Page last updated: 2024-11-13

mk 3207

Description Research Excerpts Clinical Trials Roles Classes Pathways Study Profile Bioassays Related Drugs Related Conditions Protein Interactions Research Growth Market Indicators

Cross-References

ID SourceID
PubMed CID25019940
CHEMBL ID1910936
SCHEMBL ID992191
MeSH IDM0545720

Synonyms (23)

Synonym
mk 3207
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
mk3207
unii-5c44m1qycc
6,9-diazaspiro(4.5)decane-9-acetamide, 8-(3,5-difluorophenyl)-10-oxo-n-((2r)-1,1',2',3-tetrahydro-2'-oxospiro(2h-indene-2,3'-(3h)pyrrolo(2,3-b)pyridin)-5-yl)-, (8r)-
5c44m1qycc ,
957118-49-9
BCP9000934
bdbm50356282
CHEMBL1910936 ,
NCGC00346546-01
HY-10301
CS-1449
SCHEMBL992191
2-((r)-8-(3,5-difluorophenyl)-10-oxo-6,9-diazaspiro[4.5]decan-9-yl)-n-((r)-2'-oxo-1,1',2',3-tetrahydrospiro[indene-2,3'-pyrrolo[2,3-b]pyridin]-5-yl)acetamide
DTXSID00241931
DB12424
957118-49-9 (free base)
2-[(8r)-8-(3,5-difluorophenyl)-10-oxo-6,9-diazaspiro[4.5]decan-9-yl]-n-[(2r)-2'-oxospiro[1,3-dihydroindene-2,3'-1h-pyrrolo[2,3-b]pyridine]-5-yl]acetamide
BCP02225
Q27261818
MS-30150

Research Excerpts

Bioavailability

ExcerptReferenceRelevance
" BMS-742413 has good intranasal bioavailability in the rabbit and shows a robust, dose-dependent inhibition of CGRP-induced increases in marmoset facial blood flow."( 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 migr
Cantor, GH; Chaturvedula, PV; Conway, CM; Davis, C; Denton, R; Dubowchik, GM; Keavy, D; Macci, R; Macor, JE; Mathias, N; Mercer, SE; Moench, P; Pin, SS; Schartman, R; Signor, L; Thalody, G; Whiterock, V; Xu, C, 2013
)
0.39
"The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs."( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019
)
0.51
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (5)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
EWS/FLI fusion proteinHomo sapiens (human)Potency0.02090.001310.157742.8575AID1259253
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Receptor activity-modifying protein 1Homo sapiens (human)Ki0.00000.00000.00030.0008AID665599
Calcitonin gene-related peptide 1Homo sapiens (human)IC50 (µMol)0.00010.00010.00120.0022AID625501
Calcitonin gene-related peptide 1Homo sapiens (human)Ki0.00000.00002.43367.3000AID625500
Calcitonin gene-related peptide type 1 receptorHomo sapiens (human)Ki0.00000.00000.02820.5900AID665599; AID754796; AID772350
Calcitonin gene-related peptide type 1 receptorRattus norvegicus (Norway rat)Ki0.01000.01000.01000.0100AID1180670
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (20)

