GPCR/G Protein

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  1. Alimemazine D6 is deuterium labeled Alimemazine, which is an antihistamine.
  2. Indoramin D5 is deuterium labeled Indoramin, which is a piperidine antiadrenergic agent.
  3. GPR3 inverse agonist

    AF64394 is a GPR3 inverse agonist, with a pIC50 of 7.3.
  4. angiotensin II receptor antagonist

    Losartan D4 Carboxylic Acid is the deuterium labeled Losartan(EXP-3174), which is an angiotensin II receptor antagonist.
  5. 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.
  6. Neurokinin-1 (NK-1) receptor antagonist

    Serlopitant is a selective Neurokinin-1 (NK-1) receptor antagonist.
  7. angiotensin II type 1 receptor antagonist

    Azilsartan D5 is the deuterium labeled Azilsartan(TAK-536), which is a specific and potent angiotensin II type 1 receptor antagonist.
  8. 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.
  9. 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.
  10. TSHR inverse agonist

    ML224(NCGC00242364; ANTAG3) is a selective TSHR inverse agonist; inhibits TSH-stimulated cAMP production with an IC50 = 2.3 μM.
  11. GPR40 activator

    GPR40 Activator 2 is a potent GPR40 activator from patents WO 2012147516 A1, WO 2012046869A1 and WO 2011078371 A1.
  12. sGC inhibitor

    NS-2028 is a highly selective soluble Guanylyl Cyclase (sGC) inhibitor with IC50 values of 30 nM and 200 nM for basal and NO-stimulated enzyme activity.
  13. OT-R antagonist

    OT-R antagonist 2 is a nonpeptide low molecular weight OT-R antagonist. OT-R antagonist 2 inhibitis IP3-Synthesis, rat OT-R (IC50 = 0.33 μM).
  14. adenosine A1 receptor antagonist

    Rolofylline (KW-3902) is a potent, selective adenosine A1 receptor antagonist that is under development for the treatment of patients with acute congestive heart failure and renal impairment.
  15. mGlu2 agonist/mGlu3 antagonist

    LY541850 is a selective orthosteric mGlu2 agonist and mGlu3 antagonist with IC50 values of 0.161 μM and 0.038 μM, respectively.
  16. 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.
  17. CGRP antagonist

    Ubrogepant (MK-1602) is a novel oral calcitonin gene-related peptide receptor (CGRP) antagonist in development for acute treatment of migraine.
  18. Smo receptor agonist

    SAG (hydrochloride) is a potent Smo receptor agonist, and activates the Hedgehog signaling pathway, with a Kd of 59 nM.
  19. triple reuptake inhibitor

    Dasotraline hydrochloride (SEP-225289 hydrochloride) is a triple reuptake inhibitor that blocks dopamine, norepinephrine, and serotonin transporters with IC50 values of 4, 6, and 11 nM, respectively.
  20. AT2R antagonist

    Olodanrigan (EMA401) is a highly selective, orally active, peripherally restricted angiotensin II type 2 receptor (AT2R) antagonist.
  21. CB1 antagonist/inverse agonist

    Taranabant racemate is an antagonist and/or inverse agonist of the Cannabinoid-1 (CB1) receptor extracted from patent WO 2004048317 A1.
  22. 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.
  23. 5-HT2C receptor antagonist

    SB 242084 is a 5-HT2C receptor antagonist(pKi=9.0) that displays 158- and 100-fold selectivity over 5-HT2A and 5-HT2B receptors respectively.
  24. nociceptin receptor agonist

    MCOPPB 3Hcl is a nociceptin receptor agonist with pKi of 10.07; weaker activity at other opioid receptors.
  25. 5-HT1F receptor agonist

    LY 344864 S-enantiomer is the S-enantiomer of LY344864. LY344864 is a 5-HT1F receptor agonist.
  26. 5-HT1F agonist

    LY 344864 hydrochloride is a selective 5-HT1F agonist with a Ki of 6 nM.
  27. SSTR5 antagonist

