Discovery of omecamtiv mecarbil the first, selective, small molecule activator of cardiac myosin

ACS Medicinal Chemistry Letters

Volumn 1, Issue 9, 2010, Pages 472-477

  Morgan, Bradley P ^a   Muci, Alexander ^a   Lu, Pu Ping ^a   Qian, Xiangping ^a   Tochimoto, Todd ^a   Smith, Whitney W ^a   Garard, Marc ^a   Kraynack, Erica ^a   Collibee, Scott ^a   Suehiro, Ion ^a   Tomasi, Adam ^a   Valdez, S Corey ^a   Wang, Wenyue ^a   Jiang, Hong ^a   Hartman, James ^a   Rodriguez, Hector M ^a   Kawas, Raja ^a   Sylvester, Sheila ^a   Elias, Kathleen A ^a   Godinez, Guillermo ^a   Lee, Kenneth ^a   Anderson, Robert ^a   Sueoka, Sandra ^a   Xu, Donghong ^a   Wang, Zhengping ^a   Djordjevic, Nebojsa ^a   Malik, Fady I ^a   Morgans, David J ^a   more..

^a Cytokinetics Inc   (United States)

Author keywords

cardiac myosin; Omecamtiv mecarbil; small molecule enzyme activator; systolic heart failure

Indexed keywords

CARDIAC AGENT; CARDIAC MYOSIN; CK 1316189; CK 1317138; ENZYME ACTIVATOR; OMECAMTIV MECARBIL; UNCLASSIFIED DRUG;

ANIMAL CELL; ANIMAL EXPERIMENT; ANIMAL MODEL; ARTICLE; CONTROLLED STUDY; DRUG DESIGN; DRUG POTENCY; DRUG SOLUBILITY; HIGH THROUGHPUT SCREENING; NONHUMAN; PRIORITY JOURNAL; PROTEIN BINDING; RAT; SARCOMERE; STRUCTURE ACTIVITY RELATION; SYSTOLIC HEART FAILURE;

EID: 78650221832     PISSN: None     EISSN: 19485875     Source Type: Journal    
DOI: 10.1021/ml100138q     Document Type: Article

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9. Compound specificity with respect to muscle type was evaluated by comparing the effect of the compound on the actin-stimulated ATPase activity of a panel of myosin isoforms [cardiac (bovine), skeletal (rabbit), and smooth muscle (bovine uterus or chicken gizzard)] at a single dose of 40, 50, or 100 μM compound. The data for compound 1 are shown in Figure S1 in the Supporting Information.
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