Ro 24-4736: structure given in first source; platelet activating factor antagonist [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]
| ID Source | ID |
|---|---|
| PubMed CID | 60775 |
| CHEMBL ID | 277650 |
| SCHEMBL ID | 7528667 |
| MeSH ID | M0193802 |
| Synonym |
|---|
| ro 24-4736 |
| CHEMBL277650 , |
| 5-(3-(4-(2-chlorophenyl)-9-methyl-6h-thieno(3,2-f)(1,2,4)triazolo(4,3-a)(1,4)diazepin-2-yl)-2-propynyl)phenanthridin-6(5h)-one |
| ro-24-4736 |
| 125030-71-9 |
| bdbm50011638 |
| 5-{3-[4-(2-chloro-phenyl)-9-methyl-6h-1-thia-5,7,8,9a-tetraaza-cyclopenta[e]azulen-2-yl]-prop-2-ynyl}-5h-phenanthridin-6-one |
| SCHEMBL7528667 |
| i2mj13sofo , |
| 6(5h)-phenanthridinone, 5-(3-(4-(2-chlorophenyl)-9-methyl-6h-thieno(3,2-f)(1,2,4)triazolo(4,3-a)(1,4)diazepin-2-yl)-2-propynyl)- |
| unii-i2mj13sofo |
| DTXSID80154550 |
| HY-19097 |
| CS-6683 |
| 5-[3-[7-(2-chlorophenyl)-13-methyl-3-thia-1,8,11,12-tetrazatricyclo[8.3.0.02,6]trideca-2(6),4,7,10,12-pentaen-4-yl]prop-2-ynyl]phenanthridin-6-one |
| ro24-4736 |
| 6(5h)-phenanthridinone, 5-(3-(4-(2-chlorophenyl)-9-methyl-6h-thieno(3,2-f)(1,2,4)triazolo(4,3-a)(1,4)diazepin-2-yl)-2-propyn-1-yl)- |
| 5-(3-(4-(2-chlorophenyl)-9-methyl-6h-thieno(3,2-f)(1,2,4)triazolo(4,3-a)(1,4)-diazepin-2-yl)-2-propynyl)phenanthridin-6(5h)-one |
| ro-244736 |
| ro 244736 |
| AKOS040742561 |
| Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| Platelet-activating factor receptor | Homo sapiens (human) | IC50 (µMol) | 0.0130 | 0.0003 | 0.6318 | 3.7000 | AID59351 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
| Process | via Protein(s) | Taxonomy |
|---|---|---|
| lipopolysaccharide binding | Platelet-activating factor receptor | Homo sapiens (human) |
| lipopolysaccharide immune receptor activity | Platelet-activating factor receptor | Homo sapiens (human) |
| G protein-coupled receptor activity | Platelet-activating factor receptor | Homo sapiens (human) |
| platelet activating factor receptor activity | Platelet-activating factor receptor | Homo sapiens (human) |
| protein binding | Platelet-activating factor receptor | Homo sapiens (human) |
| phospholipid binding | Platelet-activating factor receptor | Homo sapiens (human) |
| mitogen-activated protein kinase binding | Platelet-activating factor receptor | Homo sapiens (human) |
| G protein-coupled purinergic nucleotide receptor activity | Platelet-activating factor receptor | Homo sapiens (human) |
| [Information is prepared from geneontology information from the June-17-2024 release] | ||
| Process | via Protein(s) | Taxonomy |
|---|---|---|
| plasma membrane | Platelet-activating factor receptor | Homo sapiens (human) |
| membrane | Platelet-activating factor receptor | Homo sapiens (human) |
| secretory granule membrane | Platelet-activating factor receptor | Homo sapiens (human) |
| tertiary granule membrane | Platelet-activating factor receptor | Homo sapiens (human) |
| [Information is prepared from geneontology information from the June-17-2024 release] | ||
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| AID76987 | Inhibition of PAF-induced bronchoconstriction in the guinea pig after intravenous administration | 1991 | Journal of medicinal chemistry, Mar, Volume: 34, Issue:3 | Triazolobenzo- and triazolothienodiazepines as potent antagonists of platelet activating factor. |
| AID77482 | Inhibitory activity at 0.03 mg/kg was determined against PAF-induced bronchoconstriction in guinea pig | 1991 | Journal of medicinal chemistry, Mar, Volume: 34, Issue:3 | Triazolobenzo- and triazolothienodiazepines as potent antagonists of platelet activating factor. |
| AID76854 | Inhibition of PAF-induced bronchoconstriction in guinea pig after oral administration after two-hour pretreatment time | 1991 | Journal of medicinal chemistry, Mar, Volume: 34, Issue:3 | Triazolobenzo- and triazolothienodiazepines as potent antagonists of platelet activating factor. |
| AID59351 | PAF-antagonist activity determined in dog platelets by PAF-binding assay | 1991 | Journal of medicinal chemistry, Mar, Volume: 34, Issue:3 | Triazolobenzo- and triazolothienodiazepines as potent antagonists of platelet activating factor. |
| [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 | 12 (100.00) | 18.2507 |
| 2000's | 0 (0.00) | 29.6817 |
| 2010's | 0 (0.00) | 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] | ||
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 1 (8.33%) | 5.53% |
| Reviews | 0 (0.00%) | 6.00% |
| Case Studies | 0 (0.00%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 11 (91.67%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||
| Article | Year |
|---|---|
| Pharmacology of a potent platelet-activating factor antagonist: Ro 24-4736. The Journal of pharmacology and experimental therapeutics, Volume: 259, Issue: 1 | 1991 |
| [information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | |
| Article | Year |
|---|---|
| Disposition and metabolism of Ro 24-4736 in the rat. Life sciences, Volume: 54, Issue: 26 | 1994 |
| [information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | |