Target family: Calcitonin receptors (type: gpcr)
Target: CGRP receptor

Ligand: adrenomedullin (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pIC50
Reference (Journal): Cloning, characterization and central nervous system distribution of receptor activity modifying proteins in the rat.
Published in: Eur J Neurosci

Ligand: adrenomedullin (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pIC50
Reference (Journal): Mouse receptor-activity-modifying proteins 1, -2 and -3: amino acid sequence, expression and function.
Published in: Mol Cell Endocrinol

Ligand: adrenomedullin (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 7.6 pIC50
Reference (Journal): Three receptor-activity-modifying proteins define calcitonin gene-related peptide or adrenomedullin selectivity of the mouse calcitonin-like receptor in COS-7 cells.
Published in: Biochem Pharmacol

Ligand: adrenomedullin (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 8.1 pKi
Reference (Journal): Receptor activity modifying proteins interaction with human and porcine calcitonin receptor-like receptor (CRLR) in HEK-293 cells.
Published in: Mol Cell Biochem

Ligand: adrenomedullin (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 8.1 pKi
Reference (Journal): RAMPs regulate the transport and ligand specificity of the calcitonin-receptor-like receptor.
Published in: Nature

Ligand: adrenomedullin 2/intermedin (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pEC50
Reference (Journal): The pharmacology of adrenomedullin 2/intermedin.
Published in: Br J Pharmacol

Ligand: α-CGRP (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pIC50
Reference (Journal): Cloning, characterization and central nervous system distribution of receptor activity modifying proteins in the rat.
Published in: Eur J Neurosci

Ligand: α-CGRP (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pIC50
Reference (Journal): A receptor activity modifying protein (RAMP)2-dependent adrenomedullin receptor is a calcitonin gene-related peptide receptor when coexpressed with human RAMP1.
Published in: Endocrinology

Ligand: α-CGRP (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pIC50
Reference (Journal): Mouse receptor-activity-modifying proteins 1, -2 and -3: amino acid sequence, expression and function.
Published in: Mol Cell Endocrinol

Ligand: α-CGRP (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pIC50
Reference (Journal): Mammalian calcitonin receptor-like receptor/receptor activity modifying protein complexes define calcitonin gene-related peptide and adrenomedullin receptors in Drosophila Schneider 2 cells.
Published in: FEBS Lett

Ligand: α-CGRP (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): RAMPs regulate the transport and ligand specificity of the calcitonin-receptor-like receptor.
Published in: Nature

Ligand: α-CGRP (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Receptor activity modifying proteins interaction with human and porcine calcitonin receptor-like receptor (CRLR) in HEK-293 cells.
Published in: Mol Cell Biochem

Ligand: α-CGRP (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 8.2 pIC50
Reference (Journal): Three receptor-activity-modifying proteins define calcitonin gene-related peptide or adrenomedullin selectivity of the mouse calcitonin-like receptor in COS-7 cells.
Published in: Biochem Pharmacol

Ligand: α-CGRP-(8-37) (human) (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Receptor activity modifying proteins interaction with human and porcine calcitonin receptor-like receptor (CRLR) in HEK-293 cells.
Published in: Mol Cell Biochem

Ligand: α-CGRP-(8-37) (human) (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): RAMPs regulate the transport and ligand specificity of the calcitonin-receptor-like receptor.
Published in: Nature

Ligand: α-CGRP-(8-37) (rat) (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pIC50
Reference (Journal): Mammalian calcitonin receptor-like receptor/receptor activity modifying protein complexes define calcitonin gene-related peptide and adrenomedullin receptors in Drosophila Schneider 2 cells.
Published in: FEBS Lett

Ligand: α-CGRP-(8-37) (rat) (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pIC50
Reference (Journal): A receptor activity modifying protein (RAMP)2-dependent adrenomedullin receptor is a calcitonin gene-related peptide receptor when coexpressed with human RAMP1.
Published in: Endocrinology

Ligand: α-CGRP-(8-37) (rat) (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pIC50
Reference (Journal): Mouse receptor-activity-modifying proteins 1, -2 and -3: amino acid sequence, expression and function.
Published in: Mol Cell Endocrinol

Ligand: α-CGRP-(8-37) (rat) (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pIC50
Reference (Journal): Cloning, characterization and central nervous system distribution of receptor activity modifying proteins in the rat.
Published in: Eur J Neurosci

Ligand: atogepant (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (2021), EMA & UK (2023)
Primary target: no
Median affinity: 10.819999694824219 pKi
Reference (Patent): Piperidinone carboxamide azaindane CGRP receptor antagonists.

Ligand: β-CGRP (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Receptor activity modifying proteins interaction with human and porcine calcitonin receptor-like receptor (CRLR) in HEK-293 cells.
Published in: Mol Cell Biochem

Ligand: β-CGRP (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pIC50
Reference (Journal): Mouse receptor-activity-modifying proteins 1, -2 and -3: amino acid sequence, expression and function.
Published in: Mol Cell Endocrinol

Ligand: β-CGRP (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pIC50
Reference (Journal): Cloning, characterization and central nervous system distribution of receptor activity modifying proteins in the rat.
Published in: Eur J Neurosci

Ligand: β-CGRP (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pIC50
Reference (Journal): A receptor activity modifying protein (RAMP)2-dependent adrenomedullin receptor is a calcitonin gene-related peptide receptor when coexpressed with human RAMP1.
Published in: Endocrinology

Ligand: β-CGRP (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): RAMPs regulate the transport and ligand specificity of the calcitonin-receptor-like receptor.
Published in: Nature

Ligand: β-CGRP (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pIC50
Reference (Journal): Mammalian calcitonin receptor-like receptor/receptor activity modifying protein complexes define calcitonin gene-related peptide and adrenomedullin receptors in Drosophila Schneider 2 cells.
Published in: FEBS Lett

