GPCR/G Protein

Items 5401-5450 of 6977

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  1. mGluR5 antagonist

    AZD 2066 is a selective, orally active and brain-penetrant mGluR5 antagonist, with analgesia activity.
  2. CRTh2 antagonist

    CRTh2 antagonist 1 is a CRTh2 antagonist with an IC50 of 89 nM.
  3. mGluR5 antagonist

    AZD 9272 is a brain penetrant mGluR5 antagonist.
  4. ETA antagonist

    ETA antagonist 1 is a ETA selective antagonist with an IC50 of 0.08 μM.
  5. angiotensin II receptor antagonist

    CGP48369 is a nonpeptidic angiotensin II receptor antagonist, used for anti-hypertensive research.
  6. mGluR4 modulator

    Foliglurax (PXT002331) is a highly selective and potent, brain-penetrant metabotropic glutamate receptor 4 positive allosteric modulator (mGluR4 PAM) with an EC50 of 79 nM. Antiparkinsonian effect.
  7. CGRP receptor antagonist

    CGRP antagonist 1 is a highly potent CGRP receptor antagonist with a Ki and IC50 of 35 and 57 nM, respectively.
  8. neuropeptide Y1 receptor antagonist

    Y1 receptor antagonist 1 (H 409-22 isomer) is a neuropeptide Y1 receptor antagonist.
  9. PGF2α analogue

    Tiaprost is a prostaglandin F2α (PGF2α) analogue.
  10. 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.
  11. TXA2 receptor

    LCB-2853 is an antagonist of thromboxane A2 (TXA2) receptor, with antiplatelet and antithrombotic activities.
  12. GRK2/GRK3 inhibitor

    CMPD101, is a novel membrane-permeable, small-molecule inhibitor of both GRK2 and GRK3 with IC50s of 18 nM and 5.4 nM. CMPD101 also inhibits ROCK-2 and PKCα (IC50s=1.4 μM and 8.1 μM, respectively).
  13. 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.
  14. EP1 antagonist

    EP1-antanoist-1 is a EP1 antagonist with a pKi of 7.54 and an pIC50 of 8.5.
  15. NPY5-R antagonist

    L 152804 is an orally active and selective neuropeptide Y Y5 receptor (NPY5-R) antagonist, with a Ki of 26 nM for hY5. L 152804 causes weight loss in diet-induced obese mice by modulating food intake and energy expenditure.
  16. Lipid-lowering Agent

    AZ-1355 is an effctive lipid-lowering compound, which also inhibits platelet aggregation in vivo and elevates the prostaglandin I2/thromboxane A2 ratio in vitro.
  17. oxytocin receptor antagonist

    L-368,899 hydrochloride is a potent, selective, orally bioavailable, non-peptide oxytocin receptor antagonist, with IC50s of 8.9 nM and 26 nM for rat uterus and human uterus oxytocin receptor, respectively, used as a tocolytic agent.
  18. neuropeptide Y5 receptor antagonist

    CGP71683 hydrochloride is a competitive neuropeptide Y5 receptor antagonist with a Ki of 1.3 nM, and shows no obvious activity at Y1 receptor (Ki, >4000 nM) and Y2 receptor (Ki, 200 nM) in cell membranes.
  19. beta adrenergic receptor antagonist

    Ecastolol is a beta adrenergic receptor antagonist, with antianginal activities.
  20. α1 adrenergic receptor antagonist

    QF0301B is an α1 adrenergic receptor antagonist and a low α2 adrenoceptor, 5-HT2A, and histamine H1 receptor blocker.
  21. NK2 antagonist

    GR 159897 is a highly potent, selective, competitive, brain-penetrated non-peptide antagonist at tachykinin NK2 receptors, inhibits binding of [3H]GR100679 to hNK2-CHO cells and rat colon membranes with pKis of 9.51 and 10, respectively. Antagonizes bronchoconstriction, with anxiolytic-like activity.
  22. CysLT1 receptor antagonist

    LM-1484 is an antagonist of CysLT1 receptor and displays a higher affinity for 3H-LTC4 sites.
  23. 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.
  24. peripheral adrenoceptor antagonist

    Deriglidole is a peripheral adrenoceptor antagonist with a high affinity for α2-adrenoceptors.
  25. PAF antagonist

    Apafant (WEB 2086), a potent platelet-activating factor (PAF) antagonist, inhibits PAF binding to human PAF receptors with a Ki of 9.9 nM.
  26. 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.
  27. 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.
  28. melatonin agonist

