GPCR/G Protein

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  1. CXCR2 ligand

    SRT3109 is a CXCR2 ligand for use in the treatment of chemokine mediated diseases and conditions.
  2. D2 receptor antagonist

    Adoprazine is part of the Antidepressant Agent group
  3. glucagon receptor antagonist

    Glucagon receptor antagonists-1 is a highly potent glucagon receptor antagonist.
  4. Glucagon receptor antagonist

    Glucagon receptor antagonists-2 is a highly potent glucagon receptor antagonist.
  5. Glucagon receptor antagonist

    Glucagon receptor antagonists-3 is a highly potent glucagon receptor antagonist.
  6. mGlu2 agonist

    LY2979165 is a mGlu2 agonist.
  7. GCGR inhibitor

    MK 0893 is glucagon receptor antagonist as antidiabetic agents.
  8. ETA receptor antagonist

    Sitaxsentan (IPI 1040; TBC-11251) is a selective endothelin A (ETA) receptor antagonist. Antihypertensive. Sitaxsentan is used in treatment of chronic heart failure.
  9. PGF2α/LTB4 production inhibitor

    Darbufelone mesylate (CI-1004 mesylate) is a dual inhibitor of cellular PGF2α and LTB4 production. Darbufelone potently inhibits PGHS-2 (IC50 = 0.19 μM) but is much less potent with PGHS-1 (IC50= 20 μM).
  10. FFAR1/GPR40 agonist

    LY2922470 is a potent, selective and orally available agonist of the G protein-coupled receptor 40 (GPR40), with EC50s of 7 nM, 1 nM and 3 nM for human GPR40, mouse GPR40 and rat GPR40, respectively.

  11. antagonist of melanin concentrating hormone receptor 1

    MCHr1 antagonist 2 is an antagonist of melanin concentrating hormone receptor 1, with an IC50 of 65 nM; MCHr1 antagonist 2 also inhibits hERG, with an IC50 of 4.0 nM in IMR-32 cells.
  12. Nur77 LBD Antagonist

    TMPA is a novel small molecule that binds to orphan Nuclear Receptor Nur77 with high affinity (Kd = 1.45 ?? 0.35 μM), and interferes with the Nur77-LKB1 interaction.
  13. Sigma-2 receptor agonist

    Siramesine Hydrochloride is a selective sigma-2 receptor agonist, which has been shown to trigger cell death of cancer cells and to exhibit a potent anticancer activity in vivo.
  14. sigma-1 receptor antagonist

    S1RA is a selective sigma-1 receptor antagonist, with a reported binding affinity of Ki = 17.0 ?? 7.0 nM, selective over the sigma-2 receptor and against a panel of other 170 receptors, enzymes, transporters and ion channels.
  15. 5-HT6R antagonist

    Lu AE58054 is a potent and selective 5-HT6 receptor antagonist.
  16. beta2-adrenergic agonist

    Arformoterol tartrate is a beta2-adrenergic agonist
  17. mGluR2 PAM

    JNJ-40411813 is a novel mGluR2 PAM.
  18. 5-HT1A receptor agonist

    Lesopitron dihydrochloride is a full and selective 5-HT1A receptor agonist with IC50 of 125 nM in rat hippocampal membranes.
  19. GPR109A agonist

    MK-6892 is a potent, selective, and full agonist for the high affinity nicotinic acid (NA) receptor GPR109A.K i and GTPγS EC 50 of MK-6892 on the Human GPR109A is 4 nM and 16 nM, respectively.
  20. FFA1/GPR40 Agonist

    TUG-770 is a Highly Potent Free Fatty Acid Receptor 1 (FFA1/GPR40) Agonist for Treatment of Type 2 Diabetes.
  21. Sigma-2 receptor agonist

    Anti-cancer agent siramesine is a lysosomotropic detergent that induces cytoprotective autophagosome accumulation.
  22. Histamine H2-receptor antagonist

    Metiamide is a histamine H2-receptor antagonist developed from another H2 antagonist, burimamide. It was an intermediate compound in the development of the successful anti-ulcer drug cimetidine.
  23. D2 agonist

    Naxagolide is a dopamine D2-receptor agonist which is used for the treatment of extrapyramidal disorders.
  24. dopamine D2-receptor agonist

    ent Naxagolide Hydrochloride is a dopamine D2-receptor agonist which is used for the treatment of extrapyramidal disorders. This compound is an antiparkinsonian drug.
  25. ultra-long-acting β??? adrenoreceptor agonist

