Page last updated: 2024-12-11
a 286982
Description
Research Excerpts
Clinical Trials
Roles
Classes
Pathways
Study Profile
Bioassays
Related Drugs
Related Conditions
Protein Interactions
Research Growth
Market Indicators
Description
A 286982: inhibits the interaction between leukocyte function-associated antigen-1 and intracellular adhesion molecule-1; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]
Cross-References
| ID Source | ID |
|---|---|
| PubMed CID | 9846729 |
| CHEMBL ID | 19677 |
| SCHEMBL ID | 5829786 |
| SCHEMBL ID | 12063498 |
| MeSH ID | M0372587 |
Synonyms (34)
| Synonym |
|---|
| 1-(4-acetylpiperazin-1-yl)-3-(4-(2-isopropylphenylthio)-3-nitrophenyl)prop-2-en-1-one |
| 1-(4-acetyl-piperazin-1-yl)-3-[4-(2-isopropyl-phenylsulfanyl)-3-nitro-phenyl]-propenone |
| bdbm50092956 |
| CHEMBL19677 , |
| a-286982 |
| gtpl6592 |
| (e)-1-(4-acetylpiperazin-1-yl)-3-[3-nitro-4-(2-propan-2-ylphenyl)sulfanylphenyl]prop-2-en-1-one |
| a286982 |
| 2-propen-1-one, 1-(4-acetyl-1-piperazinyl)-3-(4-((2-(1-methylethyl)phenyl)thio)-3-nitrophenyl)- |
| 2-isopropylphenyl 2-nitro-4-(((4-acetylpiperazin-1-yl)carbonyl)ethenyl)phenyl sulfide |
| piperazine, 1-acetyl-4-((2e)-3-(4-((2-(1-methylethyl)phenyl)thio)-3-nitrophenyl)-1-oxo-2-propenyl)- |
| a-286,982 |
| a 286982 |
| 2-propen-1-one, 1-(4-acetyl-1-piperazinyl)-3-(4-((2-(1-methylethyl)phenyl)thio)-3-nitrophenyl)-, (2e)- |
| unii-5i8wfs075a |
| 280749-17-9 |
| 5i8wfs075a , |
| a 286,982 |
| SCHEMBL5829786 |
| SCHEMBL12063498 |
| (2e)-1-(4-acetyl-1-piperazinyl)-3-[4-[[2-(1-methylethyl)phenyl]thio]-3-nitrophenyl]-2-propen-1-one |
| AKOS024458044 |
| J-016962 |
| Q27074059 |
| AS-16426 |
| A899560 |
| HY-107587 |
| EX-A4719 |
| CS-0028915 |
| (e)-1-(4-acetylpiperazin-1-yl)-3-(4-((2-isopropylphenyl)thio)-3-nitrophenyl)prop-2-en-1-one |
| DTXSID601328277 |
| AC-36582 |
| F77491 |
| Z2607847156 |
Research Excerpts
Bioavailability
| Excerpt | Reference | Relevance |
|---|---|---|
| " In addition to excellent in vitro potency, 6q shows good pharmacokinetic properties and its ethyl ester (6t) demonstrates good oral bioavailability in both mouse and rat." | ( Discovery of tetrahydroisoquinoline (THIQ) derivatives as potent and orally bioavailable LFA-1/ICAM-1 antagonists. Arbitrario, JP; Arkin, MR; Barr, KJ; Bui, M; Chen, T; Cunningham, BC; Evanchik, MJ; Flanagan, WM; Hanan, EJ; Hoch, U; Huen, K; Hyde, J; Kumer, JL; Lac, T; Lawrence, CE; Martell, JR; Oslob, JD; Paulvannan, K; Prabhu, S; Shen, W; Silverman, JA; Wright, J; Yu, CH; Zhong, M; Zhu, J, 2010) | 0.36 |
| "Many lead compounds fail to reach clinical trials despite being potent because of low bioavailability attributed to their insufficient solubility making solubility a primary and crucial factor in early phase drug discovery." | ( Structural modification aimed for improving solubility of lead compounds in early phase drug discovery. Baidya, ATK; Das, B; Kumar, R; Mathew, AT; Yadav, AK, 2022) | 0.72 |
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
Protein Targets (3)
Inhibition Measurements
| Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| Integrin beta-2 | Homo sapiens (human) | IC50 (µMol) | 0.0412 | 0.0008 | 0.5905 | 3.7800 | AID100087; AID181507; AID501388; AID94613; AID99583 |
| Intercellular adhesion molecule 1 | Homo sapiens (human) | IC50 (µMol) | 0.0402 | 0.0030 | 1.2122 | 10.0000 | AID100087; AID181507; AID501388; AID94613; AID94747; AID99583 |
| Integrin alpha-L | Homo sapiens (human) | IC50 (µMol) | 0.0417 | 0.0008 | 0.6020 | 3.7800 | AID100087; AID181507; AID501388; AID91750; AID94613; AID99583 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
Biological Processes (51)
Molecular Functions (13)
Ceullar Components (20)
Bioassays (23)
Research
Studies (7)
| Timeframe | Studies, This Drug (%) | All Drugs % |
|---|---|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 0 (0.00) | 18.2507 |
| 2000's | 4 (57.14) | 29.6817 |
| 2010's | 2 (28.57) | 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] | ||
Market Indicators
Research Demand Index: 12.93
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 (12.93) All Compounds (24.57) |
Study Types
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 0 (0.00%) | 5.53% |
| Reviews | 2 (28.57%) | 6.00% |
| Case Studies | 0 (0.00%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 5 (71.43%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||