UK-356,202: structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]
| ID Source | ID |
|---|---|
| PubMed CID | 9885167 |
| CHEMBL ID | 111576 |
| SCHEMBL ID | 6437325 |
| MeSH ID | M0534894 |
| Synonym |
|---|
| 3-(4-chloro-1-guanidino-isoquinolin-7-yl)-benzoic acid |
| bdbm50147422 |
| uk-356202 |
| 1-isoquinolinylguanidine 3 |
| bdbm16129 |
| 3-{4-chloro-1-[(diaminomethylidene)amino]isoquinolin-7-yl}benzoic acid |
| 3-[4-chloro-1-(diaminomethylideneamino)isoquinolin-7-yl]benzoic acid |
| CHEMBL111576 , |
| AKOS015966399 |
| uk-356,202 |
| compound 13j [pmid: 15149680] |
| gtpl6543 |
| SCHEMBL6437325 |
| DTXSID40432402 |
| 223671-94-1 |
| 3-(4-chloro-1-guanidinoisoquinolin-7-yl)benzoic acid |
| Q27089077 |
| Excerpt | Reference | Relevance |
|---|---|---|
| " Subsequent optimization led to 15, a potent, selective, and orally bioavailable inhibitor of uPA." | ( Fragment-based discovery of mexiletine derivatives as orally bioavailable inhibitors of urokinase-type plasminogen activator. Callaghan, O; Chessari, G; Congreve, M; Cowan, SR; Frederickson, M; Matthews, JE; McMenamin, R; Smith, DM; Vinković, M; Wallis, NG, 2008) | 0.35 |
| Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| Plasminogen | Homo sapiens (human) | Ki | 0.0170 | 0.0170 | 1.1560 | 4.4000 | AID1797470 |
| Urokinase-type plasminogen activator | Homo sapiens (human) | IC50 (µMol) | 0.0370 | 0.0370 | 3.3859 | 10.0000 | AID312586 |
| Urokinase-type plasminogen activator | Homo sapiens (human) | Ki | 0.0303 | 0.0170 | 2.6268 | 7.0000 | AID1265737; AID1797470; AID215979 |
| Tissue-type plasminogen activator | Homo sapiens (human) | Ki | 0.0170 | 0.0170 | 3.7196 | 8.6000 | AID1797470 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| AID312586 | Inhibition of uPA | 2008 | Journal of medicinal chemistry, Jan-24, Volume: 51, Issue:2 | Fragment-based discovery of mexiletine derivatives as orally bioavailable inhibitors of urokinase-type plasminogen activator. |
| AID215979 | Inhibitory activity against human urokinase-type plasminogen activator was evaluated using S-2444 as substrate | 2004 | Bioorganic & medicinal chemistry letters, Jun-21, Volume: 14, Issue:12 | Selective urokinase-type plasminogen activator (uPA) inhibitors. Part 3: 1-isoquinolinylguanidines. |
| AID210746 | Inhibitory activity against human tissue type plasminogen activator was evaluated using S-2444 as substrate and tissue plasminogen activator stimulator at 100 mM | 2004 | Bioorganic & medicinal chemistry letters, Jun-21, Volume: 14, Issue:12 | Selective urokinase-type plasminogen activator (uPA) inhibitors. Part 3: 1-isoquinolinylguanidines. |
| AID157835 | Inhibitory activity against human plasmin was evaluated using chromozym-PL as substrate at 10 uM | 2004 | Bioorganic & medicinal chemistry letters, Jun-21, Volume: 14, Issue:12 | Selective urokinase-type plasminogen activator (uPA) inhibitors. Part 3: 1-isoquinolinylguanidines. |
| AID1265737 | Inhibition of human uPA using S-2444 as substrate | 2015 | Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23 | Discovery and SAR of Novel and Selective Inhibitors of Urokinase Plasminogen Activator (uPA) with an Imidazo[1,2-a]pyridine Scaffold. |
| AID1797470 | Determination of Inhibitor Potency and Selectivity from Article 10.1021/jm061066t: \\Selective Urokinase-Type Plasminogen Activator Inhibitors. 4. 1-(7-Sulfonamidoisoquinolinyl)guanidines.\\ | 2007 | Journal of medicinal chemistry, May-17, Volume: 50, Issue:10 | Selective urokinase-type plasminogen activator inhibitors. 4. 1-(7-sulfonamidoisoquinolinyl)guanidines. |
| [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 | 4 (80.00) | 29.6817 |
| 2010's | 1 (20.00) | 24.3611 |
| 2020's | 0 (0.00) | 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 (12.50) 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 | 5 (100.00%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||