Processvia Protein(s)Taxonomy
angiogenesisReceptor activity-modifying protein 1Homo sapiens (human)
calcium ion transportReceptor activity-modifying protein 1Homo sapiens (human)
intracellular protein transportReceptor activity-modifying protein 1Homo sapiens (human)
adenylate cyclase-activating G protein-coupled receptor signaling pathwayReceptor activity-modifying protein 1Homo sapiens (human)
regulation of G protein-coupled receptor signaling pathwayReceptor activity-modifying protein 1Homo sapiens (human)
protein transportReceptor activity-modifying protein 1Homo sapiens (human)
receptor internalizationReceptor activity-modifying protein 1Homo sapiens (human)
positive regulation of protein glycosylationReceptor activity-modifying protein 1Homo sapiens (human)
protein localization to plasma membraneReceptor activity-modifying protein 1Homo sapiens (human)
amylin receptor signaling pathwayReceptor activity-modifying protein 1Homo sapiens (human)
calcitonin gene-related peptide receptor signaling pathwayReceptor activity-modifying protein 1Homo sapiens (human)
G protein-coupled receptor signaling pathwayReceptor activity-modifying protein 1Homo sapiens (human)
cellular response to hormone stimulusReceptor activity-modifying protein 1Homo sapiens (human)
angiogenesisCalcitonin gene-related peptide type 1 receptorHomo sapiens (human)
calcium ion transportCalcitonin gene-related peptide type 1 receptorHomo sapiens (human)
cell surface receptor signaling pathwayCalcitonin gene-related peptide type 1 receptorHomo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messengerCalcitonin gene-related peptide type 1 receptorHomo sapiens (human)
adenylate cyclase-activating G protein-coupled receptor signaling pathwayCalcitonin gene-related peptide type 1 receptorHomo sapiens (human)
heart developmentCalcitonin gene-related peptide type 1 receptorHomo sapiens (human)
protein transportCalcitonin gene-related peptide type 1 receptorHomo sapiens (human)
receptor internalizationCalcitonin gene-related peptide type 1 receptorHomo sapiens (human)
cellular response to sucrose stimulusCalcitonin gene-related peptide type 1 receptorHomo sapiens (human)
positive regulation of vascular associated smooth muscle cell proliferationCalcitonin gene-related peptide type 1 receptorHomo sapiens (human)
calcitonin gene-related peptide receptor signaling pathwayCalcitonin gene-related peptide type 1 receptorHomo sapiens (human)
adrenomedullin receptor signaling pathwayCalcitonin gene-related peptide type 1 receptorHomo sapiens (human)
vascular associated smooth muscle cell proliferationCalcitonin gene-related peptide type 1 receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (9)

Processvia Protein(s)Taxonomy
calcitonin gene-related peptide receptor activityReceptor activity-modifying protein 1Homo sapiens (human)
protein bindingReceptor activity-modifying protein 1Homo sapiens (human)
amylin receptor activityReceptor activity-modifying protein 1Homo sapiens (human)
calcitonin gene-related peptide bindingReceptor activity-modifying protein 1Homo sapiens (human)
coreceptor activityReceptor activity-modifying protein 1Homo sapiens (human)
adrenomedullin receptor activityCalcitonin gene-related peptide type 1 receptorHomo sapiens (human)
calcitonin gene-related peptide receptor activityCalcitonin gene-related peptide type 1 receptorHomo sapiens (human)
G protein-coupled receptor activityCalcitonin gene-related peptide type 1 receptorHomo sapiens (human)
calcitonin receptor activityCalcitonin gene-related peptide type 1 receptorHomo sapiens (human)
protein bindingCalcitonin gene-related peptide type 1 receptorHomo sapiens (human)
adrenomedullin bindingCalcitonin gene-related peptide type 1 receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (10)

Processvia Protein(s)Taxonomy
plasma membraneReceptor activity-modifying protein 1Homo sapiens (human)
plasma membraneReceptor activity-modifying protein 1Homo sapiens (human)
cell surfaceReceptor activity-modifying protein 1Homo sapiens (human)
receptor complexReceptor activity-modifying protein 1Homo sapiens (human)
CGRP receptor complexReceptor activity-modifying protein 1Homo sapiens (human)
cell surfaceReceptor activity-modifying protein 1Homo sapiens (human)
extracellular regionCalcitonin gene-related peptide 1Homo sapiens (human)
plasma membraneCalcitonin gene-related peptide type 1 receptorHomo sapiens (human)
cytoplasmCalcitonin gene-related peptide type 1 receptorHomo sapiens (human)
lysosomeCalcitonin gene-related peptide type 1 receptorHomo sapiens (human)
endosomeCalcitonin gene-related peptide type 1 receptorHomo sapiens (human)
endoplasmic reticulumCalcitonin gene-related peptide type 1 receptorHomo sapiens (human)
plasma membraneCalcitonin gene-related peptide type 1 receptorHomo sapiens (human)
adrenomedullin receptor complexCalcitonin gene-related peptide type 1 receptorHomo sapiens (human)
CGRP receptor complexCalcitonin gene-related peptide type 1 receptorHomo sapiens (human)
plasma membraneCalcitonin gene-related peptide type 1 receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (67)

