General Information of Drug (ID: DMT3RUE)

Drug Name
PMID16451062C46 Drug Info
Synonyms GTPL8355; GSK-623906A; BDBM50181532
Indication
Disease Entry ICD 11 Status REF
Discovery agent N.A. Investigative [1]
Cross-matching ID
PubChem CID
9916282
TTD Drug ID
DMT3RUE

Molecule-Related Drug Atlas

Molecule-Related Drug Atlas
Molecule Type:
DTT
Drug Status:
Clinical Trial Drug(s)
Investigative Drug(s)
Discontinued Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
PHA-739358 DMGYBZI Prostate cancer 2C82.0 Phase 2 [2]
Indirubin-3'-monoxime DMLRQH0 Discovery agent N.A. Investigative [3]
SU 6656 DMF1P6W Discovery agent N.A. Investigative [4]
6-bromoindirubin-3-oxime DM12WYV Discovery agent N.A. Investigative [3]
7-fluoroindirubin-3-oxime DMQD34N Discovery agent N.A. Investigative [3]
PMID21742770C1 DME3JMH Discovery agent N.A. Investigative [5]
Indirubin-3-acetoxime DM3UR1E Discovery agent N.A. Investigative [3]
CGP-57380 DMFPOUC Discovery agent N.A. Investigative [4]
PMID20855207C25 DMNEB6J Discovery agent N.A. Investigative [6]
Indirubin-3-methoxime DMZ5ODC Discovery agent N.A. Investigative [3]
⏷ Show the Full List of 10 Drug(s)
Drug(s) Targeting Aurora kinase C (AURKC)
Drug Name Drug ID Indication ICD 11 Highest Status REF
PHA-739358 DMGYBZI Prostate cancer 2C82.0 Phase 2 [2]
ABT-348 DMMZOYN Haematological malignancy 2B33.Y Phase 2 [7]
HPP-607 DM5VSZR Solid tumour/cancer 2A00-2F9Z Phase 1 [8]
AMG 900 DMASGXJ Solid tumour/cancer 2A00-2F9Z Phase 1 [9]
SNS-314 DMAC5F2 Solid tumour/cancer 2A00-2F9Z Phase 1 [10]
GSK1070916 DMXRPT6 Advanced solid tumour 2A00-2F9Z Phase 1 [11]
GSK1070916A DMCJUI9 Solid tumour/cancer 2A00-2F9Z Phase 1 [11]
MK-6592 DMB5NOI Solid tumour/cancer 2A00-2F9Z Discontinued in Phase 1 [12]
Indirubin-3'-monoxime DMLRQH0 Discovery agent N.A. Investigative [3]
SU 6656 DMF1P6W Discovery agent N.A. Investigative [4]
⏷ 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
Aurora B messenger RNA (AURKB mRNA) TT9RTBL AURKB_HUMAN Inhibitor [1]
Aurora kinase C (AURKC) TTLYXIT AURKC_HUMAN Inhibitor [1]

References

1 Discovery of novel and potent thiazoloquinazolines as selective Aurora A and B kinase inhibitors. J Med Chem. 2006 Feb 9;49(3):955-70.
2 Potent and selective Aurora inhibitors identified by the expansion of a novel scaffold for protein kinase inhibition. J Med Chem. 2005 Apr 21;48(8):3080-4.
3 An integrated computational approach to the phenomenon of potent and selective inhibition of aurora kinases B and C by a series of 7-substituted in... J Med Chem. 2007 Aug 23;50(17):4027-37.
4 The selectivity of protein kinase inhibitors: a further update. Biochem J. 2007 Dec 15;408(3):297-315.
5 A Potent and Selective Quinoxalinone-Based STK33 Inhibitor Does Not Show Synthetic Lethality in KRAS-Dependent Cells. ACS Med Chem Lett. 2012 Dec 13;3(12):1034-1038.
6 Discovery of orally bioavailable imidazo[1,2-a]pyrazine-based Aurora kinase inhibitors. Bioorg Med Chem Lett. 2010 Nov 15;20(22):6739-43.
7 Preclinical characterization of ABT-348, a kinase inhibitor targeting the aurora, vascular endothelial growth factor receptor/platelet-derived growth factor receptor, and Src kinase families. J Pharmacol Exp Ther. 2012 Dec;343(3):617-27.
8 URL: 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. (Target id: 1936).
9 Preclinical evaluation of AMG 900, a novel potent and highly selective pan-aurora kinase inhibitor with activity in taxane-resistant tumor cell lines. Cancer Res. 2010 Dec 1;70(23):9846-54.
10 SNS-314, a pan-Aurora kinase inhibitor, shows potent anti-tumor activity and dosing flexibility in vivo. Cancer Chemother Pharmacol. 2010 Mar;65(4):707-17.
11 Discovery of GSK1070916, a potent and selective inhibitor of Aurora B/C kinase. J Med Chem. 2010 May 27;53(10):3973-4001.
12 Clinical experience with aurora kinase inhibitors: a review. Oncologist. 2009 Aug;14(8):780-93.