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

General Information of Drug (ID: DMRI1LF)

Drug Name

PV-1019 Drug Info

Synonyms

Checkpoint kinase 2 inhibitor (cancer), Provid Pharmaceuticals; Chk2 inhibitor (cancer), Provid Pharmaceuticals

Indication

Disease Entry	ICD 11	Status	REF
Solid tumour/cancer	2A00-2F9Z	Investigative	[1]

Cross-matching ID

Molecule-Related Drug Atlas

Molecule Type:

DTT

Drug Status:

Clinical Trial Drug(s)

Patented Agent(s)

Discontinued Drug(s)

Investigative Drug(s)

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Drug(s) Targeting Serine/threonine-protein kinase Chk2 (RAD53)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
E7850	DM8K5IF	Solid tumour/cancer	2A00-2F9Z	Phase 2	[2]
PMID27410995-Compound-Figure3j	DMJRZLB	N. A.	N. A.	Patented	[3]
XL844	DMHTG38	Solid tumour/cancer	2A00-2F9Z	Discontinued in Phase 1	[4]
PMID22564207C25b	DMBMYKQ	Discovery agent	N.A.	Investigative	[5]
DEBROMOHYMENIALDISINE	DMDLER8	Discovery agent	N.A.	Investigative	[6]
2-(4-Phenoxy-phenyl)-1H-benzoimidazol-5-ylamine	DMSPOAT	Discovery agent	N.A.	Investigative	[7]
5-Nitro-2-(4-phenoxy-phenyl)-1H-benzoimidazole	DM26MIC	Discovery agent	N.A.	Investigative	[7]
CCT-241533	DMZXFT9	Solid tumour/cancer	2A00-2F9Z	Investigative	[8]
Chk2 inhibitor II	DMNSPFG	Discovery agent	N.A.	Investigative	[9]
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Molecular Interaction Atlas of This Drug

Molecular Interaction Atlas

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Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Serine/threonine-protein kinase Chk2 (RAD53)	TT9ABMF	CHK2_HUMAN	Inhibitor	[1]

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References

1	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.
2	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).
3	Ribosomal S6 kinase (RSK) modulators: a patent review.Expert Opin Ther Pat. 2016 Sep;26(9):1061-78.
4	Interpreting expression profiles of cancers by genome-wide survey of breadth of expression in normal tissues. Genomics 2005 Aug;86(2):127-41.
5	Discovery of an orally efficacious inhibitor of anaplastic lymphoma kinase. J Med Chem. 2012 May 24;55(10):4580-93.
6	Potent inhibition of checkpoint kinase activity by a hymenialdisine-derived indoloazepine. Bioorg Med Chem Lett. 2004 Aug 16;14(16):4319-21.
7	Checkpoint kinase inhibitors: SAR and radioprotective properties of a series of 2-arylbenzimidazoles. J Med Chem. 2005 Mar 24;48(6):1873-85.
8	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.
9	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.