Synthesis and characterization of [125I]TZ6544, a promising radioligand for investigating sphingosine-1-phosphate receptor 2

Synthesis and characterization of [125I]TZ6544, a promising radioligand for investigating sphingosine-1-phosphate receptor 2GPCR Target: S1PR4 lysophospholipid receptor membraneAuthors: Luo, Z., et al.Journal: Nucl Med Biol. 2020;88-89:52-61. doi:10.1016/j.nucmedbio.2020.07.007Year Published: 2020

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The effect of fatty diacid acylation of human PYY3-36 on Y2 receptor potency and half-life in minipigs

The effect of fatty diacid acylation of human PYY3-36 on Y2 receptor potency and half-life in minipigsGPCR Target: CHO cells stably expressing the human Y2R Cat # CG1274Authors: Østergaard, S.,…

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Discovery of CVN636: A Highly Potent, Selective, and CNS Penetrant mGluR7 Allosteric Agonist

Discovery of CVN636: A Highly Potent, Selective, and CNS Penetrant mGluR7 Allosteric AgonistGPCR Target: mGluR2,6,8 cAMP, mGluR1,3,5 Gαqi5 calcium flux assaysAuthors: Dickson, L., et al.Journal: ACS Medicinal Chemistry Letters 2023…

Continue ReadingDiscovery of CVN636: A Highly Potent, Selective, and CNS Penetrant mGluR7 Allosteric Agonist

Discovery of a potent, selective, and tumor-suppressing antibody antagonist of adenosine A2A receptor

Discovery of a potent, selective, and tumor-suppressing antibody antagonist of adenosine A2A receptorGPCR Target: MULTISCREEN Division-Arrested HEK293TAuthors: Wang, L., et al.Journal: PLOS ONE 19(6): e0301223. doi.org/10.1371/journal.pone.0301223Year Published: 2024

Continue ReadingDiscovery of a potent, selective, and tumor-suppressing antibody antagonist of adenosine A2A receptor

Retro Drug Design: From Target Properties to Molecular Structures

Retro Drug Design: From Target Properties to Molecular StructuresGPCR Target: hMOR-CHO-K1Authors: Wang, Y., et alJournal: Journal of Chemical Information and Modeling 2022 62 (11), 2659-2669 DOI: 10.1021/acs.jcim.2c00123Year Published: 2022

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Field and laboratory perspectives on fentanyl and carfentanil decontamination

Field and laboratory perspectives on fentanyl and carfentanil decontaminationGPCR Target: hMOR-CHO-K1-Gαqi5Authors: Lindén, P., et al.Journal: Sci Rep 14, 25381 (2024). doi.org/10.1038/s41598-024-74594-zYear Published: 2024

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Discovery of N-substituted-2-oxoindolin benzoylhydrazines as c-MET/SMO modulators in EGFRi-resistant non-small cell lung cancer

Discovery of N-substituted-2-oxoindolin benzoylhydrazines as c-MET/SMO modulators in EGFRi-resistant non-small cell lung cancerGPCR Target: HEK293T-WT SMO membranesAuthors: Tomassi S, et al.Journal: RSC Med Chem. 2024;16(1):77-97. doi:10.1039/d4md00553hYear Published: 2024

Continue ReadingDiscovery of N-substituted-2-oxoindolin benzoylhydrazines as c-MET/SMO modulators in EGFRi-resistant non-small cell lung cancer

Palmitic Acid Hydroxystearic Acids Activate GPR40, Which Is Involved in Their Beneficial Effects on Glucose Homeostasis

Palmitic Acid Hydroxystearic Acids Activate GPR40, Which Is Involved in Their Beneficial Effects on Glucose HomeostasisGPCR Target: GPR40 stable cell line, Cyclic AMP AssayAuthors: Syed, I., et al.Journal: Cell Metab.…

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Discovery of Novel and Selective GPR17 Antagonists as Pharmacological Tools for Developing New Therapeutic Strategies in Diabetes and Obesity

Discovery of Novel and Selective GPR17 Antagonists as Pharmacological Tools for Developing New Therapeutic Strategies in Diabetes and ObesityGPCR Target: 1321N1 GPR17 stable cell line (Catalog# Cr1525–3)Authors: Zhu, H., et…

Continue ReadingDiscovery of Novel and Selective GPR17 Antagonists as Pharmacological Tools for Developing New Therapeutic Strategies in Diabetes and Obesity