AK 295: a dipeptide alpha-ketoamide calpain inhibitor [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]
| ID Source | ID |
|---|---|
| PubMed CID | 183798 |
| CHEMBL ID | 1242959 |
| SCHEMBL ID | 12841026 |
| MeSH ID | M0238223 |
| Synonym |
|---|
| ak 295 |
| benzyl n-[(2s)-4-methyl-1-[[1-(3-morpholin-4-ylpropylamino)-1,2-dioxopentan-3-yl]amino]-1-oxopentan-2-yl]carbamate |
| ak295 |
| carbamic acid, (1-(((1-ethyl-3-((3-(4-morpholinyl)propyl)amino)-2,3-dioxopropyl)amino)carbonyl)-3-methylbutyl)-, phenylmethyl ester, stereoisomer |
| cx 295 |
| cx-295 |
| ak-295 |
| z-leu-aminobutyric acid-conh(ch2)3-morpholine |
| cbz-leu-aminobutyrate-conh(ch2)3-morpholine |
| cbz-leu-abu-conh(ch2)3-mpl |
| carbamic acid, ((1s)-1-(((1-ethyl-3-((3-(4-morpholinyl)propyl)amino)-2,3-dioxopropyl)amino)carbonyl)-3-methylbutyl)-, phenylmethyl ester |
| cx295 cpd |
| 160399-35-9 |
| CHEMBL1242959 |
| SCHEMBL12841026 |
| DTXSID60936290 |
| 2-{[(benzyloxy)(hydroxy)methylidene]amino}-4-methyl-n-(1-{[3-(morpholin-4-yl)propyl]amino}-1,2-dioxopentan-3-yl)pentanimidic acid |
| AKOS040746510 |
| Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| Cathepsin B | Homo sapiens (human) | Ki | 6.9000 | 0.0000 | 1.2180 | 8.6000 | AID512111 |
| Calpain-1 catalytic subunit | Sus scrofa (pig) | Ki | 0.1500 | 0.0100 | 0.8640 | 3.9600 | AID512109 |
| Calpain-2 catalytic subunit | Sus scrofa (pig) | Ki | 0.0410 | 0.0410 | 0.0410 | 0.0410 | AID512110 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
| Process | via Protein(s) | Taxonomy |
|---|---|---|
| proteolysis | Cathepsin B | Homo sapiens (human) |
| thyroid hormone generation | Cathepsin B | Homo sapiens (human) |
| collagen catabolic process | Cathepsin B | Homo sapiens (human) |
| epithelial cell differentiation | Cathepsin B | Homo sapiens (human) |
| regulation of apoptotic process | Cathepsin B | Homo sapiens (human) |
| decidualization | Cathepsin B | Homo sapiens (human) |
| symbiont entry into host cell | Cathepsin B | Homo sapiens (human) |
| proteolysis involved in protein catabolic process | Cathepsin B | Homo sapiens (human) |
| cellular response to thyroid hormone stimulus | Cathepsin B | Homo sapiens (human) |
| [Information is prepared from geneontology information from the June-17-2024 release] | ||
| Process | via Protein(s) | Taxonomy |
|---|---|---|
| cysteine-type endopeptidase activity | Cathepsin B | Homo sapiens (human) |
| protein binding | Cathepsin B | Homo sapiens (human) |
| collagen binding | Cathepsin B | Homo sapiens (human) |
| peptidase activity | Cathepsin B | Homo sapiens (human) |
| cysteine-type peptidase activity | Cathepsin B | Homo sapiens (human) |
| proteoglycan binding | Cathepsin B | Homo sapiens (human) |
| [Information is prepared from geneontology information from the June-17-2024 release] | ||
| Process | via Protein(s) | Taxonomy |
|---|---|---|
| collagen-containing extracellular matrix | Cathepsin B | Homo sapiens (human) |
| extracellular region | Cathepsin B | Homo sapiens (human) |
| extracellular space | Cathepsin B | Homo sapiens (human) |
| lysosome | Cathepsin B | Homo sapiens (human) |
| external side of plasma membrane | Cathepsin B | Homo sapiens (human) |
| apical plasma membrane | Cathepsin B | Homo sapiens (human) |
| endolysosome lumen | Cathepsin B | Homo sapiens (human) |
| melanosome | Cathepsin B | Homo sapiens (human) |
| perinuclear region of cytoplasm | Cathepsin B | Homo sapiens (human) |
| collagen-containing extracellular matrix | Cathepsin B | Homo sapiens (human) |
| extracellular exosome | Cathepsin B | Homo sapiens (human) |
| peptidase inhibitor complex | Cathepsin B | Homo sapiens (human) |
| ficolin-1-rich granule lumen | Cathepsin B | Homo sapiens (human) |
| extracellular space | Cathepsin B | Homo sapiens (human) |
| lysosome | Cathepsin B | Homo sapiens (human) |
| [Information is prepared from geneontology information from the June-17-2024 release] | ||
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| AID512118 | Drug level in C57BL/6 mouse spleen at 24 mg/kg, sc after 1 hr by HPLC analysis | 2010 | Journal of medicinal chemistry, Sep-09, Volume: 53, Issue:17 | Peptidyl alpha-ketoamides with nucleobases, methylpiperazine, and dimethylaminoalkyl substituents as calpain inhibitors. |
