| ID Source | ID |
|---|---|
| PubMed CID | 5311139 |
| CHEMBL ID | 37630 |
| SCHEMBL ID | 4349143 |
| MeSH ID | M0253747 |
| Synonym |
|---|
| ac-tyr-val-ala-asp-aldehyde |
| ac-yvad-cho |
| chembl37630 , |
| bdbm10355 |
| (3s)-3-[(2s)-2-[(2s)-2-[(2s)-2-acetamido-3-(4-hydroxyphenyl)propanamido]-3-methylbutanamido]propanamido]-4-oxobutanoic acid |
| caspase-1 inhibitor i |
| l-709049 |
| (s)-n-acetyl-l-tyrosyl-l-valyl-n-(2-carboxy-1-formylethyl)-l-alaninamide |
| l 709,049 |
| ycad-cho |
| n-acetyltyrosyl-valyl-alanyl-aspartyl aldehyde |
| l-alaninamide, n-acetyl-l-tyrosyl-l-valyl-n-(2-carboxy-1-formylethyl)-, (s)- |
| l-709,049 |
| acetyl-tyrosyl-valyl-alanyl-aspartinal |
| NCGC00167338-01 |
| SCHEMBL4349143 |
| (3s)-3-[[(2s)-2-[[(2s)-2-[[(2s)-2-acetamido-3-(4-hydroxyphenyl)propanoyl]amino]-3-methylbutanoyl]amino]propanoyl]amino]-4-oxobutanoic acid |
| acetyl-tyrosyl-valyl-alanyl-aspartal |
| nvf6uyc3cm , |
| unii-nvf6uyc3cm |
| mfcd00237123 |
| J-007797 |
| (4s,7s,10s,13s)-13-formyl-4-(4-hydroxybenzyl)-7-isopropyl-10-methyl-2,5,8,11-tetraoxo-3,6,9,12-tetraazapentadecan-15-oic acid |
| caspase-1 inhibitor i - cas 143313-51-3 |
| ac-tyr-val-ala-asp-h |
| acetyl-tyr-val-ala-asp-aldehyde |
| n-acetyl-tyr-val-ala-asp-aldehyde |
| n-acetyl-tyr-val-ala-asp aldehyde |
| HY-120019 |
| n-acetyl-l-tyrosyl-l-valyl-n-((1s)-2-carboxy-1-formylethyl)-l-alaninamide |
| CS-0068866 |
| n-ac-tyr-val-ala-asp-cho |
| AKOS040744457 |
| Protein | Taxonomy | Measurement | Average (µ) | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| DNA polymerase kappa isoform 1 | Homo sapiens (human) | Potency | 23.7781 | 0.0316 | 22.3146 | 100.0000 | AID588579 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
| Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| Interleukin-1 beta | Homo sapiens (human) | IC50 (µMol) | 2.0000 | 2.0000 | 3.2000 | 4.4000 | AID627038 |
| Caspase-1 | Mus musculus (house mouse) | Ki | 0.0090 | 0.0090 | 0.0120 | 0.0150 | AID501506 |
| Caspase-1 | Homo sapiens (human) | IC50 (µMol) | 11.3417 | 0.0020 | 1.7013 | 8.8000 | AID1796431; AID1799017; AID415376; AID501505; AID591188; AID93667 |
| Caspase-1 | Homo sapiens (human) | Ki | 0.0007 | 0.0002 | 0.0063 | 0.0180 | AID501505 |
| Caspase-3 | Homo sapiens (human) | IC50 (µMol) | 63.3388 | 0.0002 | 1.1979 | 8.8000 | AID1796431; AID1799017; AID49509 |
| Caspase-7 | Homo sapiens (human) | IC50 (µMol) | 0.0082 | 0.0022 | 0.5477 | 5.0000 | AID1796431; AID1799017 |
| Caspase-6 | Homo sapiens (human) | IC50 (µMol) | 0.0082 | 0.0022 | 0.8652 | 5.0000 | AID1796431; AID1799017 |
| Caspase-8 | Homo sapiens (human) | IC50 (µMol) | 0.0082 | 0.0022 | 0.6845 | 5.0000 | AID1796431; AID1799017 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| AID501508 | Inhibition of LPS-induced IL1-beta production in human PBMC by ELISA | 2010 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 20, Issue:17 | Succinic acid amides as P2-P3 replacements for inhibitors of interleukin-1beta converting enzyme (ICE or caspase 1). |
| AID501515 | Selectivity ratio of human ICE to caspase 6 | 2010 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 20, Issue:17 | Succinic acid amides as P2-P3 replacements for inhibitors of interleukin-1beta converting enzyme (ICE or caspase 1). |
| AID501513 | Selectivity ratio of human ICE to caspase 3 | 2010 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 20, Issue:17 | Succinic acid amides as P2-P3 replacements for inhibitors of interleukin-1beta converting enzyme (ICE or caspase 1). |
| AID501505 | Inhibition of human ICE | 2010 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 20, Issue:17 | Succinic acid amides as P2-P3 replacements for inhibitors of interleukin-1beta converting enzyme (ICE or caspase 1). |
| AID501507 | Selectivity ratio of Ki for mouse ICE to Ki for human ICE | 2010 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 20, Issue:17 | Succinic acid amides as P2-P3 replacements for inhibitors of interleukin-1beta converting enzyme (ICE or caspase 1). |
| AID93665 | Ability to inhibit IL-1 beta converting enzyme was evaluated in LPS-stimulated human whole blood | 1998 | Bioorganic & medicinal chemistry letters, Jun-16, Volume: 8, Issue:12 | Peptidyl beta-homo-aspartals: specific inhibitors of interleukin-1 beta converting enzyme and its homologues (caspases). |
