General Information of Drug (ID: DMQDUG4)

Drug Name
ISIS-CRP Drug Info
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]
Cross-matching ID
TTD Drug ID
DMQDUG4

Molecule(s) Related to 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]

The Expression Level of Molecule(s) in Normal Tissue of Major ADME-Related Organs

Molecule Molecule Type Gene Name Liver Colon Kidney Small Intestine
LCK tyrosine protein kinase (LCK) DTT LCK 5.2 4.443 4.53 6.325
Proto-oncogene c-Src (SRC) DTT SRC 2.907 3.35 3.498 4.75
Molecule Expression Atlas in Normal Tissue of Major ADME-related organs

The Expression Level of Molecule(s) between Disease Section and Healthy Individual Tissue

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 between Disease Section and Healthy Individual Tissue

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.