Compounds > 5-((1-(2,6-dichlorobenzyl)piperidin-4-yl)methoxy)quinazoline-2,4-diamine
Page last updated: 2024-11-13

5-((1-(2,6-dichlorobenzyl)piperidin-4-yl)methoxy)quinazoline-2,4-diamine

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

Description

5-((1-(2,6-dichlorobenzyl)piperidin-4-yl)methoxy)quinazoline-2,4-diamine: inhibits DcpS protein [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID53258905
CHEMBL ID4072132
SCHEMBL ID2166498
MeSH IDM0593651

Synonyms (38)

Synonym
S0063
d-157495
d 157495
d157495
ksv93l7urw ,
2,4-quinazolinediamine, 5-((1-((2,6-dichlorophenyl)methyl)-4-piperidinyl)methoxy)-
1005504-62-0
unii-ksv93l7urw
5-(1-(2,6-dichlorobenzyl)-piperidin-4-yl)methoxyquinazoline-2,4-diamine
pf-06687859
rg-3039 free base
SCHEMBL2166498
AC-35200
DTXSID00143380
AKOS025396466
rg3039(pf-06687859)
rg3039
5-({1-[(2,6-dichlorophenyl)methyl]piperidin-4-yl}methoxy)quinazoline-2,4-diamine
rg-3039
pf-0668759
pf-6687859 free
1466525-84-7
5-[[1-[(2,6-dichlorophenyl)methyl]piperidin-4-yl]methoxy]quinazoline-2,4-diamine;5-[[1-[(2,6-dichlorophenyl)methyl]piperidin-4-yl]methoxy]quinazoline-2,4-diamine
pf-6687859
5-((1-(2,6-dichlorobenzyl)piperidin-4-yl)methoxy)quinazoline-2,4-diaminedihydrochloride;5-((1-(2,6-dichlorobenzyl)piperidin-4-yl)methoxy)quinazoline-2,4-diaminedihydrochloride
HY-102020
pf-06687859/rg-3039
CS-6976
5-[[1-[(2,6-dichlorophenyl)methyl]piperidin-4-yl]methoxy]quinazoline-2,4-diamine
5-((1-(2,6-dichlorobenzyl)piperidin-4-yl)methoxy)quinazoline-2,4-diamine
BCP08729
EX-A2971
BS-14159
2,4-quinazolinediamine, 5-[[1-[(2,6-dichlorophenyl)methyl]-4-piperidinyl]methoxy]-
CHEMBL4072132 ,
bdbm50237200
Q27282418
F81693

Research Excerpts

Dosage Studied

ExcerptRelevanceReference
" In 2B/- SMA mice, RG3039 provided a >600% survival benefit (median 18 days to >112 days) when dosing began at P4, highlighting the importance of early intervention."( The DcpS inhibitor RG3039 improves survival, function and motor unit pathologies in two SMA mouse models.
Bail, S; Barlow, C; Cardona, H; DiDonato, CJ; Durens, M; Emery, C; Gogliotti, RG; Heier, CR; Jacques, V; Jarecki, J; Jorgensen, M; Kiledjian, M; Kuntz, N; Plasterer, HL; Rusche, J; Singh, J; Xia, B, 2013)		0.39
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (1)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
m7GpppX diphosphataseHomo sapiens (human)IC50 (µMol)0.00010.00010.07130.1426AID1442738
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (4)

Processvia Protein(s)Taxonomy
nuclear-transcribed mRNA catabolic process, deadenylation-dependent decaym7GpppX diphosphataseHomo sapiens (human)
mRNA cis splicing, via spliceosomem7GpppX diphosphataseHomo sapiens (human)
mRNA methylguanosine-cap decappingm7GpppX diphosphataseHomo sapiens (human)
deadenylation-dependent decapping of nuclear-transcribed mRNAm7GpppX diphosphataseHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (5)

