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 Source | ID |
|---|---|
| PubMed CID | 25071151 |
| CHEMBL ID | 2315158 |
| SCHEMBL ID | 13448863 |
| SCHEMBL ID | 1146577 |
| MeSH ID | M0585764 |
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
| Excerpt | Reference | Relevance |
|---|---|---|
| "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
| Excerpt | Relevance | Reference |
|---|---|---|
| " 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
| Protein | Taxonomy | Measurement | Average (µ) | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| cytochrome P450 family 3 subfamily A polypeptide 4 | Homo sapiens (human) | Potency | 15.0916 | 0.0123 | 7.9835 | 43.2770 | AID1645841 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
Activation Measurements
| Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| Toll-like receptor 7 | Mus musculus (house mouse) | EC50 (µMol) | 0.0046 | 0.0046 | 0.0046 | 0.0046 | AID721199 |
| Toll-like receptor 7 | Homo sapiens (human) | EC50 (µMol) | 0.0072 | 0.0072 | 1.5744 | 6.8000 | AID721201 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
Biological Processes (23)
Molecular Functions (5)
| Process | via Protein(s) | Taxonomy |
|---|---|---|
| double-stranded RNA binding | Toll-like receptor 7 | Homo sapiens (human) |
| single-stranded RNA binding | Toll-like receptor 7 | Homo sapiens (human) |
| protein binding | Toll-like receptor 7 | Homo sapiens (human) |
| siRNA binding | Toll-like receptor 7 | Homo sapiens (human) |
| pattern recognition receptor activity | Toll-like receptor 7 | Homo sapiens (human) |
| [Information is prepared from geneontology information from the June-17-2024 release] | ||
Ceullar Components (11)
| Process | via Protein(s) | Taxonomy |
|---|---|---|
| Golgi membrane | Toll-like receptor 7 | Homo sapiens (human) |
| cytoplasm | Toll-like receptor 7 | Homo sapiens (human) |
| lysosome | Toll-like receptor 7 | Homo sapiens (human) |
| endosome | Toll-like receptor 7 | Homo sapiens (human) |
| endoplasmic reticulum | Toll-like receptor 7 | Homo sapiens (human) |
| endoplasmic reticulum membrane | Toll-like receptor 7 | Homo sapiens (human) |
| plasma membrane | Toll-like receptor 7 | Homo sapiens (human) |
| endosome membrane | Toll-like receptor 7 | Homo sapiens (human) |
| early phagosome | Toll-like receptor 7 | Homo sapiens (human) |
| endolysosome membrane | Toll-like receptor 7 | Homo sapiens (human) |
| receptor complex | Toll-like receptor 7 | Homo sapiens (human) |
| plasma membrane | Toll-like receptor 7 | Homo sapiens (human) |
| [Information is prepared from geneontology information from the June-17-2024 release] | ||
Bioassays (15)
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| 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. |
| AID1347160 | Primary screen NINDS Rhodamine 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. |
| 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. |
| 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. |
| AID1347159 | Primary screen GU Rhodamine qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay | 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. |
| AID721199 | Agonist activity at mouse TLR7 | 2013 | Bioorganic & 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. |
| AID721195 | Half life in Balb/c mouse at 1 mg/kg, iv | 2013 | Bioorganic & 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. |
| AID721200 | Volume of distribution at steady state in Balb/c mouse at 1 mg/kg, iv | 2013 | Bioorganic & 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. |
| AID721194 | Antitumor 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 xenografting | 2013 | Bioorganic & 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. |
| AID721198 | Aqueous solubility in pH 7.4 buffer | 2013 | Bioorganic & 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. |
| AID721191 | Potency index, ratio of antitumor activity of 852A to test compound against mouse HM1 cells xenografted in B6C3F1 mouse | 2013 | Bioorganic & 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. |
| AID721201 | Agonist activity at human TLR7 expressed in HEK293 cells by NFkappaB SEAP reporter gene assay | 2013 | Bioorganic & 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. |
| AID721193 | Antitumor 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 xenografting | 2013 | Bioorganic & 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. |
| AID721190 | Potency index, ratio of EC50 of 852A to EC50 of test compound for human TLR7 expressed in HEK293 cells by NFkappaB SEAP reporter gene assay | 2013 | Bioorganic & 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. |
| AID721196 | Increase 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 bioassay | 2013 | Bioorganic & 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)
| 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 | 4 (66.67) | 24.3611 |
| 2020's | 2 (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.
| This Compound (17.74) All Compounds (24.57) |
Study Types
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 0 (0.00%) | 5.53% |
| Reviews | 0 (0.00%) | 6.00% |
| Case Studies | 0 (0.00%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 6 (100.00%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||