Discovery of <i>N</i>-(2-Chloro-6-methyl- phenyl)-2-(6-(4-(2-hydroxyethyl)- piperazin-1-yl)-2-methylpyrimidin-4- ylamino)thiazole-5-carboxamide (BMS-354825), a Dual Src/Abl Kinase Inhibitor with Potent Antitumor Activity in Preclinical Assays

Louis J. Lombardo, Francis Y. Lee, Ping Chen, +24

Journal of Medicinal Chemistry

Drug TargetPreclinical AssaysPharmacotherapyCompound 13Pharmaceutical Chemistry +17

The Structure of Dasatinib (BMS-354825) Bound to Activated ABL Kinase Domain Elucidates Its Inhibitory Activity against Imatinib-Resistant ABL Mutants

John S. Tokarski, John A. Newitt, Chieh Ying J. Chang, +10

Cancer Research

Highly Selective Inhibition of Tyrosine Kinase 2 (TYK2) for the Treatment of Autoimmune Diseases: Discovery of the Allosteric Inhibitor BMS-986165

Stephen T. Wrobleski, Ryan Moslin, Shuqun Lin, +29

Journal of Medicinal Chemistry

Discovery of <i>N</i>-(4-(2-Amino-3-chloropyridin-4-yloxy)-3-fluorophenyl)-4-ethoxy-1-(4-fluorophenyl)-2-oxo-1,2-dihydropyridine-3-carboxamide (BMS-777607), a Selective and Orally Efficacious Inhibitor of the Met Kinase Superfamily

Gretchen M. Schroeder, Yongmi An, Zhen‐Wei Cai, +28

Journal of Medicinal Chemistry

Orally Efficacious InhibitorDrug TargetPharmacotherapyPharmaceutical ChemistryTumor Biology +19

Protein Farnesyltransferase Inhibitors Exhibit Potent Antimalarial Activity

Laxman Nallan, Kevin D. Bauer, Pravin Bendale, +14

Journal of Medicinal Chemistry

Pft InhibitorsBiochemistryParasite PftMedicineAntiparasitic Agent +9

Discovery of Brivanib Alaninate ((<i>S</i>)-((<i>R</i>)-1-(4-(4-Fluoro-2-methyl-1<i>H</i>-indol-5-yloxy)-5-methylpyrrolo[2,1-<i>f</i>][1,2,4]triazin-6-yloxy)propan-2-yl)2-aminopropanoate), A Novel Prodrug of Dual Vascular Endothelial Growth Factor Receptor-2 and Fibroblast Growth Factor Receptor-1 Kinase Inhibitor (BMS-540215)

Zhen‐Wei Cai, Yongzheng Zhang, R. M. Borzilleri, +21

Journal of Medicinal Chemistry

Pharmaceutical ScienceOral BioavailabilityL-alanine Prodrug 8PharmacotherapyPharmaceutical Chemistry +18

Discovery and Preclinical Studies of (<i>R</i>)-1-(4-(4-Fluoro-2-methyl-1<i>H</i>-indol-5-yloxy)-5- methylpyrrolo[2,1-<i>f</i>][1,2,4]triazin-6-yloxy)propan- 2-ol (BMS-540215), an In Vivo Active Potent VEGFR-2 Inhibitor

Rajeev S. Bhide, Zhen‐Wei Cai, Yong‐Zheng Zhang, +25

Journal of Medicinal Chemistry

Discovery of Pyrrolopyridine−Pyridone Based Inhibitors of Met Kinase: Synthesis, X-ray Crystallographic Analysis, and Biological Activities

Kyoung Soon Kim, Liping Zhang, Robert J. Schmidt, +23

Journal of Medicinal Chemistry

Drug TargetBiological ActivitiesChemical BiologyPharmaceutical ChemistryCompound 2 +17

Discovery of Clinical Candidate BMS-906024: A Potent Pan-Notch Inhibitor for the Treatment of Leukemia and Solid Tumors

Ashvinikumar V. Gavai, Claude Quesnelle, Derek Norris, +35

ACS Medicinal Chemistry Letters

Solid TumorsPharmacotherapyTumor BiologyMyeloid NeoplasiaHematological Malignancy +16

Identification of <i>N</i>-Methyl Nicotinamide and <i>N</i>-Methyl Pyridazine-3-Carboxamide Pseudokinase Domain Ligands as Highly Selective Allosteric Inhibitors of Tyrosine Kinase 2 (TYK2)

Ryan Moslin, Yanlei Zhang, Stephen T. Wrobleski, +26

Journal of Medicinal Chemistry