Details of the Drug-Related molecule(s) Interaction Atlas

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

Drug(s) Targeting Aurora B messenger RNA (AURKB mRNA)

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]

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]

Molecular Interaction Atlas of This Drug

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.