246 articles for thisTarget
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Design and Discovery of N-(2-Methyl-5'-morpholino-6'-((tetrahydro-2H-pyran-4-yl)oxy)-[3,3'-bipyridin]-5-yl)-3-(trifluoromethyl)benzamide (RAF709): A Potent, Selective, and Efficacious RAF Inhibitor Targeting RAS Mutant Cancers.
Novartis Institutes For Biomedical Research
Discovery of an Acrylic Acid Based Tetrahydroisoquinoline as an Orally Bioavailable Selective Estrogen Receptor Degrader for ERa+ Breast Cancer.
Novartis Institutes For Biomedical Research
Structure-Based Library Design and Fragment Screening for the Identification of Reversible Complement Factor D Protease Inhibitors.
Novartis Institutes For Biomedical Research
Discovery of First-in-Class, Potent, and Orally Bioavailable Embryonic Ectoderm Development (EED) Inhibitor with Robust Anticancer Efficacy.
Novartis Institutes For Biomedical Research
"Addition" and"Subtraction": Selectivity Design for Type II Maternal Embryonic Leucine Zipper Kinase Inhibitors.
Novartis Institutes For Biomedical Research
Discovery of Potent, Selective, and Structurally Novel Dot1L Inhibitors by a Fragment Linking Approach.
Novartis Institutes For Biomedical Research
Indolyl-naphthyl-maleimides as potent and selective inhibitors of protein kinase C-a/ß.
Novartis Institutes For Biomedical Research
Discovery of Fevipiprant (NVP-QAW039), a Potent and Selective DP
Novartis Institutes For Biomedical Research
Discovery of novel pyrrolidineoxy-substituted heteroaromatics as potent and selective PI3K delta inhibitors with improved physicochemical properties.
Novartis Institutes For Biomedical Research
Increasing metabolic stability via the deuterium kinetic isotope effect: An example from a proline-amide-urea aminothiazole series of phosphatidylinositol-3 kinase alpha inhibitors.
Novartis Institutes For Biomedical Research
Discovery of Imidazoquinolines as a Novel Class of Potent, Selective, and in Vivo Efficacious Cancer Osaka Thyroid (COT) Kinase Inhibitors.
Novartis Institutes For Biomedical Research
Toward the Validation of Maternal Embryonic Leucine Zipper Kinase: Discovery, Optimization of Highly Potent and Selective Inhibitors, and Preliminary Biology Insight.
Novartis Institutes For Biomedical Research
Evolution of a New Class of VEGFR-2 Inhibitors from Scaffold Morphing and Redesign.
Novartis Institutes For Biomedical Research
Core Replacements in a Potent Series of VEGFR-2 Inhibitors and Their Impact on Potency, Solubility, and hERG.
Novartis Institutes For Biomedical Research
Identification of a 5-[3-phenyl-(2-cyclic-ether)-methylether]-4-aminopyrrolo[2,3-d]pyrimidine series of IGF-1R inhibitors.
Novartis Institutes For Biomedical Research
Design, synthesis and structure activity relationship of potent pan-PIM kinase inhibitors derived from the pyridyl carboxamide scaffold.
Novartis Institutes For Biomedical Research
Optimisation of a 5-[3-phenyl-(2-cyclic-ether)-methyl-ether]-4-aminopyrrolopyrimidine series of IGF-1R inhibitors.
Novartis Institutes For Biomedical Research
Potent, Selective, and Orally Bioavailable Inhibitors of VPS34 Provide Chemical Tools to Modulate Autophagy in Vivo.
Novartis Institutes For Biomedical Research
Discovery of diamide compounds as diacylglycerol acyltransferase 1 (DGAT1) inhibitors.
Novartis Institutes For Biomedical Research
Discovery of imidazo[1,2-a]-pyridine inhibitors of pan-PI3 kinases that are efficacious in a mouse xenograft model.
Novartis Institutes For Biomedical Research
Discovery of 1H-pyrazolo[3,4-b]pyridines as potent dual orexin receptor antagonists (DORAs).
Novartis Institutes For Biomedical Research
Discovery of RAF265: A Potent mut-B-RAF Inhibitor for the Treatment of Metastatic Melanoma.
Novartis Institutes For Biomedical Research
Orally bioavailable Syk inhibitors with activity in a rat PK/PD model.
Novartis Institutes For Biomedical Research
Tetrahydropyrrolo-diazepenones as inhibitors of ERK2 kinase.
Novartis Institutes For Biomedical Research
Discovery and Optimization of 4-(8-(3-Fluorophenyl)-1,7-naphthyridin-6-yl)transcyclohexanecarboxylic Acid, an Improved PDE4 Inhibitor for the Treatment of Chronic Obstructive Pulmonary Disease (COPD).