| AID415376 | Inhibition of human recombinant caspase 1 assessed as accumulation of fluorogenic product by fluorometric assay | 2009 | Journal of medicinal chemistry, Apr-23, Volume: 52, Issue:8 | Synthesis and in vitro evaluation of sulfonamide isatin Michael acceptors as small molecule inhibitors of caspase-6. |
| AID501514 | Selectivity ratio of human ICE to caspase 4 | 2010 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 20, Issue:17 | Succinic acid amides as P2-P3 replacements for inhibitors of interleukin-1beta converting enzyme (ICE or caspase 1). |
| AID49509 | Amidolytic activity of THP.1 cell lysate against Caspase-3 using C3-Asp-AMC as a substrate | 1998 | Bioorganic & medicinal chemistry letters, Jun-16, Volume: 8, Issue:12 | Peptidyl beta-homo-aspartals: specific inhibitors of interleukin-1 beta converting enzyme and its homologues (caspases). |
| AID501516 | Selectivity ratio of human ICE to caspase 8 | 2010 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 20, Issue:17 | Succinic acid amides as P2-P3 replacements for inhibitors of interleukin-1beta converting enzyme (ICE or caspase 1). |
| AID627037 | Inhibition of caspase1 in differentiated human THP-1 cells at 0.0005 ug/ml after 24 hrs by fluorometric assay | 2011 | Journal of natural products, Oct-28, Volume: 74, Issue:10 | Berkeleyones and related meroterpenes from a deep water acid mine waste fungus that inhibit the production of interleukin 1-β from induced inflammasomes. |
| AID93667 | Amidolytic activity of THP.1 cell lysate against IL-1 beta converting enzyme using C1-Asp-AMC as a substrate | 1998 | Bioorganic & medicinal chemistry letters, Jun-16, Volume: 8, Issue:12 | Peptidyl beta-homo-aspartals: specific inhibitors of interleukin-1 beta converting enzyme and its homologues (caspases). |
| AID501509 | Reduction of IL1-beta level in human PBMC cells xenografted SCID mouse at 3 mg/kg, iv after 2 hrs | 2010 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 20, Issue:17 | Succinic acid amides as P2-P3 replacements for inhibitors of interleukin-1beta converting enzyme (ICE or caspase 1). |
| AID501506 | Inhibition of mouse ICE | 2010 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 20, Issue:17 | Succinic acid amides as P2-P3 replacements for inhibitors of interleukin-1beta converting enzyme (ICE or caspase 1). |
| AID591188 | Inhibition of caspase 1 by fluorometric assay | 2011 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 21, Issue:8 | Synthesis and evaluation of isatin analogs as caspase-3 inhibitors: introduction of a hydrophilic group increases potency in a whole cell assay. |
| AID627038 | Induction of IL-1 beta production in LPS-induced human THP-1 cells by ELISA | 2011 | Journal of natural products, Oct-28, Volume: 74, Issue:10 | Berkeleyones and related meroterpenes from a deep water acid mine waste fungus that inhibit the production of interleukin 1-β from induced inflammasomes. |
| AID1799017 | Enzyme Inhibition Assay from Article 10.1021/jm900135r: \\Synthesis and in vitro evaluation of sulfonamide isatin Michael acceptors as small molecule inhibitors of caspase-6.\\ | 2009 | Journal of medicinal chemistry, Apr-23, Volume: 52, Issue:8 | Synthesis and in vitro evaluation of sulfonamide isatin Michael acceptors as small molecule inhibitors of caspase-6. |
| AID1796431 | Caspase Inhibition Assay from Article 10.1021/jm0506625: \\N-benzylisatin sulfonamide analogues as potent caspase-3 inhibitors: synthesis, in vitro activity, and molecular modeling studies.\\ | 2005 | Journal of medicinal chemistry, Dec-01, Volume: 48, Issue:24 | N-benzylisatin sulfonamide analogues as potent caspase-3 inhibitors: synthesis, in vitro activity, and molecular modeling studies. |
| [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 | 1 (16.67) | 18.2507 |
| 2000's | 2 (33.33) | 29.6817 |
| 2010's | 3 (50.00) | 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 (12.79) 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 | 6 (100.00%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||