Page last updated: 2024-12-07
c 1303
Description
Research Excerpts
Clinical Trials
Roles
Classes
Pathways
Study Profile
Bioassays
Related Drugs
Related Conditions
Protein Interactions
Research Growth
Market Indicators
Description
C 1303: DNa-binding drug; structure given indicates that the cpd should be the dimethylamino cpd, but it is named as the diethylamino cpd [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]
Cross-References
| ID Source | ID |
|---|---|
| PubMed CID | 124496 |
| CHEMBL ID | 95704 |
| MeSH ID | M0214056 |
Synonyms (17)
| Synonym |
|---|
| smr001565158 |
| CHEMBL95704 |
| NCI60_015716 |
| nsc645827 |
| 5-(2-(dimethylamino)ethylamino)-8-hydroxy-6h-[1,3]triazolo[4,5,1-de]acridin-6-one |
| nsc-645827 |
| mls002701557 , |
| 6h-(1,2,3)triazolo(4,5,1-de)acridin-6-one, 5-((2-(dimethylamino)ethyl)amino)-8-hydroxy- |
| 5-(2-(diethylamino)ethylamino)-8-hydroxy-6h-(1,2,3)triazolo(4,5-1-de)acridin-6-one |
| 128113-19-9 |
| c-1303 , |
| c 1303 |
| DTXSID30155810 |
| 5VNA4LC5RU |
| 5-[[2-(dimethylamino)ethyl]amino]-8-hydroxy-6h-[1,2,3]triazolo[4,5,1-de]acridin-6-one |
| 6h-[1,2,3]triazolo[4,5,1-de]acridin-6-one, 5-[[2-(dimethylamino)ethyl]amino]-8-hydroxy- |
| 10-(2-(dimethylamino)ethylamino)-5-oxidanyl-1,14,15-triazatetracyclo(7.6.1.02,7.013,16)hexadeca-2,4,6,9(16),10,12,14-heptaen-8-one |
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
Protein Targets (15)
Potency Measurements
| Protein | Taxonomy | Measurement | Average (µ) | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| glp-1 receptor, partial | Homo sapiens (human) | Potency | 7.9433 | 0.0184 | 6.8060 | 14.1254 | AID624417 |
| TDP1 protein | Homo sapiens (human) | Potency | 0.1836 | 0.0008 | 11.3822 | 44.6684 | AID686978; AID686979 |
| Smad3 | Homo sapiens (human) | Potency | 15.8489 | 0.0052 | 7.8098 | 29.0929 | AID588855 |
| 67.9K protein | Vaccinia virus | Potency | 1.4502 | 0.0001 | 8.4406 | 100.0000 | AID720579; AID720580 |
| IDH1 | Homo sapiens (human) | Potency | 23.1093 | 0.0052 | 10.8652 | 35.4813 | AID686970 |
| flap endonuclease 1 | Homo sapiens (human) | Potency | 10.5407 | 0.1337 | 25.4129 | 89.1251 | AID588795; AID720498 |
| eyes absent homolog 2 isoform a | Homo sapiens (human) | Potency | 1.6947 | 1.1998 | 14.6419 | 50.1187 | AID720540 |
| DNA polymerase eta isoform 1 | Homo sapiens (human) | Potency | 14.1254 | 0.1000 | 28.9256 | 213.3130 | AID588591 |
| DNA polymerase iota isoform a (long) | Homo sapiens (human) | Potency | 89.1251 | 0.0501 | 27.0736 | 89.1251 | AID588590 |
| DNA dC->dU-editing enzyme APOBEC-3F isoform a | Homo sapiens (human) | Potency | 35.4813 | 0.0259 | 11.2398 | 31.6228 | AID602313 |
| Guanine nucleotide-binding protein G | Homo sapiens (human) | Potency | 7.9433 | 1.9953 | 25.5327 | 50.1187 | AID624287 |
| C-terminal-binding protein 1 | Homo sapiens (human) | Potency | 1.1998 | 0.3014 | 9.3210 | 19.0148 | AID720541 |
| [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) |
|---|---|---|---|---|---|---|---|
| rac GTPase-activating protein 1 isoform a | Homo sapiens (human) | IC50 (µMol) | 62.5600 | 7.3900 | 57.8904 | 301.2400 | AID624330 |
| NAD | Homo sapiens (human) | IC50 (µMol) | 0.7000 | 0.0026 | 0.8076 | 3.4000 | AID277029 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
Other Measurements
| Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| Microphthalmia-associated transcription factor | Homo sapiens (human) | AC50 | 15.0603 | 0.0150 | 10.9049 | 46.0480 | AID493073; AID493102; AID493177; AID540346 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
Biological Processes (53)
Molecular Functions (20)
Ceullar Components (12)
| Process | via Protein(s) | Taxonomy |
|---|---|---|
| nucleus | NAD | Homo sapiens (human) |
| cytoplasm | NAD | Homo sapiens (human) |
| cytosol | NAD | Homo sapiens (human) |
| dendrite | NAD | Homo sapiens (human) |
| neuronal cell body | NAD | Homo sapiens (human) |
| synapse | NAD | Homo sapiens (human) |
| cytosol | NAD | Homo sapiens (human) |
| plasma membrane | Guanine nucleotide-binding protein G | Homo sapiens (human) |
| nucleus | C-terminal-binding protein 1 | Homo sapiens (human) |
| nucleoplasm | C-terminal-binding protein 1 | Homo sapiens (human) |
| presynaptic active zone cytoplasmic component | C-terminal-binding protein 1 | Homo sapiens (human) |
| glutamatergic synapse | C-terminal-binding protein 1 | Homo sapiens (human) |
| GABA-ergic synapse | C-terminal-binding protein 1 | Homo sapiens (human) |
| transcription repressor complex | C-terminal-binding protein 1 | Homo sapiens (human) |
| nucleus | C-terminal-binding protein 1 | Homo sapiens (human) |
| [Information is prepared from geneontology information from the June-17-2024 release] | ||
Bioassays (20)
