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 Source	ID
PubMed CID	25019940
CHEMBL ID	1910936
SCHEMBL ID	992191
MeSH ID	M0545720

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

Excerpt	Reference	Relevance
" 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

Protein	Taxonomy	Measurement	Average (µ)	Min (ref.)	Avg (ref.)	Max (ref.)	Bioassay(s)
EWS/FLI fusion protein	Homo sapiens (human)	Potency	0.0209	0.0013	10.1577	42.8575	AID1259253
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Inhibition Measurements

Protein	Taxonomy	Measurement	Average	Min (ref.)	Avg (ref.)	Max (ref.)	Bioassay(s)
Receptor activity-modifying protein 1	Homo sapiens (human)	Ki	0.0000	0.0000	0.0003	0.0008	AID665599
Calcitonin gene-related peptide 1	Homo sapiens (human)	IC50 (µMol)	0.0001	0.0001	0.0012	0.0022	AID625501
Calcitonin gene-related peptide 1	Homo sapiens (human)	Ki	0.0000	0.0000	2.4336	7.3000	AID625500
Calcitonin gene-related peptide type 1 receptor	Homo sapiens (human)	Ki	0.0000	0.0000	0.0282	0.5900	AID665599; AID754796; AID772350
Calcitonin gene-related peptide type 1 receptor	Rattus norvegicus (Norway rat)	Ki	0.0100	0.0100	0.0100	0.0100	AID1180670
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (20)

Process	via Protein(s)	Taxonomy
angiogenesis	Receptor activity-modifying protein 1	Homo sapiens (human)
calcium ion transport	Receptor activity-modifying protein 1	Homo sapiens (human)
intracellular protein transport	Receptor activity-modifying protein 1	Homo sapiens (human)
adenylate cyclase-activating G protein-coupled receptor signaling pathway	Receptor activity-modifying protein 1	Homo sapiens (human)
regulation of G protein-coupled receptor signaling pathway	Receptor activity-modifying protein 1	Homo sapiens (human)
protein transport	Receptor activity-modifying protein 1	Homo sapiens (human)
receptor internalization	Receptor activity-modifying protein 1	Homo sapiens (human)
positive regulation of protein glycosylation	Receptor activity-modifying protein 1	Homo sapiens (human)
protein localization to plasma membrane	Receptor activity-modifying protein 1	Homo sapiens (human)
amylin receptor signaling pathway	Receptor activity-modifying protein 1	Homo sapiens (human)
calcitonin gene-related peptide receptor signaling pathway	Receptor activity-modifying protein 1	Homo sapiens (human)
G protein-coupled receptor signaling pathway	Receptor activity-modifying protein 1	Homo sapiens (human)
cellular response to hormone stimulus	Receptor activity-modifying protein 1	Homo sapiens (human)
angiogenesis	Calcitonin gene-related peptide type 1 receptor	Homo sapiens (human)
calcium ion transport	Calcitonin gene-related peptide type 1 receptor	Homo sapiens (human)
cell surface receptor signaling pathway	Calcitonin gene-related peptide type 1 receptor	Homo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger	Calcitonin gene-related peptide type 1 receptor	Homo sapiens (human)
adenylate cyclase-activating G protein-coupled receptor signaling pathway	Calcitonin gene-related peptide type 1 receptor	Homo sapiens (human)
heart development	Calcitonin gene-related peptide type 1 receptor	Homo sapiens (human)
protein transport	Calcitonin gene-related peptide type 1 receptor	Homo sapiens (human)
receptor internalization	Calcitonin gene-related peptide type 1 receptor	Homo sapiens (human)
cellular response to sucrose stimulus	Calcitonin gene-related peptide type 1 receptor	Homo sapiens (human)
positive regulation of vascular associated smooth muscle cell proliferation	Calcitonin gene-related peptide type 1 receptor	Homo sapiens (human)
calcitonin gene-related peptide receptor signaling pathway	Calcitonin gene-related peptide type 1 receptor	Homo sapiens (human)
adrenomedullin receptor signaling pathway	Calcitonin gene-related peptide type 1 receptor	Homo sapiens (human)
vascular associated smooth muscle cell proliferation	Calcitonin gene-related peptide type 1 receptor	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (9)

