ArticleACS medicinal chemistry letters2010
Discovery of MK-3207: A Highly Potent, Orally Bioavailable CGRP Receptor Antagonist.
Article in ACS medicinal chemistry letters, 2010. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 13 papers.
What it found
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
13 citing papers in PubMed, 63 citations in OpenAlex.
- Construction and validation of pharmacophore model of calcitonin gene-related peptide receptor antagonists using ligand- and structure-based approaches.Journal of molecular modeling · 2026Article
- Antimicrobial Neuropeptides and Their Receptors: Immunoregulator and Therapeutic Targets for Immune Disorders.Molecules (Basel, Switzerland) · 2025Review
- Synthetic Routes to 2-aryl-1Molecules (Basel, Switzerland) · 2024Article
- Elucidating the Interactome of G Protein-Coupled Receptors and Receptor Activity-Modifying Proteins.Pharmacological reviews · 2023Review
- Single-Dose Pharmacokinetics and Safety of Ubrogepant in Adults With Hepatic Impairment: Results From an Open-Label, Phase 1 Trial.Clinical pharmacology in drug development · 2022Article
- Discovery of a First-In-Class Small Molecule Antagonist against the Adrenomedullin-2 Receptor: Structure-Activity Relationships and Optimization.Journal of medicinal chemistry · 2021Article
- Discovery of a First-in-Class Potent Small Molecule Antagonist against the Adrenomedullin-2 Receptor.ACS pharmacology & translational science · 2020Article
- Potential Drugs Targeting Early Innate Immune Evasion of SARS-Coronavirus 2 via 2'-O-Methylation of Viral RNA.Viruses · 2020Article
- CGRP Is Critical for Hot Flushes in Ovariectomized Mice.Frontiers in pharmacology · 2018Article
- Study on the Alkylation Reactions of N(7)-Unsubstituted 1,3-Diazaoxindoles.Molecules (Basel, Switzerland) · 2017Article
- Mechanistic investigation of aziridine aldehyde-driven peptide macrocyclization: the imidoanhydride pathway.Chemical science · 2015Article
- [(11)C]MK-4232: The First Positron Emission Tomography Tracer for the Calcitonin Gene-Related Peptide Receptor.ACS medicinal chemistry letters · 2013Article
- Targeting a family B GPCR/RAMP receptor complex: CGRP receptor antagonists and migraine.British journal of pharmacology · 2012Review
Corrections and comments
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Authors and funding
18 authors at 5 institutions in 3 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Incorporation of polar functionality into a series of highly potent calcitonin gene-related peptide (CGRP) receptor antagonists was explored in an effort to improve pharmacokinetics. This strategy identified piperazinone analogues that possessed improved solubility at acidic pH and increased oral bioavailability in monkeys. Further optimization led to the discovery of the clinical candidate 2-[(8R)-8-(3,5-difluorophenyl)-10-oxo-6,9-diazaspiro[4.5]dec-9-yl]-N-[(2R)-2'-oxo-1,1',2',3-tetrahydrospiro[indene-2,3'-pyrrolo[2,3-b]pyridin]-5-yl]acetamide (MK-3207) (4), the most potent orally active CGRP receptor antagonist described to date.
Indexed as
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What OpenQuestion holds
Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.