GPCR/G Protein

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  1. 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).
  2. 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.
  3. α2 adrenergic agonist

    Rilmenidine is a second-generation imidazoline-α2 adrenergic agonist.
  4. 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.
  5. Adrenergic Receptor agonist

    Synephrine (Oxedrine) is an amine compound commonly used for weight loss.
  6. 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
  7. 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.
  8. GPR3 inverse agonist

    AF64394 is a GPR3 inverse agonist, with a pIC50 of 7.3.
  9. glucagon-like peptide-1 receptor agonist

    Exendin-4 (Exenatide), a 39 amino acid peptide, is a long-acting glucagon-like peptide-1 receptor agonist with an IC50 of 3.22 nM.
  10. β1-selective adrenergic receptor agonist

    Norepinephrine hydrochloride (Levarterenol hydrochloride; L-Noradrenaline hydrochloride) is a β1-selective adrenergic receptor agonist with EC50 of 5.37 μM.
  11. partial dopamine D2 and D3 receptor agonist

    Pardoprunox hydrochloride is a novel partial dopamine D2 and D3 receptor agonist and serotonin 5-HT1A receptor agonist, D2 (pKi = 8.1) and D3 receptor (pKi = 8.6) partial agonist and 5-HT1A receptor (pKi = 8.5) full agonist.
  12. TSHR inverse agonist

    ML224(NCGC00242364; ANTAG3) is a selective TSHR inverse agonist; inhibits TSH-stimulated cAMP production with an IC50 = 2.3 μM.
  13. GPR88 receptor agonist

    (1R,2R)-2-PCCA hydrochloride is a diastereomer of 2-PCCA, and acts as a potent GPR88 receptor agonist, with an EC50 of 3 nM in cell-free assay, and 603 nM in cell assay.
  14. Smo receptor agonist

    SAG (hydrochloride) is a potent Smo receptor agonist, and activates the Hedgehog signaling pathway, with a Kd of 59 nM.
  15. CB1 receptor inverse agonist

    Taranabant (1R,2R)stereoisomer is the R-enantiomer of Taranabant. Taranabant is a highly potent and selective cannabinoid 1 (CB1) receptor inverse agonist.
  16. nociceptin receptor agonist

    MCOPPB 3Hcl is a nociceptin receptor agonist with pKi of 10.07; weaker activity at other opioid receptors.
  17. 5-HT1F receptor agonist

    LY 344864 S-enantiomer is the S-enantiomer of LY344864. LY344864 is a 5-HT1F receptor agonist.
  18. 5-HT1F agonist

    LY 344864 hydrochloride is a selective 5-HT1F agonist with a Ki of 6 nM.
  19. D1/D5 receptor full agonist

    SKF-82958 hydrobromide is a D1/D5 receptor full agonist.
  20. GPR40 agonist

    AM-4668 is a GPR40 agonist for type 2 diabetes. EC50s of 3.6 nM and 36 nM for GPR40 in A9 cells (GPR40 IP3 assay) and CHO cells (GPR40 aequorin assay), respectively.
  21. ghrelin receptor inverse agonist

    PF-5190457 is a potent and selective ghrelin receptor inverse agonist with a pKi of 8.36.
  22. GPR40 agonist

    AMG 837 sodium salt is a potent GPR40 agonist(EC50=13 nM) with a superior pharmacokinetic profile and robust glucose-dependent stimulation of insulin secretion in rodents.
  23. D1/D5 receptor full agonist

    SKF 82958 is a D1/D5 receptor full agonist.
  24. mGluRs M3 agonist

    L-APB is a potent and specific agonist for the group III mGluRs, with EC50s of 0.13, 0.29, 1.0, 249 μM for mGlu4, mGlu8, mGlu6 and mGlu7 receptors, respectively.
  25. δ opioid receptor agonist

    AR-M 1000390 hydrochloride is an exceptionally selective, potent δ opioid receptor agonist with an EC50 of 7.2??0.9 nM for δ agonist potency.
  26. non-peptide nociceptin receptor (NOP) agonist

    MT-7716 free base (W-212393) is a selective non-peptide nociceptin receptor (NOP) agonist and promising potential treatment drug for alcohol abuse and relapse prevention.
  27. partial mGluR4 agonist