Process	via Protein(s)	Taxonomy
calcitonin gene-related peptide receptor activity	Receptor activity-modifying protein 1	Homo sapiens (human)
protein binding	Receptor activity-modifying protein 1	Homo sapiens (human)
amylin receptor activity	Receptor activity-modifying protein 1	Homo sapiens (human)
calcitonin gene-related peptide binding	Receptor activity-modifying protein 1	Homo sapiens (human)
coreceptor activity	Receptor activity-modifying protein 1	Homo sapiens (human)
adrenomedullin receptor activity	Calcitonin gene-related peptide type 1 receptor	Homo sapiens (human)
calcitonin gene-related peptide receptor activity	Calcitonin gene-related peptide type 1 receptor	Homo sapiens (human)
G protein-coupled receptor activity	Calcitonin gene-related peptide type 1 receptor	Homo sapiens (human)
calcitonin receptor activity	Calcitonin gene-related peptide type 1 receptor	Homo sapiens (human)
protein binding	Calcitonin gene-related peptide type 1 receptor	Homo sapiens (human)
adrenomedullin binding	Calcitonin gene-related peptide type 1 receptor	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (10)

Process	via Protein(s)	Taxonomy
plasma membrane	Receptor activity-modifying protein 1	Homo sapiens (human)
plasma membrane	Receptor activity-modifying protein 1	Homo sapiens (human)
cell surface	Receptor activity-modifying protein 1	Homo sapiens (human)
receptor complex	Receptor activity-modifying protein 1	Homo sapiens (human)
CGRP receptor complex	Receptor activity-modifying protein 1	Homo sapiens (human)
cell surface	Receptor activity-modifying protein 1	Homo sapiens (human)
extracellular region	Calcitonin gene-related peptide 1	Homo sapiens (human)
plasma membrane	Calcitonin gene-related peptide type 1 receptor	Homo sapiens (human)
cytoplasm	Calcitonin gene-related peptide type 1 receptor	Homo sapiens (human)
lysosome	Calcitonin gene-related peptide type 1 receptor	Homo sapiens (human)
endosome	Calcitonin gene-related peptide type 1 receptor	Homo sapiens (human)
endoplasmic reticulum	Calcitonin gene-related peptide type 1 receptor	Homo sapiens (human)
plasma membrane	Calcitonin gene-related peptide type 1 receptor	Homo sapiens (human)
adrenomedullin receptor complex	Calcitonin gene-related peptide type 1 receptor	Homo sapiens (human)
CGRP receptor complex	Calcitonin gene-related peptide type 1 receptor	Homo sapiens (human)
plasma membrane	Calcitonin gene-related peptide type 1 receptor	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (67)

