General Information of Drug (ID: DMQ6YAZ)

Drug Name
EMD-534085 Drug Info
Synonyms
EMD-534085; 858668-07-2; EMD534085; EMD 534085; UNII-AL67QX8036; CHEMBL1077204; AL67QX8036; 1-(2-(Dimethylamino)ethyl)-3-(((2R,4aS,5R,10bS)-5-phenyl-9-(trifluoromethyl)-3,4,4a,5,6,10b-hexahydro-2H-pyrano(3,2-C)quinolin-2-yl)methyl)urea; 1-[2-(dimethylamino)ethyl]-3-{[(2R,4aS,5R,10bS)-5-phenyl-9-(trifluoromethyl)-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinolin-2-yl]methyl}urea
Indication
Disease Entry ICD 11 Status REF
Haematological malignancy 2B33.Y Phase 1 [1]
Cross-matching ID
PubChem CID
23634407
CAS Number
CAS 858668-07-2
TTD Drug ID
DMQ6YAZ

Molecule-Related Drug Atlas

Molecule-Related Drug Atlas
Molecule Type:
DTT
DOT
Drug Status:
Clinical Trial Drug(s)
Investigative Drug(s)
Approved Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
ALN-VSP DM89DHO Liver cancer 2C12 Phase 1 [4]
N-[4'-(trifluoromethyl)-4-biphenylyl]thiourea DMPVKWG Discovery agent N.A. Investigative [5]
N-[3'-(trifluoromethyl)-4-biphenylyl]urea DM7OA4R Discovery agent N.A. Investigative [5]
4'-(trifluoromethyl)-4-biphenylsulfonamide DMLP67R Discovery agent N.A. Investigative [5]
N-(4'-chloro-4-biphenylyl)methanesulfonamide DM0ARP8 Discovery agent N.A. Investigative [5]
ISIS 183881 DMOU9EP Discovery agent N.A. Investigative [6]
ISIS 183911 DMTB350 Discovery agent N.A. Investigative [7]
4'-(trifluoromethyl)-4-biphenylyl carbamate DMT3BX9 Discovery agent N.A. Investigative [5]
ISIS 183910 DMMQ2L7 Discovery agent N.A. Investigative [7]
2-(difluoromethyl)-9H-carbazole DMZVMDO Discovery agent N.A. Investigative [8]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Cisplatin DMRHGI9 Adenocarcinoma 2D40 Approved [9]
Methotrexate DM2TEOL Anterior urethra cancer Approved [10]
Zidovudine DM4KI7O Human immunodeficiency virus infection 1C62 Approved [11]
Arsenic trioxide DM61TA4 Acute lymphoblastic leukaemia 2A85 Approved [12]
Cidofovir DMA13GD Cytomegalovirus infection 1D82 Approved [13]
Paclitaxel DMLB81S Breast carcinoma Approved [14]
Floxuridine DM04LR2 Colorectal cancer 2B91.Z Approved [15]
Cannabidiol DM0659E Dravet syndrome 8A61.11 Approved [16]
Mechlorethamine DM0CVXA Chronic myelogenous leukaemia 2A20.0 Approved [17]
Fulvestrant DM0YZC6 Breast cancer 2C60-2C65 Approved [18]
⏷ Show the Full List of 10 Drug(s)
Drug(s) Affected By Histone H2AX (H2AX)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Cannabidiol DM0659E Dravet syndrome 8A61.11 Approved [19]
Hydrogen peroxide DM1NG5W Infectious disease 1A00-CA43.1 Approved [20]
Selenium DM25CGV N. A. N. A. Approved [21]
Ribavirin DMEYLH9 Hepatitis C virus infection 1E51.1 Approved [22]
Etretinate DM2CZFA Keratosis ED56 Approved [23]
Methotrexate DM2TEOL Anterior urethra cancer Approved [24]
Dactinomycin DM2YGNW Adult kidney Wilms tumor Approved [25]
Simvastatin DM30SGU Arteriosclerosis BD40 Approved [26]
Lapatinib DM3BH1Y Breast cancer 2C60-2C65 Approved [27]
Quercetin DM3NC4M Obesity 5B81 Approved [28]
⏷ Show the Full List of 10 Drug(s)

Molecular Interaction Atlas of This Drug

Molecular Interaction Atlas

Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
Kinesin spindle messenger RNA (KIF11 mRNA) TTBGTCW KIF11_HUMAN Inhibitor [2]

Drug Off-Target (DOT)
DOT Name DOT ID UniProt ID Interaction REF
Cellular tumor antigen p53 (TP53) OTIE1VH3 P53_HUMAN Gene/Protein Processing [3]
E3 ubiquitin-protein ligase XIAP OT24GP9B XIAP_HUMAN Gene/Protein Processing [3]
Histone H2AX (H2AX) OT18UX57 H2AX_HUMAN Gene/Protein Processing [3]

