Discovery of a JAK3-Selective Inhibitor: Functional Differentiation of JAK3-Selective Inhibition over pan-JAK or JAK1-Selective Inhibition

Jean‐Baptiste Telliez, Martin E. Dowty, Lu Wang, +33

ACS Chemical Biology

Jak1 InhibitionImmunologyImmune RegulationInnate ImmunityInflammatory Arthritis +28

Dual Inhibition of TYK2 and JAK1 for the Treatment of Autoimmune Diseases: Discovery of (( <i>S</i> )-2,2-Difluorocyclopropyl)((1 <i>R</i> ,5 <i>S</i> )-3-(2-((1-methyl-1 <i>H</i> -pyrazol-4-yl)amino)pyrimidin-4-yl)-3,8-diazabicyclo[3.2.1]octan-8-yl)methanone (PF-06700841)

Andrew Fensome, Catherine M. Ambler, Eric P. Arnold, +30

Journal of Medicinal Chemistry

Identification of <i>N</i>-{<i>cis</i>-3-[Methyl(7<i>H</i>-pyrrolo[2,3-<i>d</i>]pyrimidin-4-yl)amino]cyclobutyl}propane-1-sulfonamide (PF-04965842): A Selective JAK1 Clinical Candidate for the Treatment of Autoimmune Diseases

Michael L. Vazquez, Neelu Kaila, Joseph W. Strohbach, +32

Journal of Medicinal Chemistry

ImmunodeficienciesJanus KinasesImmunologyPharmacotherapyImmunotherapy +20

Design of a Janus Kinase 3 (JAK3) Specific Inhibitor 1-((2<i>S</i>,5<i>R</i>)-5-((7<i>H</i>-Pyrrolo[2,3-<i>d</i>]pyrimidin-4-yl)amino)-2-methylpiperidin-1-yl)prop-2-en-1-one (PF-06651600) Allowing for the Interrogation of JAK3 Signaling in Humans

Atli Thorarensen, Martin E. Dowty, Mary Ellen Banker, +24

Journal of Medicinal Chemistry

Specific InhibitorDrug TargetPharmacotherapyChemical BiologyPharmaceutical Chemistry +23

Identification of Cyanamide-Based Janus Kinase 3 (JAK3) Covalent Inhibitors

Agustin Casimiro‐Garcia, John I. Trujillo, F.F. Vajdos, +18

Journal of Medicinal Chemistry

Medicinal ChemistryCovalent InhibitorsPharmaceutical ChemistryBiochemistrySelective Jak3 Inhibitors +10

The advantages of describing covalent inhibitor in vitro potencies by IC50 at a fixed time point. IC50 determination of covalent inhibitors provides meaningful data to medicinal chemistry for SAR optimization

Atli Thorarensen, Paul Balbo, Mary Ellen Banker, +6

Bioorganic & Medicinal Chemistry

Medicinal ChemistrySar OptimizationCovalent InhibitorPharmaceutical ScienceBiochemistry +10

Binding site elucidation and structure guided design of macrocyclic IL-17A antagonists

Shenping Liu, Leslie Dakin, Xing Li, +25

Scientific Reports

ATP-Mediated Kinome Selectivity: The Missing Link in Understanding the Contribution of Individual JAK Kinase Isoforms to Cellular Signaling

Atli Thorarensen, Mary Ellen Banker, Andrew Fensome, +5

ACS Chemical Biology

Atp-mediated Kinome SelectivityMolecular BiologyCytoskeletonCellular PhysiologyAtp Km +18

The use of plasma aldosterone and urinary sodium to potassium ratio as translatable quantitative biomarkers of mineralocorticoid receptor antagonism

Rena J Eudy, Vaishali Sahasrabudhe, Kevin Sweeney, +7

Journal of Translational Medicine

Inhibiting complex IL-17A and IL-17RA interactions with a linear peptide

Shenping Liu, Joel Desharnais, Parag V. Sahasrabudhe, +20

Scientific Reports