Assay IDTitleYearJournalArticle
AID1347095qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347101qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347103qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1346987P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1347093qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1296008Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening2020SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID1347154Primary screen GU AMC qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347096qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347086qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347106qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347102qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347107qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347094qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347092qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1346986P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1745845Primary qHTS for Inhibitors of ATXN expression
AID1347105qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347104qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347091qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347090qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347083qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347082qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347098qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347099qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347100qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347089qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347097qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1508630Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay2021Cell reports, 04-27, Volume: 35, Issue:4
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID1347108qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1180675Selectivity for human CGRP receptor over AM2 receptor (unknown origin)2014Journal of medicinal chemistry, Oct-09, Volume: 57, Issue:19
Calcitonin gene-related peptide receptor antagonists: new therapeutic agents for migraine.
AID1180703Inhibition of capsaicin-induced dermal vasodilation in human by laser Doppler imaging method2014Journal of medicinal chemistry, Oct-09, Volume: 57, Issue:19
Calcitonin gene-related peptide receptor antagonists: new therapeutic agents for migraine.
AID665602Displacement of [125I]CGRP from CGRP receptor in dog brain membrane after 3 hrs2012Bioorganic & medicinal chemistry letters, Jun-15, Volume: 22, Issue:12
MK-8825: a potent and selective CGRP receptor antagonist with good oral activity in rats.
AID772345Lipophilicity, log D of the compound at pH 7.0 by HPLC analysis2013ACS medicinal chemistry letters, Sep-12, Volume: 4, Issue:9
[(11)C]MK-4232: The First Positron Emission Tomography Tracer for the Calcitonin Gene-Related Peptide Receptor.
AID1180673Binding affinity to rhesus monkey CGRP receptor2014Journal of medicinal chemistry, Oct-09, Volume: 57, Issue:19
Calcitonin gene-related peptide receptor antagonists: new therapeutic agents for migraine.
AID772349Efflux ratio of human MDR1-mediated drug transport from basolateral to apical side over apical to basolateral side in pig LLC cells expressing human MDR1 at 5 uM2013ACS medicinal chemistry letters, Sep-12, Volume: 4, Issue:9
[(11)C]MK-4232: The First Positron Emission Tomography Tracer for the Calcitonin Gene-Related Peptide Receptor.
AID1180749Antimigraine activity in migraine patient assessed as pain relief incidence at 10 mg after 2 hrs (Rvb = 36.1%)2014Journal of medicinal chemistry, Oct-09, Volume: 57, Issue:19
Calcitonin gene-related peptide receptor antagonists: new therapeutic agents for migraine.
AID665603Antimigraine activity in iv dosed rat assessed as inhibition of capsaicin-induced dermal vasodilation administered 10 mins post capsaicin-challenge measured after 20 mins by laser doppler scanning2012Bioorganic & medicinal chemistry letters, Jun-15, Volume: 22, Issue:12
