GPCR/G Protein

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  1. D1 receptor agonist

    PF-06256142 is a potent and selective orthosteric agonist of the D1 receptor, with D1 EC50=30 nM and D1 binding Ki = 12 nM.
  2. GLP-1 receptor agonist

    Semaglutide, a long-acting GLP-1 analogue, is a glucagon-like peptide-1 (GLP-1) receptor agonist that can be used in the treatment of type 2 diabetes.
  3. TSHR agonist

    ML-109 is a potent and full thyroid stimulating hormone receptor (TSHR) agonist, with an EC50 of 40 nM.
  4. histamine H4 receptor inverse agonist

    H4 Receptor antagonist 1 is a potent and selective histamine H4 receptor inverse agonist, with an IC50 of 19 nM.
  5. angiotensin 1 (AT1) and AT2 receptor agonist

    Angiotensin III is an angiotensin 1 (AT1) and AT2 receptor agonist.
  6. apelin agonist

    Apelin agonist 1 is an oral selective apelin agonist AM-2995, a agonist of the APJ (APLNR, angiotensin receptor like-1) receptor, may be used in the treatment of cardiovascular conditions.
  7. mGlu3 receptor agonist

    LY2794193 is a highly potent and selective mGlu3 receptor agonist (hmGlu3 Ki=0.927 nM??EC50=0.47 nM; hmGlu2 Ki=412 nM??EC50=47.5 nM).
  8. GPR40 full agonist

    GPR40 agonist 1 is a potent and novel GPR40 full agonist with an EC50 of 2 nM and 17 nM for hGPR40 and rGPR40, respectively.
  9. GPR120 agonist

    GPR120 Agonist 2 is a GPR120 agonist extracted from patent US 20110313003 A1, example 209.
  10. 5-HT agonist

    8-OH-DPAT is a potent and selective 5-HT agonist, with a pIC50 of 8.19 for 5-HT1A and a Ki of 466 nM for 5-HT7; 8-OH-DPAT weakly binds to 5-HT1B (pIC50, 5.42), 5-HT (pIC50 <5).
  11. β-adrenergic agonist

    Imoxiterol (RP 58802B) is a β-adrenergic agonist.
  12. 5-HT2C receptor-selective agonist

    Vabicaserin hydrochloride is a 5-hydroxytryptamine 2C (5-HT2C) receptor-selective agonist with an EC50 of 8 nM.
  13. Human CXCR3 agonist

    PS372424, a three amino-acid fragment of CXCL10, is a specific human CXCR3 agonist with anti-inflammatory activity, which inhibits the binding of CXCR3 ligand CXCL10 to CXCR3 receptor with IC50 of 42 nM.
  14. CB2 agonist

    Olorinab (APD 371) is a highly potent, selective and fully efficacious cannabinoid receptor type 2 (CB2) agonist, with an EC50 of 6.2 nM for hCB2.
  15. β2-adrenoceptor agonist

    Formoterol is a long-acting β2 agonist used in the management of asthma and chronic obstructive pulmonary disease (COPD).
  16. μ-opioid receptor agonist

    Alvimopan dihydrate(LY 246736, ADL 8-2698) is a peripherally acting mu-opioid receptor (PAM-OR, IC50= 1.7 nM) antagonist for accelerating gastrointestinal recovery after surgery.
  17. μ-opioid receptor agonist

    Alvimopan monohydrate is a peripherally acting mu-opioid receptor (PAM-OR, IC50= 1.7 nM) antagonist for accelerating gastrointestinal recovery after surgery.
  18. α-adrenergic receptor agonist

    Brimonidine Tartrate is a highly selective α-adrenergic receptor agonist with EC50 of 0.45 nM for the α2A adrenoreceptor, and used to treat open-angle glaucoma or ocular hypertension.
  19. dopamine agonist

    Dexpramipexole dihydrochloride is a neuroprotective agent and weak non-ergoline dopamine agonist.
  20. α2A-adrenoceptor agonist

    Guanfacine hydrochloride, an anti-hypertensive agent, is a selective α2A-adrenoceptor agonist with Kd of 31 nM and displays 60-fold selectivity over α2B-adrenoceptors.
  21. 5HT1F agonist

    LY344864 is a selective receptor agonist with an affinity of 6 nM (Ki) at the recently cloned 5-HT1F receptor.
  22. Nonimidazole inverse agonist

    Pitolisant hydrochloride is a novel, potent, and selective nonimidazole inverse agonist at the recombinant human H3 receptor (Ki=0.16 nM).
  23. Nonimidazole inverse agonist

    Pitolisant oxalate is a novel, potent, and selective nonimidazole inverse agonist at the recombinant human H3 receptor (Ki=0.16 nM).
  24. D2 receptor agonist

    rac-Rotigotine Hydrochloride is a high potency and selectivity agonist for D-2 receptor with Ki of 0.69 nM.
  25. LPA2 agonist

    GRI 977143, selective lysophosphatidic acid 2 (LPA2) receptor non-lipid agonist (EC50 = 3.3 uM).
  26. glutamate receptors agonist

    (S)-Glutamic acid acts as an excitatory transmitter and an agonist at all subtypes of glutamate receptors (metabotropic, kainate, NMDA, and AMPA).
  27. 5-HT1E/5-HT1F receptor agonist

