GPCR/G Protein

Items 5101-5150 of 6977

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  1. 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.
  2. CGRP antagonist

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

    SAG (hydrochloride) is a potent Smo receptor agonist, and activates the Hedgehog signaling pathway, with a Kd of 59 nM.
  4. 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.
  5. AT2R antagonist

    Olodanrigan (EMA401) is a highly selective, orally active, peripherally restricted angiotensin II type 2 receptor (AT2R) antagonist.
  6. 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.
  7. 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.
  8. 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.
  9. nociceptin receptor agonist

    MCOPPB 3Hcl is a nociceptin receptor agonist with pKi of 10.07; weaker activity at other opioid receptors.
  10. 5-HT1F receptor agonist

    LY 344864 S-enantiomer is the S-enantiomer of LY344864. LY344864 is a 5-HT1F receptor agonist.
  11. 5-HT1F agonist

    LY 344864 hydrochloride is a selective 5-HT1F agonist with a Ki of 6 nM.
  12. 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).
  13. D1/D5 receptor full agonist

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

    NVS-CRF38 is a novel corticotropin-releasing factor receptor 1 (CRF1) antagonist with low water solubility.
  15. 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.
  16. ghrelin receptor inverse agonist

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

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

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

     
  19. 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.
  20. Bretylium (tosylate) is an inhibitor of the presynaptic release of vasoconstrictor neurotransmitters.
  21. mGlu5 receptor antagonist

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

    (+)-Penbutolol is a β-adrenoceptor antagonist, with an IC50 of 0.74 μM.
  23. 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).
  24. guanylate cyclase (GC) activator

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

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

    BMS-986020 sodium is a high-affinity lysophosphatidic acid receptor 1 (LPA1) antagonist.
  27. 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).
  28. 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.
  29. D1/D5 receptor full agonist

    SKF 82958 is a D1/D5 receptor full agonist.
  30. 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.
  31. CXCR3 antagonist

    AMG 487 S-enantiomer is the S enantiomer of AMG 487. AMG 487 is an antagonist of the chemokine receptor CXCR3.
  32. 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.
  33. 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.
  34. mGluR5 positive allosteric modulator

    (R)-ADX-47273 is a potent mGluR5 positive allosteric modulator, with an EC50 of 168 nM for potentiation .
  35. 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.
  36. leukotriene A4 hydrolase inhibitor

    DG051 is a potent leukotriene A4 hydrolase inhibitor of leukotriene B4 biosynthesis in the enzyme assay with an IC50=47 nM.
  37. DPP4 inhibitor

    Vildagliptin (LAF237 dihydrate;NVP-LAF 237 dihydrate) is a dipeptidyl peptidase 4 (DPP4) inhibitor that delays the degradation of glucagon-like peptide-1 (GLP-1).
  38. mGlu5 receptor antagonist

    Methoxy-PEPy is a potent and highly selective mGlu5 receptor antagonist with IC50 of 1 nM.
  39. CGRP1 receptor antagonist

    Olcegepant hydrochloride is the first potent and selective non-peptide antagonist of the calcitonin gene-related peptide 1 (CGRP1) receptor with IC50 of 0.03 nM and with a Ki of 14.4 pM for human CGRP.
  40. EP and DP receptor antagonist

    AH 6809 is an EP and DP receptor antagonist with nearly equal affinity for the cloned human EP1, EP2, EP3-III, and DP1 receptors.
  41. 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.
  42. 5-HT1B receptor antagonist

    SB-224289 hydrochloride is a selective 5-HT1B receptor antagonist, with anxiolytic effect.
  43. dopamine reuptake inhibitor

    Vanoxerine (GBR-12909) is a competitive, potent, and highly selective dopamine reuptake inhibitor (Ki=1 nM).
  44. 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.
  45. partial mGluR4 agonist

    (1R,2S)-VU0155041, Cis regioisomer of VU0155041, is a partial mGluR4 agonist with an EC50 of 2.35 μM.
  46. LTC4 inhibitor

    Nedocromil sodium suppresses the action or formation of multiple mediators, including histamine, leukotriene C4 (LTC4), and prostaglandin D2 (PGD2).
  47. EP4 antagonist

    CJ-42794 is a selective prostaglandin E receptor subtype 4 (EP4) antagonist, inhibits [3H]-PGE2 binding to the human EP4 receptor with a mean pKi of 8.5, a binding affinity that was at least 200-fold more selective for the human EP4 receptor than other human EP receptor subtypes (EP1, EP2, and EP3).
  48. 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.
  49. dopamine reuptake inhibitor

    GBR 12935 is a potent, and selective dopamine reuptake inhibitor.
  50. 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.

Items 5101-5150 of 6977

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