MK-8825: a potent and selective CGRP receptor antagonist with good oral activity in rats.
AID665606Fraction unbound in monkey plasma2012Bioorganic & medicinal chemistry letters, Jun-15, Volume: 22, Issue:12
MK-8825: a potent and selective CGRP receptor antagonist with good oral activity in rats.
AID772351Ratio of Bmax to Ki for human CGRP receptor expressed in HEK293 cells2013ACS medicinal chemistry letters, Sep-12, Volume: 4, Issue:9
[(11)C]MK-4232: The First Positron Emission Tomography Tracer for the Calcitonin Gene-Related Peptide Receptor.
AID665647Ratio of Ki for rat CGRP receptor to Ki for rhesus monkey CGRP receptor2012Bioorganic & medicinal chemistry letters, Jun-15, Volume: 22, Issue:12
MK-8825: a potent and selective CGRP receptor antagonist with good oral activity in rats.
AID665646Antimigraine activity in iv dosed rhesus monkey assessed as inhibition of capsaicin-induced dermal vasodilation administered 5 mins post capsaicin-challenge measured after 20 mins by laser doppler scanning2012Bioorganic & medicinal chemistry letters, Jun-15, Volume: 22, Issue:12
MK-8825: a potent and selective CGRP receptor antagonist with good oral activity in rats.
AID1180682Inhibition of capsaicin-induced dermal vasodilation in rhesus monkey model by laser Doppler imaging method2014Journal of medicinal chemistry, Oct-09, Volume: 57, Issue:19
Calcitonin gene-related peptide receptor antagonists: new therapeutic agents for migraine.
AID772347Apparent passive permeability across pig LLC-PK1 cells2013ACS medicinal chemistry letters, Sep-12, Volume: 4, Issue:9
[(11)C]MK-4232: The First Positron Emission Tomography Tracer for the Calcitonin Gene-Related Peptide Receptor.
AID1180747Antimigraine activity in migraine patient assessed as pain freedom incidence at 10 mg after 2 hrs (Rvb = 9.8%)2014Journal of medicinal chemistry, Oct-09, Volume: 57, Issue:19
Calcitonin gene-related peptide receptor antagonists: new therapeutic agents for migraine.
AID1180694Selectivity for human CGRP receptor over AMY1 receptor (unknown origin)2014Journal of medicinal chemistry, Oct-09, Volume: 57, Issue:19
Calcitonin gene-related peptide receptor antagonists: new therapeutic agents for migraine.
AID625500Displacement of [125I]adrenomedullin form CGRP receptor in human SK-N-MC cell membrane by competitive binding assay2011Bioorganic & medicinal chemistry letters, Nov-15, Volume: 21, Issue:22
Identification of a novel RAMP-independent CGRP receptor antagonist.
AID625501Inhibition of human CGRP receptor expressed in huamn HEK293 cells coexpressing CLR/RAMP1 assessed as inhibition of CGRP-stimulated cAMP production after 1 hr2011Bioorganic & medicinal chemistry letters, Nov-15, Volume: 21, Issue:22
Identification of a novel RAMP-independent CGRP receptor antagonist.
AID1180670Binding affinity to rat CGRP receptor2014Journal of medicinal chemistry, Oct-09, Volume: 57, Issue:19
Calcitonin gene-related peptide receptor antagonists: new therapeutic agents for migraine.
AID1180750Antimigraine activity in migraine patient assessed as pain relief incidence at 200 mg after 2 hrs (Rvb = 36.1%)2014Journal of medicinal chemistry, Oct-09, Volume: 57, Issue:19
Calcitonin gene-related peptide receptor antagonists: new therapeutic agents for migraine.
AID772350Displacement of [125I]-hCGRP from human CGRP receptor expressed in HEK293 cells2013ACS medicinal chemistry letters, Sep-12, Volume: 4, Issue:9
[(11)C]MK-4232: The First Positron Emission Tomography Tracer for the Calcitonin Gene-Related Peptide Receptor.
AID1180674Selectivity for human CGRP receptor over AM1 receptor (unknown origin)2014Journal of medicinal chemistry, Oct-09, Volume: 57, Issue:19
Calcitonin gene-related peptide receptor antagonists: new therapeutic agents for migraine.
AID754796Antagonist activity at human CGRP receptor2013Bioorganic & medicinal chemistry letters, Jun-01, Volume: 23, Issue:11
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 migr
AID665605Fraction unbound in dog plasma2012Bioorganic & medicinal chemistry letters, Jun-15, Volume: 22, Issue:12
