PMID

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Discovery of (R,E)-N-(7-Chloro-1-(1-[4-(dimethylamino)but-2-enoyl]azepan-3-yl)-1H-benzo[d]imidazol-2-yl)-2-methylisonicotinamide (EGF816), a Novel, Potent, and WT Sparing Covalent Inhibitor of Oncogenic (L858R, ex19del) and Resistant (T790M) EGFR Mutants for the Treatment of EGFR Mutant Non-Small-Ce

Genomics Institute of The Novartis Research Foundation

(R)-2-Phenylpyrrolidine Substituted Imidazopyridazines: A New Class of Potent and Selective Pan-TRK Inhibitors.

Genomics Institute of The Novartis Research Foundation

Novel tricyclic pyrazolopyrimidines as potent and selective GPR119 agonists.

Genomics Institute of The Novartis Research Foundation

Discovery, optimization, and biological evaluation of 5-(2-(trifluoromethyl)phenyl)indazoles as a novel class of transient receptor potential A1 (TRPA1) antagonists.

Genomics Institute of The Novartis Research Foundation

Discovery of structurally novel, potent and orally efficacious GPR119 agonists.

Genomics Institute of The Novartis Research Foundation

Discovery of trifluoromethyl(pyrimidin-2-yl)azetidine-2-carboxamides as potent, orally bioavailable TGR5 (GPBAR1) agonists: structure-activity relationships, lead optimization, and chronic in vivo efficacy.

Genomics Institute of The Novartis Research Foundation

Synthesis, structure-activity relationships, and in vivo efficacy of the novel potent and selective anaplastic lymphoma kinase (ALK) inhibitor 5-chloro-N2-(2-isopropoxy-5-methyl-4-(piperidin-4-yl)phenyl)-N4-(2-(isopropylsulfonyl)phenyl)pyrimidine-2,4-diamine (LDK378) currently in phase 1 and phase

Genomics Institute of The Novartis Research Foundation

Discovery of BAF312 (Siponimod), a Potent and Selective S1P Receptor Modulator.

Genomics Institute of The Novartis Research Foundation

Design, synthesis, and structure-activity-relationship of phenyl imidazoles as potent Smoothened antagonists.

Genomics Institute of The Novartis Research Foundation

Imidazolopiperazines: lead optimization of the second-generation antimalarial agents.

Genomics Institute of The Novartis Research Foundation

Design and synthesis of benzoazepin-2-one analogs as allosteric binders targeting the PIF pocket of PDK1.

Genomics Institute of The Novartis Research Foundation

Discovery and biological evaluation of benzo[a]carbazole-based small molecule agonists of the thrombopoietin (Tpo) receptor.

Genomics Institute of The Novartis Research Foundation

Synthesis and evaluation of N-aryl pyrrolidinones as novel anti-HIV-1 agents. Part 1.

Genomics Institute of The Novartis Research Foundation

Imidazolopiperazines: hit to lead optimization of new antimalarial agents.

Genomics Institute of The Novartis Research Foundation

Allosteric inhibitors of Bcr-abl-dependent cell proliferation.

Genomics Institute of The Novartis Research Foundation

Discovery of pyrimidine benzimidazoles as Src-family selective Lck inhibitors. Part II.

Genomics Institute of The Novartis Research Foundation

Discovery of pyrimidine benzimidazoles as Lck inhibitors: part I.

Genomics Institute of The Novartis Research Foundation

Optimization of small molecule agonists of the thrombopoietin (Tpo) receptor derived from a benzo[a]carbazole hit scaffold.

Genomics Institute of The Novartis Research Foundation

Discovery of inhibitors of the channel-activating protease prostasin (CAP1/PRSS8) utilizing structure-based design.

Genomics Institute of The Novartis Research Foundation

Substrate optimization for monitoring cathepsin C activity in live cells.

Genomics Institute of The Novartis Research Foundation

Identification of NVP-TAE684, a potent, selective, and efficacious inhibitor of NPM-ALK.

Genomics Institute of The Novartis Research Foundation

Design and synthesis of 7H-pyrrolo[2,3-d]pyrimidines as focal adhesion kinase inhibitors. Part 2.

Genomics Institute of The Novartis Research Foundation

Design and synthesis of 7H-pyrrolo[2,3-d]pyrimidines as focal adhesion kinase inhibitors. Part 1.

Genomics Institute of The Novartis Research Foundation

Identification of coumarin derivatives as a novel class of allosteric MEK1 inhibitors.

Genomics Institute of The Novartis Research Foundation

Crystal structures of human HSP90alpha-complexed with dihydroxyphenylpyrazoles.

Genomics Institute of The Novartis Research Foundation

Identification of novel potent bicyclic peptide deformylase inhibitors.

Genomics Institute of The Novartis Research Foundation

Structure-Based Design of Selective LONP1 Inhibitors for Probing

Genomics Institute of The Novartis Research Foundation

Discovery of potent, orally bioavailable in vivo efficacious antagonists of the TLR7/8 pathway.

Genomics Institute of The Novartis Research Foundation

Design and synthesis of novel selective anaplastic lymphoma kinase inhibitors.

Genomics Institute of The Novartis Research Foundation

Target-Based Identification and Optimization of 5-Indazol-5-yl Pyridones as Toll-like Receptor 7 and 8 Antagonists Using a Biochemical TLR8 Antagonist Competition Assay.

Genomics Institute of The Novartis Research Foundation

Discovery of Pyridinyl Acetamide Derivatives as Potent, Selective, and Orally Bioavailable Porcupine Inhibitors.

Genomics Institute of The Novartis Research Foundation

Identification of Potent and Selective RIPK2 Inhibitors for the Treatment of Inflammatory Diseases.

Genomics Institute of The Novartis Research Foundation

Discovery of Tropifexor (LJN452), a Highly Potent Non-bile Acid FXR Agonist for the Treatment of Cholestatic Liver Diseases and Nonalcoholic Steatohepatitis (NASH).

Genomics Institute of The Novartis Research Foundation

Discovery of phenyl acetic acid substituted quinolines as novel liver X receptor agonists for the treatment of atherosclerosis.

Wyeth Research