Pharmacological profile of upacicalcet, a novel positive allosteric modulator of calcium-sensing receptor, in vitro and in vivoGPCR Target: Stably human CaSR-expressing HEK-293TAuthors: Moritaka Goto, et al.Journal: European Journal of Pharmacology, Volume…
Xelaglifam, a novel GPR40/FFAR1 agonist, exhibits enhanced β-arrestin recruitment and sustained glycemic control for type 2 diabetesGPCR Target: MULTISCREENᵀᴹ TR-FRET cAMP 1.0 No Wash Assay KitAuthors: Jongmin Yoon, et al.Journal: Biomedicine…
Preclinical development of EXT608, an investigational parathyroid hormone derivative with extended half-life for the treatment of hypoparathyroidismGPCR Target: PTHR1Authors: Daniel B. Hall, et al.Journal: JBMR Plus, Volume 8, Issue 6,…
Structure-Based Drug Design of ADRA2A Antagonists Derived from YohimbineGPCR Target: Calcium assayAuthors: Chayka A, et al.Journal: J Med Chem. 2024 Jun 27;67(12):10135-10151. doi: 10.1021/acs.jmedchem.4c00323.Year Published: 2024
D-VITylation: Harnessing the biology of vitamin D to improve the pharmacokinetic properties of peptides and small proteinsAuthors: Daniel B. Hall, et al.Company: Pharvaris Netherlands B.V., Leiden, NetherlandsJournal: International Journal of…
Competitive Binding of Ozanimod and Other Sphingosine 1-Phosphate Receptor Modulators at Receptor Subtypes 1 and 5In Vitro Pharmacological Profile of a New Small Molecule Bradykinin B2 Receptor AntagonistGPCR Target: S1p2,…
Isoquinolone derivatives as lysophosphatidic acid receptor 5 (LPA5) antagonists: Investigation of structure-activity relationships, ADME properties and analgesic effectsGPCR Target: LPA5Authors: Zhang D, et al.Journal: Eur J Med Chem. 2022 Dec…
In vitro pharmacodynamic studies of IDG-16177, a Potent GPR40 agonist, for the Treatment of Type 2 DiabetesGPCR Target: GPR40Authors: Jongmin Yoon, et al.Journal: Diabetes 1 June 2021; 70 (Supplement_1): 122–LB. Year Published: 2021
Identification and In Vivo Evaluation of Myelination Agent PIPE-3297, a Selective Kappa Opioid Receptor Agonist Devoid of β-Arrestin-2 Recruitment EfficacyGPCR Target: Membranes isolated from CHO-K1 cells stably expressing human KORs…
A FFAR1 full agonist restores islet function in models of impaired glucose-stimulated insulin secretion and diabetic non-human primatesAuthors: Rady, B., et al.Journal: Frontiers in Endocrinology, 13. Year Published: 2022