| ID Source | ID |
|---|---|
| PubMed CID | 659101 |
| CHEMBL ID | 428064 |
| CHEMBL ID | 1589921 |
| CHEBI ID | 93609 |
| SCHEMBL ID | 11973195 |
| Synonym |
|---|
| CBDIVE_011354 |
| OPREA1_666568 |
| EU-0033328 |
| CU-01000003156-2 |
| NCGC00070544-03 |
| smr000040050 |
| MLS000038106 , |
| CHEMBL428064 |
| dndi1318477 |
| 5h-quinolino[8,7-c][1,2]benzothiazine 6,6-dioxide |
| HMS2479M21 |
| 5h-quino[8,7-c][1,2]benzothiazine 6,6-dioxide |
| STL328289 |
| CYSOFAOLQAYKGU-UHFFFAOYSA-N |
| 5h-6-thia-4,5-diaza-chrysene 6,6-dioxide |
| AKOS022139691 |
| CHEMBL1589921 |
| cid_659101 |
| bdbm36894 |
| SCHEMBL11973195 |
| SR-01000388300-1 |
| sr-01000388300 |
| CHEBI:93609 |
| Q27165302 |
| 5h-benzo[5,6][1,2]thiazino[4,3-h]quinoline 6,6-dioxide |
| ml063 |
| 21868-80-4 |
| Class | Description |
|---|---|
| benzothiazine | |
| [compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res] | |
| Protein | Taxonomy | Measurement | Average (µ) | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| Chain A, MAJOR APURINIC/APYRIMIDINIC ENDONUCLEASE | Homo sapiens (human) | Potency | 1.4125 | 0.0032 | 45.4673 | 12,589.2998 | AID2517 |
| Chain A, TYROSYL-DNA PHOSPHODIESTERASE | Homo sapiens (human) | Potency | 1.8447 | 0.0040 | 23.8416 | 100.0000 | AID485290 |
| Chain A, Putative fructose-1,6-bisphosphate aldolase | Giardia intestinalis | Potency | 20.0374 | 0.1409 | 11.1940 | 39.8107 | AID2451 |
| Chain A, HADH2 protein | Homo sapiens (human) | Potency | 39.8107 | 0.0251 | 20.2376 | 39.8107 | AID893 |
| Chain B, HADH2 protein | Homo sapiens (human) | Potency | 39.8107 | 0.0251 | 20.2376 | 39.8107 | AID893 |
| Chain A, JmjC domain-containing histone demethylation protein 3A | Homo sapiens (human) | Potency | 12.7880 | 0.6310 | 35.7641 | 100.0000 | AID504339 |
| Chain A, 2-oxoglutarate Oxygenase | Homo sapiens (human) | Potency | 39.8107 | 0.1778 | 14.3909 | 39.8107 | AID2147 |
| Nrf2 | Homo sapiens (human) | Potency | 7.0795 | 0.0920 | 8.2222 | 23.1093 | AID624171 |
| glp-1 receptor, partial | Homo sapiens (human) | Potency | 5.0119 | 0.0184 | 6.8060 | 14.1254 | AID624417 |
| BRCA1 | Homo sapiens (human) | Potency | 12.5893 | 0.8913 | 7.7225 | 25.1189 | AID624202 |
| 15-lipoxygenase, partial | Homo sapiens (human) | Potency | 0.6310 | 0.0126 | 10.6917 | 88.5700 | AID887 |
| ATAD5 protein, partial | Homo sapiens (human) | Potency | 19.1464 | 0.0041 | 10.8903 | 31.5287 | AID504466; AID504467 |
| TDP1 protein | Homo sapiens (human) | Potency | 1.3081 | 0.0008 | 11.3822 | 44.6684 | AID686978; AID686979 |
| Microtubule-associated protein tau | Homo sapiens (human) | Potency | 12.5893 | 0.1800 | 13.5574 | 39.8107 | AID1460 |
| Smad3 | Homo sapiens (human) | Potency | 1.2589 | 0.0052 | 7.8098 | 29.0929 | AID588855 |
| aldehyde dehydrogenase 1 family, member A1 | Homo sapiens (human) | Potency | 39.8107 | 0.0112 | 12.4002 | 100.0000 | AID1030 |
| thyroid stimulating hormone receptor | Homo sapiens (human) | Potency | 10.0000 | 0.0013 | 18.0743 | 39.8107 | AID926; AID938 |
| nonstructural protein 1 | Influenza A virus (A/WSN/1933(H1N1)) | Potency | 1.0000 | 0.2818 | 9.7212 | 35.4813 | AID2326 |
| 67.9K protein | Vaccinia virus | Potency | 16.8037 | 0.0001 | 8.4406 | 100.0000 | AID720579; AID720580 |
