| ID Source | ID |
|---|---|
| PubMed CID | 11488110 |
| CHEMBL ID | 1182714 |
| SCHEMBL ID | 4042827 |
| MeSH ID | M0555369 |
| Synonym |
|---|
| CHEMBL1182714 |
| cevipabulin , |
| cevipabulin [inn] |
| 849550-05-6 |
| p14m0dws2j , |
| tti-237 |
| cevipabulin [who-dd] |
| SCHEMBL4042827 |
| CS-4196 |
| DTXSID00233997 |
| 5-chloro-6-{2,6-difluoro-4-[3-(methylamino)propoxy]phenyl}-n-[(1s)-2,2,2-trifluoro-1-methylethyl][1,2,4]triazolo[1,5-a]pyrimidin-7-amine |
| 5-chloro-6-{2,6-difluoro-4-[3-(methylamino) propoxy]phenyl}-n-[(1s)-2,2,2-trifluoro-1-methylethyl][1,2,4]triazolo[1,5-a]pyrimidin-7-amine |
| 5-chloro-6{2,6-difluoro-4-[3-(methylamino)propoxy]phenyl}-n-[(1s)-2,2,2-trifluoro-1-methylethyl][1,2,4]triazolo[1,5-a]pyrimidin-7-amine |
| HY-14949 |
| J-690362 |
| EX-A607 |
| AKOS030526926 |
| 5-chloro-6-[2,6-difluoro-4-[3-(methylamino)propoxy]phenyl]-n-((1s)-2,2,2-trifluoro-1-methylethyl)-[1,2,4]triazolo[1,5-a]pyrimidin-7-amine |
| 5-chloro-6-{2,6-difluoro-4-[3-(methylamino)propoxy]phenyl}-n-[(2s)-1,1,1-trifluoropropan-2-yl]-[1,2,4]triazolo[1,5-a]pyrimidin-7-amine |
| cevipabulin(tti 237) |
| mfcd09832720 |
| DB12533 |
| 849550-05-6 (free base) |
| 5-chloro-6-[2,6-difluoro-4-[3-(methylamino)propoxy]phenyl]-n-[(1s)-2,2,2-trifluoro-1- methylethyl]-[1,2,4]triazolo[1,5-a]pyrimidin-7-amine. |
| tti 237; tti-237; tti237; d06576; d 06576; d-06576 |
| BCP28162 |
| 5-chloro-6-[2,6-difluoro-4-[3-(methylamino)propoxy]phenyl]-n-[(2s)-1,1,1-trifluoropropan-2-yl]-[1,2,4]triazolo[1,5-a]pyrimidin-7-amine |
| (s)-5-chloro-6-(2,6-difluoro-4-(3-(methylamino)propoxy)phenyl)-n-(1,1,1-trifluoropropan-2-yl)-[1,2,4]triazolo[1,5-a]pyrimidin-7-amine |
| Q27285989 |
| MS-28564 |
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| AID1182024 | Drug level in CD1 mouse plasma at 5 mg/kg, ip after 1 hr by LC-MS/MS system | 2014 | Journal of medicinal chemistry, Jul-24, Volume: 57, Issue:14 ISSN: 1520-4804 | Brain-penetrant, orally bioavailable microtubule-stabilizing small molecules are potential candidate therapeutics for Alzheimer's disease and related tauopathies. |
| AID1182025 | Ratio of drug level in brain to plasma in CD1 mouse at 5 mg/kg, ip after 1 hr by LC-MS/MS system | 2014 | Journal of medicinal chemistry, Jul-24, Volume: 57, Issue:14 ISSN: 1520-4804 | Brain-penetrant, orally bioavailable microtubule-stabilizing small molecules are potential candidate therapeutics for Alzheimer's disease and related tauopathies. |
| AID1496233 | Induction of microtubule disruption in HEK293 cells assessed as total alpha tubulin levels at 1 uM after 4 hrs by ELISA relative to control | 2018 | Bioorganic & medicinal chemistry letters, 07-01, Volume: 28, Issue:12 ISSN: 1464-3405 | Design, synthesis and evaluation of photoactivatable derivatives of microtubule (MT)-active [1,2,4]triazolo[1,5-a]pyrimidines. |
| AID1182022 | Inhibition of human P-glycoprotein expressed in NCI/ADR-RES cells assessed as reduction of calcein-AM transport after 20 mins by fluorescence assay | 2014 | Journal of medicinal chemistry, Jul-24, Volume: 57, Issue:14 ISSN: 1520-4804 | Brain-penetrant, orally bioavailable microtubule-stabilizing small molecules are potential candidate therapeutics for Alzheimer's disease and related tauopathies. |
| AID1496232 | Induction of microtubule stabilization in HEK293 cells assessed as increase in acetylated alpha tubulin levels at 10 uM after 4 hrs by ELISA relative to control | 2018 | Bioorganic & medicinal chemistry letters, 07-01, Volume: 28, Issue:12 ISSN: 1464-3405 | Design, synthesis and evaluation of photoactivatable derivatives of microtubule (MT)-active [1,2,4]triazolo[1,5-a]pyrimidines. |
| AID1182023 | Drug level in CD1 mouse brain at 5 mg/kg, ip after 1 hr by LC-MS/MS system | 2014 | Journal of medicinal chemistry, Jul-24, Volume: 57, Issue:14 ISSN: 1520-4804 | Brain-penetrant, orally bioavailable microtubule-stabilizing small molecules are potential candidate therapeutics for Alzheimer's disease and related tauopathies. |
| AID1496234 | Induction of microtubule disruption in HEK293 cells assessed as total alpha tubulin levels at 10 uM after 4 hrs by ELISA relative to control | 2018 | Bioorganic & medicinal chemistry letters, 07-01, Volume: 28, Issue:12 ISSN: 1464-3405 | Design, synthesis and evaluation of photoactivatable derivatives of microtubule (MT)-active [1,2,4]triazolo[1,5-a]pyrimidines. |
| AID1182021 | Induction of microtubule stabilization in human QBI293 cells assessed as increase in acetylated alpha-tubulin at 100 nM after 4 hrs by immunofluorescence assay relative to control | 2014 | Journal of medicinal chemistry, Jul-24, Volume: 57, Issue:14 ISSN: 1520-4804 | Brain-penetrant, orally bioavailable microtubule-stabilizing small molecules are potential candidate therapeutics for Alzheimer's disease and related tauopathies. |
| AID1496231 | Induction of microtubule stabilization in HEK293 cells assessed as increase in acetylated alpha tubulin levels at 1 uM after 4 hrs by ELISA relative to control | 2018 | Bioorganic & medicinal chemistry letters, 07-01, Volume: 28, Issue:12 ISSN: 1464-3405 | Design, synthesis and evaluation of photoactivatable derivatives of microtubule (MT)-active [1,2,4]triazolo[1,5-a]pyrimidines. |
| AID1347411 | qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Mechanism Interrogation Plate v5.0 (MIPE) Libary | 2020 | ACS chemical biology, 07-17, Volume: 15, Issue:7 ISSN: 1554-8937 | High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle. |
| Timeframe | Studies, This Drug (%) | All Drugs % |
|---|---|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 0 (0.00) | 18.2507 |
| 2000's | 4 (36.36) | 29.6817 |
| 2010's | 5 (45.45) | 24.3611 |
| 2020's | 2 (18.18) | 2.80 |
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 1 (9.09%) | 5.53% |
| Reviews | 1 (9.09%) | 6.00% |
| Case Studies | 0 (0.00%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 9 (81.82%) | 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 |
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| verapamil | aromatic ether; nitrile; polyether; tertiary amino compound | 2014 | 2014 | 10.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | ||
| desoxyepothilone b | epothilone | microtubule-stabilising agent | 2014 | 2014 | 10.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |
| cyclosporine | homodetic cyclic peptide | anti-asthmatic drug; anticoronaviral agent; antifungal agent; antirheumatic drug; carcinogenic agent; dermatologic drug; EC 3.1.3.16 (phosphoprotein phosphatase) inhibitor; geroprotector; immunosuppressive agent; metabolite | 2014 | 2014 | 10.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |
| 2-(2,6-diisopropylphenyl)-5-hydroxy-1h-isoindole-1,3-dione | 2014 | 2014 | 10.0 | medium | 0 | 0 | 0 | 0 | 1 | 0 |
| Substance | Studies | Classes | Roles | First Year | Last Year | Average Age | Relationship Strength | Trials | pre-1990 | 1990's | 2000's | 2010's | post-2020 |
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| paclitaxel | taxane diterpenoid; tetracyclic diterpenoid | antineoplastic agent; human metabolite; metabolite; microtubule-stabilising agent | 2009 | 2019 | 10.0 | medium | 0 | 0 | 0 | 1 | 1 | 0 | |
| triazoles | 1,2,3-triazole | 2007 | 2020 | 11.5 | high | 1 | 0 | 0 | 4 | 4 | 0 | ||
| guanosine triphosphate | guanosine 5'-phosphate; purine ribonucleoside 5'-triphosphate | Escherichia coli metabolite; mouse metabolite; uncoupling protein inhibitor | 2009 | 2009 | 15.0 | low | 0 | 0 | 0 | 1 | 0 | 0 |
| Condition | Indicated | Studies | First Year | Last Year | Average Age | Relationship Strength | Trials | pre-1990 | 1990's | 2000's | 2010's | post-2020 |
|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Acute Confusional Senile Dementia | 0 | 2014 | 2016 | 9.0 | medium | 0 | 0 | 0 | 0 | 2 | 0 | |
| Alzheimer Disease | 0 | 2014 | 2016 | 9.0 | medium | 0 | 0 | 0 | 0 | 2 | 0 | |
| Amyloid Deposits | 0 | 2020 | 2020 | 4.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |
| Benign Neoplasms | 0 | 2009 | 2012 | 13.5 | medium | 1 | 0 | 0 | 1 | 1 | 0 | |
| Carcinoma, Epidermoid | 0 | 2008 | 2008 | 16.0 | low | 0 | 0 | 0 | 1 | 0 | 0 | |
| Carcinoma, Squamous Cell | 0 | 2008 | 2008 | 16.0 | low | 0 | 0 | 0 | 1 | 0 | 0 | |
| Disease Models, Animal | 0 | 2020 | 2020 | 4.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |
| Neoplasms | 1 | 2009 | 2012 | 13.5 | medium | 1 | 0 | 0 | 1 | 1 | 0 | |
| Tauopathies | 0 | 2014 | 2016 | 9.0 | medium | 0 | 0 | 0 | 0 | 2 | 0 |
| Article | Year |
|---|---|
| Characterization of Brain-Penetrant Pyrimidine-Containing Molecules with Differential Microtubule-Stabilizing Activities Developed as Potential Therapeutic Agents for Alzheimer's Disease and Related Tauopathies. The Journal of pharmacology and experimental therapeutics, , Volume: 357, Issue:2 | 2016 |
| Brain-penetrant, orally bioavailable microtubule-stabilizing small molecules are potential candidate therapeutics for Alzheimer's disease and related tauopathies. Journal of medicinal chemistry, , Jul-24, Volume: 57, Issue:14 | 2014 |
| Article | Year |
|---|---|
| A phase I dose escalation study of TTI-237 in patients with advanced malignant solid tumors. Investigational new drugs, , Volume: 30, Issue:1 | 2012 |
| TTI-237: a novel microtubule-active compound with in vivo antitumor activity. Cancer research, , Apr-01, Volume: 68, Issue:7 | 2008 |