filanesib: a kinesin spindle protein inhibitor [MeSH]
| ID Source | ID |
|---|---|
| PubMed CID | 44224257 |
| CHEMBL ID | 2347655 |
| SCHEMBL ID | 368043 |
| MeSH ID | M0540486 |
| Synonym |
|---|
| filanesib |
| HY-15187 |
| 885060-09-3 |
| bdbm50431893 |
| arry 520 |
| ARRY-520 , |
| arry520 |
| CS-0867 |
| CHEMBL2347655 , |
| 1,3,4-thiadiazole-3(2h)-carboxamide, 2-(3-aminopropyl)-5-(2,5-difluorophenyl)-n-methoxy-n-methyl-2-phenyl-, (2s)- |
| filanesib [usan:inn] |
| unii-8a49oso368 |
| filanesib [inn] |
| 8a49oso368 , |
| (2s)-2-(3-aminopropyl)-5-(2,5-difluorophenyl)-n-methoxy-n-methyl-2-phenyl-1,3,4-thiadiazole-3(2h)-carboxamide |
| filanesib [who-dd] |
| filanesib [usan] |
| SCHEMBL368043 |
| AC-35274 |
| J-519598 |
| DTXSID50237086 |
| EX-A678 |
| arry-520; filanesib |
| filanesib(arry-520) |
| NCGC00381751-02 |
| NCGC00381751-04 |
| BCP07442 |
| 885060-09-3 (free base) |
| (s)-2-(3-aminopropyl)-5-(2,5-difluorophenyl)-n-methoxy-n-methyl-2-phenyl-1,3,4-thiadiazole-3(2h)-carboxamide. |
| DB06040 |
| Q15634095 |
| SB19209 |
| HMS3750A15 |
| D11754 |
| filanesib (usan/inn) |
| MS-27382 |
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) |
|---|---|---|---|---|
| cytochrome P450 family 3 subfamily A polypeptide 4 | Homo sapiens (human) | Potency | 1.5092 | AID1645841 |
| G | Vesicular stomatitis virus | Potency | 3.0112 | AID1645842 |
| cytochrome P450 2D6 | Homo sapiens (human) | Potency | 18.9991 | AID1645840 |
| Interferon beta | Homo sapiens (human) | Potency | 3.0112 | AID1645842 |
| HLA class I histocompatibility antigen, B alpha chain | Homo sapiens (human) | Potency | 3.0112 | AID1645842 |
| Inositol hexakisphosphate kinase 1 | Homo sapiens (human) | Potency | 3.0112 | AID1645842 |
| cytochrome P450 2C9, partial | Homo sapiens (human) | Potency | 3.0112 | AID1645842 |
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) |
|---|---|---|---|---|
| Kinesin-like protein KIF11 | Homo sapiens (human) | IC50 | 0.0090 | AID1255273; AID1398519; AID1406288; AID740791 |
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| AID1882264 | Induction of mitotic arrest in human multiple myeloma cells | 2022 | European journal of medicinal chemistry, Feb-05, Volume: 229ISSN: 1768-3254 | A review on the treatment of multiple myeloma with small molecular agents in the past five years. |
| AID1255274 | Growth inhibition of human HCT116 cells after 72 hrs by MTS assay | 2015 | ACS medicinal chemistry letters, Sep-10, Volume: 6, Issue:9 ISSN: 1948-5875 | Structure-Guided Design of Novel l-Cysteine Derivatives as Potent KSP Inhibitors. |
| AID1398519 | Inhibition EG5 (unknown origin) | 2018 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 28, Issue:17 ISSN: 1464-3405 | Design and synthesis of novel thiadiazole-thiazolone hybrids as potential inhibitors of the human mitotic kinesin Eg5. |
| AID1406288 | Inhibition of microtubule-stimulated Eg5 ATPase activity in human HL-60 cells after 48 hrs by Western blot analysis | 2018 | European journal of medicinal chemistry, Aug-05, Volume: 156ISSN: 1768-3254 | Crystal structure of the Eg5 - K858 complex and implications for structure-based design of thiadiazole-containing inhibitors. |
