Drug Information
| Drug General Information | |||||
|---|---|---|---|---|---|
| Drug ID |
D02RJY
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| Former ID |
DCL001078
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| Drug Name |
PHA-739358
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| Synonyms |
Danusertib; PHA 739358; Danusertib, PHA-739358; (R)-N-(5-(2-methoxy-2-phenylacetyl)-1,4,5,6-tetrahydropyrrolo[3,4-c]pyrazol-3-yl)-4-(4-methylpiperazin-1-yl)benzamide; 5-Amido-pyrrolopyrazole 9d
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| Drug Type |
Small molecular drug
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| Indication | Prostate cancer [ICD9: 185; ICD10:C61] | Phase 2 | [1], [2] | ||
| Company |
Pfizer; Nerviano
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| Structure |
|
Download2D MOL |
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| Formula |
C26H30N6O3
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| InChI |
InChI=1S/C26H30N6O3/c1-30-12-14-31(15-13-30)20-10-8-19(9-11-20)25(33)27-24-21-16-32(17-22(21)28-29-24)26(34)23(35-2)18-6-4-3-5-7-18/h3-11,23H,12-17H2,1-2H3,(H2,27,28,29,33)/t23-/m1/s1
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| InChIKey |
XKFTZKGMDDZMJI-HSZRJFAPSA-N
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| PubChem Compound ID | |||||
| PubChem Substance ID |
16541138, 23585151, 42521925, 46394298, 46513412, 57304411, 77307760, 93581266, 99373541, 99436985, 103573135, 124757005, 125163810, 126626959, 126634887, 126665979, 126730902, 131480684, 134964424, 135261930, 136340130, 136367305, 136367975, 136920406, 137147906, 137276047, 140478603, 143499036, 144115881, 152036110, 152134559, 152164575, 152186748, 152239915, 152258104, 152344035, 160646943, 162011705, 162037440, 162202553, 163109117, 164193992, 164838824, 174006483, 177748769, 180177283, 188899502, 198940281, 223682527, 223704702
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| Target and Pathway | |||||
| Target(s) | Aurora protein kinase | Target Info | Inhibitor | [3] | |
| mRNA of Aurora B | Target Info | Inhibitor | [3] | ||
| Aurora kinase B | Target Info | Inhibitor | [4] | ||
| Aurora kinase A | Target Info | Inhibitor | [4] | ||
| KEGG Pathway | Oocyte meiosishsa04114:Oocyte meiosis | ||||
| Pathway Interaction Database | Aurora B signaling | ||||
| Signaling by Aurora kinases | |||||
| Aurora C signaling | |||||
| FOXM1 transcription factor network | |||||
| Aurora A signalingaurora_b_pathway:Aurora B signaling | |||||
| Integrin-linked kinase signaling | |||||
| PLK1 signaling events | |||||
| Aurora A signaling | |||||
| Reactome | APC/C:Cdh1 mediated degradation of Cdc20 and other APC/C:Cdh1 targeted proteins in late mitosis/early G1 | ||||
| Separation of Sister Chromatids | |||||
| Resolution of Sister Chromatid Cohesion | |||||
| RHO GTPases Activate ForminsR-HSA-174178:APC/C:Cdh1 mediated degradation of Cdc20 and other APC/C:Cdh1 targeted proteins in late mitosis/early G1 | |||||
| RHO GTPases Activate Formins | |||||
| Mitotic PrometaphaseR-HSA-174178:APC/C:Cdh1 mediated degradation of Cdc20 and other APC/C:Cdh1 targeted proteins in late mitosis/early G1 | |||||
| Regulation of PLK1 Activity at G2/M Transition | |||||
| WikiPathways | EGF/EGFR Signaling Pathway | ||||
| JAK/STAT | |||||
| Gastric Cancer Network 1 | |||||
| Integrated Breast Cancer Pathway | |||||
| APC/C-mediated degradation of cell cycle proteinsWP2757:Mitotic Metaphase and Anaphase | |||||
| Mitotic Prometaphase | |||||
| Regulation of Microtubule Cytoskeleton | |||||
| miR-targeted genes in lymphocytes - TarBase | |||||
| miR-targeted genes in epithelium - TarBase | |||||
| APC/C-mediated degradation of cell cycle proteinsWP437:EGF/EGFR Signaling Pathway | |||||
| APC/C-mediated degradation of cell cycle proteins | |||||
| References | |||||
| REF 1 | (http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7937). | ||||
| REF 2 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800025382) | ||||
| REF 3 | J Med Chem. 2005 Apr 21;48(8):3080-4.Potent and selective Aurora inhibitors identified by the expansion of a novel scaffold for protein kinase inhibition. | ||||
| REF 4 | Cell cycle kinases as therapeutic targets for cancer. Nat Rev Drug Discov. 2009 Jul;8(7):547-66. | ||||
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