| # | Title | Journal | Year | Citations |
|---|
| 1 | Identification of Potent, Selective, Cell-Active Inhibitors of the Histone Lysine Methyltransferase EZH2 | ACS Medicinal Chemistry Letters | 2012 | 332 |
| 2 | Discovery of GSK2126458, a Highly Potent Inhibitor of PI3K and the Mammalian Target of Rapamycin | ACS Medicinal Chemistry Letters | 2010 | 320 |
| 3 | Discovery of AG-120 (Ivosidenib): A First-in-Class Mutant IDH1 Inhibitor for the Treatment of IDH1 Mutant Cancers | ACS Medicinal Chemistry Letters | 2018 | 292 |
| 4 | Discovery of RG7112: A Small-Molecule MDM2 Inhibitor in Clinical Development | ACS Medicinal Chemistry Letters | 2013 | 286 |
| 5 | Discovery of NVP-LDE225, a Potent and Selective Smoothened Antagonist | ACS Medicinal Chemistry Letters | 2010 | 280 |
| 6 | Biocatalysis in the Pharmaceutical Industry: The Need for Speed | ACS Medicinal Chemistry Letters | 2017 | 272 |
| 7 | Discovery of a Potent and Selective BCL-XL Inhibitor with in Vivo Activity | ACS Medicinal Chemistry Letters | 2014 | 242 |
| 8 | INCB24360 (Epacadostat), a Highly Potent and Selective Indoleamine-2,3-dioxygenase 1 (IDO1) Inhibitor for Immuno-oncology | ACS Medicinal Chemistry Letters | 2017 | 235 |
| 9 | SMARTCyp: A 2D Method for Prediction of Cytochrome P450-Mediated Drug Metabolism | ACS Medicinal Chemistry Letters | 2010 | 233 |
| 10 | Practical High-Throughput Experimentation for Chemists | ACS Medicinal Chemistry Letters | 2017 | 233 |
| 11 | Discovery of TAK-875: A Potent, Selective, and Orally Bioavailable GPR40 Agonist | ACS Medicinal Chemistry Letters | 2010 | 225 |
| 12 | Drawing the PDB: Protein−Ligand Complexes in Two Dimensions | ACS Medicinal Chemistry Letters | 2010 | 223 |
| 13 | Identification of NVP-BKM120 as a Potent, Selective, Orally Bioavailable Class I PI3 Kinase Inhibitor for Treating Cancer | ACS Medicinal Chemistry Letters | 2011 | 223 |
| 14 | Structures of Human Acetylcholinesterase Bound to Dihydrotanshinone I and Territrem B Show Peripheral Site Flexibility | ACS Medicinal Chemistry Letters | 2013 | 204 |
| 15 | Identification of Niclosamide as a New Small-Molecule Inhibitor of the STAT3 Signaling Pathway | ACS Medicinal Chemistry Letters | 2010 | 196 |
| 16 | Distinct Binding Mode of Multikinase Inhibitor Lenvatinib Revealed by Biochemical Characterization | ACS Medicinal Chemistry Letters | 2015 | 194 |
| 17 | Marine Natural Products in Medicinal Chemistry | ACS Medicinal Chemistry Letters | 2018 | 193 |
| 18 | Discovery of Dabrafenib: A Selective Inhibitor of Raf Kinases with Antitumor Activity against B-Raf-Driven Tumors | ACS Medicinal Chemistry Letters | 2013 | 186 |
| 19 | Discovery of MK-5172, a Macrocyclic Hepatitis C Virus NS3/4a Protease Inhibitor | ACS Medicinal Chemistry Letters | 2012 | 181 |
| 20 | Discovery of GSK2656157: An Optimized PERK Inhibitor Selected for Preclinical Development | ACS Medicinal Chemistry Letters | 2013 | 176 |
| 21 | Identification of 14 Known Drugs as Inhibitors of the Main Protease of SARS-CoV-2 | ACS Medicinal Chemistry Letters | 2020 | 176 |
| 22 | Discovery of the First Potent Inhibitors of Mutant IDH1 That Lower Tumor 2-HG in Vivo | ACS Medicinal Chemistry Letters | 2012 | 175 |
| 23 | PROTAC Technology: Opportunities and Challenges | ACS Medicinal Chemistry Letters | 2020 | 169 |
| 24 | Discovery and Evaluation of BMS-708163, a Potent, Selective and Orally Bioavailable γ-Secretase Inhibitor | ACS Medicinal Chemistry Letters | 2010 | 166 |
| 25 | Advent of Imidazo[1,2-a]pyridine-3-carboxamides with Potent Multi- and Extended Drug Resistant Antituberculosis Activity | ACS Medicinal Chemistry Letters | 2011 | 161 |