    SSTR5 Antagonist 1 (compound 10) is a highly potent, oral active and selective somatostatin (receptor) subtype 5 (SSTR5) antagonist and has potential to treat type 2 diabetes mellitus (T2DM).
  28. D1/D5 receptor full agonist

    SKF-82958 hydrobromide is a D1/D5 receptor full agonist.
  29. CRF1 antagonist

    NVS-CRF38 is a novel corticotropin-releasing factor receptor 1 (CRF1) antagonist with low water solubility.
  30. 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.
  31. ghrelin receptor inverse agonist

    PF-5190457 is a potent and selective ghrelin receptor inverse agonist with a pKi of 8.36.
  32. LTB4 antagonist

    BIIL-260 hydrochloride is a potent and long-acting orally active leukotriene B(4) receptor LTB4 antagonist, with anti-inflammatory activity.
  33. μ-opioid receptor (MOR) antagonist

    GSK1521498 hydrochloride is a potent and selective μ-opioid receptor (MOR) antagonist.

     
  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. Bretylium (tosylate) is an inhibitor of the presynaptic release of vasoconstrictor neurotransmitters.
  36. mGlu5 receptor antagonist

    Mavoglurant (racemate) is the racemate of mavoglurant. Mavoglurant is a novel, non-competitive mGlu5 receptor antagonist.
  37. β-adrenoceptor antagonist

    (+)-Penbutolol is a β-adrenoceptor antagonist, with an IC50 of 0.74 μM.
  38. immune modulator

    Anandamide is an immune modulator in the central nervous system acts via not only cannabinoid receptors (CB1 and CB2) but also other targets (e.g., GPR18/GPR55).
  39. guanylate cyclase (GC) activator

    Cinaciguat hydrochloride is a potent soluble guanylate cyclase (GC) activator with EC50 of 15 nM in platelets.
  40. glucagon receptor antagonist

    LGD-6972 is a glucagon receptor antagonist.
  41. LPA1 antagonist

    BMS-986020 sodium is a high-affinity lysophosphatidic acid receptor 1 (LPA1) antagonist.
  42. endothelin ETA and ETB receptor antagonist

    Macitentan n-butyl analogue is a n-butyl analogue of Macitentan. Macitentan is an orally active, non-peptide dual endothelin ETA and ETB receptor antagonist for the potential treatment of idiopathic pulmonary fibrosis (IPF) and pulmonary arterial hypertension (PAH).
  43. Smo allosteric activator

    20(S)-hydroxyCholesterol (20α-Hydroxycholesterol) is an allosteric activator of the oncoprotein smoothened (Smo) that activates the hedgehog (Hh) signaling pathway with an EC50 of 3 μM in a gene transcription reporter assay using NIH3T3 cells.
  44. D1/D5 receptor full agonist

    SKF 82958 is a D1/D5 receptor full agonist.
  45. 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.
  46. CXCR3 antagonist

    AMG 487 S-enantiomer is the S enantiomer of AMG 487. AMG 487 is an antagonist of the chemokine receptor CXCR3.
  47. SSR inhibitor / 5-HT1A receptor partial agonist

    Vilazodone D8 is the a deuterium labeled vilazodone, which is a combined serotonin specific reuptake inhibitor (SSRI) and 5-HT1A receptor partial agonist.
  48. non-peptide CCR1 antagonist

    BX471 hydrochloride (ZK-811752 hydrochloride) is a potent, selective non-peptide CCR1 antagonist with Ki of 1 nM for human CCR1, and exhibits 250-fold selectivity for CCR1 over CCR2, CCR5 and CXCR4.
  49. mGluR5 positive allosteric modulator

    (R)-ADX-47273 is a potent mGluR5 positive allosteric modulator, with an EC50 of 168 nM for potentiation .
  50. 5-HT7 receptor antagonist

    SB269970 hydrochloride (SB-269970A) is a hydrochloride salt form of SB-269970, which is a 5-HT7 receptor antagonist with the pKi of 8.3, exhibits >50-fold selectivity against other receptors.

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