Page last updated: 2024-12-10
LSM-16826
Description
Research Excerpts
Clinical Trials
Roles
Classes
Pathways
Study Profile
Bioassays
Related Drugs
Related Conditions
Protein Interactions
Research Growth
Cross-References
| ID Source | ID |
|---|---|
| PubMed CID | 4325987 |
| CHEMBL ID | 1535539 |
| CHEBI ID | 105463 |
Synonyms (16)
| Synonym |
|---|
| smr000145385 |
| 4-(10-methyl-8-phenyl-6-phenylamino-8,11-dihydro-5,7,8,9,11a-pentaaza-cyclopenta[b]phenanthren-11 -yl)-benzene-1,2-diol |
| MLS000551460 , |
| CHEBI:105463 |
| MLS002582190 |
| AKOS005477970 |
| STK550659 |
| 4-[10-methyl-8-phenyl-6-(phenylamino)-8,11-dihydropyrazolo[3',4':4,5]pyrimido[1,2-a]quinoxalin-11-yl]benzene-1,2-diol |
| HMS2174C05 |
| cid_4325987 |
| bdbm41604 |
| CHEMBL1535539 |
| lsm-16826 |
| Q27183201 |
| 4-(10-methyl-8-phenyl-6-phenylamino-8,11-dihydro-5,7,8,9,11a-pentaaza-cyclopenta[b]phenanthren-11-yl)-benzene-1,2-diol |
| 4-(9-anilino-15-methyl-13-phenyl-1,8,11,13,14-pentazatetracyclo[8.7.0.02,7.012,16]heptadeca-2,4,6,8,10,12(16),14-heptaen-17-yl)benzene-1,2-diol |
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
Drug Classes (2)
| Class | Description |
|---|---|
| ring assembly | Two or more cyclic systems (single rings or fused systems) which are directly joined to each other by double or single bonds are named ring assemblies when the number of such direct ring junctions is one less than the number of cyclic systems involved. |
| pyrazoles | |
| [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 Targets (22)
Potency Measurements
| Protein | Taxonomy | Measurement | Average (µ) | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| Chain A, 2-oxoglutarate Oxygenase | Homo sapiens (human) | Potency | 17.7828 | 0.1778 | 14.3909 | 39.8107 | AID2147 |
| Chain A, Cruzipain | Trypanosoma cruzi | Potency | 0.3162 | 0.0020 | 14.6779 | 39.8107 | AID1476 |
| Microtubule-associated protein tau | Homo sapiens (human) | Potency | 17.7828 | 0.1800 | 13.5574 | 39.8107 | AID1460 |
| Smad3 | Homo sapiens (human) | Potency | 35.4813 | 0.0052 | 7.8098 | 29.0929 | AID588855 |
| isocitrate dehydrogenase 1, partial | Homo sapiens (human) | Potency | 34.5598 | 6.3096 | 27.0990 | 79.4328 | AID602179; AID624002 |
| nonstructural protein 1 | Influenza A virus (A/WSN/1933(H1N1)) | Potency | 19.9526 | 0.2818 | 9.7212 | 35.4813 | AID2326 |
| lysosomal alpha-glucosidase preproprotein | Homo sapiens (human) | Potency | 11.2202 | 0.0366 | 19.6376 | 50.1187 | AID2100 |
| chromobox protein homolog 1 | Homo sapiens (human) | Potency | 44.6684 | 0.0060 | 26.1688 | 89.1251 | AID540317 |
| importin subunit beta-1 isoform 1 | Homo sapiens (human) | Potency | 37.6460 | 5.8048 | 36.1306 | 65.1308 | AID540253; AID540263 |
| snurportin-1 | Homo sapiens (human) | Potency | 37.6460 | 5.8048 | 36.1306 | 65.1308 | AID540253; AID540263 |
| peptidyl-prolyl cis-trans isomerase NIMA-interacting 1 | Homo sapiens (human) | Potency | 84.9214 | 0.4256 | 12.0591 | 28.1838 | AID504891 |
| GTP-binding nuclear protein Ran isoform 1 | Homo sapiens (human) | Potency | 35.4813 | 5.8048 | 16.9962 | 25.9290 | AID540253 |
| nuclear receptor ROR-gamma isoform 1 | Mus musculus (house mouse) | Potency | 35.4813 | 0.0079 | 8.2332 | 1,122.0200 | AID2546 |
| geminin | Homo sapiens (human) | Potency | 19.4763 | 0.0046 | 11.3741 | 33.4983 | AID624296; AID624297 |
| lamin isoform A-delta10 | Homo sapiens (human) | Potency | 0.0316 | 0.8913 | 12.0676 | 28.1838 | AID1487 |
