Crystallographic structure of a small molecule SIRT1 activator-enzyme complex

Han Dai, April Case, Thomas V. Riera, +30

Nature Communications

Conformationally constrained farnesoid X receptor (FXR) agonists: Naphthoic acid-based analogs of GW 4064

Adwoa Akwabi-Ameyaw, Jonathan Y. Bass, Richard D. Caldwell, +17

Bioorganic & Medicinal Chemistry Letters

Naphthoic Acid-based AnalogsBiochemistryG Protein-coupled ReceptorMedicineNatural Sciences +10

Discovery of Evobrutinib: An Oral, Potent, and Highly Selective, Covalent Bruton’s Tyrosine Kinase (BTK) Inhibitor for the Treatment of Immunological Diseases

Richard D. Caldwell, Hui Qiu, Ben Askew, +30

Journal of Medicinal Chemistry

Novel TherapyMedicineTyrosine KinaseHighly SelectiveImmunology +12

FXR agonist activity of conformationally constrained analogs of GW 4064

Adwoa Akwabi-Ameyaw, Jonathan Y. Bass, Richard D. Caldwell, +14

Bioorganic & Medicinal Chemistry Letters

G Protein-coupled ReceptorFunctional SelectivityMolecular BiologyConformational StudyFxr Agonist Activity +2

Substituted isoxazole analogs of farnesoid X receptor (FXR) agonist GW4064

Jonathan Y. Bass, Richard D. Caldwell, Justin A. Caravella, +11

Bioorganic & Medicinal Chemistry Letters

Molecular PharmacologyBiochemistryFunctional SelectivityMedicineReceptor (Biochemistry) +7

Btk inhibition treats TLR7/IFN driven murine lupus

Andrew T. Bender, Albertina Pereira, Kai Fu, +13

Clinical Immunology

InflammationRheumatologySystems BiologyAutoimmune DiseaseAllergy +12

Discovery of potent, highly selective covalent irreversible BTK inhibitors from a fragment hit

Hui Qiu, Lesley Liu‐Bujalski, Richard D. Caldwell, +11

Bioorganic & Medicinal Chemistry Letters

Combinatorial ChemistryMedicinal ChemistryDrug TargetNatural SciencesMedicine +5

Discovery of 6,7-Dihydro-5<i>H</i>-pyrrolo[2,3-<i>a</i>]pyrimidines as Orally Available G Protein-Coupled Receptor 119 Agonists

Subba R. Katamreddy, Andrew J. Carpenter, Carina Ämmälä, +21

Journal of Medicinal Chemistry

Molecular PharmacologyMedicinal ChemistryBiochemistryFunctional SelectivityMedicine +11

Discovery of a novel series of pyridine and pyrimidine carboxamides as potent and selective covalent inhibitors of Btk

Richard D. Caldwell, Lesley Liu‐Bujalski, Hui Qiu, +11

Bioorganic & Medicinal Chemistry Letters

Combinatorial ChemistryMedicinal ChemistryDerivative (Chemistry)Novel SeriesNatural Sciences +9

Selective Wee1 Inhibitors Led to Antitumor Activity <i>In Vitro</i> and Correlated with Myelosuppression

Satenig Guler, Maria C. DiPoto, Alejandro Crespo, +15

ACS Medicinal Chemistry Letters