MK-8825: a potent and selective CGRP receptor antagonist with good oral activity in rats.
AID665600Displacement of [125I]CGRP from CGRP receptor in rat brain membrane after 3 hrs2012Bioorganic & medicinal chemistry letters, Jun-15, Volume: 22, Issue:12
MK-8825: a potent and selective CGRP receptor antagonist with good oral activity in rats.
AID665608Aqueous solubility of the compound in phosphate buffer at pH 72012Bioorganic & medicinal chemistry letters, Jun-15, Volume: 22, Issue:12
MK-8825: a potent and selective CGRP receptor antagonist with good oral activity in rats.
AID772337Binding affinity to rhesus monkey cerebellum CGRP receptor2013ACS medicinal chemistry letters, Sep-12, Volume: 4, Issue:9
[(11)C]MK-4232: The First Positron Emission Tomography Tracer for the Calcitonin Gene-Related Peptide Receptor.
AID665604Fraction unbound in human plasma2012Bioorganic & medicinal chemistry letters, Jun-15, Volume: 22, Issue:12
MK-8825: a potent and selective CGRP receptor antagonist with good oral activity in rats.
AID1180693Selectivity for human CGRP receptor over AM3 receptor (unknown origin)2014Journal of medicinal chemistry, Oct-09, Volume: 57, Issue:19
Calcitonin gene-related peptide receptor antagonists: new therapeutic agents for migraine.
AID665612Displacement of [125I]CGRP from CGRP receptor in rhesus monkey cerebellum after 3 hrs2012Bioorganic & medicinal chemistry letters, Jun-15, Volume: 22, Issue:12
MK-8825: a potent and selective CGRP receptor antagonist with good oral activity in rats.
AID665599Displacement of [125I]CGRP from human recombinant CALCRL/RAMP1 receptor expressed in HEK293 cells after 3 hrs2012Bioorganic & medicinal chemistry letters, Jun-15, Volume: 22, Issue:12
MK-8825: a potent and selective CGRP receptor antagonist with good oral activity in rats.
AID772348Fraction unbound in monkey plasma by equillibrium dialysis method2013ACS medicinal chemistry letters, Sep-12, Volume: 4, Issue:9
[(11)C]MK-4232: The First Positron Emission Tomography Tracer for the Calcitonin Gene-Related Peptide Receptor.
AID1180681Binding affinity to human CGRP receptor using [3H]-labeled compound assessed as receptor binding half life2014Journal of medicinal chemistry, Oct-09, Volume: 57, Issue:19
Calcitonin gene-related peptide receptor antagonists: new therapeutic agents for migraine.
AID1180748Antimigraine activity in migraine patient assessed as pain freedom incidence at 200 mg after 2 hrs (Rvb = 9.8%)2014Journal of medicinal chemistry, Oct-09, Volume: 57, Issue:19
Calcitonin gene-related peptide receptor antagonists: new therapeutic agents for migraine.
AID665601Fraction unbound in rat plasma2012Bioorganic & medicinal chemistry letters, Jun-15, Volume: 22, Issue:12
MK-8825: a potent and selective CGRP receptor antagonist with good oral activity in rats.
AID772346Ratio of AUC in rhesus monkey CSF to AUC in rhesus monkey plasma2013ACS medicinal chemistry letters, Sep-12, Volume: 4, Issue:9
[(11)C]MK-4232: The First Positron Emission Tomography Tracer for the Calcitonin Gene-Related Peptide Receptor.
AID665650Selectivity ratio of Ki for rat CGRP receptor to Ki for human CGRP receptor2012Bioorganic & medicinal chemistry letters, Jun-15, Volume: 22, Issue:12
MK-8825: a potent and selective CGRP receptor antagonist with good oral activity in rats.
AID1347411qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Mechanism Interrogation Plate v5.0 (MIPE) Libary2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (13)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's0 (0.00)29.6817
2010's7 (53.85)24.3611
2020's6 (46.15)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 27.51

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be moderate demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index27.51 (24.57)
Research Supply Index2.64 (2.92)
Research Growth Index4.54 (4.65)
Search Engine Demand Index24.28 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (27.51)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews1 (7.69%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other12 (92.31%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]