Assay ID	Title	Year	Journal	Article
AID1347095	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347101	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347103	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1346987	P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen	2019	Molecular pharmacology, 11, Volume: 96, Issue:5	A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1347093	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1296008	Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening	2020	SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1	Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID1347154	Primary screen GU AMC qHTS for Zika virus inhibitors	2020	Proceedings 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.
AID1347096	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347086	qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal	2020	Antiviral research, 01, Volume: 173	A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347106	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347102	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347107	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347094	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347092	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1346986	P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen	2019	Molecular pharmacology, 11, Volume: 96, Issue:5	A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1745845	Primary qHTS for Inhibitors of ATXN expression
AID1347105	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347104	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347091	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347090	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347083	qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen	2020	Antiviral research, 01, Volume: 173	A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347082	qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal	2020	Antiviral research, 01, Volume: 173	A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347098	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347099	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347100	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347089	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347097	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1508630	Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay	2021	Cell reports, 04-27, Volume: 35, Issue:4	A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID1347108	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1180675	Selectivity for human CGRP receptor over AM2 receptor (unknown origin)	2014	Journal of medicinal chemistry, Oct-09, Volume: 57, Issue:19	Calcitonin gene-related peptide receptor antagonists: new therapeutic agents for migraine.
AID1180703	Inhibition of capsaicin-induced dermal vasodilation in human by laser Doppler imaging method	2014	Journal of medicinal chemistry, Oct-09, Volume: 57, Issue:19	Calcitonin gene-related peptide receptor antagonists: new therapeutic agents for migraine.
AID665602	Displacement of [125I]CGRP from CGRP receptor in dog brain membrane after 3 hrs	2012	Bioorganic & medicinal chemistry letters, Jun-15, Volume: 22, Issue:12	MK-8825: a potent and selective CGRP receptor antagonist with good oral activity in rats.
AID772345	Lipophilicity, log D of the compound at pH 7.0 by HPLC analysis	2013	ACS 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.
AID1180673	Binding affinity to rhesus monkey CGRP receptor	2014	Journal of medicinal chemistry, Oct-09, Volume: 57, Issue:19	Calcitonin gene-related peptide receptor antagonists: new therapeutic agents for migraine.
AID772349	Efflux 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 uM	2013	ACS 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.
AID1180749	Antimigraine activity in migraine patient assessed as pain relief incidence at 10 mg after 2 hrs (Rvb = 36.1%)	2014	Journal of medicinal chemistry, Oct-09, Volume: 57, Issue:19	Calcitonin gene-related peptide receptor antagonists: new therapeutic agents for migraine.
AID665603	Antimigraine 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 scanning	2012	Bioorganic & medicinal chemistry letters, Jun-15, Volume: 22, Issue:12	MK-8825: a potent and selective CGRP receptor antagonist with good oral activity in rats.
AID665606	Fraction unbound in monkey plasma	2012	Bioorganic & medicinal chemistry letters, Jun-15, Volume: 22, Issue:12	MK-8825: a potent and selective CGRP receptor antagonist with good oral activity in rats.
AID772351	Ratio of Bmax to Ki for human CGRP receptor expressed in HEK293 cells	2013	ACS 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.
AID665647	Ratio of Ki for rat CGRP receptor to Ki for rhesus monkey CGRP receptor	2012	Bioorganic & medicinal chemistry letters, Jun-15, Volume: 22, Issue:12	MK-8825: a potent and selective CGRP receptor antagonist with good oral activity in rats.
AID665646	Antimigraine 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 scanning	2012	Bioorganic & medicinal chemistry letters, Jun-15, Volume: 22, Issue:12	MK-8825: a potent and selective CGRP receptor antagonist with good oral activity in rats.
AID1180682	Inhibition of capsaicin-induced dermal vasodilation in rhesus monkey model by laser Doppler imaging method	2014	Journal of medicinal chemistry, Oct-09, Volume: 57, Issue:19	Calcitonin gene-related peptide receptor antagonists: new therapeutic agents for migraine.
