Itk kinase inhibitors: Initial efforts to improve the metabolical stability and the cell activity of the benzimidazole lead

Bioorganic and Medicinal Chemistry Letters

Volumn 18, Issue 20, 2008, Pages 5537-5540

  Moriarty, Kevin J ^b   Winters, Michael ^b   Qiao, Lei ^b   Ryan, Declan ^b   DesJarlis, Renee ^b   Robinson, Darius ^b   Cook, Brian N ^a   Kashem, Mohammed A ^a   Kaplita, Paul V ^a   Liu, Lisa H ^a   Farrell, Thomas M ^a   Khine, Hnin Hnin ^a   King, Josephine ^a   Pullen, Steven S ^a   Roth, Gregory P ^c   Magolda, Ronald ^a   Takahashi, Hidenori ^a  

^a BOEHRINGER INGELHEIM PHARMACEUTICALS INC   (United States)

^b PRDUS LLC   (United States)

^c Burnham Institute for Medical Research at Lake Nona   (United States)

Author keywords

Itk inhibitor; Liver microsomes; Metabolic stability; SAR

Indexed keywords

BENZIMIDAZOLE; ITK KINASE INHIBITOR; PHOSPHOTRANSFERASE INHIBITOR; UNCLASSIFIED DRUG;

ARTICLE; CELL ACTIVITY; DRUG POTENCY; DRUG SELECTIVITY; DRUG STABILITY; LIVER MICROSOME; STRUCTURE ACTIVITY RELATION;

ADENOSINE TRIPHOSPHATE; ADMINISTRATION, ORAL; ANTIGENS, CD3; BENZIMIDAZOLES; BINDING SITES; CHEMISTRY, PHARMACEUTICAL; CRYSTALLOGRAPHY, X-RAY; DRUG DESIGN; ENZYME INHIBITORS; HUMANS; INHIBITORY CONCENTRATION 50; MICROSOMES, LIVER; PROTEIN-TYROSINE KINASES; STRUCTURE-ACTIVITY RELATIONSHIP; T-LYMPHOCYTES;

EID: 53349102853     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2008.09.017     Document Type: Article

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