GPCR/G Protein

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  1. mGluR agonist

    (S)-3,5-DHPG is an agonist of the group I metabotropic glutamate receptors (mGluRs), binding both mGluR1a and mGluR5a (Ki = 0.9 and 3.9 uM, respectively) but not ionotropic glutamate receptors.
  2. GLP-1 receptor agonist

    Liraglutide is a long-acting glucagon-like peptide-1(GLP-1) receptor agonist.
  3. Histamine H1-receptor agonist

    Lidocaine hydrochloride is a local anesthetic and cardiac depressant used as an antiarrhythmia agent.
  4. REV-ERBα/β agonist

    SR9011 is the agonist for REV-ERB-α with IC50 of 670 nM and REV-ERB-β with IC50 of 800 nM.
  5. CB1/CB2 receptor agonist

    Bay 59-3074 is a novel, selective CB1/CB2 receptor partial agonist with Ki values of 48.3 and 45.5 nM at human CB1 and CB2 receptors respectively .
  6. CXCR4 agonist

    ATI-2341, pepducin targeting the C-X-C chemokine receptor type 4 (CXCR4) (EC50 = 194 nM, is an allosteric agonist activating the inhibitory heterotrimeric G protein (Gi) to promote inhibition of cAMP production and induce calcium mobilization.
  7. CB2 receptor agonist

    AM1241 is a selective cannabinoid CB2 receptor agonist with Ki of 3.4 nM, exhibits 82-fold selectivity over CB1 receptor.
  8. Adenosine A2 receptor agonist

    CGS 21680 HCl is an adenosine A2 receptor agonist with IC50 of 22 nM, exhibits 140-fold over A1 receptor.
  9. β2-adrenergic receptor agonist

    Clorprenaline HCl is a β2-receptor agonist, it has a significant expansion of the bronchial effect.
  10. GPR35/CXCR8 agonist

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

    Indacaterol (QAB149) maleate is an ultra-long-acting β-adrenoceptor agonist.
  12. β3-AR agonist

    L755507 is a potent, selective agonist of β3-AR with an IC50 of 35 nM.
  13. adenosine A2B receptor agonist

    MRS1706 is a selective adenosine A2B receptor inverse agonist with Ki values of 1.39, 157, 112, and 230 nM for human A2B, A1, A2A, and A3 receptors, respectively.
  14. Endogenous galanin receptor agonist

    Galanin (1-30) (human) is an endogenous peptide with multiple endocrine, metabolic and behavioral effects
  15. 5-HT7 receptor agonist

    LP-211 is a a selective agonist of the serotonin 5-HT7 receptor with a Ki value of 0.58 nM at rat cloned 5-HT7 receptors, and >300-fold selectivity over the 5-HT1A receptor.
  16. KOR agonist

    Asimadoline is a potent κ-opioid receptor (KOR) agonist (IC50s = 5.6 and 1.2 nM for guinea pig and human receptors, respectively).
  17. NK3 receptor agonist

    Senktide is a potent, selective agonist of the neuromedin K3 (NK3) receptor (EC50 = 0.5-3 nM).
  18. Adenosine receptor agonist

    NECA is a high-affinity adenosine receptor agonist (Ki values are 6.2, 14, and 20 nM for human A3, A1 and A2A receptors respectively; EC50 = 2.4 μM for human A2B).
  19. CaSR agonist

    Evocalcet is a calcium-sensing receptor agonist. The calcium-sensing receptor (CaSR) is a Class C G-protein coupled receptor which senses extracellular levels of calcium ion.
  20. GPR3 inverse agonist

    AF64394 is a GPR3 inverse agonist, with a pIC50 of 7.3.
  21. 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.
  22. 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.
  23. 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.
  24. TSHR inverse agonist

    ML224(NCGC00242364; ANTAG3) is a selective TSHR inverse agonist; inhibits TSH-stimulated cAMP production with an IC50 = 2.3 μM.
  25. 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.
  26. Smo receptor agonist

    SAG (hydrochloride) is a potent Smo receptor agonist, and activates the Hedgehog signaling pathway, with a Kd of 59 nM.
  27. 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.
  28. nociceptin receptor agonist

    MCOPPB 3Hcl is a nociceptin receptor agonist with pKi of 10.07; weaker activity at other opioid receptors.
  29. 5-HT1F receptor agonist

    LY 344864 S-enantiomer is the S-enantiomer of LY344864. LY344864 is a 5-HT1F receptor agonist.
  30. 5-HT1F agonist

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

    SKF-82958 hydrobromide is a D1/D5 receptor full agonist.
  32. 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.
  33. ghrelin receptor inverse agonist

    PF-5190457 is a potent and selective ghrelin receptor inverse agonist with a pKi of 8.36.
  34. 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.
  35. D1/D5 receptor full agonist

    SKF 82958 is a D1/D5 receptor full agonist.
  36. 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.
  37. 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.
  38. 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.
  39. partial mGluR4 agonist

    (1R,2S)-VU0155041, Cis regioisomer of VU0155041, is a partial mGluR4 agonist with an EC50 of 2.35 μM.
  40. 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.
  41. 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.
  42. 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.
  43. dopamine D4 receptor partial agonist

    Ro 10-5824 dihydrochloride is a selective dopamine D4 receptor partial agonist, with Ki of 5.2 nM.
  44. 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.
  45. 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.
  46. 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.
  47. 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.
  48. A1 adenosine receptor agonist

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

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

    Clenproperol is a β2-adrenergic agonist.

Items 151-200 of 367

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