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

General Information of DTT (ID: TT9ABMF)

• DTT Name: Serine/threonine-protein kinase Chk2 (RAD53) DTT Info
• UniProt ID: CHK2_HUMAN
• Gene Name: CHEK2

Molecule-Related Drug & Molecule List

1 Clinical Trial Drug(s) Transported by This DTP

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
E7850	DM8K5IF	Solid tumour/cancer	2A00-2F9Z	Phase 2	[1]

1 Patented Agent(s) Transported by This DTP

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
PMID27410995-Compound-Figure3j	DMJRZLB	N. A.	N. A.	Patented	[2]

1 Discontinued Drug(s) Transported by This DTP

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
XL844	DMHTG38	Solid tumour/cancer	2A00-2F9Z	Discontinued in Phase 1	[3]

7 Investigative Drug(s) Transported by This DTP

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
2-(4-Phenoxy-phenyl)-1H-benzoimidazol-5-ylamine	DMSPOAT	Discovery agent	N.A.	Investigative	[4]
5-Nitro-2-(4-phenoxy-phenyl)-1H-benzoimidazole	DM26MIC	Discovery agent	N.A.	Investigative	[4]
CCT-241533	DMZXFT9	Solid tumour/cancer	2A00-2F9Z	Investigative	[5]
Chk2 inhibitor II	DMNSPFG	Discovery agent	N.A.	Investigative	[6]
DEBROMOHYMENIALDISINE	DMDLER8	Discovery agent	N.A.	Investigative	[7]
PMID22564207C25b	DMBMYKQ	Discovery agent	N.A.	Investigative	[8]
PV-1019	DMRI1LF	Solid tumour/cancer	2A00-2F9Z	Investigative	[9]

References

• [1] 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: 1988).
• [2] Ribosomal S6 kinase (RSK) modulators: a patent review.Expert Opin Ther Pat. 2016 Sep;26(9):1061-78.
• [3] Interpreting expression profiles of cancers by genome-wide survey of breadth of expression in normal tissues. Genomics 2005 Aug;86(2):127-41.
• [4] Checkpoint kinase inhibitors: SAR and radioprotective properties of a series of 2-arylbenzimidazoles. J Med Chem. 2005 Mar 24;48(6):1873-85.
• [5] CCT241533 Is a Potent and Selective Inhibitor of CHK2 that Potentiates the Cytotoxicity of PARP Inhibitors. Cancer Res. 2011 Jan 15;71(2):463-72.
• [6] A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. Proc Natl Acad Sci U S A. 2007 Dec 18;104(51):20523-8.
• [7] Potent inhibition of checkpoint kinase activity by a hymenialdisine-derived indoloazepine. Bioorg Med Chem Lett. 2004 Aug 16;14(16):4319-21.
• [8] Discovery of an orally efficacious inhibitor of anaplastic lymphoma kinase. J Med Chem. 2012 May 24;55(10):4580-93.
• [9] Cellular inhibition of checkpoint kinase 2 (Chk2) and potentiation of camptothecins and radiation by the novel Chk2 inhibitor PV1019 [7-nitro-1H-indole-2-carboxylic acid {4-[1-(guanidinohydrazone)-ethyl]-phenyl}-amide]. J Pharmacol Exp Ther. 2009 Dec;331(3):816-26.