S. Chmait

发表

Discovery of potent, selective, and metabolically stable 4-(pyridin-3-yl)cinnolines as novel phosphodiesterase 10A (PDE10A) inhibitors.

E. Hu, R. Kunz, Shannon Rumfelt, 2012, Bioorganic & medicinal chemistry letters.

Discovery and Structure-Guided Optimization of Diarylmethanesulfonamide Disrupters of Glucokinase-Glucokinase Regulatory Protein (GK-GKRP) Binding: Strategic Use of a N → S (nN → σ*S-X) Interaction for Conformational Constraint.

Kristin L. Andrews, Jiandong Zhang, S. Chmait, 2015, Journal of medicinal chemistry.

Small molecule disruptors of the glucokinase-glucokinase regulatory protein interaction: 4. Exploration of a novel binding pocket.

S. Chmait, M. Bartberger, S. Jordan, 2014, Journal of medicinal chemistry.

Small molecule disruptors of the glucokinase-glucokinase regulatory protein interaction: 2. Leveraging structure-based drug design to identify analogues with improved pharmacokinetic profiles.

R. Kunz, Jiandong Zhang, S. Chmait, 2014, Journal of medicinal chemistry.

Identification of triazolopyridazinones as potent p38α inhibitors.

S. Chmait, B. Herberich, Matthew R. Lee, 2012, Bioorganic & medicinal chemistry letters.

Part 2: Structure-activity relationship (SAR) investigations of fused pyrazoles as potent, selective and orally available inhibitors of p38alpha mitogen-activated protein kinase.

S. Chmait, K. Miner, Matthew R. Lee, 2010, Bioorganic & medicinal chemistry letters.

Discovery and evaluation of 7-alkyl-1,5-bis-aryl-pyrazolopyridinones as highly potent, selective, and orally efficacious inhibitors of p38alpha mitogen-activated protein kinase.

Christopher Mohr, Lisa Sherman, S. Chmait, 2010, Journal of medicinal chemistry.

Small Molecule Disruptors of the Glucokinase-Glucokinase Regulatory Protein Interaction: 5. A Novel Aryl Sulfone Series, Optimization Through Conformational Analysis.

S. Chmait, M. Bartberger, S. Jordan, 2015, Journal of medicinal chemistry.

Discovery of Novel Imidazo[4,5-b]pyridines as Potent and Selective Inhibitors of Phosphodiesterase 10A (PDE10A).

E. Hu, S. Chmait, J. Treanor, 2014, ACS medicinal chemistry letters.

Small molecule disruptors of the glucokinase-glucokinase regulatory protein interaction: 3. Structure-activity relationships within the aryl carbinol region of the N-arylsulfonamido-N'-arylpiperazine series.

R. Kunz, S. Chmait, M. Bartberger, 2014, Journal of medicinal chemistry.

Small molecule disruptors of the glucokinase-glucokinase regulatory protein interaction: 1. Discovery of a novel tool compound for in vivo proof-of-concept.

R. Wahl, Jiandong Zhang, S. Chmait, 2014, Journal of medicinal chemistry.

Antidiabetic effects of glucokinase regulatory protein small-molecule disruptors

R. Wahl, Jiandong Zhang, S. Chmait, 2013, Nature.

Part 1: Structure-Activity Relationship (SAR) investigations of fused pyrazoles as potent, selective and orally available inhibitors of p38alpha mitogen-activated protein kinase.

S. Chmait, K. Miner, Matthew R. Lee, 2009, Bioorganic & medicinal chemistry letters.

Design, optimization, and biological evaluation of novel keto-benzimidazoles as potent and selective inhibitors of phosphodiesterase 10A (PDE10A).

E. Hu, R. Kunz, Shannon Rumfelt, 2013, Journal of medicinal chemistry.

Discovery of clinical candidate 1-(4-(3-(4-(1H-benzo[d]imidazole-2-carbonyl)phenoxy)pyrazin-2-yl)piperidin-1-yl)ethanone (AMG 579), a potent, selective, and efficacious inhibitor of phosphodiesterase 10A (PDE10A).

E. Hu, R. Kunz, N. Chen, 2014, Journal of medicinal chemistry.

Synthesis and preliminary biological evaluation of potent and selective 2-(3-alkoxy-1-azetidinyl) quinolines as novel PDE10A inhibitors with improved solubility.

E. Hu, R. Kunz, N. Chen, 2014, Bioorganic & medicinal chemistry.

Discovery of selective biaryl ethers as PDE10A inhibitors: improvement in potency and mitigation of Pgp-mediated efflux.

E. Hu, Shannon Rumfelt, N. Chen, 2012, Bioorganic & medicinal chemistry letters.

Discovery and evaluation of 7-alkyl-1,5-bis-aryl-pyrazolopyridinones as highly potent, selective, and orally efficacious inhibitors of p38alpha mitogen-activated protein kinase.

S. Chmait, B. Herberich, Matthew R. Lee, 2010, Journal of medicinal chemistry.

Discovery of clinical candidate 1-(4-(3-(4-(1H-benzo[d]imidazole-2-carbonyl)phenoxy)pyrazin-2-yl)piperidin-1-yl)ethanone (AMG 579), a potent, selective, and efficacious inhibitor of phosphodiesterase 10A (PDE10A).

E. Hu, R. Kunz, N. Chen, 2014, Journal of medicinal chemistry.