| bromodomain adjacent to zinc finger domain 2B | Homo sapiens (human) | Potency | 6.3096 | 0.7079 | 36.9043 | 89.1251 | AID504333 |
| P53 | Homo sapiens (human) | Potency | 56.2341 | 0.0731 | 9.6858 | 31.6228 | AID504706 |
| IDH1 | Homo sapiens (human) | Potency | 0.5623 | 0.0052 | 10.8652 | 35.4813 | AID686970 |
| heat shock 70kDa protein 5 (glucose-regulated protein, 78kDa) | Homo sapiens (human) | Potency | 17.7828 | 0.0165 | 25.3078 | 41.3999 | AID602332 |
| beta-2 adrenergic receptor | Homo sapiens (human) | Potency | 5.6234 | 0.0058 | 6.0263 | 32.6427 | AID492947 |
| nuclear factor erythroid 2-related factor 2 isoform 2 | Homo sapiens (human) | Potency | 6.5131 | 0.0041 | 9.9848 | 25.9290 | AID504444 |
| huntingtin isoform 2 | Homo sapiens (human) | Potency | 1.5849 | 0.0006 | 18.4198 | 1,122.0200 | AID1688 |
| DNA polymerase iota isoform a (long) | Homo sapiens (human) | Potency | 25.1189 | 0.0501 | 27.0736 | 89.1251 | AID588590 |
| urokinase-type plasminogen activator precursor | Mus musculus (house mouse) | Potency | 1.0000 | 0.1585 | 5.2879 | 12.5893 | AID540303 |
| plasminogen precursor | Mus musculus (house mouse) | Potency | 1.0000 | 0.1585 | 5.2879 | 12.5893 | AID540303 |
| urokinase plasminogen activator surface receptor precursor | Mus musculus (house mouse) | Potency | 1.0000 | 0.1585 | 5.2879 | 12.5893 | AID540303 |
| nuclear receptor ROR-gamma isoform 1 | Mus musculus (house mouse) | Potency | 2.1295 | 0.0079 | 8.2332 | 1,122.0200 | AID2546; AID2551 |
| lethal(3)malignant brain tumor-like protein 1 isoform I | Homo sapiens (human) | Potency | 7.1068 | 0.0752 | 15.2253 | 39.8107 | AID485360; AID540279 |
| Vpr | Human immunodeficiency virus 1 | Potency | 12.5893 | 1.5849 | 19.6264 | 63.0957 | AID651644 |
| survival motor neuron protein isoform d | Homo sapiens (human) | Potency | 10.0000 | 0.1259 | 12.2344 | 35.4813 | AID1458 |
| muscleblind-like protein 1 isoform 1 | Homo sapiens (human) | Potency | 25.1189 | 0.0041 | 9.9625 | 28.1838 | AID2675 |
| DNA dC->dU-editing enzyme APOBEC-3G isoform 1 | Homo sapiens (human) | Potency | 7.0795 | 0.0580 | 10.6949 | 26.6086 | AID602310 |
| muscarinic acetylcholine receptor M1 | Rattus norvegicus (Norway rat) | Potency | 1.0000 | 0.0010 | 6.0009 | 35.4813 | AID1492 |
| lamin isoform A-delta10 | Homo sapiens (human) | Potency | 0.7943 | 0.8913 | 12.0676 | 28.1838 | AID1487 |
| neuropeptide S receptor isoform A | Homo sapiens (human) | Potency | 3.3147 | 0.0158 | 12.3113 | 615.5000 | AID1461; AID1489; AID1491; AID2567; AID2568 |
| Glycoprotein hormones alpha chain | Homo sapiens (human) | Potency | 2.8184 | 4.4668 | 8.3448 | 10.0000 | AID624291 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
| Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| nonstructural protein 1 | Influenza A virus (A/California/07/2009(H1N1)) | IC50 (µMol) | 3.6260 | 0.2000 | 24.4540 | 100.0000 | AID504329 |
| toll-like receptor 9 | Homo sapiens (human) | IC50 (µMol) | 49.7450 | 1.8690 | 5.4371 | 9.2420 | AID588340 |
| kappa-type opioid receptor isoform 1 | Homo sapiens (human) | IC50 (µMol) | 16.6500 | 0.0032 | 2.6737 | 15.6000 | AID1778; AID2136 |
| Vif | Human immunodeficiency virus 1 | IC50 (µMol) | 100.0000 | 0.2700 | 34.0015 | 100.0000 | AID1117319 |
