LY3463251   Click here for help

GtoPdb Ligand ID: 12843

Comment: LY3463251 is a synthetic peptide of the growth differentiation factor 15 (GDF15) ligand fused to IgG4-Fc [1]. The Fc moiety extends the agents circulating half-life. LY3463251 acts as a agonist at the GDF15 receptor GFRAL/RET. This action decreases food intake and body weight in animal models, providing proof of concept for this mechanism as a weight-loss approach.
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Selectivity at catalytic receptors
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Target Sp. Type Action Value Parameter Concentration range (M) Reference
GDNF family receptor alpha like Hs Agonist Agonist 8.5 pKd - 1
pKd 8.5 (Kd 3.1x10-9 M) [1]
Description: Binding affinity for GFRAL receptor construct D2-D3-ECD-HIS
GDNF family receptor alpha like Hs Agonist Agonist 7.3 pEC50 - 1
pEC50 7.3 (EC50 5.47x10-8 M) [1]
Description: In vitro functional activity of LY3463251
GDNF family receptor alpha like Mm Agonist Agonist 6.9 pEC50 - 1
pEC50 6.9 (EC50 1.362x10-7 M) [1]
Description: In vitro functional activity of LY3463251