GPCR/G Protein

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  1. mGluR2 modulator

    BINA is a selective positive allosteric modulator of mGlu2 (EC50 = 33.2 nM in CHO cells expressing human mGlu2).
  2. mGluR5 modulator

    ADX-47273 is a drug used in scientific research which acts as a positive allosteric modulator selective for the metabotropic glutamate receptor subtype mGluR5.

  3. CB1 modulator?€?

    Org 27569 is a potent CB1 receptor allosteric modulator (pEC50 = 8.24).
  4. mGluR5 PAM

    VU 0357121 is a positive allosteric modulator (PAM) of the metabotropic glutamate receptor 5 (mGlu5) with EC50 = 33 nM, 92% Glumax.
  5. mGlu4 receptors modulator

    VU 0364770 is a positive allosteric modulator at mGlu4 receptors with EC50 value of 290 nM in mGlu4-expressing HEK 293 cells.
  6. mGlu4 receptor modulator

    Lu AF21934 is a selective and brain-penetrant mGlu4 receptor positive allosteric modulator with an IC50 of 500 nM for human mGlu4.
  7. mGluR5 positive allosteric modulator

    BMT-145027 is an mGluR5 positive allosteric modulator without inherent agonist activity, exhibits an EC50 of 47 nM.
  8. mGlu4 receptors modulator

    VU 0361737 is a selective positive allosteric modulator at mGluR-4 (EC50 values are 240 and 110 nM at human and rat receptors respectively).
  9. 5-HT Receptor modulator

    Lu-AA21004 is an oral multimodal serotonergic agent, inhibits 5-HT(1A), 5-HT(1B), 5-HT(3A), 5-HT(7) and SERT with IC50 of 15 nM, 33 nM, 3.7 nM, 19 nM and 1.6 nM, respectively.
  10. GluR modulator

    VU 0364439 is a positive allosteric modulator (PAM) of mGlu4 receptors (EC50 = 19.8 nM in vitro for human mGlu4).
  11. mGluR2 PAM

    JNJ-40411813 is a novel mGluR2 PAM.
  12. endothelin receptor modulator

    Endothelin Mordulator 1 is a endothelin receptor modulator, used for the research of endothelin-mediated disorders.
  13. S1P1 receptor modulator

    Ponesimod is an orally active, selective sphingosine-1-phosphate receptor 1 (S1P1) immunomodulator with EC50 of 5.7 nM.
  14. 5-HT3 Receptor Modulator

    PU 02 is a negative allosteric modulator of 5-HT3 receptors.
  15. mGluR4 modulator

    VU6001376 is a potent and selective positive allosteric modulator of the metabotropic glutamate receptor 4 (mGlu4 PAM) with an EC50 of 50.1 nM.
  16. mGluR-2 modulator

    JNJ-42153605 is a positive allosteric modulator of the metabotropic glutamate 2 receptor.
  17. mGluR1 modulator

    CPPHA is a selective positive allosteric modulator of mGluR5 receptor.
  18. GPR120 modulator 1 is useful for modulating G protein-coupled receptor 120 (GPR120).
  19. GPR120 modulator 2 is useful for modulating G protein-coupled receptor 120 (GPR120).
  20. mGlu2 receptor modulator

    CBiPES hydrochloride is a selective positive allosteric modulator of the mGluR-2 with IC50 value of 98.2 nM
  21. S1PR1 modulators

    RPC1063 is a selective sphingosine 1 phosphate receptor modulators and methods which may be useful in the treatment of S1P1-?associated diseases.
  22. mGluR5 Modulator

    VU0364289 is a novel N-aryl piperazine mGlu5 positive allosteric modulator.
  23. SK2 modulator

    NS13001 is a selective SK2/3 modulator that acts as a potential therapeutic agent for treatment of SCA2 and possibly other cerebellar ataxias.
  24. CXCR4 receptor modulator

    NSC-23026 is a CXCR4 receptor modulator.
  25. NTR1 allosteric modulator

    SBI-553 is a potent and brain penetrant NTR1 allosteric modulator.
  26. Thyrotropin receptor modulator

    D3-βArr is a positive allosteric modulator for thyrotropin receptor (TSHR), which initiates translocation of β-Arr 1 by direct TSHR activation and potentiates TSH-mediated preosteoblast differentiation in vitro.
  27. GLP-1R modulator

    VU0453379 is a CNS-penetrant glucagon-like peptide 1 receptor (GLP-1R) positive allosteric modulator (PAM) with an EC50 of 1.3 μM.
  28. sigma-1 receptors modulator

    E1R is a novel positive allosteric modulator of sigma-1 receptors.
  29. mGlu5 modulator

    VU0652835 is a metabotropic glutamate receptor subtype 5 (mGlu5) negative allosteric modulator with an IC50 of 81 nM.
  30. GLP-1R modulator

    NNC0640 is a negative allosteric modulator of glucagon-like peptide-1 receptor (GLP-1R).
  31. 5-HT1 receptor modulator

    NEO 376 is a selective modulator of 5-HT1 receptor, GABA receptor and dopamine receptor, with anti-psychotic actively.
  32. CXCR7 modulator

    CXCR7 modulator 1 (compound 25) is a potent and orally bioavailable peptoid hybrid CXCR7 modulator, with a Ki of 9 nM.
  33. CNS penetrant modulator

    VU0650786 is a potent and selective CNS penetrant negative allosteric modulator of metabotropic glutamate receptor subtype 3 (mGlu3 NAM), with an IC50 of 392 nM. VU0650786 has antidepressant and anxiolytic activity in rodents.
  34. 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.
  35. 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.
  36. mGlu1 receptor modulator

    FITM is a negative allosteric modulator of mGlu1 receptor with a Ki of 2.5 nM.
  37. 5-HT1A modulator

    5-HT1A modulator 1 displays very high affinities for the 5HT1A, adrenergic α1 and dopamine D2 receptor with IC50s of 2 ±0.3 nM, 10 ± 3 nM and 40 ±9 nM, respectively.
  38. mGluR1 receptors Modulator

    DFMTI is an allosteric negative modulator of mGluR1 receptors.
  39. mGlu1 receptors modulator

    Ro 67-7476 is a positive allosteric modulator of mGlu1 receptors.
  40. mGlu5 modulator

    JNJ-46778212 (VU 0409551) is an mGlu5 positive allosteric modulator with an EC50 of 260 nM.
  41. mGluR4 PAM

    ADX88178 is a potent metabotropic glutamate receptor 4 positive allosteric modulator (mGluR4 PAM) with an EC50 of 4 nM for human mGluR4.
  42. mGlu4 receptor modulator

    TCN238 is a positive allosteric mGlu4 receptor modulator with an EC50 of 1 μM.
  43. mGlu5 negative allosteric modulator

    Basimglurant (RG7090) is a potent, selective and orally available mGlu5 negative allosteric modulator with a Kd of 1.1 nM.
  44. human CX3CR1 receptor modulator

    AZD8797 is an allosteric non-competitive and orally active modulator of the human CX3CR1 receptor; antagonizes CX3CR1 and CXCR2 with Kis of 3.9 and 2800 nM, respectively.
  45. mGluR4 modulator

    Foliglurax monohydrochloride (PXT002331 monohydrochloride) 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.
  46. A3 adenosine receptor allosteric modulator

    LUF6000 is an allosteric modulator of the human A3 adenosine receptor (AR).
  47. 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).
  48. mGluR5 positive allosteric modulator

    (R)-ADX-47273 is a potent mGluR5 positive allosteric modulator, with an EC50 of 168 nM for potentiation .
  49. GAL2 receptor PAM

    CYM2503 is a positive allosteric modulator (PAM) of the GAL2 receptor that potentiates galanin-induced IP1 production in vitro.
  50. δ-opioid receptor modulator

    BMS-986188 is a novel Potent and Selective Positive Allosteric Modulator of the delta-Opioid Receptor.

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