERT inhibitor

    DSP-1053 is a potent Serotonin Transporter (SERT) (Ki=1.02 nM) inhibitor with partial 5-HT1A receptor (Ki=5.05 nM) agonistic activity.
  41. SOCE inhibitor

    SOCE inhibitor 1 is a store-operated calcium entry (SOCE) inhibitor with an IC50 of 4.4 μM.
  42. Nav1.7 inhibitor

    PF-05241328 is a potent and selective inhibitor of human Nav1.7 voltage-dependent sodium channels (Nav1.7), with an IC50 of 31 nM.
  43. ENT1 inhibitor

    Draflazine (R-75231) is a ENT1 inhibitor.
  44. TRPC3 inhibitor

    Pyr3 is a selective inhibitor of transient receptor potential canonical channel 3 (TRPC3), with an IC50 of 700 nM for TRPC3-mediated Ca2+ influx.
  45. ABCG2 inhibitor

    ML230 (CID44640177; SID 88095709) is a selective inhibitor of ATP-binding cassette (ABC) transporter ABCG2, and 36-fold selective for ABCG2 over ABCB1 with EC50s values of 0.13 μM and 4.65 μM, respectively.
  46. tropomyosin inhibitor

    ATM-3507 is a potent tropomyosin inhibitor with IC50s from 3.83-6.84 μM in human melanoma cell lines.
  47. broad-spectrum arenavirus inhibitor

    ST-193 is a potent broad-spectrum arenavirus inhibitor; inhibits Guanarito, Junin, Lassa and Machupo virus with IC50 values of 0.44, 0.62, 1.4 and 3.1 nM, respectively.
  48. proton pump inhibitor

    Bamaquimast is an inhibitor of proton pump extracted from patent US2005165041, example 138.
  49. anion conductance inhibitor

    NS1652 is a reversible anion conductance inhibitor, blocks chloride channel, with an IC50 of 1.6 μM in human and mouse red blood cells.
  50. MCT1 inhibitor

    BAY-8002 is a potent, selective, orally active inhibitor of monocarboxylate transporter 1 (MCT1), with an IC50 of 85 nM in the MCT1-expressing DLD-1 cells, displays excellent selectivity against MCT4. Anti-tumor activity.

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