| DNA dC->dU-editing enzyme APOBEC-3G isoform 1 | Homo sapiens (human) | IC50 (µMol) | 100.0000 | 0.2700 | 26.3638 | 100.0000 | AID1117319 |
| Transcription factor p65 | Homo sapiens (human) | IC50 (µMol) | 1.0000 | 0.0001 | 1.8981 | 8.8000 | AID317146 |
| Solute carrier family 40 member 1 | Homo sapiens (human) | IC50 (µMol) | 2.9000 | 2.9000 | 3.7450 | 4.5900 | AID1342645 |
| Beta lactamase (plasmid) | Pseudomonas aeruginosa | IC50 (µMol) | 49.7450 | 0.7091 | 5.0549 | 7.7510 | AID588341 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
| Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| matrix metalloproteinase 1, partial | Homo sapiens (human) | EC50 (µMol) | 24.6000 | 1.0600 | 10.7594 | 27.6000 | AID618 |
| Hsf1 protein | Mus musculus (house mouse) | EC50 (µMol) | 2.7610 | 0.1600 | 24.4900 | 236.5000 | AID435004 |
| Alpha-1B adrenergic receptor | Rattus norvegicus (Norway rat) | EC50 (µMol) | 31.5000 | 0.0013 | 2.6129 | 25.7000 | AID1966 |
| Alpha-1D adrenergic receptor | Rattus norvegicus (Norway rat) | EC50 (µMol) | 31.5000 | 0.0013 | 3.3946 | 25.7000 | AID1966 |
| NF-kappa-B inhibitor alpha | Homo sapiens (human) | EC50 (µMol) | 2.4000 | 1.0000 | 2.7500 | 5.2000 | AID317143; AID317145 |
| Alpha-1A adrenergic receptor | Rattus norvegicus (Norway rat) | EC50 (µMol) | 31.5000 | 0.0013 | 3.3946 | 25.7000 | AID1966 |
| Beta-galactosidase | Escherichia coli | EC50 (µMol) | 31.5000 | 25.7000 | 25.7000 | 25.7000 | AID1966 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
| Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| heat shock protein HSP 90-alpha isoform 2 | Homo sapiens (human) | AC50 | 0.1950 | 0.1950 | 3.6679 | 18.6960 | AID540270 |
| heat shock protein 90, putative | Plasmodium falciparum 3D7 | AC50 | 0.8940 | 0.1950 | 4.9920 | 98.5000 | AID540268 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| 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. |
| 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. |
| AID504810 | Antagonists of the Thyroid Stimulating Hormone Receptor: HTS campaign | 2010 | Endocrinology, Jul, Volume: 151, Issue:7 | A small molecule inverse agonist for the human thyroid-stimulating hormone receptor. |
| AID504812 | Inverse Agonists of the Thyroid Stimulating Hormone Receptor: HTS campaign | 2010 | Endocrinology, Jul, Volume: 151, Issue:7 | A small molecule inverse agonist for the human thyroid-stimulating hormone receptor. |
| AID651635 | Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression | |||
| AID1745845 | Primary qHTS for Inhibitors of ATXN expression | |||
| AID317147 | Inhibition of TNF-alpha-stimulated human NF-kappaB p65 RelA subunit nuclear translocation in HUVEC relative to control | 2008 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 18, Issue:1 | Identification of N-(quinolin-8-yl)benzenesulfonamides as agents capable of down-regulating NFkappaB activity within two separate high-throughput screens of NFkappaB activation. |
| AID448438 | Inhibition of NF-kappaB activation | 2009 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 19, Issue:19 | The first pharmacophore model for potent NF-kappaB inhibitors. |
