KPT-185: binds CRM1 to inhibit nuclear export; has antineoplastic activity [MeSH]
| ID Source | ID |
|---|---|
| PubMed CID | 53495165 |
| CHEMBL ID | 3898452 |
| SCHEMBL ID | 1335182 |
| MeSH ID | M0579400 |
| Synonym |
|---|
| SCHEMBL1335182 |
| S7125 |
| (z)-isopropyl 3-(3-(3-methoxy-5-(trifluoromethyl)phenyl)-1h-1,2,4-triazol-1-yl)acrylate |
| 1333151-73-7 |
| kpt-185 |
| kpt185 |
| AC-32679 |
| n-[3-({2-[(4-{[1-(2-fluoroethyl)-3-azetidinyl]amino}-2-methoxyphenyl)amino]-5-(trifluoromethyl)-4-pyrimidinyl}amino)phenyl]acrylamid e |
| J-690131 |
| EX-A318 |
| AKOS030526414 |
| kpt 185 |
| NCGC00386294-01 |
| CHEMBL3898452 |
| SW219337-1 |
| isopropyl (z)-3-(3-(3-methoxy-5-(trifluoromethyl)phenyl)-1h-1,2,4-triazol-1-yl)acrylate |
| CCG-268093 |
| propan-2-yl (z)-3-[3-[3-methoxy-5-(trifluoromethyl)phenyl]-1,2,4-triazol-1-yl]prop-2-enoate |
| nsc-757568 |
| nsc757568 |
| nsc772595 |
| nsc-772595 |
| nlngwflrrrynil-plngdyqasa-n |
| HY-15611 |
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) |
|---|---|---|---|---|
| Exportin-1 | Homo sapiens (human) | IC50 | 1.0000 | AID1339772 |
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| AID1296008 | Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening | 2020 | SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1 ISSN: 2472-5560 | Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening. |
| AID1346987 | P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5 ISSN: 1521-0111 | A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
| AID1347160 | Primary screen NINDS Rhodamine qHTS for Zika virus inhibitors | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49 ISSN: 1091-6490 | Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
| AID1347159 | Primary screen GU Rhodamine qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49 ISSN: 1091-6490 | Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
| AID1346986 | P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5 ISSN: 1521-0111 | A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
| Timeframe | Studies, This Drug (%) | All Drugs % |
|---|---|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 0 (0.00) | 18.2507 |
| 2000's | 0 (0.00) | 29.6817 |
| 2010's | 21 (87.50) | 24.3611 |
| 2020's | 3 (12.50) | 2.80 |
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 1 (4.17%) | 5.53% |
| Reviews | 0 (0.00%) | 6.00% |
| Case Studies | 0 (0.00%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 23 (95.83%) | 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 |
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| thiazoles | 1,3-thiazoles; mancude organic heteromonocyclic parent; monocyclic heteroarene | 2012 | 2016 | 9.7 | low | 1 | 0 | 0 | 0 | 3 | 0 | ||
| hydrazine | azane; hydrazines | EC 4.3.1.10 (serine-sulfate ammonia-lyase) inhibitor | 2015 | 2017 | 8.0 | low | 0 | 0 | 0 | 0 | 4 | 0 | |
| triazoles | 1,2,3-triazole | 2012 | 2021 | 9.2 | high | 1 | 0 | 0 | 0 | 20 | 1 | ||
| angiotensin ii | amino acid zwitterion; angiotensin II | human metabolite | 2018 | 2018 | 6.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |
| leptomycin b | 2013 | 2016 | 9.3 | low | 0 | 0 | 0 | 0 | 3 | 0 | |||
| azd2014 | 2017 | 2017 | 7.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |||
| selinexor | 2015 | 2016 | 8.3 | low | 0 | 0 | 0 | 0 | 3 | 0 | |||
| verdinexor | 2016 | 2017 | 7.5 | medium | 0 | 0 | 0 | 0 | 2 | 0 | |||
| kpt-276 | 2012 | 2016 | 9.7 | high | 1 | 0 | 0 | 0 | 3 | 0 | |||
| cyclin d1 | 2015 | 2015 | 9.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| Condition | Indicated | Studies | First Year | Last Year | Average Age | Relationship Strength | Trials | pre-1990 | 1990's | 2000's | 2010's | post-2020 |
|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Acute Disease | 0 | 2012 | 2012 | 12.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |
| Acute Myelogenous Leukemia | 0 | 2013 | 2013 | 11.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |
| Adenocarcinoma Of Kidney | 0 | 2013 | 2013 | 11.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |
| AIDS-Associated Lymphoma | 0 | 2015 | 2015 | 9.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |
| B-Cell Chronic Lymphocytic Leukemia | 0 | 2012 | 2012 | 12.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |
| B-Cell Lymphoma | 0 | 2016 | 2016 | 8.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |
| Breast Cancer | 0 | 2017 | 2017 | 7.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |
| Breast Neoplasms | 0 | 2017 | 2017 | 7.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |
| Brill-Symmers Disease | 0 | 2013 | 2013 | 11.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |
| Cancer of Kidney | 0 | 2013 | 2013 | 11.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |
