GPCR/G Protein

Items 5451-5500 of 6977

Page
per page
Set Descending Direction
Catalog No.
Product Name
Application
Product Information
Citations
  1. histamine H3 receptor antagonist

    Cipralisant is a potent and selective histamine H3 receptor antagonist in vivo, and an agonist in vitro, with a pKi of 9.9 for histamine H3 receptor and a Ki of 0.47 nM for rat histamine H3 receptor; Cipralisant has entered in clinical trials for the treatment of attention-deficit hyperactivity disorder.
  2. NK2 receptor antagonist

    Saredutant is a selective NK2 receptor antagonist.
  3. EP4 partial agonist

    GSK726701A is a novel prostaglandin E2 receptor 4 (EP4) partial agonist with a pEC50 of 7.4.
  4. S1P antagonist

    VPC 23019, an aryl amide-containing Sphingosine 1-phosphate (S1P) analog, is a competitive antagonist at the S1P1 and S1P3 receptors (pKi= 7.86 and 5.93, respectively) and an agonist at the S1P4 and S1P5 receptors (pEC50= 6.58 and 7.07, respectively).
  5. A2B adenosine receptor antagonist

    BAY-545 is a potent and selective A2B adenosine receptor antagonist, with an IC50 of 59 nM.
  6. Dopamine D4 receptor antagonist

    NRA-0160 is a selective dopamine D4 receptor antagonist, with a Ki value of 0.48 nM and with negligible affinity for dopamine D2 receptor (Ki: >10000 nM), D3 receptor (Ki: 39 nM), rat 5-HT2A receptor (Ki: 180 nM) and rat α1 adrenoceptor (Ki: 237 nM).
  7. GPR40/FFAR1 agonist

    GPR40/FFAR1 modulator 1 is an agonist and an allosteric modulator for Gq-coupled free fatty acid receptor 1 (GPR40/FFAR1).
  8. GRKs-IN-1, Compound 14as, has remarkable potency against and selectivity for G protein-coupled receptor kinase 2 GRK2 (IC50=30 nM) and GRK5 (IC50=7.1 μM). GRKs-IN-1 is a derivative 14as of paroxetine, shows a 100-fold improvement in cardiomyocyte contractility assays over paroxetine.
  9. PAF antagonist

    YM-264 is a selective, potent and orally active platelet-activating factor (PAF) antagonist with a pKi value of 8.85 for rabbit platelet membranes.
  10. 5-HT7 receptor agonist

    5-HT7 agonist 1 is a selective 5-HT7 receptor agonist, with an IC50 of 222.93 nM, can be used for the 5-HT7 receptor related disease, such as CNS disorders.
  11. 5-HT3 /5-HT4 receptor dual antagonist

    FK1052 hydrochloride is a potent 5-HT3 and 5-HT4 receptor dual antagonist.
  12. H1 receptor antagonist

    Wy 49051 is a potent, orally active H1 receptor antagonist, with IC50 of 44 nM.
  13. serotonin 5-HT2 antagonist

    Irindalone is a novel serotonin 5-HT2 antagonist.
  14. adenosine receptor antagonist

    Taminadenant is an antagonist of adenosine receptor.
  15. Levophacetoperane inhibits in vitro in a competitive manner, norepinephrin uptake and dopamine uptake.
  16. 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.
  17. 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.
  18. PAR2 antagonist

    AZ3451 is a potent protease-activated receptor-2 (PAR2) antagonist with IC50 of 23 nM.
  19. 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.
  20. MCH1 receptor antagonist

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

    Foslevodopa is a dopamine receptor agonist.
  22. 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).
  23. dopamine receptor agonist

    Foscarbidopa (Carbidopa 4??-monophosphate) is a prodrug of Carbidopa, acts as a dopamine receptor agonist.
  24. 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.
  25. 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).
  26. β adrenergic receptor antagonist

    Spirendolol is a β adrenergic receptor antagonist.
  27. 5-HT2A/α1-adrenergic receptor antagonist

    Lidanserin is a drug which acts as a combined 5-HT2A and α1-adrenergic receptor antagonist.
  28. 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.
  29. angiotensin AT1 receptor antagonist

    L162389 is a potent antagonist of angiotensin AT1 receptor with Ki of 28 nM.
  30. 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.
  31. Gpr120 agonist

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

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

    Pirolate is a histamine H1 receptor antagonist.

  34. 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).
  35. AA3R antagonist

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

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

    BMS-986020 is a high-affinity lysophosphatidic acid receptor 1 (LPA1) antagonist.
  38. 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.
  39. 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.
  40. CXCR4 antagonist

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

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

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

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

    CGP 25454A is a novel and selective presynaptic dopamine autoreceptor antagonist.
  45. 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.
  46. 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.
  47. S1P receptor agonist

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

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

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

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

Items 5451-5500 of 6977

Page
per page
Set Descending Direction