Target Validation Information
Target ID T77764
Target Name mRNA of Aurora B
Target Type
Clinical Trial
Drug Potency against Target 6-bromoindirubin-3-oxime Drug Info IC50 = 900 nM [528968]
4-(1H-pyrazol-4-yl)-1H-pyrrolo[2,3-b]pyridine Drug Info IC50 = 782 nM [530806]
7-fluoroindirubin-3-acetoxime Drug Info IC50 = 8000 nM [528968]
Indirubin-3-methoxime Drug Info IC50 = 3000 nM [528968]
CGP-57380 Drug Info IC50 = 2500 nM [529039]
7-iodoindirubin-3-oxime Drug Info IC50 = 10000 nM [528968]
Indirubin-3-acetoxime Drug Info IC50 = 2100 nM [528968]
Indirubin-3-oxime Drug Info IC50 = 2300 nM [528968]
7-bromoindirubin-3-oxime Drug Info IC50 = 4600 nM [528968]
SU 6656 Drug Info IC50 = 19 nM [529039]
4-(4'-Benzamidoanilino)-6,7-dimethoxyquinazoline Drug Info IC50 = 1250 nM [529213]
AZD-1152-HQPA Drug Info IC50 = 17 nM [530037]
HESPERADIN Drug Info IC50 = 250 nM [528000]
PHA-739358 Drug Info IC50 = 135 nM [527513]
7-fluoroindirubin-3-oxime Drug Info IC50 = 7000 nM [528968]
7-chloroindirubin-3-oxime Drug Info IC50 = 8000 nM [528968]
References
Ref 528968J Med Chem. 2007 Aug 23;50(17):4027-37. Epub 2007 Aug 1.An integrated computational approach to the phenomenon of potent and selective inhibition of aurora kinases B and C by a series of 7-substituted indirubins.
Ref 530806Bioorg Med Chem Lett. 2010 Apr 15;20(8):2552-5. Epub 2010 Mar 1.Discovery of a new series of Aurora inhibitors through truncation of GSK1070916.
Ref 528968J Med Chem. 2007 Aug 23;50(17):4027-37. Epub 2007 Aug 1.An integrated computational approach to the phenomenon of potent and selective inhibition of aurora kinases B and C by a series of 7-substituted indirubins.
Ref 528968J Med Chem. 2007 Aug 23;50(17):4027-37. Epub 2007 Aug 1.An integrated computational approach to the phenomenon of potent and selective inhibition of aurora kinases B and C by a series of 7-substituted indirubins.
Ref 529039Biochem J. 2007 Dec 15;408(3):297-315.The selectivity of protein kinase inhibitors: a further update.
Ref 528968J Med Chem. 2007 Aug 23;50(17):4027-37. Epub 2007 Aug 1.An integrated computational approach to the phenomenon of potent and selective inhibition of aurora kinases B and C by a series of 7-substituted indirubins.
Ref 528968J Med Chem. 2007 Aug 23;50(17):4027-37. Epub 2007 Aug 1.An integrated computational approach to the phenomenon of potent and selective inhibition of aurora kinases B and C by a series of 7-substituted indirubins.
Ref 528968J Med Chem. 2007 Aug 23;50(17):4027-37. Epub 2007 Aug 1.An integrated computational approach to the phenomenon of potent and selective inhibition of aurora kinases B and C by a series of 7-substituted indirubins.
Ref 528968J Med Chem. 2007 Aug 23;50(17):4027-37. Epub 2007 Aug 1.An integrated computational approach to the phenomenon of potent and selective inhibition of aurora kinases B and C by a series of 7-substituted indirubins.
Ref 529039Biochem J. 2007 Dec 15;408(3):297-315.The selectivity of protein kinase inhibitors: a further update.
Ref 529213Proc Natl Acad Sci U S A. 2007 Dec 18;104(51):20523-8. Epub 2007 Dec 11.A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases.
Ref 530037J Med Chem. 2009 May 14;52(9):2629-51.Discovery and development of aurora kinase inhibitors as anticancer agents.
Ref 528000J Med Chem. 2006 Feb 9;49(3):955-70.Discovery of novel and potent thiazoloquinazolines as selective Aurora A and B kinase inhibitors.
Ref 527513J 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 528968J Med Chem. 2007 Aug 23;50(17):4027-37. Epub 2007 Aug 1.An integrated computational approach to the phenomenon of potent and selective inhibition of aurora kinases B and C by a series of 7-substituted indirubins.
Ref 528968J Med Chem. 2007 Aug 23;50(17):4027-37. Epub 2007 Aug 1.An integrated computational approach to the phenomenon of potent and selective inhibition of aurora kinases B and C by a series of 7-substituted indirubins.

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