| AID512121 | Drug level in C57BL/6 mouse liver at 24 mg/kg, iv after 1 hr by HPLC analysis | 2010 | Journal of medicinal chemistry, Sep-09, Volume: 53, Issue:17 | Peptidyl alpha-ketoamides with nucleobases, methylpiperazine, and dimethylaminoalkyl substituents as calpain inhibitors. |
| AID512111 | Inhibition of human liver cathepsin B | 2010 | Journal of medicinal chemistry, Sep-09, Volume: 53, Issue:17 | Peptidyl alpha-ketoamides with nucleobases, methylpiperazine, and dimethylaminoalkyl substituents as calpain inhibitors. |
| AID512120 | Drug level in C57BL/6 mouse kidney at 24 mg/kg, iv after 1 hr by HPLC analysis | 2010 | Journal of medicinal chemistry, Sep-09, Volume: 53, Issue:17 | Peptidyl alpha-ketoamides with nucleobases, methylpiperazine, and dimethylaminoalkyl substituents as calpain inhibitors. |
| AID512115 | Drug level in C57BL/6 mouse kidney at 24 mg/kg, sc after 1 hr by HPLC analysis | 2010 | Journal of medicinal chemistry, Sep-09, Volume: 53, Issue:17 | Peptidyl alpha-ketoamides with nucleobases, methylpiperazine, and dimethylaminoalkyl substituents as calpain inhibitors. |
| AID512109 | Inhibition of porcine erythrocyte calpain 1 | 2010 | Journal of medicinal chemistry, Sep-09, Volume: 53, Issue:17 | Peptidyl alpha-ketoamides with nucleobases, methylpiperazine, and dimethylaminoalkyl substituents as calpain inhibitors. |
| AID512122 | Drug level in C57BL/6 mouse peripheral nerve at 24 mg/kg, iv after 1 hr by HPLC analysis | 2010 | Journal of medicinal chemistry, Sep-09, Volume: 53, Issue:17 | Peptidyl alpha-ketoamides with nucleobases, methylpiperazine, and dimethylaminoalkyl substituents as calpain inhibitors. |
| AID512119 | Drug level in C57BL/6 mouse heart at 24 mg/kg, iv after 1 hr by HPLC analysis | 2010 | Journal of medicinal chemistry, Sep-09, Volume: 53, Issue:17 | Peptidyl alpha-ketoamides with nucleobases, methylpiperazine, and dimethylaminoalkyl substituents as calpain inhibitors. |
| AID512110 | Inhibition of porcine kidney calpain 2 | 2010 | Journal of medicinal chemistry, Sep-09, Volume: 53, Issue:17 | Peptidyl alpha-ketoamides with nucleobases, methylpiperazine, and dimethylaminoalkyl substituents as calpain inhibitors. |
| AID512117 | Drug level in C57BL/6 mouse serum at 24 mg/kg, sc after 1 hr by HPLC analysis | 2010 | Journal of medicinal chemistry, Sep-09, Volume: 53, Issue:17 | Peptidyl alpha-ketoamides with nucleobases, methylpiperazine, and dimethylaminoalkyl substituents as calpain inhibitors. |
| AID512114 | Drug level in C57BL/6 mouse heart at 24 mg/kg, sc after 1 hr by HPLC analysis | 2010 | Journal of medicinal chemistry, Sep-09, Volume: 53, Issue:17 | Peptidyl alpha-ketoamides with nucleobases, methylpiperazine, and dimethylaminoalkyl substituents as calpain inhibitors. |
| AID512112 | Selectivity ratio of Ki for porcine erythrocyte calpain 1 to Ki for human liver cathepsin B | 2010 | Journal of medicinal chemistry, Sep-09, Volume: 53, Issue:17 | Peptidyl alpha-ketoamides with nucleobases, methylpiperazine, and dimethylaminoalkyl substituents as calpain inhibitors. |
| AID512116 | Drug level in C57BL/6 mouse liver at 24 mg/kg, sc after 1 hr by HPLC analysis | 2010 | Journal of medicinal chemistry, Sep-09, Volume: 53, Issue:17 | Peptidyl alpha-ketoamides with nucleobases, methylpiperazine, and dimethylaminoalkyl substituents as calpain inhibitors. |
| AID512123 | Drug level in C57BL/6 mouse spleen at 24 mg/kg, iv after 1 hr by HPLC analysis | 2010 | Journal of medicinal chemistry, Sep-09, Volume: 53, Issue:17 | Peptidyl alpha-ketoamides with nucleobases, methylpiperazine, and dimethylaminoalkyl substituents as calpain inhibitors. |
| [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 | 5 (38.46) | 18.2507 |
| 2000's | 7 (53.85) | 29.6817 |
| 2010's | 1 (7.69) | 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 strong demand-to-supply ratio for research on this compound.
| This Compound (47.74) 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 | 13 (100.00%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||