A novel, potent, and selective inhibitor of cardiac late sodium current suppresses experimental arrhythmias
Belardinelli, Luiz, Liu, Gongxin, Smith-Maxwell, Cathy, Wang, Wei-Qun, El-Bizri, Nesrine, Hirakawa, Ryoko, Karpinski, Serge, Li, Cindy Hong, Hu, Lufei, Li, Xiao-Jun, Crumb, William, Wu, Lin, Koltun, Dmitry, Zablocki, Jeff, Yao, Lina, Dhalla, Arvinder K, Rajamani, Sridharan, Shryock, John C
Published in The Journal of pharmacology and experimental therapeutics (01.01.2013)
Published in The Journal of pharmacology and experimental therapeutics (01.01.2013)
Get full text
Journal Article
Discovery of the pan-genotypic hepatitis C virus NS3/4A protease inhibitor voxilaprevir (GS-9857): A component of Vosevi
Taylor, James G., Zipfel, Sheila, Ramey, Kyla, Vivian, Randy, Schrier, Adam, Karki, Kapil K., Katana, Ashley, Kato, Darryl, Kobayashi, Tetsuya, Martinez, Ruben, Sangi, Michael, Siegel, Dustin, Tran, Chinh V., Yang, Zheng-Yu, Zablocki, Jeff, Yang, Cheng Y., Wang, Yujin, Wang, Kelly, Chan, Katie, Barauskas, Ona, Cheng, Guofeng, Jin, Debi, Schultz, Brian E., Appleby, Todd, Villaseñor, Armando G., Link, John O.
Published in Bioorganic & medicinal chemistry letters (15.08.2019)
Published in Bioorganic & medicinal chemistry letters (15.08.2019)
Get full text
Journal Article
Discovery of Dihydrobenzoxazepinone (GS-6615) Late Sodium Current Inhibitor (Late I Nai), a Phase II Agent with Demonstrated Preclinical Anti-Ischemic and Antiarrhythmic Properties
Zablocki, Jeff A, Elzein, Elfatih, Li, Xiaofen, Koltun, Dmitry O, Parkhill, Eric Q, Kobayashi, Tetsuya, Martinez, Ruben, Corkey, Britton, Jiang, Haibo, Perry, Thao, Kalla, Rao, Notte, Gregory T, Saunders, Oliver, Graupe, Michael, Lu, Yafan, Venkataramani, Chandru, Guerrero, Juan, Perry, Jason, Osier, Mark, Strickley, Robert, Liu, Gongxin, Wang, Wei-Qun, Hu, Lufei, Li, Xiao-Jun, El-Bizri, Nesrine, Hirakawa, Ryoko, Kahlig, Kris, Xie, Cheng, Li, Cindy Hong, Dhalla, Arvinder K, Rajamani, Sridharan, Mollova, Nevena, Soohoo, Daniel, Lepist, Eve-Irene, Murray, Bernard, Rhodes, Gerry, Belardinelli, Luiz, Desai, Manoj C
Published in Journal of medicinal chemistry (13.10.2016)
Published in Journal of medicinal chemistry (13.10.2016)
Get full text
Journal Article
Selectivity switch between FAK and Pyk2: Macrocyclization of FAK inhibitors improves Pyk2 potency
Farand, Julie, Mai, Nicholas, Chandrasekhar, Jayaraman, Newby, Zachary E., Van Veldhuizen, Josh, Loyer-Drew, Jennifer, Venkataramani, Chandrasekar, Guerrero, Juan, Kwok, Amy, Li, Ning, Zherebina, Yelena, Wilbert, Sibylle, Zablocki, Jeff, Phillips, Gary, Watkins, William J., Mourey, Robert, Notte, Gregory T.
Published in Bioorganic & medicinal chemistry letters (15.12.2016)
Published in Bioorganic & medicinal chemistry letters (15.12.2016)
Get full text
Journal Article
Discovery of triazolopyridine GS-458967, a late sodium current inhibitor (Late INai) of the cardiac NaV 1.5 channel with improved efficacy and potency relative to ranolazine
Koltun, Dmitry O., Parkhill, Eric Q., Elzein, Elfatih, Kobayashi, Tetsuya, Notte, Gregory T., Kalla, Rao, Jiang, Robert H., Li, Xiaofen, Perry, Thao D., Avila, Belem, Wang, Wei-Qun, Smith-Maxwell, Catherine, Dhalla, Arvinder K., Rajamani, Sridharan, Stafford, Brian, Tang, Jennifer, Mollova, Nevena, Belardinelli, Luiz, Zablocki, Jeff A.
Published in Bioorganic & medicinal chemistry letters (01.07.2016)
Published in Bioorganic & medicinal chemistry letters (01.07.2016)
Get full text
Journal Article
Discovery of potent and selective inhibitors of calmodulin-dependent kinase II (CaMKII)
Koltun, Dmitry O., Parkhill, Eric Q., Kalla, Rao, Perry, Thao D., Elzein, Elfatih, Li, Xiaofen, Simonovich, Scott P., Ziebenhaus, Christopher, Hansen, Timothy R., Marchand, Bruno, Hung, WaiLok K., Lagpacan, Leanna, Hung, Magdeleine, Aoyama, Ron G., Murray, Bernard P., Perry, Jason K., Somoza, John R., Villaseñor, Armando G., Pagratis, Nikos, Zablocki, Jeff A.
