Compounds > dsr-6434
Page last updated: 2024-11-13

dsr-6434

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

Description

DSR-6434: structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID25071151
CHEMBL ID2315158
SCHEMBL ID13448863
SCHEMBL ID1146577
MeSH IDM0585764

Synonyms (24)

Synonym
CHEMBL2315158 ,
bdbm50425234
SCHEMBL13448863
SCHEMBL1146577
AKOS025147319
6-amino-2-(butylamino)-9-[[6-[2-(dimethylamino)ethoxy]-3-pyridinyl]methyl]-7,9-dihydro-8h-purin-8-one
dsr 6434
1059070-10-8
6-amino-2-(butylamino)-9-((6-(2-(dimethylamino)ethoxy)pyridin-3-yl)methyl)-7,9-dihydro-8h-purin-8-one
NCGC00387452-01
CS-0032972
HY-110120
dsr-6434
BS-14261
D80530
unii-8ybw739lj0
8ybw739lj0 ,
6-amino-2-(butylamino)-9-((6-(2-(dimethylamino)ethoxy)-3-pyridinyl)methyl)-7,9-dihydro-8h-purin-8-one
8h-purin-8-one, 6-amino-2-(butylamino)-9-((6-(2-(dimethylamino)ethoxy)-3-pyridinyl)methyl)-7,9-dihydro-
6-amino-2-(butylamino)-9-[[6-[2-(dimethylamino)ethoxy]pyridin-3-yl]methyl]-7h-purin-8-one
mfcd30182245
6-amino-2-(butylamino)-9-[[6-[2-(dimethylamino)ethoxy]pyridin-3-yl]methyl]-7h-purin-8(9h)-one
SY347007
6-amino-2-(butylamino)-9-({6-[2-(dimethylamino)ethoxy]pyridin-3-yl}methyl)-7h-purin-8-one

Research Excerpts

Bioavailability

ExcerptReferenceRelevance
"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

Dosage Studied

ExcerptRelevanceReference
" In a preclinical model of renal cell cancer, systemic administration of DSR-6434 dosed once weekly resulted in a significant anti-tumor response."( TLR7 tolerance is independent of the type I IFN pathway and leads to loss of anti-tumor efficacy in mice.
Dovedi, SJ; Harada, H; Hirose, Y; Jewsbury, PJ; Koga-Yamakawa, E; Li, CJ; Murata, M; Ota, Y; Robinson, DT; Sugaru, E; Umehara, H; Wilkinson, RW; Yamamoto, S, 2015)		0.65
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (3)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
cytochrome P450 family 3 subfamily A polypeptide 4Homo sapiens (human)Potency15.09160.01237.983543.2770AID1645841
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Activation Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Toll-like receptor 7Mus musculus (house mouse)EC50 (µMol)0.00460.00460.00460.0046AID721199
Toll-like receptor 7Homo sapiens (human)EC50 (µMol)0.00720.00721.57446.8000AID721201
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (23)

Processvia Protein(s)Taxonomy
regulation of protein phosphorylationToll-like receptor 7Homo sapiens (human)
inflammatory responseToll-like receptor 7Homo sapiens (human)
canonical NF-kappaB signal transductionToll-like receptor 7Homo sapiens (human)
I-kappaB phosphorylationToll-like receptor 7Homo sapiens (human)
JNK cascadeToll-like receptor 7Homo sapiens (human)
positive regulation of chemokine productionToll-like receptor 7Homo sapiens (human)
positive regulation of interferon-alpha productionToll-like receptor 7Homo sapiens (human)
positive regulation of interferon-beta productionToll-like receptor 7Homo sapiens (human)
positive regulation of type II interferon productionToll-like receptor 7Homo sapiens (human)
positive regulation of interleukin-8 productionToll-like receptor 7Homo sapiens (human)
toll-like receptor 7 signaling pathwayToll-like receptor 7Homo sapiens (human)
positive regulation of canonical NF-kappaB signal transductionToll-like receptor 7Homo sapiens (human)
innate immune responseToll-like receptor 7Homo sapiens (human)
positive regulation of transcription by RNA polymerase IIToll-like receptor 7Homo sapiens (human)
positive regulation of inflammatory responseToll-like receptor 7Homo sapiens (human)
defense response to virusToll-like receptor 7Homo sapiens (human)
positive regulation of macrophage cytokine productionToll-like receptor 7Homo sapiens (human)
response to cGMPToll-like receptor 7Homo sapiens (human)
cellular response to mechanical stimulusToll-like receptor 7Homo sapiens (human)
cellular response to virusToll-like receptor 7Homo sapiens (human)
positive regulation of non-canonical NF-kappaB signal transductionToll-like receptor 7Homo sapiens (human)
toll-like receptor signaling pathwayToll-like receptor 7Homo sapiens (human)
positive regulation of interleukin-6 productionToll-like receptor 7Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (5)

