variabilin: an RGD-containing antagonist of glycoprotein IIb-IIIa from the hard tick, Dermacentor variabilis; amino acid sequence given in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]
| ID Source | ID |
|---|---|
| PubMed CID | 54682873 |
| CHEMBL ID | 464276 |
| MeSH ID | M0264054 |
| Synonym |
|---|
| variabilin |
| CHEMBL464276 , |
| 7e,12e,20z-variabilin |
| (7e,12e,20z,18s)-variabilin |
| 2(5h)-furanone, 5-(13-(3-furanyl)-2,6,10-trimethyl-6,10-tridecadienylidene)-4-hydroxy-3-methyl- |
| nsc 227263 |
| 5-(13-(3-furanyl)-2,6,10-trimethyl-6,10-tridecadienylidene)-4-hydroxy-3-methyl-2(5h)-furanone |
| bdbm50232636 |
| Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| Receptor-type tyrosine-protein phosphatase C | Homo sapiens (human) | IC50 (µMol) | 1.2000 | 0.3000 | 2.7571 | 10.0000 | AID1430419 |
| Tyrosine-protein phosphatase non-receptor type 2 | Homo sapiens (human) | IC50 (µMol) | 0.8000 | 0.7000 | 4.5804 | 9.4500 | AID1430418 |
| Tyrosine-protein phosphatase non-receptor type 1 | Homo sapiens (human) | IC50 (µMol) | 1.5000 | 0.0005 | 3.4984 | 9.7600 | AID1430417 |
| Dual specificity protein phosphatase 3 | Homo sapiens (human) | IC50 (µMol) | 6.0000 | 4.0000 | 5.9750 | 8.5000 | AID1430420 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| AID474942 | Agonist activity at human recombinant alpha 1 GlyR expressed in HEK293 cells assessed as potentiation of glycine current by whole cell patch clamp assay | 2010 | Bioorganic & medicinal chemistry, Apr-15, Volume: 18, Issue:8 | Ircinialactams: subunit-selective glycine receptor modulators from Australian sponges of the family Irciniidae. |
| AID1430425 | Inhibition of PTP1B in human HuH7 cells assessed as reduction in insulin-stimulated Akt phosphorylation at 50 uM preincubated for 2 hrs followed by insulin stimulation for 5 mins by Western blot method | 2017 | Bioorganic & medicinal chemistry letters, 03-01, Volume: 27, Issue:5 | Furanoterpenes, new types of protein tyrosine phosphatase 1B inhibitors, from two Indonesian marine sponges, Ircinia and Spongia spp. |
| AID1430418 | Inhibition of full length recombinant N-terminal GST-tagged human TCPTP expressed in Escherichia coli using pNPP as substrate preincubated for 10 mins followed by substrate addition measured after 30 mins | 2017 | Bioorganic & medicinal chemistry letters, 03-01, Volume: 27, Issue:5 | Furanoterpenes, new types of protein tyrosine phosphatase 1B inhibitors, from two Indonesian marine sponges, Ircinia and Spongia spp. |
| AID1430424 | Selectivity ratio of IC50 for human CD45 cytoplasmic domain (584 to 1281 residues) expressed in yeast to IC50 for recombinant human PTP1B (1 to 322 residues) expressed in Escherichia coli | 2017 | Bioorganic & medicinal chemistry letters, 03-01, Volume: 27, Issue:5 | Furanoterpenes, new types of protein tyrosine phosphatase 1B inhibitors, from two Indonesian marine sponges, Ircinia and Spongia spp. |
| AID474945 | Agonist activity at human recombinant alpha 3 GlyR expressed in HEK293 cells assessed as potentiation of glycine current by whole cell patch clamp assay | 2010 | Bioorganic & medicinal chemistry, Apr-15, Volume: 18, Issue:8 | Ircinialactams: subunit-selective glycine receptor modulators from Australian sponges of the family Irciniidae. |
| AID1430421 | Cytotoxicity against human HuH7 cells assessed as reduction in cell viability after 72 hrs by WST1 assay | 2017 | Bioorganic & medicinal chemistry letters, 03-01, Volume: 27, Issue:5 | Furanoterpenes, new types of protein tyrosine phosphatase 1B inhibitors, from two Indonesian marine sponges, Ircinia and Spongia spp. |
| AID1430417 | Inhibition of recombinant human PTP1B (1 to 322 residues) expressed in Escherichia coli using pNPP as substrate preincubated for 10 mins followed by substrate addition measured after 30 mins | 2017 | Bioorganic & medicinal chemistry letters, 03-01, Volume: 27, Issue:5 | Furanoterpenes, new types of protein tyrosine phosphatase 1B inhibitors, from two Indonesian marine sponges, Ircinia and Spongia spp. |
| AID474949 | Antagonist activity at human recombinant alpha 3 GlyR expressed in HEK293 cells assessed as inhibition of glycine current influx by whole cell patch clamp assay | 2010 | Bioorganic & medicinal chemistry, Apr-15, Volume: 18, Issue:8 | Ircinialactams: subunit-selective glycine receptor modulators from Australian sponges of the family Irciniidae. |
| AID474948 | Antagonist activity at human recombinant alpha 1 GlyR expressed in HEK293 cells assessed as inhibition of glycine current influx by whole cell patch clamp assay | 2010 | Bioorganic & medicinal chemistry, Apr-15, Volume: 18, Issue:8 | Ircinialactams: subunit-selective glycine receptor modulators from Australian sponges of the family Irciniidae. |
| AID1430422 | Cytotoxicity against human EJ1 cells assessed as reduction in cell viability after 72 hrs by WST1 assay | 2017 | Bioorganic & medicinal chemistry letters, 03-01, Volume: 27, Issue:5 | Furanoterpenes, new types of protein tyrosine phosphatase 1B inhibitors, from two Indonesian marine sponges, Ircinia and Spongia spp. |
| AID1430423 | Selectivity ratio of IC50 for full length recombinant N-terminal GST-tagged human TCPTP expressed in Escherichia coli to IC50 for recombinant human PTP1B (1 to 322 residues) expressed in Escherichia coli | 2017 | Bioorganic & medicinal chemistry letters, 03-01, Volume: 27, Issue:5 | Furanoterpenes, new types of protein tyrosine phosphatase 1B inhibitors, from two Indonesian marine sponges, Ircinia and Spongia spp. |
| AID1430419 | Inhibition of human CD45 cytoplasmic domain (584 to 1281 residues) expressed in yeast using pNPP as substrate preincubated for 10 mins followed by substrate addition measured after 30 mins | 2017 | Bioorganic & medicinal chemistry letters, 03-01, Volume: 27, Issue:5 | Furanoterpenes, new types of protein tyrosine phosphatase 1B inhibitors, from two Indonesian marine sponges, Ircinia and Spongia spp. |
| AID1430420 | Inhibition of human VHR expressed in Escherichia coli using pNPP as substrate preincubated for 10 mins followed by substrate addition measured after 30 mins | 2017 | Bioorganic & medicinal chemistry letters, 03-01, Volume: 27, Issue:5 | Furanoterpenes, new types of protein tyrosine phosphatase 1B inhibitors, from two Indonesian marine sponges, Ircinia and Spongia spp. |
| [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 | 2 (25.00) | 18.2507 |
| 2000's | 0 (0.00) | 29.6817 |
| 2010's | 5 (62.50) | 24.3611 |
| 2020's | 1 (12.50) | 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 moderate demand-to-supply ratio for research on this compound.
| This Compound (22.16) 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 | 9 (100.00%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||