AID772347	Apparent passive permeability across pig LLC-PK1 cells	2013	ACS 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.
AID1180747	Antimigraine activity in migraine patient assessed as pain freedom incidence at 10 mg after 2 hrs (Rvb = 9.8%)	2014	Journal of medicinal chemistry, Oct-09, Volume: 57, Issue:19	Calcitonin gene-related peptide receptor antagonists: new therapeutic agents for migraine.
AID1180694	Selectivity for human CGRP receptor over AMY1 receptor (unknown origin)	2014	Journal of medicinal chemistry, Oct-09, Volume: 57, Issue:19	Calcitonin gene-related peptide receptor antagonists: new therapeutic agents for migraine.
AID625500	Displacement of [125I]adrenomedullin form CGRP receptor in human SK-N-MC cell membrane by competitive binding assay	2011	Bioorganic & medicinal chemistry letters, Nov-15, Volume: 21, Issue:22	Identification of a novel RAMP-independent CGRP receptor antagonist.
AID625501	Inhibition of human CGRP receptor expressed in huamn HEK293 cells coexpressing CLR/RAMP1 assessed as inhibition of CGRP-stimulated cAMP production after 1 hr	2011	Bioorganic & medicinal chemistry letters, Nov-15, Volume: 21, Issue:22	Identification of a novel RAMP-independent CGRP receptor antagonist.
AID1180670	Binding affinity to rat CGRP receptor	2014	Journal of medicinal chemistry, Oct-09, Volume: 57, Issue:19	Calcitonin gene-related peptide receptor antagonists: new therapeutic agents for migraine.
AID1180750	Antimigraine activity in migraine patient assessed as pain relief incidence at 200 mg after 2 hrs (Rvb = 36.1%)	2014	Journal of medicinal chemistry, Oct-09, Volume: 57, Issue:19	Calcitonin gene-related peptide receptor antagonists: new therapeutic agents for migraine.
AID772350	Displacement of [125I]-hCGRP from human CGRP receptor expressed in HEK293 cells	2013	ACS 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.
AID1180674	Selectivity for human CGRP receptor over AM1 receptor (unknown origin)	2014	Journal of medicinal chemistry, Oct-09, Volume: 57, Issue:19	Calcitonin gene-related peptide receptor antagonists: new therapeutic agents for migraine.
AID754796	Antagonist activity at human CGRP receptor	2013	Bioorganic & 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
AID665605	Fraction unbound in dog plasma	2012	Bioorganic & medicinal chemistry letters, Jun-15, Volume: 22, Issue:12	MK-8825: a potent and selective CGRP receptor antagonist with good oral activity in rats.
AID665600	Displacement of [125I]CGRP from CGRP receptor in rat brain membrane after 3 hrs	2012	Bioorganic & medicinal chemistry letters, Jun-15, Volume: 22, Issue:12	MK-8825: a potent and selective CGRP receptor antagonist with good oral activity in rats.
AID665608	Aqueous solubility of the compound in phosphate buffer at pH 7	2012	Bioorganic & medicinal chemistry letters, Jun-15, Volume: 22, Issue:12	MK-8825: a potent and selective CGRP receptor antagonist with good oral activity in rats.
AID772337	Binding affinity to rhesus monkey cerebellum CGRP receptor	2013	ACS 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.
AID665604	Fraction unbound in human plasma	2012	Bioorganic & medicinal chemistry letters, Jun-15, Volume: 22, Issue:12	MK-8825: a potent and selective CGRP receptor antagonist with good oral activity in rats.
AID1180693	Selectivity for human CGRP receptor over AM3 receptor (unknown origin)	2014	Journal of medicinal chemistry, Oct-09, Volume: 57, Issue:19	Calcitonin gene-related peptide receptor antagonists: new therapeutic agents for migraine.
AID665612	Displacement of [125I]CGRP from CGRP receptor in rhesus monkey cerebellum after 3 hrs	2012	Bioorganic & medicinal chemistry letters, Jun-15, Volume: 22, Issue:12	MK-8825: a potent and selective CGRP receptor antagonist with good oral activity in rats.
AID665599	Displacement of [125I]CGRP from human recombinant CALCRL/RAMP1 receptor expressed in HEK293 cells after 3 hrs	2012	Bioorganic & medicinal chemistry letters, Jun-15, Volume: 22, Issue:12	MK-8825: a potent and selective CGRP receptor antagonist with good oral activity in rats.
AID772348	Fraction unbound in monkey plasma by equillibrium dialysis method	2013	ACS 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.
AID1180681	Binding affinity to human CGRP receptor using [3H]-labeled compound assessed as receptor binding half life	2014	Journal of medicinal chemistry, Oct-09, Volume: 57, Issue:19	Calcitonin gene-related peptide receptor antagonists: new therapeutic agents for migraine.
AID1180748	Antimigraine activity in migraine patient assessed as pain freedom incidence at 200 mg after 2 hrs (Rvb = 9.8%)	2014	Journal of medicinal chemistry, Oct-09, Volume: 57, Issue:19	Calcitonin gene-related peptide receptor antagonists: new therapeutic agents for migraine.
AID665601	Fraction unbound in rat plasma	2012	Bioorganic & medicinal chemistry letters, Jun-15, Volume: 22, Issue:12	MK-8825: a potent and selective CGRP receptor antagonist with good oral activity in rats.
AID772346	Ratio of AUC in rhesus monkey CSF to AUC in rhesus monkey plasma	2013	ACS 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.
AID665650	Selectivity ratio of Ki for rat CGRP receptor to Ki for human CGRP receptor	2012	Bioorganic & medicinal chemistry letters, Jun-15, Volume: 22, Issue:12	MK-8825: a potent and selective CGRP receptor antagonist with good oral activity in rats.
AID1347411	qHTS 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) Libary	2020	ACS 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)

