GPCR/G Protein

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Product Citation
  1. PPARγ and CB2 receptor dual agonist

    VCE-004.8, a semi-synthetic multitarget cannabinoquinoid, is a specific PPARγ and CB2 receptor dual agonist with potent anti-inflammatory activity.
  2. LPA2 agonist

    Radioprotectin-1 is a potent and specific nonlipid agonist of lysophosphatidic acid receptor 2 (LPA2), with an EC50 value of 25 nM for murine LPA2 subtype.
  3. Rev-Erbα/β agonist

    SR10067 is a potent, selective and brain penetrant Rev-Erbα/β agonist, with IC50 values are 160 and 170 nM for Rev-Erbβ and Rev-Erbα, respectively. SR10067 has anxiolytic activity.
  4. β2 adrenergic receptor agonist

    BI-167107 is a high affinity, full agonist that binds to the β2 adrenergic receptor (β2AR) with a dissociation constant Kd of 84 pM.
  5. non-peptide PAR2 agonist

    GB110 is a Novel potent non-peptide PAR2 agonist. GB-110 selectively induces PAR2-mediated intracellular Ca2+ release in HT29 cells with an EC50 of 0.28 μM.
  6. GPRC6A agonist

    DJ-V-159 is an agonist for G protein-coupled receptor family C group 6 member A (GPRC6A).
  7. non-peptide MAS agonist

    AR234960, a non-peptide MAS (a G protein-coupled receptor) agonist, increases both mRNA and protein levels of CTGF via ERK1/2 signaling in HEK293-MAS cells and adult human cardiac fibroblasts.
  8. 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.
  9. 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.
  10. TSHR agonist

    ML-109 is a potent and full thyroid stimulating hormone receptor (TSHR) agonist, with an EC50 of 40 nM.
  11. 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.
  12. angiotensin 1 (AT1) and AT2 receptor agonist

    Angiotensin III is an angiotensin 1 (AT1) and AT2 receptor agonist.
  13. 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).
  14. 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.
  15. GPR120 agonist

    GPR120 Agonist 2 is a GPR120 agonist extracted from patent US 20110313003 A1, example 209.
  16. 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).
  17. β-adrenergic agonist

    Imoxiterol (RP 58802B) is a β-adrenergic agonist.
  18. 5-HT2C receptor-selective agonist

    Vabicaserin hydrochloride is a 5-hydroxytryptamine 2C (5-HT2C) receptor-selective agonist with an EC50 of 8 nM.
  19. 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.
  20. 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.
  21. β3-adrenoceptor agonist

    Amibegron hydrochloride is a selective β3-adrenoceptor agonist, with an EC50 of 3.5 nM for β-adrenoceptor in rat colon; Amibegron hydrochloride has anxiolytic and antidepressant activity.
  22. S1P1 and S1P5 agonist

    ASP-4058 is a next-generation, selective and oral bioactive agonist for Sphingosine 1-Phosphate receptors 1 and 5 (S1P1 and S1P5), ameliorates rodent experimental autoimmune encephalomyelitis with a favorable safety profile.
  23. Adenosine A1 receptor agonist

    N6-Cyclopentyladenosine (CPA) is a selective Adenosine A1 receptor agonist, with Ki values of 2.3 nM, 790 nM and 43 nM for human A1, A2A and A3 receptors, respectively.
  24. 5-HT6 agonist

    EMDT oxalate is a selective 5-HT6 agonist, and has antidepressant effects.
  25. GPR120 agonist

    GPR120 Agonist 1 is a potent and selective GPR120 agonist, and possesses promising antidiabetic effect and good safety profile to be a development candidate.
  26. GLP-1R agonist

    GLP-1 receptor agonist 2 is a glucagon-like peptide-1 receptor (GLP-1R) agonist.
  27. CaSR agonist

    GSK3004774 is a potent, nonabsorbable agonist of CaSR, with an pEC50 of 7.3, 6.6 and 6.5 for human, mouse and rat CaSR, respectively. GSK3004774 shows an EC50 of 50 nM for human CaSR.
  28. 5-HT1B/1D receptors agonist

    Alniditan is a potent 5-HT1B/1D receptors agonist, with IC50 of 1.7 and 1.3 nM in HEK?293 cells, and pKi value of 8.96 and 9.40 for 5-HT1B/1D receptors, respectively.
  29. 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.
  30. 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.
  31. 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.
  32. 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.
  33. 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.
  34. A1 adenosine receptor agonist

    N6-(2-Phenylethyl)adenosine is a selective A1 adenosine receptor agonist.
  35. EP4 partial agonist

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

    Foslevodopa is a dopamine receptor agonist.
  39. dopamine receptor agonist

    Foscarbidopa (Carbidopa 4??-monophosphate) is a prodrug of Carbidopa, acts as a dopamine receptor agonist.
  40. Gpr120 agonist

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

    (+)-Dihydrexidine hydrochloride ((+)-DAR-0100 hydrochloride) is a dopamine D1 receptor agonist with an EC50 of 72± 21 nM.
  42. A2A adenosine agonist

    PD 117519 (CI947) is an A2A adenosine agonist which has shown oral antihypertensive activity in pharmacological animal models.
  43. 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.
  44. GPBAR1 agonist

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

    BAR502 is a dual FXR and GPBAR1 agonist with IC50 values of 2 μM and 0.4 μM, respectively.
  46. S1P receptor agonist

    S1p receptor agonist 1 is an S1P receptor agonist extracted from patent WO 2015039587 A1, compound example 2.
  47. histamine H4 receptor agonist

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

    CYM-5541 (ML249) is an selective and allosteric S1P3 receptor agonist with an EC50 between 72 and 132 nM.
  49. 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.
  50. μ opioid receptor agonist

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

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