2. Academic Validation
  3. Discovery of omecamtiv mecarbil the first, selective, small molecule activator of cardiac Myosin

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

  • ACS Med Chem Lett. 2010 Aug 20;1(9):472-7. doi: 10.1021/ml100138q.
Bradley P Morgan 1,  Alexander Muci 1,  Pu-Ping Lu 1,  Xiangping Qian 1,  Todd Tochimoto 1,  Whitney W Smith 1,  Marc Garard 1,  Erica Kraynack 1,  Scott Collibee 1,  Ion Suehiro 1,  Adam Tomasi 1,  S Corey Valdez 1,  Wenyue Wang 1,  Hong Jiang 1,  James Hartman 1,  Hector M Rodriguez 1,  Raja Kawas 1,  Sheila Sylvester 1,  Kathleen A Elias 1,  Guillermo Godinez 1,  Kenneth Lee 1,  Robert Anderson 1,  Sandra Sueoka 1,  Donghong Xu 1,  Zhengping Wang 1,  Nebojsa Djordjevic 1,  Fady I Malik 1,  David J Morgans Jr 1
Affiliations

Affiliation

  • 1 Cytokinetics, Inc., 280 East Grand Avenue, South San Francisco, California 94080.
PMID: 24900233 DOI: 10.1021/ml100138q
Abstract

We report the design, synthesis, and optimization of the first, selective activators of cardiac Myosin. Starting with a poorly soluble, nitro-aromatic hit compound (1), potent, selective, and soluble Myosin activators were designed culminating in the discovery of omecamtiv mecarbil (24). Compound 24 is currently in clinical trials for the treatment of systolic heart failure.

Keywords

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

Figures
Products
嗨！很高兴为您提供帮助！

尊敬的 MCE 客户您好，
请您选择所在区域，我们将转接对应客服为您服务！

热门区域

A

B

C

F

G

H

J

L

N

Q

S

T

X

Y

Z

热 A B C F G H J L N Q S T X Y Z