    Vilanterol is a novel and selective agonist of Beta2-AR with a PEC50 value of 10.37??0.05.
  26. MK-447 is a free radical scavenger, also a nonsteroidal antiinflammatory agent, and enhances the formation of the endoperoxide, PGH2, and other prostaglandins.
  27. Urotensin-II receptor antagonist

    Palosuran is a new potent and specific antagonist of the human UT receptor with an IC50 of 3.6??0.2 nM.
  28. A1 adenosine receptor agonist

    Tecadenoson (CVT-510) is a selective A1 adenosine receptor agonist.
  29. S1PR1 inhibitor

    KRP-203 is a selective Sphingosine-1-phosphate receptor agonist. It shows to reduce peripheral lymphocyte infiltration and to prolong survival in rat transplant models.
  30. PAF receptor antagonist

    Foropafant (SR27417) highly potent, competitive, selective and orally active antagonist of platelet-activating factor (PAF) receptor.
  31. prostanoid DP-receptor (DP1) agonist

    BW 245C is a prostanoid DP-receptor (DP1) agonist, used to treat stroke.
  32. CRF1 receptor antagonist

    R121919 is a potent small-molecule CRF1 receptor antagonist.
  33. dopamine β-hydroxylase (DBH) inhibitor

    Zamicastat (BIA 5-1058) is a dopamine β-hydroxylase (DBH) inhibitor that could cross the blood-brain barrier (BBB) and cause central as well as peripheral effects.
  34. dopamine D3 Receptor (DRD3) antagonist

    GSK598809 is a potent and selective dopamine D3 Receptor (DRD3) antagonist, with a pKi of 8.9.
  35. Beta-1 adrenergic receptor blocker

    Nebivolol is a selective inhibits Beta-1 adrenergic receptor with IC50 of 0.8 nM
  36. Guanylate cyclase C agonist

    Linaclotide is a peptide agonist of the guanylate cyclase 2C.
  37. bradykinin B1 receptor antagonist

    SSR240612 is a new antagonist of the bradykinin B1 receptor.
  38. norepinephrine reuptake inhibitor

    Edivoxetine HCl is a drug which acts as a selective norepinephrine reuptake inhibitor
  39. Adenosine Receptor agonist

    Capadenoson is a selective agonist of adenosine-A1 receptor.
  40. CB2 receptor agonist

    Tedalinab (GRC-10693) is a drug developed for the treatment of osteoarthritis and neuropathic pain, which acts as a potent and selective cannabinoid CB2 receptor agonist. It has a very high selectivity of 4700x for CB2 over the related CB1 receptor, has good oral bioavailability and has shown promising safety results and effective analgesic and antiinflammatory actions in early clinical trials.
  41. Dopamine D2 Receptor Antagonist

    SB269652 is a new chemical probe that can differentiate D2R monomers from dimers or oligomers depending on the observed pharmacology.
  42. Adenosine A Receptor antagonist

    CGS 15943 is a potent, non-selective Adenosine A Receptor antagonist. It is orally active in vivo.
  43. Capromorelin functions as a growth hormone secretagogue and ghrelin mimetic which causes the body to secrete human growth hormone in a way usually seen at puberty and in young adulthood.
  44. Endothelin antagonist receptor

    Atrasentan hydrochloride is an endothelin antagonist receptor (IC50=0.0551 nM, ETA) being developed for the treatment of prostate cancer.
  45. H3 receptor antagonist

    Bavisant dihydrochloride is a highly selective, orally active antagonist of the human H3 receptor with a novel mechanism of action, involving wakefulness and cognition, with potential as a treatment for ADHD.
  46. H2-receptor antagonist

    Ebrotidine is a competitive H2-receptor antagonist (Ki= 127.5 nM) with a potent antisecretory activity and evidenced gastroprotection.
  47. GPR120 modulator 1 is useful for modulating G protein-coupled receptor 120 (GPR120).
  48. GPR120 modulator 2 is useful for modulating G protein-coupled receptor 120 (GPR120).
  49. k-opioid receptor antagonist

    LY2795050 is a novel selective κ-opioid Receptor (KOR) antagonist (IC50=0.72 nM) and has the potential as a PET tracer to image KOR in vivo.
  50. CGRP Receptor antagonist

    MK-3207 is a potent and orally bioavailable CGRP receptor antagonist (IC50= 0.12 nM; Ki value= 0.024 nM); highly selective versus human AM1, AM2, CTR, and AMY3.

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