| neuropeptide S receptor isoform A | Homo sapiens (human) | Potency | 19.9526 | 0.0158 | 12.3113 | 615.5000 | AID1461 |
| Guanine nucleotide-binding protein G | Homo sapiens (human) | Potency | 25.1189 | 1.9953 | 25.5327 | 50.1187 | AID624287 |
| [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) |
|---|---|---|---|---|---|---|---|
| sphingosine 1-phosphate receptor 2 | Homo sapiens (human) | IC50 (µMol) | 8.5747 | 1.0810 | 2.6352 | 4.7700 | AID851; AID856 |
| BZLF2 | Human herpesvirus 4 type 2 (Epstein-Barr virus type 2) | IC50 (µMol) | 6.0500 | 0.4200 | 4.4342 | 16.2300 | AID1419 |
| [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) |
|---|---|---|---|---|---|---|---|
| streptokinase A precursor | Streptococcus pyogenes M1 GAS | EC50 (µMol) | 1.4465 | 0.0600 | 8.9128 | 130.5170 | AID1902; AID1914 |
| Estrogen receptor | Rattus norvegicus (Norway rat) | EC50 (µMol) | 1.5300 | 0.0060 | 22.3670 | 130.5170 | AID1914 |
| Estrogen receptor beta | Rattus norvegicus (Norway rat) | EC50 (µMol) | 1.5300 | 0.0060 | 22.3670 | 130.5170 | AID1914 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
Biological Processes (5)
| Process | via Protein(s) | Taxonomy |
|---|---|---|
| negative regulation of inflammatory response to antigenic stimulus | Guanine nucleotide-binding protein G | Homo sapiens (human) |
| renal water homeostasis | Guanine nucleotide-binding protein G | Homo sapiens (human) |
| G protein-coupled receptor signaling pathway | Guanine nucleotide-binding protein G | Homo sapiens (human) |
| regulation of insulin secretion | Guanine nucleotide-binding protein G | Homo sapiens (human) |
| cellular response to glucagon stimulus | Guanine nucleotide-binding protein G | Homo sapiens (human) |
| [Information is prepared from geneontology information from the June-17-2024 release] | ||
Molecular Functions (2)
| Process | via Protein(s) | Taxonomy |
|---|---|---|
| G protein activity | Guanine nucleotide-binding protein G | Homo sapiens (human) |
| adenylate cyclase activator activity | Guanine nucleotide-binding protein G | Homo sapiens (human) |
| [Information is prepared from geneontology information from the June-17-2024 release] | ||
Ceullar Components (1)
| Process | via Protein(s) | Taxonomy |
|---|---|---|
| plasma membrane | Guanine nucleotide-binding protein G | Homo sapiens (human) |
| [Information is prepared from geneontology information from the June-17-2024 release] | ||
Bioassays (13)
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| 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. |
| AID1745845 | Primary qHTS for Inhibitors of ATXN expression | |||
| 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. |
| 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. |
| AID651635 | Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression | |||
| 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. |
| 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. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||||
Research
Studies (5)
| Timeframe | Studies, This Drug (%) | All Drugs % |
|---|---|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 0 (0.00) | 18.2507 |
| 2000's | 1 (20.00) | 29.6817 |
| 2010's | 3 (60.00) | 24.3611 |
| 2020's | 1 (20.00) | 2.80 |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||
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 | 5 (100.00%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||