actinoplanic acid A: isolated from Actinoplanes; inhibits farnesyl-protein transferase; structure in first source [MeSH]
| ID Source | ID |
|---|---|
| PubMed CID | 10102380 |
| CHEMBL ID | 100684 |
| SCHEMBL ID | 8909241 |
| MeSH ID | M0252887 |
| Synonym |
|---|
| CHEMBL100684 , |
| actinoplanic acid a |
| 3-carboxy-pentanedioic acid mono-{(e)-10-[(14e,18z)-4-carboxy-19-(6-carboxy-4-ethyl-3-oxo-heptyl)-12-hydroxy-11,13,15,17-tetramethyl-2,6-dioxo-1,7dioxa-cycloicosa-14,18-dien-8-yl]-1,4-dimethyl-dec-5-enyl} ester |
| bdbm50059873 |
| SCHEMBL8909241 |
| 2-[2-[(e)-11-[(14e,18z)-4-carboxy-19-(6-carboxy-4-ethyl-3-oxoheptyl)-12-hydroxy-11,13,15,17-tetramethyl-2,6-dioxo-1,7-dioxacycloicosa-14,18-dien-8-yl]-5-methylundec-6-en-2-yl]oxy-2-oxoethyl]butanedioic acid |
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) |
|---|---|---|---|---|
| Protein farnesyltransferase/geranylgeranyltransferase type-1 subunit alpha | Homo sapiens (human) | IC50 | 0.2300 | AID73120 |
| Protein farnesyltransferase subunit beta | Homo sapiens (human) | IC50 | 0.2300 | AID73120 |
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| AID73120 | Activity against human Farnesyltransferase | 1997 | Journal of medicinal chemistry, Sep-12, Volume: 40, Issue:19 ISSN: 0022-2623 | Ras farnesyltransferase: a new therapeutic target. |
| AID1712055 | Inhibition of recombinant human FTase | 2016 | Bioorganic & medicinal chemistry, 07-15, Volume: 24, Issue:14 ISSN: 1464-3391 | Discovery and preliminary structure-activity relationship studies on tecomaquinone I and tectol as novel farnesyltransferase and plasmodial inhibitors. |
| Timeframe | Studies, This Drug (%) | All Drugs % |
|---|---|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 1 (25.00) | 18.2507 |
| 2000's | 0 (0.00) | 29.6817 |
| 2010's | 3 (75.00) | 24.3611 |
| 2020's | 0 (0.00) | 2.80 |
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 0 (0.00%) | 5.53% |
| Reviews | 1 (20.00%) | 6.00% |
| Case Studies | 0 (0.00%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 4 (80.00%) | 84.16% |
| Substance | Studies | Classes | Roles | First Year | Last Year | Average Age | Relationship Strength | Trials | pre-1990 | 1990's | 2000's | 2010's | post-2020 |
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| gliotoxin | dipeptide; organic disulfide; organic heterotetracyclic compound; pyrazinoindole | antifungal agent; EC 2.5.1.58 (protein farnesyltransferase) inhibitor; immunosuppressive agent; mycotoxin; proteasome inhibitor | 1997 | 1997 | 27.0 | medium | 0 | 0 | 1 | 0 | 0 | 0 | |
| b 581 | dipeptide | EC 2.5.1.58 (protein farnesyltransferase) inhibitor; peptidomimetic | 1997 | 1997 | 27.0 | high | 0 | 0 | 1 | 0 | 0 | 0 | |
| chaetomellic acid a | 1997 | 2016 | 17.5 | high | 0 | 0 | 1 | 0 | 1 | 0 | |||
| sch 44342 | 1997 | 1997 | 27.0 | high | 0 | 0 | 1 | 0 | 0 | 0 |
| Substance | Studies | Classes | Roles | First Year | Last Year | Average Age | Relationship Strength | Trials | pre-1990 | 1990's | 2000's | 2010's | post-2020 |
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| sirolimus | antibiotic antifungal drug; cyclic acetal; cyclic ketone; ether; macrolide lactam; organic heterotricyclic compound; secondary alcohol | antibacterial drug; anticoronaviral agent; antineoplastic agent; bacterial metabolite; geroprotector; immunosuppressive agent; mTOR inhibitor | 2018 | 2018 | 6.0 | high | 0 | 0 | 0 | 0 | 2 | 0 |
| Condition | Indicated | Studies | First Year | Last Year | Average Age | Relationship Strength | Trials | pre-1990 | 1990's | 2000's | 2010's | post-2020 |
|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Benign Neoplasms | 0 | 1997 | 1997 | 27.0 | high | 0 | 0 | 1 | 0 | 0 | 0 | |
| Neoplasms | 0 | 1997 | 1997 | 27.0 | high | 0 | 0 | 1 | 0 | 0 | 0 |