| 26 | Cobicistat (GS-9350): A Potent and Selective Inhibitor of Human CYP3A as a Novel Pharmacoenhancer | ACS Medicinal Chemistry Letters | 2010 | 159 |
| 27 | Discovery of PF-04457845: A Highly Potent, Orally Bioavailable, and Selective Urea FAAH Inhibitor | ACS Medicinal Chemistry Letters | 2011 | 159 |
| 28 | Investigation of a Bicyclo[1.1.1]pentane as a Phenyl Replacement within an LpPLA2 Inhibitor | ACS Medicinal Chemistry Letters | 2017 | 156 |
| 29 | Selective Inhibitors of Fibroblast Activation Protein (FAP) with a (4-Quinolinoyl)-glycyl-2-cyanopyrrolidine Scaffold | ACS Medicinal Chemistry Letters | 2013 | 153 |
| 30 | Discovery and Development of Potent and Selective Inhibitors of Histone Methyltransferase G9a | ACS Medicinal Chemistry Letters | 2014 | 152 |
| 31 | Selective Dual Inhibitors of the Cancer-Related Deubiquitylating Proteases USP7 and USP47 | ACS Medicinal Chemistry Letters | 2012 | 149 |
| 32 | NOSH-Aspirin: A Novel Nitric Oxide–Hydrogen Sulfide-Releasing Hybrid: A New Class of Anti-inflammatory Pharmaceuticals | ACS Medicinal Chemistry Letters | 2012 | 147 |
| 33 | Arylthioamides as H2S Donors: l-Cysteine-Activated Releasing Properties and Vascular Effects in Vitro and in Vivo | ACS Medicinal Chemistry Letters | 2013 | 144 |
| 34 | Discovery of PF-04449913, a Potent and Orally Bioavailable Inhibitor of Smoothened | ACS Medicinal Chemistry Letters | 2012 | 142 |
| 35 | Thermodynamics of Ligand Binding and Efficiency | ACS Medicinal Chemistry Letters | 2011 | 141 |
| 36 | Discovery of BI 224436, a Noncatalytic Site Integrase Inhibitor (NCINI) of HIV-1 | ACS Medicinal Chemistry Letters | 2014 | 139 |
| 37 | Discovery of BAF312 (Siponimod), a Potent and Selective S1P Receptor Modulator | ACS Medicinal Chemistry Letters | 2013 | 138 |
| 38 | Advantages of the Parent Nucleoside GS-441524 over Remdesivir for Covid-19 Treatment | ACS Medicinal Chemistry Letters | 2020 | 137 |
| 39 | Discovery of Dinaciclib (SCH 727965): A Potent and Selective Inhibitor of Cyclin-Dependent Kinases | ACS Medicinal Chemistry Letters | 2010 | 134 |
| 40 | Fragment Screening by Surface Plasmon Resonance | ACS Medicinal Chemistry Letters | 2010 | 134 |
| 41 | Novel Carboxamide-Based Allosteric MEK Inhibitors: Discovery and Optimization Efforts toward XL518 (GDC-0973) | ACS Medicinal Chemistry Letters | 2012 | 132 |
| 42 | Discovery of a Highly Potent and Selective MEK Inhibitor: GSK1120212 (JTP-74057 DMSO Solvate) | ACS Medicinal Chemistry Letters | 2011 | 131 |
| 43 | Structure-Based Design and Synthesis of Potent Cyclic Peptides Inhibiting the YAP–TEAD Protein–Protein Interaction | ACS Medicinal Chemistry Letters | 2014 | 130 |
| 44 | Design and Synthesis of Tesirine, a Clinical Antibody–Drug Conjugate Pyrrolobenzodiazepine Dimer Payload | ACS Medicinal Chemistry Letters | 2016 | 130 |
| 45 | Identification of a New Series of STAT3 Inhibitors by Virtual Screening | ACS Medicinal Chemistry Letters | 2010 | 129 |
| 46 | Discovery of GBT440, an Orally Bioavailable R-State Stabilizer of Sickle Cell Hemoglobin | ACS Medicinal Chemistry Letters | 2017 | 129 |
| 47 | Crystal Structures and Structure–Activity Relationships of Imidazothiazole Derivatives as IDO1 Inhibitors | ACS Medicinal Chemistry Letters | 2014 | 127 |
| 48 | LLY-283, a Potent and Selective Inhibitor of Arginine Methyltransferase 5, PRMT5, with Antitumor Activity | ACS Medicinal Chemistry Letters | 2018 | 127 |
| 49 | Discovery of Potent and Selective Inhibitors of CDPK1 from C. parvum and T. gondii | ACS Medicinal Chemistry Letters | 2010 | 126 |
| 50 | Analogues of the Allosteric Heat Shock Protein 70 (Hsp70) Inhibitor, MKT-077, As Anti-Cancer Agents | ACS Medicinal Chemistry Letters | 2013 | 126 |