| Cancer of Lung | 0 | 2014 | 2014 | 10.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |
| Cancer of Mediastinum | 0 | 2016 | 2016 | 8.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |
| Cancer of Pancreas | 0 | 2014 | 2014 | 10.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |
| Canine Diseases | 0 | 2017 | 2017 | 7.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |
| Carcinoma, Ductal, Pancreatic | 0 | 2014 | 2014 | 10.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |
| Carcinoma, Non-Small Cell Lung | 0 | 2014 | 2014 | 10.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |
| Carcinoma, Non-Small-Cell Lung | 0 | 2014 | 2014 | 10.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |
| Carcinoma, Pancreatic Ductal | 0 | 2014 | 2014 | 10.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |
| Carcinoma, Renal Cell | 0 | 2013 | 2013 | 11.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |
| Carcinoma, Transitional Cell | 0 | 2017 | 2017 | 7.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |
| Congenital Zika Syndrome | 0 | 2020 | 2020 | 4.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |
| Diffuse Large B-Cell Lymphoma | 0 | 2013 | 2013 | 11.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |
| Diffuse Lymphocytic Lymphoma, Poorly-Differentiated | 0 | 2013 | 2017 | 9.3 | low | 0 | 0 | 0 | 0 | 3 | 0 | |
| Diffuse Mixed Small and Large Cell Lymphoma | 0 | 2013 | 2015 | 10.0 | low | 1 | 0 | 0 | 0 | 2 | 0 | |
| Disease Models, Animal | 0 | 2013 | 2020 | 7.5 | low | 0 | 0 | 0 | 0 | 2 | 0 | |
| Familial Waldenstrom's Macroglobulinaemia | 0 | 2013 | 2013 | 11.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |
| Fibrosarcoma | 0 | 2015 | 2015 | 9.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |
| Granulocytic Leukemia | 0 | 2012 | 2012 | 12.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |
| Granuloma, Hodgkin | 0 | 2016 | 2016 | 8.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |
| HIV | 0 | 2015 | 2015 | 9.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |
| Hodgkin Disease | 0 | 2016 | 2016 | 8.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |
| Infections, Respiratory Syncytial Virus | 0 | 2021 | 2021 | 3.0 | low | 0 | 0 | 0 | 0 | 0 | 1 | |
| Kidney Neoplasms | 0 | 2013 | 2013 | 11.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |
| Leukemia, Lymphocytic, Chronic, B-Cell | 0 | 2012 | 2012 | 12.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |
| Leukemia, Myeloid | 0 | 2012 | 2012 | 12.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |
| Leukemia, Myeloid, Acute | 0 | 2013 | 2013 | 11.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |
| Lung Neoplasms | 0 | 2014 | 2014 | 10.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |
| Lymphoma, AIDS-Related | 0 | 2015 | 2015 | 9.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |
| Lymphoma, B-Cell | 0 | 2016 | 2016 | 8.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |
| Lymphoma, Follicular | 0 | 2013 | 2013 | 11.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |
| Lymphoma, Large B-Cell, Diffuse | 0 | 2013 | 2013 | 11.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |
| Lymphoma, Mantle-Cell | 0 | 2013 | 2017 | 9.3 | low | 0 | 0 | 0 | 0 | 3 | 0 | |
| Lymphoma, Non-Hodgkin | 0 | 2013 | 2015 | 10.0 | low | 1 | 0 | 0 | 0 | 2 | 0 | |
| Mediastinal Neoplasms | 0 | 2016 | 2016 | 8.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |
| Pancreatic Neoplasms | 0 | 2014 | 2014 | 10.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |
| Respiratory Syncytial Virus Infections | 0 | 2021 | 2021 | 3.0 | low | 0 | 0 | 0 | 0 | 0 | 1 | |
| Sensitivity and Specificity | 0 | 2013 | 2013 | 11.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |
| Waldenstrom Macroglobulinemia | 0 | 2013 | 2013 | 11.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |
| Zika Virus Infection | 0 | 2020 | 2020 | 4.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| Article | Year |
|---|---|
| A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. Molecular pharmacology, , Volume: 96, Issue:5 | 2019 |
| Human Exportin-1 is a Target for Combined Therapy of HIV and AIDS Related Lymphoma. EBioMedicine, , Volume: 2, Issue:9 | 2015 |
| Nuclear retention of Fbw7 by specific inhibitors of nuclear export leads to Notch1 degradation in pancreatic cancer. Oncotarget, , Jun-15, Volume: 5, Issue:11 | 2014 |
| Preclinical activity of a novel CRM1 inhibitor in acute myeloid leukemia. Blood, , Aug-30, Volume: 120, Issue:9 | 2012 |
| Article | Year |
|---|---|
| A method for quantification of exportin-1 (XPO1) occupancy by Selective Inhibitor of Nuclear Export (SINE) compounds. Oncotarget, , Jan-12, Volume: 7, Issue:2 | 2016 |