Discovery of a selective, substrate-competitive inhibitor of the lysine methyltransferase SETD8

Journal of Medicinal Chemistry

Volumn 57, Issue 15, 2014, Pages 6822-6833

  Ma, Anqi ^a   Yu, Wenyu ^d   Li, Fengling ^d   Bleich, Rachel M ^a   Herold, J Martin ^a   Butler, Kyle V ^a   Norris, Jacqueline L ^a   Korboukh, Victoria ^a   Tripathy, Ashutosh ^b   Janzen, William P ^a   Arrowsmith, Cheryl H ^d   Frye, Stephen V ^a   Vedadi, Masoud ^d   Brown, Peter J ^d   Jin, Jian ^a,b,c  

^a University of North Carolina   (United States)

^b UNIVERSITY OF NORTH CAROLINA SCHOOL OF MEDICINE   (United States)

^c UNIVERSITY OF NORTH CAROLINA   (United States)

^d UNIVERSITY OF TORONTO   (Canada)

Author keywords

[No Author keywords available]

Indexed keywords

6,7 DIMETHOXY 2 (PYRROLIDIN 1 YL) N [5 (PYRROLIDIN 1 YL)PENTYL]QUINAZOLIN 4 AMINE; HISTONE LYSINE METHYLTRANSFERASE; HISTONE LYSINE METHYLTRANSFERASE INHIBITOR; LYSINE METHYLTRANSFERASE SETD8; UNC 0379; UNCLASSIFIED DRUG; 6,7-DIMETHOXY-2-(PYRROLIDIN-1-YL)-N-(5-(PYRROLIDIN-1-YL)PENTYL)QUINAZOLIN-4-AMINE; PYRROLIDINE DERIVATIVE; QUINAZOLINE DERIVATIVE;

ARTICLE; BINDING AFFINITY; BIOASSAY; BIOCHEMICAL ASSAY; COMPETITIVE INHIBITION; CONTROLLED STUDY; DRUG IDENTIFICATION; DRUG MECHANISM; DRUG POTENCY; DRUG SELECTIVITY; DRUG SYNTHESIS; ENZYME INHIBITION; IC 50; ISOTHERMAL TITRATION CALORIMETRY; STRUCTURE ACTIVITY RELATION; SURFACE PLASMON RESONANCE; ANTAGONISTS AND INHIBITORS; CALORIMETRY; CHEMISTRY; SYNTHESIS;

CALORIMETRY; HISTONE-LYSINE N-METHYLTRANSFERASE; PYRROLIDINES; QUINAZOLINES; STRUCTURE-ACTIVITY RELATIONSHIP; SURFACE PLASMON RESONANCE;

EID: 84906094286     PISSN: 00222623     EISSN: 15204804     Source Type: Journal    
DOI: 10.1021/jm500871s     Document Type: Article

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