Enhancing the Oral Bioavailability of a Poorly Soluble Pan-CK2 Kinase Inhibitor: Leveraging a Phosphate Prodrug Strategy to Overcome Dissolution-Limited Absorption and Improve Systemic Exposure during Dose EscalationJOURNAL OF MEDICINAL CHEMISTRYIF6.82026-01-010PRE
Azatricyclic Inverse Agonists of RORγt That Demonstrate Efficacy in Models of Rheumatoid Arthritis and PsoriasisACS MEDICINAL CHEMISTRY LETTERSIF42021-04-306OA
Tricyclic-Carbocyclic RORγt Inverse Agonists-Discovery of BMS-986313JOURNAL OF MEDICINAL CHEMISTRYIF6.82021-02-1612PREAI
Novel Tricyclic Pyroglutamide Derivatives as Potent RORγt Inverse Agonists Identified using a Virtual Screening ApproachACS MEDICINAL CHEMISTRY LETTERSIF42020-11-0617OAAI
Driving Potency with Rotationally Stable Atropisomers: Discovery of Pyridopyrimidinedione-Carbazole Inhibitors of BTKACS MEDICINAL CHEMISTRY LETTERSIF42020-09-165OAAI
Discovery of BMS-986251: A Clinically Viable, Potent, and Selective RORγt Inverse AgonistACS MEDICINAL CHEMISTRY LETTERSIF42020-03-3137OAAI
Rationally Designed, Conformationally Constrained Inverse Agonists of RORγt-Identification of a Potent, Selective Series with Biologic-Like in Vivo EfficacyJOURNAL OF MEDICINAL CHEMISTRYIF6.82019-10-2233PREAI
Discovery of Branebrutinib (BMS-986195): A Strategy for Identifying a Highly Potent and Selective Covalent Inhibitor Providing Rapid in Vivo Inactivation of Bruton's Tyrosine Kinase (BTK)JOURNAL OF MEDICINAL CHEMISTRYIF6.82019-03-2086OAAI
Identification of a Potent, Selective, and Efficacious Phosphatidylinositol 3-Kinase δ (P13Kδ) Inhibitor for the Treatment of Immunological DisordersJOURNAL OF MEDICINAL CHEMISTRYIF6.82017-06-0517PREAI
The role of chromatographic and chiroptical spectroscopic techniques and methodologies in support of drug discovery for atropisomeric drug inhibitors of Bruton's tyrosine kinaseJOURNAL OF CHROMATOGRAPHY AIF42017-03-0119PREAI
Discovery of 6-Fluoro-5-(R)-(3-(S)-(8-fluoro-1-methyl-2,4-dioxo-1,2-dihydroquinazolin-3(4H)-yl)-2-methylphenyl)-2-(S)-(2-hydroxypropan-2-yl)-2,3,4,9-tetrahydro-1H-carbazole-8-carboxamide (BMS-986142): A Reversible Inhibitor of Bruton's Tyrosine Kinase (BTK) Conformationally Constrained by Two Locked AtropisomersJOURNAL OF MEDICINAL CHEMISTRYIF6.82016-09-19117PREAI
Small Molecule Reversible Inhibitors of Bruton's Tyrosine Kinase (BTK): Structure-Activity Relationships Leading to the Identification of 7-(2-Hydroxypropan-2-yl)-4-[2-methyl-3-(4-oxo-3,4-dihydroquinazolin-3-yl)phenyl]-9H-carbazole-1-carboxamide (BMS-935177)JOURNAL OF MEDICINAL CHEMISTRYIF6.82016-08-2655PREAI
Discovery of the Selective CYP17A1 Lyase Inhibitor BMS-351 for the Treatment of Prostate Cancer用于治疗前列腺癌的选择性CYP17A1裂解酶抑制剂BMS-351的发现ACS MEDICINAL CHEMISTRY LETTERSIF42015-12-147OAAI
The identification of BMS-595, an orally active imidazo[1,2-b]pyridazine CK2 inhibitor with in vivo anti-tumor activityCANCER RESEARCHIF16.62015-08-010PRE
The Discovery of Potent and Selective Inhibitors of CYP17 LyaseEUROPEAN JOURNAL OF CANCERIF7.12012-11-010PREAI
Phase I Dose-Escalation Study of the Novel Antiandrogen BMS-641988 in Patients with Castration-Resistant Prostate CancerCLINICAL CANCER RESEARCHIF10.22011-02-1535OAAI
Androgen receptor antagonists: Lead optimization and preclinical pharmacologyCANCER RESEARCHIF16.62010-04-010PRE
Discovery of BMS-641988, a Novel and Potent Inhibitor of Androgen Receptor Signaling for the Treatment of Prostate CancerCANCER RESEARCHIF16.62009-08-1252OAAI
Discovery of dapagliflozin: A potent, selective renal sodium-dependent glucose cotransporter 2 (SGLT2) inhibitor for the treatment of type 2 diabetesJOURNAL OF MEDICINAL CHEMISTRYIF6.82008-02-09619PREAI