Identification of NVP-TNKS656: The Use of Structure–Efficiency Relationships To Generate a Highly Potent, Selective, and Orally Active Tankyrase Inhibitor

Michael D. Shultz, Atwood K. Cheung, C.A. Kirby, +25

Journal of Medicinal Chemistry

Drug TargetSelective Tankyrase InhibitorsPharmacotherapyChemical BiologyPharmaceutical Chemistry +16

Novel highly selective inhibitors of ubiquitin specific protease 30 (USP30) accelerate mitophagy

Arthur F. Kluge, Bharat Lagu, Pranab Maiti, +6

Bioorganic & Medicinal Chemistry Letters

Protease InhibitorsCell AutophagyMitophagyMedicineAutophagy +6

Design and Synthesis of Novel α₁_a Adrenoceptor-Selective Antagonists. 1. Structure−Activity Relationship in Dihydropyrimidinones

Dhanapalan Nagarathnam, Shou Wu Miao, Bharat Lagu, +24

Journal of Medicinal Chemistry

Organic ChemistryPharmacotherapyChemistryPharmaceutical ChemistryMolecular Pharmacology +14

Discovery of NVP‐LEQ506, a Second‐Generation Inhibitor of Smoothened

Stefan Peukert, Feng He, Miao Dai, +20

ChemMedChem

Molecular PharmacologyContinued OptimizationCompetitor CompoundOncologyFirst Disclosure +13

Stereo- and regioselective synthesis of chiral diamines and triamines from pseudoephedrine and ephedrine

R. Karl Dieter, Niranjan Deo, Bharat Lagu, +1

The Journal of Organic Chemistry

Altmetric Attention ScoreKarl DieterOrganic ChemistryRegioselective SynthesisSocial Media Presence +7

3-Arylimino-2-indolones Are Potent and Selective Galanin GAL₃ Receptor Antagonists

Michael J. Konkel, Bharat Lagu, Lakmal W. Boteju, +13

Journal of Medicinal Chemistry

Molecular PharmacologyMedicinal ChemistryBiochemistryMedicineNatural Sciences +12

Fragment-Based Discovery of 7-Azabenzimidazoles as Potent, Highly Selective, and Orally Active CDK4/6 Inhibitors

Young Shin Cho, Hayley C. Angove, Christopher T. Brain, +33

ACS Medicinal Chemistry Letters

Drug TargetChemical BiologyPharmaceutical ChemistryMedicinal ChemistryReceptor Tyrosine Kinase +16

Stereoselectivity of Induction of the Retinoblastoma Gene Product (pRb) Dephosphorylation by D-erythro-Sphingosine Supports a Role for pRb in Growth Suppression by Sphingosine

Marina Y. Pushkareva, Richard C. Chao, Alicja Bielawska, +5

Biochemistry

Synthesis and evaluation of furo[3,4-d]pyrimidinones as selective α1a-adrenergic receptor antagonists

Bharat Lagu, Dake Tian, George Chiu, +9

Bioorganic & Medicinal Chemistry Letters

Design and Synthesis of Novel α₁_a Adrenoceptor-Selective Antagonists. 2. Approaches To Eliminate Opioid Agonist Metabolites via Modification of Linker and 4-Methoxycarbonyl-4-phenylpiperidine Moiety

T. G. Murali Dhar, Dhanapalan Nagarathnam, Mohammad R. Marzabadi, +29

Journal of Medicinal Chemistry

Molecular PharmacologyBiochemistry4-Methoxycarbonyl-4-phenylpiperidine MoietyOpioid Agonist MetabolitesMedicine +12