    Ramelteon metabolite M-II is the major metabolite of Ramelteon, with IC50s of 208 pM, 1470 pM for human melatonin receptors (MT1 or MT2). Ramelteon is a selective melatonin agonist.
  29. MCHR1 antagonist

    SNAP 94847 is a novel, high affinity selective melanin-concentrating hormonereceptor1 (MCHR1) antagonist with (Ki= 2.2 nM, Kd=530 pM), it displays >80-fold and >500-fold selectivity over MCHα1A and MCHD2 receptors respectively.
  30. peptidoleukotrienes antagonist

    RG-12525 is a a specific, competitive and orally effective antagonist of the peptidoleukotrienes, LTC4, LTD4 and LTE4, inhibiting LTC4-, LTD4- and LTE4-inducd guinea pig parenchymal strips contractions, with IC50s of 2.6 nM, 2.5 nM and 7 nM, respectively; RG-12525 is also a peroxisome proliferator-activated receptor gamma (PPAR-gamma) agonist with IC50 of appr 60 nM and a potent inhibitor of CYP3A4, with a Ki value of 0.5 ?M.
  31. adenylate cyclase inhibitor

    CB-7921220 is an adenylate cyclase inhibitor.
  32. PAF antagonist

    Setipafant is a platelet-activating factor (PAF) antagonist.
  33. Oxytocin antagonist

    OT antagonist 1 (Compound 4) is a potent, selective Oxytocin antagonist with a Ki of 50 nM.
  34. oxytocin (OT) antagonist

    OT antagonist 3 is an oxytocin (OT) antagonist extracted from patent WO2007017752A1.
  35. GPR35/CXCR8 antagonist

    ML 145 is a selective GPR35/CXCR8 antagonist with an IC50/EC50 of 20.1 nM, but not for the related GPR55 orphan receptor. GPR35 is expressed by various cells of the immune system and it may has potential as a therapeutic target in inflammatory disease.
  36. AT1 receptor antagonist

    ZD 7155 hydrochloride is an angiotensin II receptor type 1 (AT1 receptor) antagonist.
  37. γ-L-Glutamyl-L-alanine, composed of gamma-glutamate and alanine, is a proteolytic breakdown product of larger proteins.

  38. 5-HT4 receptor antagonist

    Sulamserod is a 5-HT4 receptor antagonist, with antiarrhythmic activities.
  39. 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.
  40. 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.
  41. A1 adenosine receptor agonist

    N6-(2-Phenylethyl)adenosine is a selective A1 adenosine receptor agonist.
  42. CRTh2 receptor antagonist

    MK-8318 is a potent and selective CRTh2 receptor antagonist with a Ki of 5.0 nM.
  43. β adrenergic receptor antagonist

    Pargolol hydrochloride is a β adrenergic receptor antagonist.
  44. SERT inhibitor

    DSP-1053 is a potent Serotonin Transporter (SERT) (Ki=1.02 nM) inhibitor with partial 5-HT1A receptor (Ki=5.05 nM) agonistic activity.
  45. AP5
    AP5 exhibits potent and selective agonism for the GPR40 receptor with positive allosteric modulation of endogenous ligands (AgoPAM). AP5 demonstrates a rat hIP1 EC50 of 0.49±0.28 nM against the GPR40 receptor.
  46. mGluR2 modulator

    AZD-8529 is a potent, highly selective and orally bioavailable positive allosteric modulator of mGluR2, with an EC50 of 285 nM, and shows no positive allosteric modulator responses at 20-25 M on the mGluR1, 3, 4, 5, 6, 7, and 8 subtypes.
  47. mGlu1 receptor modulator

    FITM is a negative allosteric modulator of mGlu1 receptor with a Ki of 2.5 nM.
  48. 5-HT1B receptor antagonist

    AR-A 2 is a selective 5-HT1B receptor antagonist.
  49. BRS-3 antagonist

    ML-18 is a non-peptide bombesin receptor subtype-3 (BRS-3) antagonist with an IC50 of 4.8 μM.
  50. AChE /M1/M2/5HT4/I2 inhibitor

    MHP 133 is a drug with multiple CNS targets, and inhibits acetylcholinesterase (AChE) with Ki of 69 μM; also active against muscarinic M1 and M2 receptors, serotonin 5HT4 receptors, and imidazole I2 receptors.

Items 5401-5450 of 6977

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