amylin   Click here for help

GtoPdb Ligand ID: 687

Abbreviated name: AMY
Compound class: Endogenous peptide in human, mouse or rat
Comment: Amylin acts as an appetite suppressor. Novo Nordisk have a long-acting amylin mimetic (AM833, NNC0174-0833) in clinical trials with and without semaglutide. AM833 is intended as a treatment for obesity. In the trials it is administered subcutaneously, once-weekly. Preliminary (and as yet unpublished) results from a Phase 2 trial as monotherapy demonstrated weight loss of 10.8% at week 26, meeting the study's primary endpoint (Novo Nordisk press release 18 Jun 2020).
Species: Human
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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
Natural/Endogenous Targets
Target
AMY1 receptor
AMY2 receptor
AMY3 receptor
CT receptor
Selectivity at GPCRs
Key to terms and symbols Click column headers to sort
Target Sp. Type Action Value Parameter Concentration range (M) Reference
AMY1 receptor Ligand is endogenous in the given species Hs Agonist Full agonist 9.0 – 9.7 pEC50 - 1
⤷ pEC50 9.0 – 9.7 (EC50 1x10-9 – 1.94x10-10 M) [1]
Description: Measuring ligand-induced cAMP production in COS and HEK293 cells.
AMY3 receptor Ligand is endogenous in the given species Hs Agonist Full agonist 8.9 – 9.6 pEC50 - 1
⤷ pEC50 8.9 – 9.6 (EC50 1.258x10-9 – 2.51x10-10 M) [1]
Description: Measuring ligand-induced cAMP production in COS and HEK293 cells.
AMY2 receptor Ligand is endogenous in the given species Hs Agonist Full agonist 8.3 – 9.1 pEC50 - 1
⤷ pEC50 8.3 – 9.1 (EC50 5.37x10-9 – 7.76x10-10 M) [1]
Description: Measuring ligand-induced cAMP production in COS and HEK293 cells.
CT receptor Ligand is endogenous in the given species Hs Agonist Full agonist 8.0 – 9.2 pEC50 - 1-3
⤷ pEC50 8.0 – 9.2 [1-3]
Additional information and targets (data relate to human unless otherwise stated)
Description Data Reference
Potency order of endogenous ligands at CT receptor calcitonin (CALCA, P01258) ≥ amylin (IAPP, P10997), α-CGRP (CALCA, P06881), β-CGRP (CALCB, P10092) > adrenomedullin (ADM, P35318), adrenomedullin 2/intermedin (ADM2, Q7Z4H4)
Potency order of endogenous ligands at AMY1 receptor amylin (IAPP, P10997) ≥ α-CGRP (CALCA, P06881), β-CGRP (CALCB, P10092) > adrenomedullin 2/intermedin (ADM2, Q7Z4H4) ≥ calcitonin (CALCA, P01258) > adrenomedullin (ADM, P35318)
Potency order of endogenous ligands at CGRP receptor α-CGRP (CALCA, P06881), β-CGRP (CALCB, P10092) > adrenomedullin (ADM, P35318) ≥ adrenomedullin 2/intermedin (ADM2, Q7Z4H4) > amylin (IAPP, P10997)
Potency order of endogenous ligands at AM1 receptor adrenomedullin (ADM, P35318) > adrenomedullin 2/intermedin (ADM2, Q7Z4H4) > α-CGRP (CALCA, P06881), β-CGRP (CALCB, P10092), amylin (IAPP, P10997)
Potency order of endogenous ligands at AM2 receptor adrenomedullin (ADM, P35318) ≥ adrenomedullin 2/intermedin (ADM2, Q7Z4H4) ≥ α-CGRP (CALCA, P06881), β-CGRP (CALCB, P10092) > amylin (IAPP, P10997)
Potency order of endogenous ligands at AMY3 receptor amylin (IAPP, P10997) > α-CGRP (CALCA, P06881), β-CGRP (CALCB, P10092) ≥ adrenomedullin 2/intermedin (ADM2, Q7Z4H4) ≥ calcitonin (CALCA, P01258) > adrenomedullin (ADM, P35318)
Ligand mentioned in the following text fields
Calcitonin receptors overview