Discovery of 2-{3-[2-(1-Isopropyl-3-methyl-1<i>H</i>-1,2–4-triazol-5-yl)-5,6-dihydrobenzo[f]imidazo[1,2-<i>d</i>][1,4]oxazepin-9-yl]-1<i>H</i>-pyrazol-1-yl}-2-methylpropanamide (GDC-0032): A β-Sparing Phosphoinositide 3-Kinase Inhibitor with High Unbound Exposure and Robust in Vivo Antitumor Activity

Chudi Ndubaku, Timothy P. Heffron, Steven T. Staben, +26

Journal of Medicinal Chemistry

Drug TargetUnbound Drug ExposurePharmacotherapyIntrinsic ClearanceTumor Biology +19

Development of Serine Protease Inhibitors Displaying a Multicentered Short (&lt;2.3 Å) Hydrogen Bond Binding Mode:  Inhibitors of Urokinase-Type Plasminogen Activator and Factor Xa

Erik Verner, B.A. Katz, Jeffrey R. Spencer, +17

Journal of Medicinal Chemistry

Drug TargetBioorganic ChemistrySerine Protease InhibitorsChemical BiologyNovel Scaffolds +17

Design of a brain-penetrant CDK4/6 inhibitor for glioblastoma

Sarah M. Bronner, Karl A. Merrick, Jeremy Murray, +33

Bioorganic & Medicinal Chemistry Letters

Neuro-oncologyMedicineTumor TargetingAnti-cancer AgentHigh-grade Gliomas +4

Optimization of a screening lead for factor VIIa/TF

Wendy B. Young, Aleksandr Kolesnikov, Roopa Rai, +8

Bioorganic & Medicinal Chemistry Letters

Translational MedicineHit IdentificationScreening LeadMedicineLead Identification +6

Discovery of a Potent (4<i>R</i>,5<i>S</i>)-4-Fluoro-5-methylproline Sulfonamide Transient Receptor Potential Ankyrin 1 Antagonist and Its Methylene Phosphate Prodrug Guided by Molecular Modeling

Huifen Chen, Matthew Volgraf, Steven Do, +27

Journal of Medicinal Chemistry

Drug TargetMolecular PainPharmacotherapyPharmacodynamic ModelingMolecular Pharmacology +16

Optimization of Pan-Pim Kinase Activity and Oral Bioavailability Leading to Diaminopyrazole (GDC-0339) for the Treatment of Multiple Myeloma

Xiaojing Wang, Wesley Blackaby, Vivienne Allen, +31

Journal of Medicinal Chemistry

Pim KinasesPharmacotherapyMetronomic ChemotherapyTumor BiologyPim Kinase Inhibition +16

Potent 4-amino-5-azaindole factor VIIa inhibitors

Huiyong Hu, Aleksandr Kolesnikov, Jennifer R. Riggs, +11

Bioorganic & Medicinal Chemistry Letters

Medicinal ChemistryMedicinePharmacological AgentPharmacotherapyDrug Development +3

Factor VIIa inhibitors: Chemical optimization, preclinical pharmacokinetics, pharmacodynamics, and efficacy in an arterial baboon thrombosis model

Wendy B. Young, Joyce Mordenti, Steven Torkelson, +14

Bioorganic & Medicinal Chemistry Letters

ThrombosisChemical OptimizationCardiovascular DiseaseFactor Viia InhibitorsBlood Platelet +9

Development of Potent and Selective Pyrazolopyrimidine IRAK4 Inhibitors

Marian C. Bryan, Joy Drobnick, Alberto Gobbi, +23

Journal of Medicinal Chemistry

Medicinal ChemistryDrug TargetBiochemistryMedicineNatural Sciences +11

Discovery of 5-Azaindazole (GNE-955) as a Potent Pan-Pim Inhibitor with Optimized Bioavailability

Xiaojing Wang, Aleksandr Kolesnikov, Suzanne Tay, +17

Journal of Medicinal Chemistry

Pharmaceutical ScienceBioorganic ChemistryPim KinasesPharmacotherapyLead Series +16