Timeframe	Studies, This Drug (%)	All Drugs %
pre-1990	0 (0.00)	18.7374
1990's	0 (0.00)	18.2507
2000's	0 (0.00)	29.6817
2010's	7 (53.85)	24.3611
2020's	6 (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.

Metric	This Compound (vs All)
Research Demand Index	27.51 (24.57)
Research Supply Index	2.64 (2.92)
Research Growth Index	4.54 (4.65)
Search Engine Demand Index	24.28 (26.88)
Search Engine Supply Index	2.00 (0.95)

This Compound (27.51)

All Compounds (24.57)

Study Types

Publication Type	This drug (%)	All Drugs (%)
Trials	0 (0.00%)	5.53%
Reviews	1 (7.69%)	6.00%
Case Studies	0 (0.00%)	4.05%
Observational	0 (0.00%)	0.25%
Other	12 (92.31%)	84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Substance	Relationship Strength	Studies	Classes	Roles
rizatriptan rizatriptan: structure given in first source; RN given refers to benzoate	3.19	1	tryptamines	anti-inflammatory drug; serotonergic agonist; vasoconstrictor agent
sumatriptan Sumatriptan: A serotonin agonist that acts selectively at 5HT1 receptors. It is used in the treatment of MIGRAINE DISORDERS.. sumatriptan : A sulfonamide that consists of N,N-dimethyltryptamine bearing an additional (N-methylsulfamoyl)methyl substituent at position 5. Selective agonist for a vascular 5-HT1 receptor subtype (probably a member of the 5-HT1D family). Used (in the form of its succinate salt) for the acute treatment of migraine with or without aura in adults.	3.59	2	sulfonamide; tryptamines	serotonergic agonist; vasoconstrictor agent
zolmitriptan zolmitriptan: an antimigraine compound; a serotonin (5HT)-1D receptor agonist. zolmitriptan : A member of the class of tryptamines that is N,N-dimethyltryptamine in which the hydrogen at position 5 of the indole ring has been replaced by a [(4S)-2-oxo-1,3-oxazolidin-4-yl]methyl group. A serotonin 5-HT1 B and D receptor agonist, it is used for the treatment of migraine.	3.19	1	oxazolidinone; tryptamines	anti-inflammatory drug; serotonergic agonist; vasoconstrictor agent
eletriptan eletriptan: 5-HT(1B/1D) receptor agonist; structure in first source. eletriptan : An N-alkylpyrrolidine, that is N-methylpyrrolidine in which the pro-R hydrogen at position 2 is replaced by a {5-[2-(phenylsulfonyl)ethyl]-1H-indol-3-yl}methyl group.	3.19	1	indoles; N-alkylpyrrolidine; sulfone	non-steroidal anti-inflammatory drug; serotonergic agonist; vasoconstrictor agent
5-(1,1-dioxido-1,2-thiazinan-2-yl)-n-(4-fluorobenzyl)-8-hydroxy-1,6-naphthyridine-7-carboxamide 5-(1,1-dioxido-1,2-thiazinan-2-yl)-N-(4-fluorobenzyl)-8-hydroxy-1,6-naphthyridine-7-carboxamide: structure in first source	2.06	1
telcagepant telcagepant: structure in first source	4.28	5
bms 694153 [no description available]	2.08	1
(5s,6s,9r)-5-amino-6-(2,3-difluorophenyl)-6,7,8,9-tetrahydro-5h-cyclohepta(b)pyridin-9-yl 4-(2-oxo-2,3-dihydro-1h-imidazo(4,5-b)pyridin-1-yl)piperidine-1-carboxylate [no description available]	3.19	1
mk-8825 [no description available]	2.07	1

Condition	Indicated	Relationship Strength	Studies
HIV Human immunodeficiency virus. A non-taxonomic and historical term referring to any of two species, specifically HIV-1 and/or HIV-2. Prior to 1986, this was called human T-lymphotropic virus type III/lymphadenopathy-associated virus (HTLV-III/LAV). From 1986-1990, it was an official species called HIV. Since 1991, HIV was no longer considered an official species name; the two species were designated HIV-1 and HIV-2.	0	2.06	1
Disease Models, Animal Naturally-occurring or experimentally-induced animal diseases with pathological processes analogous to human diseases.	0	2.53	2
Abdominal Migraine [description not available]	0	3.69	3
Migraine Disorders A class of disabling primary headache disorders, characterized by recurrent unilateral pulsatile headaches. The two major subtypes are common migraine (without aura) and classic migraine (with aura or neurological symptoms). (International Classification of Headache Disorders, 2nd ed. Cephalalgia 2004: suppl 1)	1	5.69	3
Congenital Zika Syndrome [description not available]	0	2.25	1
Zika Virus Infection A viral disease transmitted by the bite of AEDES mosquitoes infected with ZIKA VIRUS. Its mild DENGUE-like symptoms include fever, rash, headaches and ARTHRALGIA. The viral infection during pregnancy, in rare cases, is associated with congenital brain and ocular abnormalities, called Congenital Zika Syndrome, including MICROCEPHALY and may also lead to GUILLAIN-BARRE SYNDROME.	0	2.25	1

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