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Discovery of novel AKT inhibitors with enhanced anti-tumor effects in combination with the MEK inhibitor

PloS one, 2014-06, Vol.9 (6), p.e100880

2014

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Allosteric Wip1 phosphatase inhibition through flap-subdomain interaction

Nature chemical biology, 2014-03, Vol.10 (3), p.181-187

2014

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Discovery of GSK2656157: An Optimized PERK Inhibitor Selected for Preclinical Development

ACS medicinal chemistry letters, 2013-10, Vol.4 (10), p.964-968

2013

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Structural characterization of dicyanopyridine containing DNMT1-selective, non-nucleoside inhibitors

Structure (London), 2022-06, Vol.30 (6), p.793-802.e5

2022

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Cell-Based Drug Discovery: Identification and Optimization of Small Molecules that Reduce c‑MYC Protein Levels in Cells

Journal of medicinal chemistry, 2021-11, Vol.64 (21), p.16056-16087

2021

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Long-Range Inhibitor-Induced Conformational Regulation of Human IRE1α Endoribonuclease Activity

Molecular pharmacology, 2015-12, Vol.88 (6), p.1011-1023

2015

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1,4-Disubstituted imidazoles are potential antibacterial agents functioning as inhibitors of enoyl acyl carrier protein reductase (FabI)

Bioorganic & medicinal chemistry letters, 2001-08, Vol.11 (16), p.2061-2065

2001

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Characterization of an Akt Kinase Inhibitor with Potent Pharmacodynamic and Antitumor Activity

Cancer research (Chicago, Ill.), 2008-04, Vol.68 (7), p.2366-2374

2008

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Discovery of Isoxazole Amides as Potent and Selective SMYD3 Inhibitors

ACS medicinal chemistry letters, 2020-02, Vol.11 (2), p.133-140

2020

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Aminofurazans as potent inhibitors of AKT kinase

Bioorganic & medicinal chemistry letters, 2009-03, Vol.19 (5), p.1508-1511

2009

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Discovery of a Novel and Potent Class of FabI-Directed Antibacterial Agents

Antimicrobial Agents and Chemotherapy, 2002-10, Vol.46 (10), p.3118-3124

2002

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Aminoindazole PDK1 Inhibitors: A Case Study in Fragment-Based Drug Discovery

ACS medicinal chemistry letters, 2010-11, Vol.1 (8), p.439-442

2010

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Discovery of 5-pyrrolopyridinyl-2-thiophenecarboxamides as potent AKT kinase inhibitors

Bioorganic & medicinal chemistry letters, 2009-04, Vol.19 (8), p.2244-2248

2009

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Discovery of Aminopyridine-Based Inhibitors of Bacterial Enoyl-ACP Reductase (FabI)

Journal of medicinal chemistry, 2002-07, Vol.45 (15), p.3246-3256

2002

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2,3,5-Trisubstituted pyridines as selective AKT inhibitors. Part II: Improved drug-like properties and kinase selectivity from azaindazoles

Bioorganic & medicinal chemistry letters, 2010-01, Vol.20 (2), p.679-683

2010

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2,3,5-Trisubstituted pyridines as selective AKT inhibitors—Part I: Substitution at 2-position of the core pyridine for ROCK1 selectivity

Bioorganic & medicinal chemistry letters, 2010-01, Vol.20 (2), p.673-678

2010

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New benzimidazoles as thrombopoietin receptor agonists

Bioorganic & medicinal chemistry letters, 2006-03, Vol.16 (5), p.1212-1216

2006

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Tetrasubstituted pyridines as potent and selective AKT inhibitors: Reduced CYP450 and hERG inhibition of aminopyridines

Bioorganic & medicinal chemistry letters, 2010-01, Vol.20 (2), p.684-688

2010

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New benzylidenethiazolidinediones as antibacterial agents

Bioorganic & medicinal chemistry letters, 2003-11, Vol.13 (21), p.3771-3773

2003

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Simple method for controlling stereoselection in Mannich cyclization reactions of aldehydes

Journal of organic chemistry, 1993-12, Vol.58 (25), p.6947-6948

1993

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Phenylbutyrates as potent, orally bioavailable vitronectin receptor (integrin αvβ3) antagonists

Bioorganic & medicinal chemistry letters, 2003-04, Vol.13 (8), p.1483-1486

2003

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Abstract 2919: Discovery of small-molecule compounds targeting c-MYC using a novel cell-based screen

Cancer research (Chicago, Ill.), 2018-07, Vol.78 (13_Supplement), p.2919-2919

2018

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Discovery of 7‑Methyl-5-(1-{[3-(trifluoromethyl)phenyl]acetyl}-2,3-dihydro‑1H‑indol-5-yl)‑7H‑pyrrolo[2,3‑d]pyrimidin-4-amine (GSK2606414), a Potent and Selective First-in-Class Inhibitor of Protein Kinase R (PKR)-like Endoplasmic Reticulum Kinase (PERK)

Discovery of novel AKT inhibitors with enhanced anti-tumor effects in combination with the MEK inhibitor

Allosteric Wip1 phosphatase inhibition through flap-subdomain interaction

Discovery of GSK2656157: An Optimized PERK Inhibitor Selected for Preclinical Development

Structural characterization of dicyanopyridine containing DNMT1-selective, non-nucleoside inhibitors

Cell-Based Drug Discovery: Identification and Optimization of Small Molecules that Reduce c‑MYC Protein Levels in Cells

Long-Range Inhibitor-Induced Conformational Regulation of Human IRE1α Endoribonuclease Activity

1,4-Disubstituted imidazoles are potential antibacterial agents functioning as inhibitors of enoyl acyl carrier protein reductase (FabI)

Characterization of an Akt Kinase Inhibitor with Potent Pharmacodynamic and Antitumor Activity

Discovery of Isoxazole Amides as Potent and Selective SMYD3 Inhibitors

Identification of 4-(2-(4-Amino-1,2,5-oxadiazol-3-yl)-1-ethyl-7-{[(3S)-3-piperidinylmethyl]oxy}-1H-imidazo[4,5-c]pyridin-4-yl)-2-methyl-3-butyn-2-ol (GSK690693), a Novel Inhibitor of AKT Kinase

Aminofurazans as potent inhibitors of AKT kinase

Discovery of a Novel and Potent Class of FabI-Directed Antibacterial Agents

Aminoindazole PDK1 Inhibitors: A Case Study in Fragment-Based Drug Discovery

Discovery of 5-pyrrolopyridinyl-2-thiophenecarboxamides as potent AKT kinase inhibitors

Discovery of Aminopyridine-Based Inhibitors of Bacterial Enoyl-ACP Reductase (FabI)

2,3,5-Trisubstituted pyridines as selective AKT inhibitors. Part II: Improved drug-like properties and kinase selectivity from azaindazoles

2,3,5-Trisubstituted pyridines as selective AKT inhibitors—Part I: Substitution at 2-position of the core pyridine for ROCK1 selectivity

New benzimidazoles as thrombopoietin receptor agonists

Tetrasubstituted pyridines as potent and selective AKT inhibitors: Reduced CYP450 and hERG inhibition of aminopyridines

New benzylidenethiazolidinediones as antibacterial agents

Discovery of Orally Active Nonpeptide Vitronectin Receptor Antagonists Based on a 2-Benzazepine Gly-Asp Mimetic

Simple method for controlling stereoselection in Mannich cyclization reactions of aldehydes

Phenylbutyrates as potent, orally bioavailable vitronectin receptor (integrin αvβ3) antagonists

Abstract 2919: Discovery of small-molecule compounds targeting c-MYC using a novel cell-based screen

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