    BRL 54443 is a 5-HT1E and 5-HT1F receptor agonist with pKi of 8.7 and 9.25, respectively, with a weak binding affinity for 5-HT1A, 5-HT1B, 5-HT1D receptors.
  28. 5-HT Receptor agonist

    Clomipramine is a blocker of the following transporters:Serotonin transporter (SERT) (Ki = 0.14 nM),Norepinephrine transporter (NET) (Ki = 54 nM),Dopamine transporter (DAT) (Ki = 3,020 nM),Glycine transporter (GlyT/LeuT).
  29. Alpha adrenergic agonist

    Clonidine is classified as a centrally acting alpha adrenergic agonist.Clonidine acts centrally as an imidazoline receptor agonist.
  30. Adrenergic Receptor agonist

    Detomidine is a sedative with analgesic properties. α2-adrenergic agonists produce dose-dependent sedative and analgesic effects, mediatated by activation of α2 catecholamine receptors, thus inducing a negative feedback response, reducing production of excitatory neurotransmitters.
  31. Adrenoceptors agonist

    Dobutamine is a direct-acting agent whose primary activity results from stimulation of the β1-adrenoceptors of the heart, increasing contractility and cardiac output.
  32. mGluR Agonist

    LY-404039 is a drug used in scientific research that acts as a selective agonist for the metabotropic glutamate receptor group II subtypes mGluR2 and mGluR3. It has anxiolytic and antipsychotic effects in animal studies, but without causing sedation. Early human trials using a prodrug form of LY-404,039 called LY-214,0023 have also given encouraging results.
  33. NOP receptor agonist

    MCOPPB is a compound which acts as a potent and selective agonist for the nociceptin receptor, with a pKi of 10.07.
  34. MT1/MT2 agonist

    Melatonin is a endogenous hormone that acts as an agonist at melatonin receptors MT1 and MT2.
  35. 5-HT4-receptor agonist

    Mosapride citrate acts as 5-HT4 receptor agonist and 5-HT3 receptor antagonist.
  36. 5-HT1 receptor

    Naratriptan is a selective 5-HT1 receptor subtype agonist.
  37. alpha-1 adrenergic agonist

    Oxymetazoline is a selective alpha-1 agonist and partial alpha-2 agonist topical decongestant, used in the form of Oxymetazoline hydrochloride.
  38. Dopamine Receptor Agonist

    Pramipexole is a dopamine agonist of the non-ergoline class indicated for treating early-stage Parkinson's disease (PD) and restless legs syndrome (RLS).
  39. MT1/MT2-Receptor Agonist

    Ramelteon is a melatonin receptor agonist with both high affinity for melatonin MT1 (IC50 =28.5 ?? 8.55 pM)and MT2 (20.1 ?? 9.25 pM)receptors and selectivity over the MT3 receptor.
  40. α2 adrenergic agonist

    Rilmenidine is a second-generation imidazoline-α2 adrenergic agonist.
  41. Adrenergic Receptor agonist

    Salbutamol sulfate (Albuterol) is a short-acting β2-adrenergic receptor agonist used for the relief of bronchospasm in conditions such as asthma and chronic obstructive pulmonary disease.
  42. Adrenergic Receptor agonist

    Synephrine (Oxedrine) is an amine compound commonly used for weight loss.
  43. D2 dopamine agonist

    U-95666E is a D2 selective dopamine agonist with an ED50 of about 46 nM, was investigated for its effect on rat striatal acetylcholine (ACh) concentration
  44. Opioid Receptor agonist

    ADL5859 HCl is a highly potent and selective δ opioid receptor agonist with Ki value to be 0.84 nM and ED50 value to be 20 nM.
  45. VPAC2 agonist

    Bay 55-9837 is a potent and highly selective agonist of VPAC2, with a Kd of 0.65 nM. Bay 55-9837 may be a useful therapy for the research of type 2 diabetes.
  46. CXCR4 agonist

    CTCE-0214 is a chemokine CXC receptor 4 (CXCR4) agonist, SDF-1α (stromal cell-derived factor-1α) peptide analog. CTCE-0214 shows anti-inflammatory activity, and can be used in inflammation sepsis and systemic inflammatory syndromes research.
  47. PAR2 agonist

    AY254 is an analogue of AY77. AY254 is ERK-biased PAR2 agonist with an EC50 of 2 nM. AY254 relieves cytokine-induced caspase 3/8 activation. AY254 also promotes scratch-wound healing and induced IL-8 secretion via PAR2-ERK1/2 signaling.
  48. PAR2 agonist

    AY77 is a calcium-biased PAR2 agonist. AY77 shows an EC50 of 0.17 and 2 nM in PAR2-mediated the activation in the Gq pathway and recruitment of β-arrestin-2, respectively. AY77 potently induces intracellular Ca2+ release.
  49. Glucagon receptor agonist

    Retatrutide (LY3437943) is a triple agonist peptide of the glucagon receptor (GCGR), glucosedependent insulinotropic polypeptide receptor (GIPR), and glucagon-like peptide-1 receptor (GLP-1R). Retatrutide binds human GCGR, GIPR, and GLP-1R with EC50 values of 5.79, 0.0643 and 0.775 nM, respectively. Retatrutide can be used for the research of obesity.
  50. GLP-1 receptor agonist

    Oxyntomodulin (bovine, porcine), a 37-amino acid peptide hormone, is a glucagon-like peptide 1 (GLP-1) receptor agonist.

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