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
PubChem CID
71618507
TTD Drug ID
DMRI1LF

Molecule-Related Drug Atlas

Molecule-Related Drug Atlas
Molecule Type:
DTT
Drug Status:
Clinical Trial Drug(s)
Patented Agent(s)
Discontinued Drug(s)
Investigative Drug(s)
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]
⏷ Show the Full List of 9 Drug(s)

Molecular Interaction Atlas of This Drug

Molecular Interaction Atlas

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

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.