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A. Gα s activation profiling via luminescence-based cAMP accumulation assay ; B. β-arrestin 2 recruitment via NanoBiT based assay C. Shows the change in (Gα s /β-arr) signaling bias occurred upon Setmelanotide introduction . D. ERK activation via SRE Reporter luminescence-based assay ; E. Gα q activation via NFAT-RE Reporter luminescence-based assay ; F. Gα 12/13 activation via SRF-RE Reporter luminescence-based assay; n=3; % normalized of luminescence data in HEK293T cells; in every experiment error bar indicates ±SEM. G. Gives a comparative analysis of LogEC 50 and E max value simultaneously for each signaling profile with each of the variants which is plotted in a radar plot.

Journal: bioRxiv

Article Title: Sparsely Phosphorylable Residues, Tuned by Agonist Chemotype, Shapes GPCR Signaling

doi: 10.64898/2026.10.06.756976

Figure Lengend Snippet: A. Gα s activation profiling via luminescence-based cAMP accumulation assay ; B. β-arrestin 2 recruitment via NanoBiT based assay C. Shows the change in (Gα s /β-arr) signaling bias occurred upon Setmelanotide introduction . D. ERK activation via SRE Reporter luminescence-based assay ; E. Gα q activation via NFAT-RE Reporter luminescence-based assay ; F. Gα 12/13 activation via SRF-RE Reporter luminescence-based assay; n=3; % normalized of luminescence data in HEK293T cells; in every experiment error bar indicates ±SEM. G. Gives a comparative analysis of LogEC 50 and E max value simultaneously for each signaling profile with each of the variants which is plotted in a radar plot.

Article Snippet: The synthetic pharmacological panel, which included Melanotan I (MT-I; MedChemExpress, cat. no. HYN2466), Melanotan II (MT-II; MedChemExpress, cat. no. HYP0267), Bremelanotide (MedChemExpress, cat. no. SML2756), the small-molecule agonist THIQ (Sigma-Aldrich, cat. no. SML2449), and the FDA-approved therapeutic Setmelanotide (MedChemExpress, cat. no. HY-19870), were all purchased.

Techniques: Activation Assay, Profiling, Luminescence Assay, Analysis, Luciferase

Journal: bioRxiv

Article Title: Sparsely Phosphorylable Residues, Tuned by Agonist Chemotype, Shapes GPCR Signaling

doi: 10.64898/2026.10.06.756976

Figure Lengend Snippet: Calculation of receptor mediated bias factor with its FDA approved ligand Setmelanotide

Article Snippet: The synthetic pharmacological panel, which included Melanotan I (MT-I; MedChemExpress, cat. no. HYN2466), Melanotan II (MT-II; MedChemExpress, cat. no. HYP0267), Bremelanotide (MedChemExpress, cat. no. SML2756), the small-molecule agonist THIQ (Sigma-Aldrich, cat. no. SML2449), and the FDA-approved therapeutic Setmelanotide (MedChemExpress, cat. no. HY-19870), were all purchased.

Techniques: