Optimization of a Dibenzodiazepine Hit to a Potent and Selective Allosteric PAK1 Inhibitor

ACS Medicinal Chemistry Letters

Volumn 6, Issue 7, 2015, Pages 776-781

  Karpov, Alexei S ^a   Amiri, Payman ^b   Bellamacina, Cornelia ^b   Bellance, Marie Helene ^a   Breitenstein, Werner ^a   Daniel, Dylan ^b   Denay, Regis ^a   Fabbro, Doriano ^a   Fernandez, Cesar ^a   Galuba, Inga ^a   Guerro Lagasse, Stephanie ^a   Gutmann, Sascha ^a   Hinh, Linda ^b   Jahnke, Wolfgang ^a   Klopp, Julia ^a   Lai, Albert ^b   Lindvall, Mika K ^b   Ma, Sylvia ^b   Möbitz, Henrik ^a   Pecchi, Sabina ^b   Rummel, Gabriele ^a   Shoemaker, Kevin ^b   Trappe, Joerg ^a   Voliva, Charles ^b   Cowan Jacob, Sandra W ^a   Marzinzik, Andreas L ^a   more..

^a NOVARTIS PHARMA AG   (Switzerland)

^b NOVARTIS INSTITUTES FOR BIOMEDICAL RESEARCH   (United States)

Author keywords

allosteric inhibitor; dibenzodiazepine; p21 activated kinase; PAK1; tool compound

Indexed keywords

BENZODIAZEPINE DERIVATIVE; DIBENZODIAZEPINE DERIVATIVE; ENZYME INHIBITOR; FRAX 486; FRAX 597; IPA 3; P21 ACTIVATED KINASE 1; P21 ACTIVATED KINASE 2; P21 ACTIVATED KINASE 3; P21 ACTIVATED KINASE 4; P21 ACTIVATED KINASE 5; P21 ACTIVATED KINASE 6; PF 3758309; UNCLASSIFIED DRUG;

ALLOSTERISM; ARTICLE; AUTOPHOSPHORYLATION; BINDING SITE; DRUG POTENCY; ENZYME INHIBITION; LIVER MICROSOME; NONHUMAN; PRIORITY JOURNAL; PROCESS OPTIMIZATION; RAT; STRUCTURE ACTIVITY RELATION;

EID: 84938058345     PISSN: None     EISSN: 19485875     Source Type: Journal    
DOI: 10.1021/acsmedchemlett.5b00102     Document Type: Article

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