Processvia Protein(s)Taxonomy
RNA 7-methylguanosine cap bindingm7GpppX diphosphataseHomo sapiens (human)
RNA exonuclease activitym7GpppX diphosphataseHomo sapiens (human)
protein bindingm7GpppX diphosphataseHomo sapiens (human)
identical protein bindingm7GpppX diphosphataseHomo sapiens (human)
5'-(N(7)-methyl 5'-triphosphoguanosine)-[mRNA] diphosphatase activitym7GpppX diphosphataseHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (6)

Processvia Protein(s)Taxonomy
nucleusm7GpppX diphosphataseHomo sapiens (human)
nucleoplasmm7GpppX diphosphataseHomo sapiens (human)
cytoplasmm7GpppX diphosphataseHomo sapiens (human)
mitochondrionm7GpppX diphosphataseHomo sapiens (human)
cytosolm7GpppX diphosphataseHomo sapiens (human)
nucleusm7GpppX diphosphataseHomo sapiens (human)
P-bodym7GpppX diphosphataseHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (11)

Assay IDTitleYearJournalArticle
AID1442743Kinetic solubility of the compound at pH 6.52017Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7
Design of Potent mRNA Decapping Scavenger Enzyme (DcpS) Inhibitors with Improved Physicochemical Properties To Investigate the Mechanism of Therapeutic Benefit in Spinal Muscular Atrophy (SMA).
AID1442742Efflux ratio of permeability from basolateral to apical over apical to basolateral side of MDCK cells expressing MDR12017Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7
Design of Potent mRNA Decapping Scavenger Enzyme (DcpS) Inhibitors with Improved Physicochemical Properties To Investigate the Mechanism of Therapeutic Benefit in Spinal Muscular Atrophy (SMA).
AID1442733Drug uptake in HEK293 cells at 10 nM in presence of vacuolar type ATPase inhibitor concanamycin A measured after 2.5 hrs2017Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7
Design of Potent mRNA Decapping Scavenger Enzyme (DcpS) Inhibitors with Improved Physicochemical Properties To Investigate the Mechanism of Therapeutic Benefit in Spinal Muscular Atrophy (SMA).
AID1442749Stability in human liver microsomes at 1 uM2017Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7
Design of Potent mRNA Decapping Scavenger Enzyme (DcpS) Inhibitors with Improved Physicochemical Properties To Investigate the Mechanism of Therapeutic Benefit in Spinal Muscular Atrophy (SMA).
AID1442732Drug uptake in HEK293 cells at 10 nM in presence of vacuolar type ATPase inhibitor bafilomycin measured after 2.5 hrs2017Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7
Design of Potent mRNA Decapping Scavenger Enzyme (DcpS) Inhibitors with Improved Physicochemical Properties To Investigate the Mechanism of Therapeutic Benefit in Spinal Muscular Atrophy (SMA).
AID1442740Apparent intrinsic clearance in human liver microsomes at 1 uM2017Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7
Design of Potent mRNA Decapping Scavenger Enzyme (DcpS) Inhibitors with Improved Physicochemical Properties To Investigate the Mechanism of Therapeutic Benefit in Spinal Muscular Atrophy (SMA).
AID1442741Apparent passive permeability across apical to basolateral side in RRCK2 cells at 2 uM2017Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7
Design of Potent mRNA Decapping Scavenger Enzyme (DcpS) Inhibitors with Improved Physicochemical Properties To Investigate the Mechanism of Therapeutic Benefit in Spinal Muscular Atrophy (SMA).
AID1442736Drug uptake in lymphoblasts (unknown origin) at 10 nM in presence of vacuolar type ATPase inhibitor concanamycin A measured after 2.5 hrs2017Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7
Design of Potent mRNA Decapping Scavenger Enzyme (DcpS) Inhibitors with Improved Physicochemical Properties To Investigate the Mechanism of Therapeutic Benefit in Spinal Muscular Atrophy (SMA).
AID1442744Lipophilicity, log D of the compound at pH 7.42017Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7
Design of Potent mRNA Decapping Scavenger Enzyme (DcpS) Inhibitors with Improved Physicochemical Properties To Investigate the Mechanism of Therapeutic Benefit in Spinal Muscular Atrophy (SMA).
AID1442737Drug uptake in lymphoblasts (unknown origin) at 10 nM in presence of vacuolar type ATPase inhibitor bafilomycin measured after 2.5 hrs2017Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7
Design of Potent mRNA Decapping Scavenger Enzyme (DcpS) Inhibitors with Improved Physicochemical Properties To Investigate the Mechanism of Therapeutic Benefit in Spinal Muscular Atrophy (SMA).
AID1442738Inhibition of human DcpS assessed as increase in SMN2 promoter activity2017Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7
Design of Potent mRNA Decapping Scavenger Enzyme (DcpS) Inhibitors with Improved Physicochemical Properties To Investigate the Mechanism of Therapeutic Benefit in Spinal Muscular Atrophy (SMA).
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (6)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's0 (0.00)29.6817
2010's6 (100.00)24.3611
2020's0 (0.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 12.56