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| AID651635 | Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression | |||
| AID1745850 | Viability Counterscreen for Confirmatory qHTS for Inhibitors of ATXN expression | |||
| AID1745849 | Viability Counterscreen for CMV-Luciferase Assay of Inhibitors of ATXN expression | |||
| AID588499 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set | 2010 | Current protocols in cytometry, Oct, Volume: Chapter 13 | Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening. |
| AID588499 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set | 2006 | Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5 | Microsphere-based protease assays and screening application for lethal factor and factor Xa. |
| AID588499 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set | 2010 | Assay and drug development technologies, Feb, Volume: 8, Issue:1 | High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors. |
| AID588497 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set | 2010 | Current protocols in cytometry, Oct, Volume: Chapter 13 | Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening. |
| AID588497 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set | 2006 | Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5 | Microsphere-based protease assays and screening application for lethal factor and factor Xa. |
| AID588497 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set | 2010 | Assay and drug development technologies, Feb, Volume: 8, Issue:1 | High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors. |
| AID1745847 | CMV-Luciferase Counterscreen for Inhibitors of ATXN expression | |||
| AID588501 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set | 2010 | Current protocols in cytometry, Oct, Volume: Chapter 13 | Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening. |
| AID588501 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set | 2006 | Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5 | Microsphere-based protease assays and screening application for lethal factor and factor Xa. |
| AID588501 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set | 2010 | Assay and drug development technologies, Feb, Volume: 8, Issue:1 | High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors. |
| AID1745845 | Primary qHTS for Inhibitors of ATXN expression | |||
| AID1745848 | Confirmatory qHTS for Inhibitors of ATXN expression | |||
| AID153634 | In vivo antileukemic activity against P388 leukemia at dose 25 mp/kg administered intraperitoneally (30 days survivors, 3/6) | 1990 | Journal of medicinal chemistry, Oct, Volume: 33, Issue:10 | 8-Substituted 5-[(aminoalkyl)amino]-6H-v-triazolo[4,5,1-de]acridin-6-ones as potential antineoplastic agents. Synthesis and biological activity. |
| AID1096392 | Binding affinity to Bos taurus (calf) thymus DNA assessed as change in melting temperature at drug to DNA base pair ratio 0.25 M | 2011 | Medicinal chemistry research : an international journal for rapid communications on design and mechanisms of action of biologically active agents, Nov, Volume: 20, Issue:8 | Physicochemical interaction of antitumor acridinone derivatives with DNA in view of QSAR studies. |
| AID87734 | In vitro cytotoxicity against HeLa S3 cell lines | 1990 | Journal of medicinal chemistry, Oct, Volume: 33, Issue:10 | 8-Substituted 5-[(aminoalkyl)amino]-6H-v-triazolo[4,5,1-de]acridin-6-ones as potential antineoplastic agents. Synthesis and biological activity. |
| AID277029 | Inhibition of human recombinant NQO1 | 2006 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 16, Issue:24 | In silico identification and biochemical characterization of novel inhibitors of NQO1. |
| AID1096393 | Antitumor activity against Mus musculus (mouse) P388 cells xenografted in Mus musculus (mouse) assessed as increase in survival time relative to control | 2011 | Medicinal chemistry research : an international journal for rapid communications on design and mechanisms of action of biologically active agents, Nov, Volume: 20, Issue:8 | Physicochemical interaction of antitumor acridinone derivatives with DNA in view of QSAR studies. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||||
Research
Studies (8)
| Timeframe | Studies, This Drug (%) | All Drugs % |
|---|---|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 2 (25.00) | 18.2507 |
| 2000's | 2 (25.00) | 29.6817 |
| 2010's | 3 (37.50) | 24.3611 |
| 2020's | 1 (12.50) | 2.80 |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||
Market Indicators
Research Demand Index: 32.45
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 (32.45) 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 | 8 (100.00%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||