References

1 Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800027260)
2 The discovery and optimization of hexahydro-2H-pyrano[3,2-c]quinolines (HHPQs) as potent and selective inhibitors of the mitotic kinesin-5. Bioorg Med Chem Lett. 2010 Mar 1;20(5):1491-5.
3 Cell type variation in responses to antimitotic drugs that target microtubules and kinesin-5. Cancer Res. 2008 May 1;68(9):3269-76. doi: 10.1158/0008-5472.CAN-07-6699.
4 Clinical pipeline report, company report or official report of Alnylam Pharmaceuticals, Inc (2011).
5 Novel ATP-competitive kinesin spindle protein inhibitors. J Med Chem. 2007 Oct 4;50(20):4939-52.
6 US patent application no. 7,407,943, Antisense modulation of apolipoprotein B expression.
7 US patent application no. 7,163,927, Antisense modulation of kinesin-like 1 expression.
8 Kinesin spindle protein (KSP) inhibitors with 2,3-fused indole scaffolds. J Med Chem. 2010 Jul 8;53(13):5054-8.
9 p53-R175H mutant gains new function in regulation of doxorubicin-induced apoptosis. Int J Cancer. 2005 Apr 10;114(3):331-6. doi: 10.1002/ijc.20818.
10 The contribution of methotrexate exposure and host factors on transcriptional variance in human liver. Toxicol Sci. 2007 Jun;97(2):582-94.
11 Azidothymidine and cisplatin increase p14ARF expression in OVCAR-3 ovarian cancer cell line. Toxicol Appl Pharmacol. 2006 Oct 1;216(1):89-97. doi: 10.1016/j.taap.2006.04.015. Epub 2006 May 19.
12 Quantitative analysis of gene expression changes in response to genotoxic compounds. Toxicol In Vitro. 2017 Mar;39:15-28. doi: 10.1016/j.tiv.2016.11.004. Epub 2016 Nov 5.
13 Induction of apoptosis by cidofovir in human papillomavirus (HPV)-positive cells. Oncol Res. 2000;12(9-10):397-408. doi: 10.3727/096504001108747855.
14 Gallic acid potentiates the apoptotic effect of paclitaxel and carboplatin via overexpression of Bax and P53 on the MCF-7 human breast cancer cell line. J Biochem Mol Toxicol. 2021 Feb;35(2):e22638. doi: 10.1002/jbt.22638. Epub 2020 Oct 1.
15 Regulation of human dUTPase gene expression and p53-mediated transcriptional repression in response to oxaliplatin-induced DNA damage. Nucleic Acids Res. 2009 Jan;37(1):78-95. doi: 10.1093/nar/gkn910. Epub 2008 Nov 16.
16 Role of miRNA in the regulation of cannabidiol-mediated apoptosis in neuroblastoma cells. Oncotarget. 2019 Jan 1;10(1):45-59. doi: 10.18632/oncotarget.26534. eCollection 2019 Jan 1.
17 Nitrogen Mustard Alkylates and Cross-Links p53 in Human Keratinocytes. Chem Res Toxicol. 2022 Apr 18;35(4):636-650. doi: 10.1021/acs.chemrestox.1c00420. Epub 2022 Mar 21.
18 Fulvestrant induces resistance by modulating GPER and CDK6 expression: implication of methyltransferases, deacetylases and the hSWI/SNF chromatin remodelling complex. Br J Cancer. 2013 Nov 12;109(10):2751-62. doi: 10.1038/bjc.2013.583. Epub 2013 Oct 29.
19 Cannabinoids synergize with carfilzomib, reducing multiple myeloma cells viability and migration. Oncotarget. 2016 Nov 22;7(47):77543-77557. doi: 10.18632/oncotarget.12721.
20 Hsa-let-7g miRNA regulates the anti-tumor effects of gastric cancer cells under oxidative stress through the expression of DDR genes. J Toxicol Sci. 2015 Jun;40(3):329-38. doi: 10.2131/jts.40.329.
21 Selenium and vitamin E: cell type- and intervention-specific tissue effects in prostate cancer. J Natl Cancer Inst. 2009 Mar 4;101(5):306-20.
22 Inhibition of cardiomyocyte differentiation of human induced pluripotent stem cells by Ribavirin: Implication for its cardiac developmental toxicity. Toxicology. 2020 Apr 15;435:152422. doi: 10.1016/j.tox.2020.152422. Epub 2020 Feb 26.
23 Synthesis and structure-activity relationships of new antiproliferative and proapoptotic retinoid-related biphenyl-4-yl-acrylic acids. Bioorg Med Chem. 2007 Jul 15;15(14):4863-75. doi: 10.1016/j.bmc.2007.04.057. Epub 2007 May 3.
24 Methotrexate induces apoptosis through p53/p21-dependent pathway and increases E-cadherin expression through downregulation of HDAC/EZH2. Biochem Pharmacol. 2011 Feb 15;81(4):510-7. doi: 10.1016/j.bcp.2010.11.014. Epub 2010 Nov 27.
25 Actinomycin D inhibits the expression of the cystine/glutamate transporter xCT via attenuation of CD133 synthesis in CD133(+) HCC. Chem Biol Interact. 2019 Aug 25;309:108713. doi: 10.1016/j.cbi.2019.06.026. Epub 2019 Jun 19.
26 Simvastatin and purine analogs have a synergic effect on apoptosis of chronic lymphocytic leukemia cells. Ann Hematol. 2010 Nov;89(11):1115-24. doi: 10.1007/s00277-010-0988-z. Epub 2010 May 25.
27 The involvement of hepatic cytochrome P450s in the cytotoxicity of lapatinib. Toxicol Sci. 2023 Dec 21;197(1):69-78. doi: 10.1093/toxsci/kfad099.
28 The isoflavonoids genistein and quercetin activate different stress signaling pathways as shown by analysis of site-specific phosphorylation of ATM, p53 and histone H2AX. DNA Repair (Amst). 2004 Mar 4;3(3):235-44. doi: 10.1016/j.dnarep.2003.10.014.