GPCR/G Protein

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  1. Levophacetoperane inhibits in vitro in a competitive manner, norepinephrin uptake and dopamine uptake.
  2. soluble guanylate cyclase stimulator

    Runcaciguat is an orally active stimulator of soluble guanylate cyclase, and is used in the research of cardiovascular and renal diseases combined with selective partial adenosine A1 receptor agonists.
  3. NK-1 receptor antagonist

    NK-1 Antagonist 1 (Rolapitant intermediate) is an antagonist of NK-1 receptor, used in the research of NK-1 related diseases and conditions such as cough, overactive bladder, alcohol dependency and depression.
  4. PAR2 antagonist

    AZ3451 is a potent protease-activated receptor-2 (PAR2) antagonist with IC50 of 23 nM.
  5. CBP inhibitor

    GNE-049 is a highly potent and selective CBP inhibitor with an IC50 of 1.1 nM in TR-FRET assay. GNE-049 also inhibits BRET and BRD4(1) with IC50s of 12 nM and 4200 nM, respectively.
  6. MCH1 receptor antagonist

    ALB-127158(a) is a potent and selective melanin concentrating hormone 1 (MCH1) receptor antagonist.
  7. dopamine receptor agonist

    Foslevodopa is a dopamine receptor agonist.
  8. SSTR5 antagonist

    SSTR5 antagonist 1 is a potent, selective, and orally available somatostatin receptor subtype 5 (SSTR5) antagonist with IC50s of 9.6 and 57 nM for hSSTR5 and mSSTR5, respectively. (Compound 25a).
  9. dopamine receptor agonist

    Foscarbidopa (Carbidopa 4??-monophosphate) is a prodrug of Carbidopa, acts as a dopamine receptor agonist.
  10. Sigma receptor ligand

    Sigma-LIGAND-1 is a selective sigma receptor ligand, has receptor IC50s of 16 nM at the DTG site, 19 nM at the PPP site, and a Ki of 4000 nM at the dopamine D2 receptor.
  11. 5-HT6 receptor antagonist

    Masupirdine free base (SUVN-502 free base) is a potent, selective, orally bioavailable, and brain penetrant 5-HT6 receptor antagonist (Ki of 2.04 nM for human 5-HT6 receptor).
  12. β adrenergic receptor antagonist

    Spirendolol is a β adrenergic receptor antagonist.
  13. 5-HT2A/α1-adrenergic receptor antagonist

    Lidanserin is a drug which acts as a combined 5-HT2A and α1-adrenergic receptor antagonist.
  14. 5-HT2A/dopamine D2 antagonist

    Abaperidone is a potent antagonist of 5-HT2A?receptor and dopamine D2 receptor with IC50s of 6.2 and 17 nM.
  15. angiotensin AT1 receptor antagonist

    L162389 is a potent antagonist of angiotensin AT1 receptor with Ki of 28 nM.
  16. 5-HT1A modulator

    5-HT1A modulator 1 displays very high affinities for the 5HT1A, adrenergic α1 and dopamine D2 receptor with IC50s of 2 ±0.3 nM, 10 ± 3 nM and 40 ±9 nM, respectively.
  17. Gpr120 agonist

    GPR120-IN-1 is a selective Gpr120 agonist with a logEC50 of ?7.62.
  18. dopamine D1 receptor agonist

    (+)-Dihydrexidine hydrochloride ((+)-DAR-0100 hydrochloride) is a dopamine D1 receptor agonist with an EC50 of 72± 21 nM.
  19. histamine H1 receptor antagonist

    Pirolate is a histamine H1 receptor antagonist.

  20. mGluR5 antagonist

    Fenobam is a selective, orally active, and non-competitive mGluR5 antagonist acting at an allosteric modulatory site (Kd values are 54 and 31 nM for rat and human recombinant mGlu5 receptors, respectively).
  21. AA3R antagonist

    Adenosine antagonist-1 is an adenosine A3 receptor (AA3R) antagonist.
  22. A2A adenosine agonist

    PD 117519 (CI947) is an A2A adenosine agonist which has shown oral antihypertensive activity in pharmacological animal models.
  23. LPA1 antagonist

    BMS-986020 is a high-affinity lysophosphatidic acid receptor 1 (LPA1) antagonist.
  24. FPR1 antagonist

    HCH6-1 is a competitive antagonist of Formyl peptide receptor 1 (FPR1), an emerging therapeutic target for the discovery of drugs to treat neutrophilic inflammatory diseases.
  25. LHCGR/TSHR agonist

    Org41841 is a partial agonist of both luteinizing hormone/chorionic gonadotropin receptor (LHCGR) and thyroid-stimulating hormone receptor (TSHR) with EC50s of 0.2 and 7.7 μM, respectively.
  26. CXCR4 antagonist

