ABT 299: converted in vivo to A-85783.0; a platelet activating factor antagonist; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]
| ID Source | ID |
|---|---|
| PubMed CID | 9830503 |
| CHEMBL ID | 317090 |
| MeSH ID | M0246116 |
| Synonym |
|---|
| abt-299 |
| CHEMBL317090 , |
| [3-[(3r)-7-[1-(dimethylcarbamoyl)-6-(4-fluorophenyl)indole-3-carbonyl]-1,3-dihydropyrrolo[1,2-c][1,3]thiazol-3-yl]pyridin-1-ium-1-yl]methyl acetate chloride |
| abt299 |
| gtpl1849 |
| abt 299 |
| unii-742qgp819q |
| 742QGP819Q , |
| 161395-35-3 |
| pyridinium, 1-((acetyloxy)methyl)-3-((3r)-7-((1-((dimethylamino)carbonyl)-6-(4-fluorophenyl)-1h-indol-3-yl)carbonyl)-1h,3h-pyrrolo(1,2-c)thiazol-3-yl)-, chloride (1:1) |
| Q27074121 |
| [3-[(3r)-7-[1-(dimethylcarbamoyl)-6-(4-fluorophenyl)indole-3-carbonyl]-1,3-dihydropyrrolo[1,2-c][1,3]thiazol-3-yl]pyridin-1-ium-1-yl]methyl acetate;chloride |
| AKOS040747742 |
| Excerpt | Relevance | Reference |
|---|---|---|
| "Peripheral blood taken over 12 h after dosing was used for ex vivo beta-TG release and, in the case of the 70 mg dose, measurement of plasma drug concentration." | ( Ex vivo inhibition of beta-thromboglobulin release following administration to man of ABT-299, a novel prodrug of a potent platelet activating factor antagonist. Albert, DH; Carter, GW; Kleinert, HD; Magoc, TJ; Menacherry, SD; Morgan, DW; Reyes, AE; Summers, JB; Sun, E, 1997) | 0.3 |
| Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| Platelet-activating factor receptor | Cavia porcellus (domestic guinea pig) | Ki | 0.0038 | 0.0004 | 0.3386 | 3.2500 | AID161089 |
| Platelet-activating factor receptor | Homo sapiens (human) | Ki | 0.0010 | 0.0002 | 0.5376 | 2.2700 | AID161085 |
| [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 |
|---|---|---|---|---|
| AID18641 | The compound was evaluated for its bioavailability in monkey | 1998 | Journal of medicinal chemistry, Jan-01, Volume: 41, Issue:1 | Discovery and evaluation of a series of 3-acylindole imidazopyridine platelet-activating factor antagonists. |
| AID161089 | The compound was evaluated for its binding affinity against PAF receptor in rabbit platelet | 1998 | Journal of medicinal chemistry, Jan-01, Volume: 41, Issue:1 | Discovery and evaluation of a series of 3-acylindole imidazopyridine platelet-activating factor antagonists. |
| AID180180 | The compound was evaluated for its PAF-induced vascular permeability in rat when dosed intravenously | 1998 | Journal of medicinal chemistry, Jan-01, Volume: 41, Issue:1 | Discovery and evaluation of a series of 3-acylindole imidazopyridine platelet-activating factor antagonists. |
| AID77408 | The compound was evaluated for its PAF-induced vascular permeability in guinea pig when dosed orally | 1998 | Journal of medicinal chemistry, Jan-01, Volume: 41, Issue:1 | Discovery and evaluation of a series of 3-acylindole imidazopyridine platelet-activating factor antagonists. |
| AID180181 | The compound was evaluated for its PAF-induced vascular permeability in rat when dosed orally | 1998 | Journal of medicinal chemistry, Jan-01, Volume: 41, Issue:1 | Discovery and evaluation of a series of 3-acylindole imidazopyridine platelet-activating factor antagonists. |
| AID21976 | The compound was evaluated for its solubility in lactate buffer at pH 3 | 1998 | Journal of medicinal chemistry, Jan-01, Volume: 41, Issue:1 | Discovery and evaluation of a series of 3-acylindole imidazopyridine platelet-activating factor antagonists. |
| AID24106 | The rate of hydrolytic cleavage in plasma was assessed by incubating compounds (30 uM) at 37 degrees Celsius with human plasma adjusted to pH 7 | 1994 | Journal of medicinal chemistry, Dec-23, Volume: 37, Issue:26 | N-(acyloxyalkyl)pyridinium salts as soluble prodrugs of a potent platelet activating factor antagonist. |
| AID161085 | The compound was evaluated for its binding affinity against PAF receptor in human platelet | 1998 | Journal of medicinal chemistry, Jan-01, Volume: 41, Issue:1 | Discovery and evaluation of a series of 3-acylindole imidazopyridine platelet-activating factor antagonists. |
| AID23173 | Half-life values were derived from the decay rate constant (k) by fitting the concentration and time values to the exponential decay function at pH 7 | 1994 | Journal of medicinal chemistry, Dec-23, Volume: 37, Issue:26 | N-(acyloxyalkyl)pyridinium salts as soluble prodrugs of a potent platelet activating factor antagonist. |
| AID77406 | The compound was evaluated for its PAF-induced vascular permeability in guinea pig when dosed intravenously | 1998 | Journal of medicinal chemistry, Jan-01, Volume: 41, Issue:1 | Discovery and evaluation of a series of 3-acylindole imidazopyridine platelet-activating factor antagonists. |
| AID18643 | The compound was evaluated for its bioavailability in rat | 1998 | Journal of medicinal chemistry, Jan-01, Volume: 41, Issue:1 | Discovery and evaluation of a series of 3-acylindole imidazopyridine platelet-activating factor antagonists. |
| AID1346403 | Human PAF receptor (Platelet-activating factor receptor) | 1996 | The Journal of pharmacology and experimental therapeutics, Jun, Volume: 277, Issue:3 | Properties of ABT-299, a prodrug of A-85783, a highly potent platelet activating factor receptor antagonist. |
| [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 | 9 (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] | ||
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 (11.96) All Compounds (24.57) |
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 2 (22.22%) | 5.53% |
| Reviews | 0 (0.00%) | 6.00% |
| Case Studies | 0 (0.00%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 7 (77.78%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||