Details of the Drug

General Information of Drug (ID: DMQDUG4)

Drug Name
ISIS-CRP
Synonyms
1-(Tert-butyl)-3-(4-chlorophenyl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine; 172889-27-9; pp2; PP 2; 1-(tert-butyl)-3-(4-chlorophenyl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine; AG 1879; 1-tert-butyl-3-(4-chlorophenyl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine; PP2; 4-Amino-5-(4-chlorophenyl)-7-(t-butyl)pyrazolo[3,4-d]pyrimidine; AG-1879; CHEMBL406845; CHEBI:78331; AK-60369; 1-tert-butyl-3-(4-chlorophenyl)pyrazolo[3,4-d]pyrimidin-4-amine; 3-(4-chlorophenyl) 1-(1,1-dimethylethyl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine; C15H16ClN5; 1qpe; 4few; PBBRWFOVCUAONR-UHFFFAOYSA-N; AG1879; PP 2 (AG 1879)
Indication
Disease Entry ICD 11 Status REF
Cardiovascular disease BA00-BE2Z Phase 1 [1]
Inflammation 1A00-CA43.1 Phase 1 [1]
Drug Type
Antisense drug
Cross-matching ID
TTD ID
D06CIJ

Molecular Interaction Atlas of This Drug


Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
CRP messenger RNA (CRP mRNA) TTWRN6M CRP_HUMAN Not Available [2], [1]
LCK tyrosine protein kinase (LCK) TT860QF LCK_HUMAN Inhibitor [3]
Proto-oncogene c-Src (SRC) TT6PKBN SRC_HUMAN Inhibitor [3]
RIP2 messenger RNA (RIP2 mRNA) TTCQ2E5 RIPK2_HUMAN Inhibitor [3]
Tyrosine-protein kinase ABL1 (ABL) TT3PJMV ABL1_HUMAN Inhibitor [4]
Tyrosine-protein kinase BRK (PTK6) TT6TH8V PTK6_HUMAN Inhibitor [5]
Molecular Interaction Atlas (MIA) Jump to Detail Molecular Interaction Atlas of This Drug

Molecular Expression Atlas of This Drug

The Studied Disease Cardiovascular disease
ICD Disease Classification BA00-BE2Z
Molecule Name Molecule Type Gene Name p-value Fold-Change Z-score
LCK tyrosine protein kinase (LCK) DTT LCK 4.46E-02 -0.13 -1.09
Proto-oncogene c-Src (SRC) DTT SRC 7.46E-03 -0.2 -1.24
Tyrosine-protein kinase ABL1 (ABL) DTT ABL1 6.28E-04 0.33 2.07
Molecular Expression Atlas (MEA) Jump to Detail Molecular Expression Atlas of This Drug

References

1 Clinical pipeline report, company report or official report of ISIS Pharmaceuticals (2011).
2 Clinical pipeline report, company report or official report of ISIS Pharmaceuticals (2009).
3 The selectivity of protein kinase inhibitors: a further update. Biochem J. 2007 Dec 15;408(3):297-315.
4 Structure-based optimization of pyrazolo[3,4-d]pyrimidines as Abl inhibitors and antiproliferative agents toward human leukemia cell lines. J Med Chem. 2008 Mar 13;51(5):1252-9.
5 Inhibition of SRC tyrosine kinase impairs inherent and acquired gemcitabine resistance in human pancreatic adenocarcinoma cells. Clin Cancer Res. 2004 Apr 1;10(7):2307-18.
6 A comparison of physicochemical property profiles of marketed oral drugs and orally bioavailable anti-cancer protein kinase inhibitors in clinical development. Curr Top Med Chem. 2007;7(14):1408-22.
7 National Cancer Institute Drug Dictionary (drug id 596693).
8 Specificity and mechanism of action of some commonly used protein kinase inhibitors. Biochem J. 2000 Oct 1;351(Pt 1):95-105.
9 Optimization of protein kinase CK2 inhibitors derived from 4,5,6,7-tetrabromobenzimidazole. J Med Chem. 2004 Dec 2;47(25):6239-47.
10 The Protein Data Bank. Nucleic Acids Res. 2000 Jan 1;28(1):235-42.
11 Discovery of a (1H-benzoimidazol-2-yl)-1H-pyridin-2-one (BMS-536924) inhibitor of insulin-like growth factor I receptor kinase with in vivo antitum... J Med Chem. 2005 Sep 8;48(18):5639-43.
12 Antisense oligonucleotides on neurobehavior, respiratory, and cardiovascular function, and hERG channel current studies. J Pharmacol Toxicol Methods. 2014 Jan-Feb;69(1):49-60.
13 US patent application no. 7,425,545, Modulation of C-reactive protein expression.
14 How many drug targets are there Nat Rev Drug Discov. 2006 Dec;5(12):993-6.
15 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
16 Synthesis and Src kinase inhibitory activity of a series of 4-[(2,4-dichloro-5-methoxyphenyl)amino]-7-furyl-3-quinolinecarbonitriles. J Med Chem. 2006 Dec 28;49(26):7868-76.
17 Targeted chronic myeloid leukemia therapy: Seeking a cure. Am J Health Syst Pharm. 2007 Dec 15;64(24 Suppl 15):S9-15.
18 Novel dual Src/Abl inhibitors for hematologic and solid malignancies.Expert Opin Investig Drugs.2010 Aug;19(8):931-45.
19 Flumatinib, a selective inhibitor of BCR-ABL/PDGFR/KIT, effectively overcomes drug resistance of certain KIT mutants. Cancer Sci. 2014 Jan;105(1):117-25.
20 Company report (Deciphera Pharmaceuticals: Tumor-Targeted Programs and Indications)
21 KW-2449, a novel multikinase inhibitor, suppresses the growth of leukemia cells with FLT3 mutations or T315I-mutated BCR/ABL translocation. Blood. 2009 Aug 20;114(8):1607-17.
22 Inhibitors of JAK-family kinases: an update on the patent literature 2013-2015, part 1.Expert Opin Ther Pat. 2017 Feb;27(2):127-143.
23 Discovery of novel imidazo[1,2-a]pyrazin-8-amines as Brk/PTK6 inhibitors. Bioorg Med Chem Lett. 2011 Oct 1;21(19):5870-5.
24 In vivo antitumor activity of herbimycin A, a tyrosine kinase inhibitor, targeted against BCR/ABL oncoprotein in mice bearing BCR/ABL-transfected cells. Leuk Res. 1994 Nov;18(11):867-73.
25 Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
26 Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
27 Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
28 Clinical pipeline report, company report or official report of Turning Point Therapeutics.
29 US patent application no. 6,426,221, Antisense modulation of RIP2 expression.