    IT1t is a potent CXCR4 antagonist; inhibits CXCL12/CXCR4 interaction with an IC50 of 2.1 nM.
  27. AC1 inhibitor

    ST034307 is a potent and selective adenylyl cyclase 1 (AC1) inhibitor, with IC50 of 2.3 μM.
  28. GPBAR1 agonist

    BAR501 is a potent and selective agonist of GPBAR1 with an EC50 of 1 μM.
  29. dual FXR and GPBAR1 agonist

    BAR502 is a dual FXR and GPBAR1 agonist with IC50 values of 2 μM and 0.4 μM, respectively.
  30. dopamine autoreceptor antagonist

    CGP 25454A is a novel and selective presynaptic dopamine autoreceptor antagonist.
  31. DP antagonist

    PGD2-IN-1 is an antagonist of DP extracted from patent WO 2006044732 A2, example 15 (d); has an IC50 of 0.3 nM.
  32. OX2R antagonist

    TCS-OX2-29 is a potent, high affinities and selective orexin-2 receptor (OX2R) antagonist with an IC50 value of 40 nM and a pKI value of 7.5. TCS-OX2-29 displays ~250-fold selectivity for OX2 over OX1.
  33. S1P receptor agonist

    S1p receptor agonist 1 is an S1P receptor agonist extracted from patent WO 2015039587 A1, compound example 2.
  34. ostsynaptic alpha adrenergic receptor antagonist

    Tiodazosin is a potent competitive postsynaptic alpha adrenergic receptor antagonist.
  35. histamine H4 receptor agonist

    VUF10460 is a non-imidazole histamine H4 receptor agonist; binds to rat H4 receptor with a pKi of 7.46.
  36. S1P3 receptor agonist

    CYM-5541 (ML249) is an selective and allosteric S1P3 receptor agonist with an EC50 between 72 and 132 nM.
  37. group III mGluR antagonist

    MSOP is a selective group III metabotropic glutamate receptor antagonist with apparent KD of 51 μM for the L-AP4-sensitive presynaptic mGluR.
  38. Antihistamine-1 is a H1-antihistamine (Ki=6.9 nM) with acceptable blood-brain barrier penetration and also an inhibitor of CYP2D6 and hERG channel with IC50s of 5.4 and 0.8 μM, respectively.
  39. CXCR2 receptor antagonist

    Nicotinamide N-oxide, an in vivo nicotinamide metabolite, is a potent, and selective antagonist of the CXCR2 receptor.
  40. δ opioid receptor antagonist

    Naltrindole hydrochloride is a highly potent and selective non-peptide δ opioid receptor antagonist with a Ki of 0.02 nM.
  41. mGlu1 receptor antagonist

    JNJ16259685 is a selective antagonist of mGlu1 receptor, and inhibits the synaptic activation of mGlu1 in a concentration-dependent manner with IC50 of 19 nM.
  42. group I/group II mGluR antagonist

    (S)-MCPG is the active isomer of (RS)-MCPG, non-selective group I/group II metabotropic glutamate receptor antagonist.

  43. mGluR 1 antagonist

    FTIDC is an orally active, noncompetitive, selective allosteric metabotropic glutamate receptor (mGluR) 1 antagonist with an IC50 of 5.8 nM for human mGluR1a.
  44. mGluR1 receptors Modulator

    DFMTI is an allosteric negative modulator of mGluR1 receptors.
  45. mGlu1 receptors modulator

    Ro 67-7476 is a positive allosteric modulator of mGlu1 receptors.
  46. mGluR 1 allosteric antagonist

    CFMTI is a potent and selective metabotropic glutamate receptor (mGluR) 1 allosteric antagonist with IC50 of 2.6 nM.
  47. S1PR1 antagonist

    W146 is a selective antagonist of sphingosine-1-phosphate receptor 1 (S1PR1) with an EC50 value of 398 nM.
  48. mGluR agonist

    L-Cysteinesulfinic acid is a potent agonist at several rat metabotropic glutamate receptors (mGluRs) with pEC50s of 3.92±0.03, 4.6±0.2, 3.9±0.2, 2.7±0.2, 4.0±0.2, and 3.94±0.08 for mGluR1, mGluR5, mGluR2, mGluR4, mGluR6, and mGluR8, respectively.
  49. μ opioid receptor agonist

    PZM21 is a potent and selective μ opioid receptor agonist with an EC50 of 1.8 nM.
  50. guanylate cyclase stimulator

    Nelociguat (BAY60-4552) is a nitric oxide sensitive soluble guanylate cyclase stimulator.

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