Novartis Institutes For Biomedical Research
Discovery of a novel tricyclic 4H-thiazolo[5',4':4,5]pyrano[2,3-c]pyridine-2-amino scaffold and its application in a PI3Ka inhibitor with high PI3K isoform selectivity and potent cellular activity.
Novartis Institutes For Biomedical Research
Ligand efficient tetrahydro-pyrazolopyridines as inhibitors of ERK2 kinase.
Novartis Institutes For Biomedical Research
Identification and optimisation of 4,5-dihydrobenzo[1,2-d:3,4-d]bisthiazole and 4,5-dihydrothiazolo[4,5-h]quinazoline series of selective phosphatidylinositol-3 kinase alpha inhibitors.
Novartis Institutes For Biomedical Research
Optimization of a Dibenzodiazepine Hit to a Potent and Selective Allosteric PAK1 Inhibitor.
Novartis Institutes For Biomedical Research
Discovery of Potent and Selective RSK Inhibitors as Biological Probes.
Novartis Institutes For Biomedical Research
Discovery of a Dihydroisoquinolinone Derivative (NVP-CGM097): A Highly Potent and Selective MDM2 Inhibitor Undergoing Phase 1 Clinical Trials in p53wt Tumors.
Novartis Institutes For Biomedical Research
Biocatalytic synthesis and structure elucidation of cyclized metabolites of the deacetylase inhibitor panobinostat (LBH589).
Novartis Institutes For Biomedical Research
CYP4F enzymes are responsible for the elimination of fingolimod (FTY720), a novel treatment of relapsing multiple sclerosis.
Novartis Institutes For Biomedical Research
Discovery and profiling of a selective and efficacious Syk inhibitor.
Novartis Institutes For Biomedical Research
3-alkoxy-pyrrolo[1,2-b]pyrazolines as selective androgen receptor modulators with ideal physicochemical properties for transdermal administration.
Novartis Institutes For Biomedical Research
The identification of 7-[(R)-2-((1S,2S)-2-benzyloxycyclopentylamino)-1-hydroxyethyl]-4-hydroxybenzothiazolone as an inhaled long-actingß2-adrenoceptor agonist.
Novartis Institutes For Biomedical Research
Structure-based design of substituted piperidines as a new class of highly efficacious oral direct Renin inhibitors.
Novartis Institutes For Biomedical Research
The discovery of potent, orally bioavailable pyrimidine-5-carbonitrile-6-alkyl CXCR2 receptor antagonists.
Novartis Institutes For Biomedical Research
From chemical tools to clinical medicines: nonimmunosuppressive cyclophilin inhibitors derived from the cyclosporin and sanglifehrin scaffolds.
Novartis Institutes For Biomedical Research
Structure-Based Drug Design of Novel, Potent, and Selective Azabenzimidazoles (ABI) as ATR Inhibitors.
Novartis Institutes For Biomedical Research
Structure-Based Drug Design of Novel Potent and Selective Tetrahydropyrazolo[1,5-a]pyrazines as ATR Inhibitors.
Novartis Institutes For Biomedical Research
Design, structure-activity relationship, and in vivo characterization of the development candidate NVP-HSP990.
Novartis Institutes For Biomedical Research
Discovery of 2-Pyridylpyrimidines as the First Orally Bioavailable GPR39 Agonists.
Novartis Institutes For Biomedical Research
Potent nonimmunosuppressive cyclophilin inhibitors with improved pharmaceutical properties and decreased transporter inhibition.
Novartis Institutes For Biomedical Research
The design and implementation of a generic lipopeptide scanning platform to enable the identification of 'locally acting' agonists for the apelin receptor.
Novartis Institutes For Biomedical Research
Design and Synthesis of Orally Bioavailable Benzimidazole Reverse Amides as Pan RAF Kinase Inhibitors.
Novartis Institutes For Biomedical Research
2-Amino-7-substituted benzoxazole analogs as potent RSK2 inhibitors.
Novartis Institutes For Biomedical Research
Orally active 7-substituted (4-benzylphthalazin-1-yl)-2-methylpiperazin-1-yl]nicotinonitriles as active-site inhibitors of sphingosine 1-phosphate lyase for the treatment of multiple sclerosis.
Novartis Institutes For Biomedical Research
Syk inhibitors with high potency in presence of blood.
Novartis Institutes For Biomedical Research
Tetra-substituted imidazoles as a new class of inhibitors of the p53-MDM2 interaction.
Novartis Institutes For Biomedical Research
Identification and characterization of small molecule modulators of the Epstein-Barr virus-induced gene 2 (EBI2) receptor.
Novartis Institutes For Biomedical Research
Discovery of C-(1-aryl-cyclohexyl)-methylamines as selective, orally available inhibitors of dipeptidyl peptidase IV.