Ligand: compound 49 [PMID: 24405707] (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 10.520000457763672 pKi
Reference (Journal): Identification of potent CNS-penetrant thiazolidinones as novel CGRP receptor antagonists.
Published in: Bioorg Med Chem Lett

Ligand: compound 8 [Avgoustou et al., 2020] (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 9.069999694824219 pIC50
Reference (Journal): Discovery of a First-in-Class Potent Small Molecule Antagonist against the Adrenomedullin-2 Receptor
Published in: ACS Pharmacol Transl Sci

Ligand: [Cys(ACM)2,7]CGRP (Peptide)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Median affinity: 8 pKi
Reference (Journal): Receptor activity modifying proteins interaction with human and porcine calcitonin receptor-like receptor (CRLR) in HEK-293 cells.
Published in: Mol Cell Biochem

Ligand: [Cys(Et)2,7]α-CGRP (human) (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 10.5 pKi
Reference (Journal): Cys2,7EtalphaCGRP is a potent agonist for CGRP1 receptors in SK-N-MC cells.
Published in: Biochem Pharmacol

Ligand: erenumab (Antibody)
Interaction type: Antibody
Action: Antagonist
Ligand approved: yes
Approval source: FDA & EMA (2018)
Primary target: yes
Median affinity: 10.699999809265137 pKi
Reference (Journal): Pharmacologic Characterization of AMG 334, a Potent and Selective Human Monoclonal Antibody against the Calcitonin Gene-Related Peptide Receptor.
Published in: J Pharmacol Exp Ther

Ligand: HTL22562 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 10.5 pKi
Reference (Journal): Structure-Based Drug Discovery of <i>N</i>-((<i>R</i>)-3-(7-Methyl-1<i>H</i>-indazol-5-yl)-1-oxo-1-(((<i>S</i>)-1-oxo-3-(piperidin-4-yl)-1-(4-(pyridin-4-yl)piperazin-1-yl)propan-2-yl)amino)propan-2-yl)-2'-oxo-1',2'-dihydrospiro[piperidine-4,4'-pyrido[2,3-<i>d</i>][1,3]oxazine]-1-carboxamide (HTL22562): A Calcitonin Gene-Related Peptide Receptor Antagonist for Acute Treatment of Migraine.
Published in: J Med Chem

Ligand: olcegepant (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): CL/RAMP2 and CL/RAMP3 produce pharmacologically distinct adrenomedullin receptors: a comparison of effects of adrenomedullin22-52, CGRP8-37 and BIBN4096BS.
Published in: Br J Pharmacol

Ligand: olcegepant (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Identification of potent CNS-penetrant thiazolidinones as novel CGRP receptor antagonists.
Published in: Bioorg Med Chem Lett

Ligand: olcegepant (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Determinants of 1-piperidinecarboxamide, N-[2-[[5-amino-l-[[4-(4-pyridinyl)-l-piperazinyl]carbonyl]pentyl]amino]-1-[(3,5-dibromo-4-hydroxyphenyl)methyl]-2-oxoethyl]-4-(1,4-dihydro-2-oxo-3(2H)-quinazolinyl) (BIBN4096BS) affinity for calcitonin gene-related peptide and amylin receptors--the role of receptor activity modifying protein 1.
Published in: Mol Pharmacol

Ligand: olcegepant (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Receptor activity-modifying protein 1 determines the species selectivity of non-peptide CGRP receptor antagonists.
Published in: J Biol Chem

Ligand: olcegepant (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Pharmacological profile of BIBN4096BS, the first selective small molecule CGRP antagonist.
Published in: Br J Pharmacol

Ligand: rimegepant (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (2020), EMA (2022)
Primary target: yes
Median affinity: 9.600000381469727 pKB
Reference (Journal): Antagonism of CGRP Signaling by Rimegepant at Two Receptors.
Published in: Front Pharmacol

Ligand: [125I]αCGRP (mouse, rat) (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  -

Ligand: [125I]αCGRP (human) (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 10 pKd

Ligand: telcagepant (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 9.1 pKi
Reference (Journal): Pharmacological characterization of MK-0974 [N-[(3R,6S)-6-(2,3-difluorophenyl)-2-oxo-1-(2,2,2-trifluoroethyl)azepan-3-yl]-4-(2-oxo-2,3-dihydro-1H-imidazo[4,5-b]pyridin-1-yl)piperidine-1-carboxamide], a potent and orally active calcitonin gene-related peptide receptor antagonist for the treatment of migraine.
Published in: J Pharmacol Exp Ther

Ligand: ubrogepant (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (2019)
Primary target: no
Median affinity: 10.800000190734863 pKB
Reference (Journal): Characterization of Ubrogepant: A Potent and Selective Antagonist of the Human Calcitonin Gene&#x2012;Related Peptide Receptor.
Published in: J Pharmacol Exp Ther

Ligand: zavegepant (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (2023)
Primary target: no
Median affinity: 10.65999984741211 pKB
Reference (Journal): Discovery of (R)-N-(3-(7-methyl-1H-indazol-5-yl)-1-(4-(1-methylpiperidin-4-yl)-1-oxopropan-2-yl)-4-(2-oxo-1,2-dihydroquinolin-3-yl)piperidine-1-carboxamide (BMS-742413): a potent human CGRP antagonist with superior safety profile for the treatment of migraine through intranasal delivery.
Published in: Bioorg Med Chem Lett

Ligand: zavegepant (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (2023)
Primary target: no
Median affinity: 10.640000343322754 pKi
Reference (Journal): Azepino-indazoles as calcitonin gene-related peptide (CGRP) receptor antagonists.
Published in: Bioorg Med Chem Lett