| AID317145 | Induction of human IkappaBalpha stabilization in OCI-Ly3 cells assessed as ratio of green light emiting IkappaBalpha-fused luciferase expression to red light emiting native luciferase expression | 2008 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 18, Issue:1 | Identification of N-(quinolin-8-yl)benzenesulfonamides as agents capable of down-regulating NFkappaB activity within two separate high-throughput screens of NFkappaB activation. |
| AID317149 | Cytotoxicity against NF-kappaB overexpressing human OCI-Ly3 cells after 4 hrs | 2008 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 18, Issue:1 | Identification of N-(quinolin-8-yl)benzenesulfonamides as agents capable of down-regulating NFkappaB activity within two separate high-throughput screens of NFkappaB activation. |
| AID317150 | Inhibition of human E3 ubiquitin ligase-mediated IkappaBalpha ubiquitination in HUVEC | 2008 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 18, Issue:1 | Identification of N-(quinolin-8-yl)benzenesulfonamides as agents capable of down-regulating NFkappaB activity within two separate high-throughput screens of NFkappaB activation. |
| AID317143 | Induction of human IkappaBalpha stabilization in OCI-Ly3 cells by green light emiting IkappaBalpha-fused luciferase reporter gene assay | 2008 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 18, Issue:1 | Identification of N-(quinolin-8-yl)benzenesulfonamides as agents capable of down-regulating NFkappaB activity within two separate high-throughput screens of NFkappaB activation. |
| AID317148 | Inhibition of TNFalpha stimulated human NF-kappaB-mediated beta lactamase gene expression in HUVEC | 2008 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 18, Issue:1 | Identification of N-(quinolin-8-yl)benzenesulfonamides as agents capable of down-regulating NFkappaB activity within two separate high-throughput screens of NFkappaB activation. |
| AID317144 | Induction of human IkappaBalpha stabilization in OCI-Ly3 cells by green light emiting IkappaBalpha-fused luciferase reporter gene assay relative to control | 2008 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 18, Issue:1 | Identification of N-(quinolin-8-yl)benzenesulfonamides as agents capable of down-regulating NFkappaB activity within two separate high-throughput screens of NFkappaB activation. |
| AID317146 | Inhibition of TNF-alpha-stimulated human NF-kappaB p65 RelA subunit nuclear translocation in HUVEC | 2008 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 18, Issue:1 | Identification of N-(quinolin-8-yl)benzenesulfonamides as agents capable of down-regulating NFkappaB activity within two separate high-throughput screens of NFkappaB activation. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||||
| Timeframe | Studies, This Drug (%) | All Drugs % |
|---|---|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 0 (0.00) | 18.2507 |
| 2000's | 3 (42.86) | 29.6817 |
| 2010's | 3 (42.86) | 24.3611 |
| 2020's | 1 (14.29) | 2.80 |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||
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.
| This Compound (12.28) All Compounds (24.57) |
| 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 | 7 (100.00%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||