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 weak demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index12.56 (24.57)
Research Supply Index1.95 (2.92)
Research Growth Index4.51 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (12.56)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews0 (0.00%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other6 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
SubstanceRelationship StrengthStudiesTrialsClassesRoles
chloroquine
Chloroquine: The prototypical antimalarial agent with a mechanism that is not well understood. It has also been used to treat rheumatoid arthritis, systemic lupus erythematosus, and in the systemic therapy of amebic liver abscesses.. chloroquine : An aminoquinoline that is quinoline which is substituted at position 4 by a [5-(diethylamino)pentan-2-yl]amino group at at position 7 by chlorine. It is used for the treatment of malaria, hepatic amoebiasis, lupus erythematosus, light-sensitive skin eruptions, and rheumatoid arthritis.		2.1510aminoquinoline;
organochlorine compound;
secondary amino compound;
tertiary amino compound		anticoronaviral agent;
antimalarial;
antirheumatic drug;
autophagy inhibitor;
dermatologic drug
quinazolines
Quinazolines: A group of aromatic heterocyclic compounds that contain a bicyclic structure with two fused six-membered aromatic rings, a benzene ring and a pyrimidine ring.. quinazoline : A mancude organic heterobicyclic parent that is naphthalene in which the carbon atoms at positions 1 and 3 have been replaced by nitrogen atoms.. quinazolines : Any organic heterobicyclic compound based on a quinazoline skeleton and its substituted derivatives.		3.2150azaarene;
mancude organic heterobicyclic parent;
ortho-fused heteroarene;
quinazolines
2,4-diaminoquinazoline
[no description available]		2.5520
ConditionIndicatedRelationship StrengthStudiesTrials
Disease Models, Animal
Naturally-occurring or experimentally-induced animal diseases with pathological processes analogous to human diseases.		03.0340
Adult Spinal Muscular Atrophy
[description not available]		03.2250
Muscular Atrophy, Spinal
A group of disorders marked by progressive degeneration of motor neurons in the spinal cord resulting in weakness and muscular atrophy, usually without evidence of injury to the corticospinal tracts. Diseases in this category include Werdnig-Hoffmann disease and later onset SPINAL MUSCULAR ATROPHIES OF CHILDHOOD, most of which are hereditary. (Adams et al., Principles of Neurology, 6th ed, p1089)		03.2250
Leucocythaemia
[description not available]		02.1710
Leukemia
A progressive, malignant disease of the blood-forming organs, characterized by distorted proliferation and development of leukocytes and their precursors in the blood and bone marrow. Leukemias were originally termed acute or chronic based on life expectancy but now are classified according to cellular maturity. Acute leukemias consist of predominately immature cells; chronic leukemias are composed of more mature cells. (From The Merck Manual, 2006)		02.1710