GPCR/G Protein

Items 951-1000 of 5455

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  1. CysLT1 receptor antagonist

    LM-1484 is an antagonist of CysLT1 receptor and displays a higher affinity for 3H-LTC4 sites.
  2. GLP-1 receptor agonist

    GLP-1 receptor agonist 1 is a glucagon-like peptide-1 (GLP-1) receptor agonist extracted from patent WO2018056453A1, Compound 67.
  3. peripheral adrenoceptor antagonist

    Deriglidole is a peripheral adrenoceptor antagonist with a high affinity for α2-adrenoceptors.
  4. PAF antagonist

    Apafant (WEB 2086), a potent platelet-activating factor (PAF) antagonist, inhibits PAF binding to human PAF receptors with a Ki of 9.9 nM.
  5. CB1 agonist

    Leelamine hydrochloride is a tricyclic diterpene molecule that is extracted from the bark of pine trees. Leelamine hydrochloride is a cannabinoid receptor type 1 (CB1) agonist and a inhibitor of SREBP1-regulated fatty acid/lipid synthesis in prostate cancer cells that is not affected by androgen receptor status.
  6. Adenosine receptor agonist

    N6-Ethyladenosine is an adenosine derivative, acts as a Adenosine receptor agonist, with Kis of 4.9 and 4.7 nM for hA1AR and hA3AR, respectively.
  7. melatonin agonist

    Ramelteon metabolite M-II is the major metabolite of Ramelteon, with IC50s of 208 pM, 1470 pM for human melatonin receptors (MT1 or MT2). Ramelteon is a selective melatonin agonist.
  8. MCHR1 antagonist

    SNAP 94847 is a novel, high affinity selective melanin-concentrating hormonereceptor1 (MCHR1) antagonist with (Ki= 2.2 nM, Kd=530 pM), it displays >80-fold and >500-fold selectivity over MCHα1A and MCHD2 receptors respectively.
  9. peptidoleukotrienes antagonist

    RG-12525 is a a specific, competitive and orally effective antagonist of the peptidoleukotrienes, LTC4, LTD4 and LTE4, inhibiting LTC4-, LTD4- and LTE4-inducd guinea pig parenchymal strips contractions, with IC50s of 2.6 nM, 2.5 nM and 7 nM, respectively; RG-12525 is also a peroxisome proliferator-activated receptor gamma (PPAR-gamma) agonist with IC50 of appr 60 nM and a potent inhibitor of CYP3A4, with a Ki value of 0.5 ?M.
  10. adenylate cyclase inhibitor

    CB-7921220 is an adenylate cyclase inhibitor.
  11. PAF antagonist

    Setipafant is a platelet-activating factor (PAF) antagonist.
  12. Oxytocin antagonist

    OT antagonist 1 (Compound 4) is a potent, selective Oxytocin antagonist with a Ki of 50 nM.
  13. oxytocin (OT) antagonist

    OT antagonist 3 is an oxytocin (OT) antagonist extracted from patent WO2007017752A1.
  14. GPR35/CXCR8 antagonist

    ML 145 is a selective GPR35/CXCR8 antagonist with an IC50/EC50 of 20.1 nM, but not for the related GPR55 orphan receptor. GPR35 is expressed by various cells of the immune system and it may has potential as a therapeutic target in inflammatory disease.
  15. AT1 receptor antagonist

    ZD 7155 hydrochloride is an angiotensin II receptor type 1 (AT1 receptor) antagonist.
  16. γ-L-Glutamyl-L-alanine, composed of gamma-glutamate and alanine, is a proteolytic breakdown product of larger proteins.

  17. 5-HT4 receptor antagonist

    Sulamserod is a 5-HT4 receptor antagonist, with antiarrhythmic activities.
  18. GPR35/CXCR8 agonist

    Kynurenic acid sodium, an endogenous tryptophan metabolite, is a broad-spectrum antagonist targeting NMDA, glutamate, α7 nicotinic acetylcholine receptor. Kynurenic acid sodium is also an agonist of GPR35/CXCR8.
  19. NOP agonist

    MT-7716 hydrochloride (W-212393 hydrochloride) is a selective non-peptide nociceptin receptor (NOP) agonist and promising potential treatment drug for alcohol abuse and relapse prevention.
  20. A1 adenosine receptor agonist

    N6-(2-Phenylethyl)adenosine is a selective A1 adenosine receptor agonist.
  21. CRTh2 receptor antagonist

    MK-8318 is a potent and selective CRTh2 receptor antagonist with a Ki of 5.0 nM.
  22. β adrenergic receptor antagonist

    Pargolol hydrochloride is a β adrenergic receptor antagonist.
  23. 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.
  24. AP5
    AP5 exhibits potent and selective agonism for the GPR40 receptor with positive allosteric modulation of endogenous ligands (AgoPAM). AP5 demonstrates a rat hIP1 EC50 of 0.49±0.28 nM against the GPR40 receptor.
  25. mGluR2 modulator

    AZD-8529 is a potent, highly selective and orally bioavailable positive allosteric modulator of mGluR2, with an EC50 of 285 nM, and shows no positive allosteric modulator responses at 20-25 M on the mGluR1, 3, 4, 5, 6, 7, and 8 subtypes.
  26. mGlu1 receptor modulator

    FITM is a negative allosteric modulator of mGlu1 receptor with a Ki of 2.5 nM.
  27. 5-HT1B receptor antagonist

    AR-A 2 is a selective 5-HT1B receptor antagonist.
  28. BRS-3 antagonist

    ML-18 is a non-peptide bombesin receptor subtype-3 (BRS-3) antagonist with an IC50 of 4.8 μM.
  29. AChE /M1/M2/5HT4/I2 inhibitor

    MHP 133 is a drug with multiple CNS targets, and inhibits acetylcholinesterase (AChE) with Ki of 69 μM; also active against muscarinic M1 and M2 receptors, serotonin 5HT4 receptors, and imidazole I2 receptors.
  30. 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.
  31. NK2 receptor antagonist

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

    GSK726701A is a novel prostaglandin E2 receptor 4 (EP4) partial agonist with a pEC50 of 7.4.
  33. 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).
  34. A2B adenosine receptor antagonist

    BAY-545 is a potent and selective A2B adenosine receptor antagonist, with an IC50 of 59 nM.
  35. 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).
  36. GPR40/FFAR1 agonist

    GPR40/FFAR1 modulator 1 is an agonist and an allosteric modulator for Gq-coupled free fatty acid receptor 1 (GPR40/FFAR1).
  37. 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.
  38. 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.
  39. 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.
  40. 5-HT3 /5-HT4 receptor dual antagonist

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

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

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

    Taminadenant is an antagonist of adenosine receptor.
  44. Levophacetoperane inhibits in vitro in a competitive manner, norepinephrin uptake and dopamine uptake.
  45. 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.
  46. 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.
  47. PAR2 antagonist

    AZ3451 is a potent protease-activated receptor-2 (PAR2) antagonist with IC50 of 23 nM.
  48. 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.
  49. MCH1 receptor antagonist

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

    Foslevodopa is a dopamine receptor agonist.

Items 951-1000 of 5455

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