    (1R,2S)-VU0155041, Cis regioisomer of VU0155041, is a partial mGluR4 agonist with an EC50 of 2.35 μM.
  28. D1-like dopamine receptor (D1/D5) agonist

    Dihydrexidine (DAR-0100) is a high potent, selective and full efficacy D1-like dopamine receptor (D1/D5) agonist with an IC50 of 10 nM for D1 receptor. Dihydrexidine exhibits potent antiparkinsonian activity.
  29. beta-adrenoceptor agonist

    Bambuterol ((??)-Bambuterol; KWD-2183) is a long acting beta-adrenoceptor agonist (LABA) used in the treatment of asthma; it also is a prodrug of terbutaline.
  30. mGluR5 agonist

    CHPG sodium salt is a selective mGluR5 agonist, and attenuates SO2-induced oxidative stress and inflammation through TSG-6/NF-κB pathway in BV2 microglial cells.
  31. dopamine D4 receptor partial agonist

    Ro 10-5824 dihydrochloride is a selective dopamine D4 receptor partial agonist, with Ki of 5.2 nM.
  32. human 5-HT1A receptor partial agonist

    Aripiprazole D8 (OPC-14597 D8) is the deuterium labeled Aripiprazole, which is a human 5-HT1A receptor partial agonist with a Ki of 4.2 nM.
  33. GPR109a receptor agonist

    MK-0354 is a partial agonist of GPR109a receptor, for hGPR109a/ mGPR109a with EC50 of 1.65/1.08 μM, showed no activation of GPR109b.
  34. 5-HT1A agonist

    Naluzotan is a novel, potent, and selective amidosulfonamide 5-HT1A agonist with IC50 and Ki of appr 20 nM and 5.1 nM, used for the treatment of anxiety and depression; Also a weak hERG K+ channel blocker, with IC50 of 3800 nM.
  35. sphingosine-1-phosphate receptor 4 (S1P4-R) agonist

    CYM50308 (ML248) is a potent, selective and high affinity sphingosine-1-phosphate receptor 4 (S1P4-R) agonist with an EC50 of 56 nM.
  36. A1 adenosine receptor agonist

    Adenosine amine congener (ADAC) is a selective A1 adenosine receptor agonist, can ameliorate noise- and Cisplatin-induced cochlear injury.
  37. cannabinoid (CB2) agonist

    LY2828360 is a slowly acting but efficacious G protein-biased cannabinoid (CB2) agonist, inhibiting cAMP accumulation and activating ERK1/2 signaling.
  38. β2-adrenergic agonist

    Clenproperol is a β2-adrenergic agonist.
  39. melanocortin receptor (MR) agonist

    AP1189 is a biased agonist at receptors MC1 and MC3. AP1189 reduced cytokine release, an effect reliant on both MC1 and MC3 as evident from the use of Mc1r(-/-) and Mc3r(-/-) macrophages.
  40. GLP-1R agonist

    PF-06882961 is a potent, orally bioavailable agonist of the glucagon-like peptide-1 receptor agonist (GLP-1R)
  41. 5-HT4 receptor partial agonist

    PF-04995274 is a partial agonist of the serotonin (5-HT) receptor subtypes 5-HT4A, 5-HT4B, 5-HT4D, and 5-HT4E (Kis = 0.36, 0.46, 0.15, and 0.32 nM, respectively, in a radioligand binding assay).1 It increases cAMP levels in HEK293 cells expressing 5-HT4A, 5-HT4B, 5-HT4D, and 5-HT4E receptors (EC50s = 0.47, 0.36, 0.37, and 0.26 nM, respectively, for the human recombinant receptors). PF-04995274 decreases scopolamine-induced increases in the distance traveled in the Morris water maze in rats when administered at a dose of 0.032 mg/kg.
  42. mGlu1 receptor agonist

    Ro0711401 is a mGlu1 receptor agonist.
  43. Melatonin receptor agonist

    ACH-000143 is a potent and peripherally preferred melatonin receptor agonist.
  44. 5-HT receptor agonist

    MK 212 hydrochloride is a 5-HT receptor agonist; displays selectivity for 5-HT2C over 5-HT2A (IC50 values are 0.028 and 0.42 μM for human 5-HT2C and 5-HT2A receptors expressed in HEK293 cells respectively).
  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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