LY3540378   Click here for help

GtoPdb Ligand ID: 12502

Comment: LY3540378 is a a long-acting relaxin analogue [1]. It is composed a human relaxin mimetic peptide fused to a serum albumin-binding VHH domain. It is selective for relaxin family peptide receptor 1 (RXFP1) compared to RXFP2, 3 and 4. VHH-serum albumin binding extends the peptide's circulating half-life.
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Selectivity at GPCRs
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Target Sp. Type Action Value Parameter Concentration range (M) Reference
RXFP1 Monkey Agonist Agonist 10.4 pKd - 1
pKd 10.4 (Kd 4x10-11 M) [1]
Description: Binding affinity determined by SPR.
RXFP1 Hs Agonist Agonist 10.1 pKd - 1
pKd 10.1 (Kd 8.1x10-11 M) [1]
Description: Binding affinity determined by SPR.
RXFP1 Mm Agonist Agonist 8.7 pKd - 1
pKd 8.7 (Kd 2x10-9 M) [1]
Description: Binding affinity determined by SPR.