eneboparatide   Click here for help

GtoPdb Ligand ID: 13815

Synonyms: AZP-3601 | AZP3601 | LA-PTH [2]
Compound class: Peptide
Comment: Eneboparatide (AZP-3601) is a synthetic long-acting PTH receptor 1 agonist [1-2]. It is a fusion of modified PTH(1-14) with amino acid substitutions and PTHrP(15-36). Compared to native human PTH, amino acid substitution in the PTH region of eneboparatide are S3>A, H5>I, L8>M, D10>Q, K11>R, G12>A, S14>W,L18>A, F22>A, H26>K Eneboparatide associates more potently with the R0 conformation of PTH1R (in the presence of 125I-PTH(1-34) and GTPγS to block receptor-G protein-coupling, compared to PTH(1-34) or PTH(1-84) [2]. All three peptides interact with the RG (G protein-coupled) conformation of PTH1R with similar potencies.
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Ligand Activity Visualisation Charts

These are box plot that provide a unique visualisation, summarising all the activity data for a ligand taken from ChEMBL and GtoPdb across multiple targets and species. Click on a plot to see the median, interquartile range, low and high data points. A value of zero indicates that no data are available. A separate chart is created for each target, and where possible the algorithm tries to merge ChEMBL and GtoPdb targets by matching them on name and UniProt accession, for each available species. However, please note that inconsistency in naming of targets may lead to data for the same target being reported across multiple charts.

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View interactive charts of activity data across species
Selectivity at GPCRs
Key to terms and symbols Click column headers to sort
Target Sp. Type Action Value Parameter Concentration range (M) Reference
PTH1 receptor Hs Agonist Agonist 8.8 – 10.0 pIC50 - 2
⤷ pIC50 10.0 (IC50 1x10-10 M) [2]
Description: Measuring radioligand displacement at the RG (G protein-coupled) conformation of hPTH1R using the radioligand 125I-M-PTH(1–15)
pIC50 8.8 (IC50 1.5x10-9 M) [2]
Description: Measuring radioligand displacement at the R0 (G protein-uncoupled) conformation of hPTH1R using the radioligand 125I-PTH(1–34) in the presence of GTPγS to block receptor-G protein coupling