Novartis Institutes For Biomedical Research
Structure Guided Optimization, in Vitro Activity, and in Vivo Activity of Pan-PIM Kinase Inhibitors.
Novartis Institutes For Biomedical Research
Discovery and in Vivo Evaluation of Potent Dual CYP11B2 (Aldosterone Synthase) and CYP11B1 Inhibitors.
Novartis Institutes For Biomedical Research
Discovery and characterization of NVP-QAV680, a potent and selective CRTh2 receptor antagonist suitable for clinical testing in allergic diseases.
Novartis Institutes For Biomedical Research
The thermodynamic basis for the use of lipophilic efficiency (LipE) in enthalpic optimizations.
Novartis Institutes For Biomedical Research
Identification of a novel series of orexin receptor antagonists with a distinct effect on sleep architecture for the treatment of insomnia.
Novartis Institutes For Biomedical Research
Structure-efficiency relationship of [1,2,4]triazol-3-ylamines as novel nicotinamide isosteres that inhibit tankyrases.
Novartis Institutes For Biomedical Research
Identification of NVP-TNKS656: the use of structure-efficiency relationships to generate a highly potent, selective, and orally active tankyrase inhibitor.
Novartis Institutes For Biomedical Research
Structure guided optimization of a fragment hit to imidazopyridine inhibitors of PI3K.
Novartis Institutes For Biomedical Research
Discovery of novel indolinone-based, potent, selective and brain penetrant inhibitors of LRRK2.
Novartis Institutes For Biomedical Research
Discovery of NVP-BYL719 a potent and selective phosphatidylinositol-3 kinase alpha inhibitor selected for clinical evaluation.
Novartis Institutes For Biomedical Research
The kinetic deuterium isotope effect as applied to metabolic deactivation of imatinib to the des-methyl metabolite, CGP74588.
Novartis Institutes For Biomedical Research
The role of the acidity of N-heteroaryl sulfonamides as inhibitors of bcl-2 family protein-protein interactions.
Novartis Institutes For Biomedical Research
Ergoline derivatives as highly potent and selective antagonists at the somatostatin sst 1 receptor.
Novartis Institutes For Biomedical Research
SAR of the arylpiperazine moiety of obeline somatostatin sst1 receptor antagonists.
Novartis Institutes For Biomedical Research
Identification and SAR of potent and selective non-peptide obeline somatostatin sst1 receptor antagonists.
Novartis Institutes For Biomedical Research
An investigation into the structure-activity relationships associated with the systematic modification of theß(2)-adrenoceptor agonist indacaterol.
Novartis Institutes For Biomedical Research
Solubility-driven optimization of phosphodiesterase-4 inhibitors leading to a clinical candidate.
Novartis Institutes For Biomedical Research
Structure-activity relationship and pharmacokinetic studies of sotrastaurin (AEB071), a promising novel medicine for prevention of graft rejection and treatment of psoriasis.
Novartis Institutes For Biomedical Research
Discovery of 1H-pyrrolo[2,3-c]pyridine-7-carboxamides as novel, allosteric mGluR5 antagonists.
Novartis Institutes For Biomedical Research
2,6-Naphthyridines as potent and selective inhibitors of the novel protein kinase C isozymes.
Novartis Institutes For Biomedical Research
The Substrate-Activity-Screening methodology applied to receptor tyrosine kinases: a proof-of-concept study.
Novartis Institutes For Biomedical Research
Development of isoform selective PI3-kinase inhibitors as pharmacological tools for elucidating the PI3K pathway.
Novartis Institutes For Biomedical Research
The central valine concept provides an entry in a new class of non peptide inhibitors of the p53-MDM2 interaction.
Novartis Institutes For Biomedical Research
[1,2,4]triazol-3-ylsulfanylmethyl)-3-phenyl-[1,2,4]oxadiazoles: antagonists of the Wnt pathway that inhibit tankyrases 1 and 2 via novel adenosine pocket binding.
Novartis Institutes For Biomedical Research
Optimization of the in vitro cardiac safety of hydroxamate-based histone deacetylase inhibitors.
Novartis Institutes For Biomedical Research
Identification of a potent Janus kinase 3 inhibitor with high selectivity within the Janus kinase family.
Novartis Institutes For Biomedical Research
Identification and structure-activity relationships of ortho-biphenyl carboxamides as potent Smoothened antagonists inhibiting the Hedgehog signaling pathway.
Novartis Institutes For Biomedical Research
"Virtual fragment linking": an approach to identify potent binders from low affinity fragment hits.
Novartis Institutes For Biomedical Research
Design and structure-activity relationships of potent and selective inhibitors of undecaprenyl pyrophosphate synthase (UPPS): tetramic, tetronic acids and dihydropyridin-2-ones.