Published in Bioorganic & medicinal chemistry letters (01.02.2018)
Published in Bioorganic & medicinal chemistry letters (01.02.2018)
Get full text
Journal Article
Marked difference in saxitoxin and tetrodotoxin affinity for the human nociceptive voltage-gated sodium channel (Nav1.7)
Walker, James R, Novick, Paul A, Parsons, William H, McGregor, Malcolm, Zablocki, Jeff, Pande, Vijay S, Du Bois, J
Published in Proceedings of the National Academy of Sciences - PNAS (30.10.2012)
Published in Proceedings of the National Academy of Sciences - PNAS (30.10.2012)
Get full text
Journal Article
Drug Annotations Series Change in Guidelines
Published in Journal of medicinal chemistry
(14.03.2019)
Get full text
Journal Article
Structure-affinity relationships of the affinity of 2-pyrazolyl adenosine analogues for the adenosine A2A receptor
PALLE, Venkata P, ELZEIN, Elfatih O, GOTHE, Scott A, ZHIHE LI, ZHENHAI GAO, MEYER, Stephanie, BLACKBURN, Brent, ZABLOCKI, Jeff A
Published in Bioorganic & medicinal chemistry letters (21.10.2002)
Published in Bioorganic & medicinal chemistry letters (21.10.2002)
Get full text
Journal Article
CVT-4325: a potent fatty acid oxidation inhibitor with favorable oral bioavailability
Elzein, Elfatih, Ibrahim, Prabha, Koltun, Dmitry O., Rehder, Ken, Shenk, Kevin D., Marquart, Timothy A., Jiang, Bob, Li, Xiaofen, Natero, Reina, Li, Yuan, Nguyen, Marie, Kerwar, Suresh, Chu, Nancy, Soohoo, Daniel, Hao, Jia, Maydanik, Victoria Y., Lustig, David A., Zeng, Dewan, Leung, Kwan, Zablocki, Jeff A.
Published in Bioorganic & medicinal chemistry letters (20.12.2004)
Published in Bioorganic & medicinal chemistry letters (20.12.2004)
Get full text
Journal Article
Novel Short-Acting A2A Adenosine Receptor Agonists for Coronary Vasodilation: Inverse Relationship between Affinity and Duration of Action of A2A Agonists
Gao, Z, Li, Z, Baker, S P, Lasley, R D, Meyer, S, Elzein, E, Palle, V, Zablocki, J A, Blackburn, B, Belardinelli, L
Published in The Journal of pharmacology and experimental therapeutics (01.07.2001)
Get full text
Published in The Journal of pharmacology and experimental therapeutics (01.07.2001)
Journal Article
Structure-affinity relationships of 5'-aromatic ethers and 5'-aromatic sulfides as partial A1 adenosine agonists, potential supraventricular anti-arrhythmic agents
MORRISON, Christopher F, ELZEIN, Elfatih, YUZHI WU, DEWAN ZENG, IRVING FONG, LUSTIG, David, KWAN LEUNG, ZABLOCKI, Jeff A, JIANG, Bob, IBRAHIM, Prabha N, MARQUART, Timothy, PALLE, Venkata, SHENK, Kevin D, VARKHEDKAR, Vaibhav, TENNING MAA, LIN WU
Published in Bioorganic & medicinal chemistry letters (16.07.2004)
Published in Bioorganic & medicinal chemistry letters (16.07.2004)
Get full text
Journal Article
Discovery of GS-9688 (Selgantolimod) as a Potent and Selective Oral Toll-Like Receptor 8 Agonist for the Treatment of Chronic Hepatitis B
Mackman, Richard L, Mish, Michael, Chin, Gregory, Perry, Jason K, Appleby, Todd, Aktoudianakis, Vangelis, Metobo, Sammy, Pyun, Peter, Niu, Congrong, Daffis, Stephane, Yu, Helen, Zheng, Jim, Villasenor, Armando G, Zablocki, Jeff, Chamberlain, Jason, Jin, Haolun, Lee, Gary, Suekawa-Pirrone, Kimberley, Santos, Rex, Delaney, William E, Fletcher, Simon P
Published in Journal of medicinal chemistry (24.09.2020)
Published in Journal of medicinal chemistry (24.09.2020)
Get full text
Journal Article
Affinity and intrinsic efficacy (IE) of 5'-carbamoyl adenosine analogues for the A1 adenosine receptor: efforts towards the discovery of a chronic ventricular rate control agent for the treatment of atrial fibrillation (AF)
PALLE, Venkata P, VARKHEDKAR, Vaibhav, KWAN LEUNG, CHU, Nancy, ZABLOCKI, Jeff A, IBRAHIM, Prabha, AHMED, Hiba, ZHIHE LI, ZHENHAI GAO, OZECK, Mark, YUZHI WU, DEWAN ZENG, LIN WU
Published in Bioorganic & medicinal chemistry letters (19.01.2004)
Published in Bioorganic & medicinal chemistry letters (19.01.2004)
Get full text
Journal Article
Marked difference in saxitoxin and tetrodoxin affinity for the human nociceptive voltage-gated sodium channel (Naᵥ1.7)
Walker, James R, Novick, Paul A, Parsons, William H, McGregor, Malcolm, Zablocki, Jeff, Pande, Vijay S, Du Bois, J
Published in Proceedings of the National Academy of Sciences - PNAS (30.10.2012)
Published in Proceedings of the National Academy of Sciences - PNAS (30.10.2012)
Get full text
Journal Article
The novel late Na+ current inhibitor, GS‐6615 (eleclazine) and its anti‐arrhythmic effects in rabbit isolated heart preparations
Rajamani, Sridharan, Liu, Gongxin, El‐Bizri, Nesrine, Guo, Donglin, Li, Cindy, Chen, Xiao‐Liang, Kahlig, Kristopher M, Mollova, Nevena, Elzein, Elfatih, Zablocki, Jeff, Belardinelli, Luiz
Published in British journal of pharmacology (01.11.2016)
Published in British journal of pharmacology (01.11.2016)
Get full text
Journal Article