| AID1255273 | Inhibition of His-tagged KSP motor domain (1 to 369) (unknown origin) assessed as inhibition of microtubule-stimulated KSP ATPase activity preincuabted for 30 mins followed by ATP addition measured after 15 mins by Kinase-Glo assay | 2015 | ACS medicinal chemistry letters, Sep-10, Volume: 6, Issue:9 ISSN: 1948-5875 | Structure-Guided Design of Novel l-Cysteine Derivatives as Potent KSP Inhibitors. |
| AID740791 | Inhibition of Eg5 (unknown origin) | 2013 | European journal of medicinal chemistry, Apr, Volume: 62ISSN: 1768-3254 | Advances in the discovery of kinesin spindle protein (Eg5) inhibitors as antitumor agents. |
| Timeframe | Studies, This Drug (%) | All Drugs % |
|---|---|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 0 (0.00) | 18.2507 |
| 2000's | 3 (11.54) | 29.6817 |
| 2010's | 15 (57.69) | 24.3611 |
| 2020's | 8 (30.77) | 2.80 |
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 6 (23.08%) | 5.53% |
| Reviews | 4 (15.38%) | 6.00% |
| Case Studies | 0 (0.00%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 16 (61.54%) | 84.16% |
| Condition | Indicated | Studies | First Year | Last Year | Average Age | Relationship Strength | Trials | pre-1990 | 1990's | 2000's | 2010's | post-2020 |
|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Abnormalities, Autosome | 0 | 2022 | 2022 | 2.0 | low | 1 | 0 | 0 | 0 | 0 | 1 | |
| Angioblastic Meningioma | 0 | 2021 | 2021 | 3.0 | low | 0 | 0 | 0 | 0 | 0 | 1 | |
| Ascites | 0 | 2009 | 2009 | 15.0 | low | 0 | 0 | 0 | 1 | 0 | 0 | |
| Benign Meningeal Neoplasms | 0 | 2021 | 2021 | 3.0 | low | 0 | 0 | 0 | 0 | 0 | 1 | |
| Benign Neoplasms | 0 | 2009 | 2015 | 11.5 | low | 1 | 0 | 0 | 1 | 3 | 0 | |
| Cancer of Ovary | 0 | 2009 | 2009 | 15.0 | low | 0 | 0 | 0 | 1 | 0 | 0 | |
| Congenital Zika Syndrome | 0 | 2020 | 2020 | 4.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |
| Disease Models, Animal | 0 | 2020 | 2020 | 4.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |
| Dysmyelopoietic Syndromes | 0 | 2012 | 2012 | 12.0 | low | 1 | 0 | 0 | 0 | 1 | 0 | |
| Granulocytic Leukemia | 0 | 2012 | 2012 | 12.0 | low | 1 | 0 | 0 | 0 | 1 | 0 | |
| Kahler Disease | 0 | 2010 | 2022 | 5.9 | high | 4 | 0 | 0 | 1 | 6 | 3 | |
| Leukemia, Myeloid | 0 | 2012 | 2012 | 12.0 | low | 1 | 0 | 0 | 0 | 1 | 0 | |
| Local Neoplasm Recurrence | 0 | 2017 | 2022 | 4.2 | low | 4 | 0 | 0 | 0 | 2 | 2 | |
| Meningeal Neoplasms | 0 | 2021 | 2021 | 3.0 | low | 0 | 0 | 0 | 0 | 0 | 1 | |
| Meningioma | 0 | 2021 | 2021 | 3.0 | low | 0 | 0 | 0 | 0 | 0 | 1 | |
| Multiple Myeloma | 1 | 2010 | 2022 | 5.9 | high | 4 | 0 | 0 | 1 | 6 | 3 | |
| Myelodysplastic Syndromes | 1 | 2012 | 2012 | 12.0 | low | 1 | 0 | 0 | 0 | 1 | 0 | |
| Neoplasms | 1 | 2009 | 2015 | 11.5 | low | 1 | 0 | 0 | 1 | 3 | 0 | |
| Ovarian Neoplasms | 0 | 2009 | 2009 | 15.0 | low | 0 | 0 | 0 | 1 | 0 | 0 | |
| Recrudescence | 0 | 2012 | 2012 | 12.0 | low | 1 | 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 |