Processvia Protein(s)Taxonomy
double-stranded RNA bindingToll-like receptor 7Homo sapiens (human)
single-stranded RNA bindingToll-like receptor 7Homo sapiens (human)
protein bindingToll-like receptor 7Homo sapiens (human)
siRNA bindingToll-like receptor 7Homo sapiens (human)
pattern recognition receptor activityToll-like receptor 7Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (11)

Processvia Protein(s)Taxonomy
Golgi membraneToll-like receptor 7Homo sapiens (human)
cytoplasmToll-like receptor 7Homo sapiens (human)
lysosomeToll-like receptor 7Homo sapiens (human)
endosomeToll-like receptor 7Homo sapiens (human)
endoplasmic reticulumToll-like receptor 7Homo sapiens (human)
endoplasmic reticulum membraneToll-like receptor 7Homo sapiens (human)
plasma membraneToll-like receptor 7Homo sapiens (human)
endosome membraneToll-like receptor 7Homo sapiens (human)
early phagosomeToll-like receptor 7Homo sapiens (human)
endolysosome membraneToll-like receptor 7Homo sapiens (human)
receptor complexToll-like receptor 7Homo sapiens (human)
plasma membraneToll-like receptor 7Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (15)

Assay IDTitleYearJournalArticle
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.
AID1347160Primary screen NINDS Rhodamine 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.
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.
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.
AID1347159Primary screen GU Rhodamine qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay2020Proceedings 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.
AID721199Agonist activity at mouse TLR72013Bioorganic & medicinal chemistry letters, Feb-01, Volume: 23, Issue:3
Synthesis and evaluation of 8-oxoadenine derivatives as potent Toll-like receptor 7 agonists with high water solubility.
AID721195Half life in Balb/c mouse at 1 mg/kg, iv2013Bioorganic & medicinal chemistry letters, Feb-01, Volume: 23, Issue:3
Synthesis and evaluation of 8-oxoadenine derivatives as potent Toll-like receptor 7 agonists with high water solubility.
AID721200Volume of distribution at steady state in Balb/c mouse at 1 mg/kg, iv2013Bioorganic & medicinal chemistry letters, Feb-01, Volume: 23, Issue:3
Synthesis and evaluation of 8-oxoadenine derivatives as potent Toll-like receptor 7 agonists with high water solubility.
AID721194Antitumor activity against mouse HM1 cells xenografted in B6C3F1 mouse assessed as inhibition of lung metastasis at 0.1 mg/kg, iv administered biweekly starting on day 1 post tumor xenografting measured on day 35 post tumor xenografting2013Bioorganic & medicinal chemistry letters, Feb-01, Volume: 23, Issue:3
Synthesis and evaluation of 8-oxoadenine derivatives as potent Toll-like receptor 7 agonists with high water solubility.
AID721198Aqueous solubility in pH 7.4 buffer2013Bioorganic & medicinal chemistry letters, Feb-01, Volume: 23, Issue:3
Synthesis and evaluation of 8-oxoadenine derivatives as potent Toll-like receptor 7 agonists with high water solubility.
AID721191Potency index, ratio of antitumor activity of 852A to test compound against mouse HM1 cells xenografted in B6C3F1 mouse2013Bioorganic & medicinal chemistry letters, Feb-01, Volume: 23, Issue:3
Synthesis and evaluation of 8-oxoadenine derivatives as potent Toll-like receptor 7 agonists with high water solubility.
AID721201Agonist activity at human TLR7 expressed in HEK293 cells by NFkappaB SEAP reporter gene assay2013Bioorganic & medicinal chemistry letters, Feb-01, Volume: 23, Issue:3
Synthesis and evaluation of 8-oxoadenine derivatives as potent Toll-like receptor 7 agonists with high water solubility.
AID721193Antitumor activity against mouse HM1 cells xenografted in B6C3F1 mouse assessed as inhibition of lung metastasis at 1 mg/kg, iv administered biweekly starting on day 1 post tumor xenografting measured on day 35 post tumor xenografting2013Bioorganic & medicinal chemistry letters, Feb-01, Volume: 23, Issue:3
Synthesis and evaluation of 8-oxoadenine derivatives as potent Toll-like receptor 7 agonists with high water solubility.
AID721190Potency index, ratio of EC50 of 852A to EC50 of test compound for human TLR7 expressed in HEK293 cells by NFkappaB SEAP reporter gene assay2013Bioorganic & medicinal chemistry letters, Feb-01, Volume: 23, Issue:3
Synthesis and evaluation of 8-oxoadenine derivatives as potent Toll-like receptor 7 agonists with high water solubility.
AID721196Increase in IFN level in Balb/c mouse plasma at 1 mg/kg, iv measured after 6 hrs post dose by L929 cells and VSV based bioassay2013Bioorganic & medicinal chemistry letters, Feb-01, Volume: 23, Issue:3
Synthesis and evaluation of 8-oxoadenine derivatives as potent Toll-like receptor 7 agonists with high water solubility.
[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's4 (66.67)24.3611
2020's2 (33.33)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 17.74

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 Index17.74 (24.57)
Research Supply Index1.95 (2.92)
Research Growth Index4.51 (4.65)
Search Engine Demand Index10.37 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (17.74)

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
adenine
[no description available]		2.79306-aminopurines;
purine nucleobase		Daphnia magna metabolite;
Escherichia coli metabolite;
human metabolite;
mouse metabolite;
Saccharomyces cerevisiae metabolite
8-hydroxyadenine
8-hydroxyadenine: xanthine oxidase reacted adenine metabolite in epidermis of hairless mice; structure. 8-oxoadenine : An oxopurine that is adenine bearing a single oxo substituent at position 8.. 8-hydroxyadenine : A nucleobase analogue that is adenine bearing a single hydroxy substituent at position 8.		2.08106-aminopurines;
heteroaryl hydroxy compound;
nucleobase analogue;
oxopurine		bacterial metabolite;
human metabolite
ConditionIndicatedRelationship StrengthStudiesTrials
Disease Models, Animal
Naturally-occurring or experimentally-induced animal diseases with pathological processes analogous to human diseases.		02.8130
Congenital Zika Syndrome
[description not available]		02.2510
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.		02.2510
Metastase
[description not available]		02.110
Benign Neoplasms
[description not available]		02.110
Neoplasm Metastasis
The transfer of a neoplasm from one organ or part of the body to another remote from the primary site.		02.110
Neoplasms
New abnormal growth of tissue. Malignant neoplasms show a greater degree of anaplasia and have the properties of invasion and metastasis, compared to benign neoplasms.		02.110
Adenocarcinoma Of Kidney
[description not available]		02.1110
Experimental Neoplasms
[description not available]		02.1110
Carcinoma, Renal Cell
A heterogeneous group of sporadic or hereditary carcinoma derived from cells of the KIDNEYS. There are several subtypes including the clear cells, the papillary, the chromophobe, the collecting duct, the spindle cells (sarcomatoid), or mixed cell-type carcinoma.		02.1110