Novartis Institutes For Biomedical Research
Reduced cardiac side-effect potential by introduction of polar groups: discovery of NIBR-1282, an orally bioavailable CCR5 antagonist which is active in vivo.
Novartis Institutes For Biomedical Research
Identification of a series of highly potent activators of the Nurr1 signaling pathway.
Novartis Institutes For Biomedical Research
Naphthalen-1-yl-(4-pentyloxynaphthalen-1-yl)methanone: a potent, orally bioavailable human CB1/CB2 dual agonist with antihyperalgesic properties and restricted central nervous system penetration.
Novartis Institutes For Biomedical Research
ABP688, a novel selective and high affinity ligand for the labeling of mGlu5 receptors: identification, in vitro pharmacology, pharmacokinetic and biodistribution studies.
Novartis Institutes For Biomedical Research
Novel CCR1 antagonists with oral activity in the mouse collagen induced arthritis.
Novartis Institutes For Biomedical Research
A new orally bioavailable dual adenosine A2B/A3 receptor antagonist with therapeutic potential.
Novartis Institutes For Biomedical Research
SAR of benzoylpyridines and benzophenones as p38alpha MAP kinase inhibitors with oral activity.
Novartis Institutes For Biomedical Research
New aromatase inhibitors from the 3-pyridyl arylether and 1-aryl pyrrolo[2,3-c]pyridine series.
Novartis Institutes For Biomedical Research
Potent and selective 2-naphthylsulfonamide substituted hydroxamic acid inhibitors of matrix metalloproteinase-13.
Novartis Institutes For Biomedical Research
Human HDAC isoform selectivity achieved via exploitation of the acetate release channel with structurally unique small molecule inhibitors.
Novartis Institutes For Biomedical Research
Special ergolines efficiently inhibit the chemokine receptor CXCR3 in blood.
Novartis Institutes For Biomedical Research
The design, synthesis and structure-activity relationships of novel isoindoline-based histone deacetylase inhibitors.
Novartis Institutes For Biomedical Research
In vivo and in vitro SAR of tetracyclic MAPKAP-K2 (MK2) inhibitors. Part I.
Novartis Institutes For Biomedical Research
In vivo and in vitro SAR of tetracyclic MAPKAP-K2 (MK2) inhibitors. Part II.
Novartis Institutes For Biomedical Research
Design and synthesis of 5,6-fused heterocyclic amides as Raf kinase inhibitors.
Novartis Institutes For Biomedical Research
Structure based design, synthesis and SAR of cyclic hydroxyethylamine (HEA) BACE-1 inhibitors.
Novartis Institutes For Biomedical Research
3,5-diarylazoles as novel and selective inhibitors of protein kinase D.
Novartis Institutes For Biomedical Research
Exploring subtype selectivity and metabolic stability of a novel series of ligands for the benzodiazepine binding site of the GABAA receptor.
Novartis Institutes For Biomedical Research
Identification and structure-activity relationship of 2-morpholino 6-(3-hydroxyphenyl) pyrimidines, a class of potent and selective PI3 kinase inhibitors.
Novartis Institutes For Biomedical Research
4-(Pyrazol-4-yl)-pyrimidines as selective inhibitors of cyclin-dependent kinase 4/6.
Novartis Institutes For Biomedical Research
Structural resemblances and comparisons of the relative pharmacological properties of imatinib and nilotinib.
Novartis Institutes For Biomedical Research
Identification and mechanistic characterization of low-molecular-weight inhibitors for HuR.
Novartis Institutes For Biomedical Research
Penta-substituted benzimidazoles as potent antagonists of the calcium-sensing receptor (CaSR-antagonists).
Novartis Institutes For Biomedical Research
A physical properties based approach for the exploration of a 4-hydroxybenzothiazolone series of beta2-adrenoceptor agonists as inhaled long-acting bronchodilators.
Novartis Institutes For Biomedical Research
Identification of potent and selective amidobipyridyl inhibitors of protein kinase D.
Novartis Institutes For Biomedical Research
Identification of orally available naphthyridine protein kinase D inhibitors.
Novartis Institutes For Biomedical Research
The discovery of potent inhibitors of aldosterone synthase that exhibit selectivity over 11-beta-hydroxylase.
Novartis Institutes For Biomedical Research
The identification of indacaterol as an ultralong-acting inhaled beta2-adrenoceptor agonist.
Novartis Institutes For Biomedical Research
Discovery and SAR of potent, orally available 2,8-diaryl-quinoxalines as a new class of JAK2 inhibitors.
Novartis Institutes For Biomedical Research
Conformational refinement of hydroxamate-based histone deacetylase inhibitors and exploration of 3-piperidin-3-ylindole analogues of dacinostat (LAQ824).
Novartis Institutes For Biomedical Research
Design of two new chemotypes for inhibiting the Janus kinase 2 by scaffold morphing.
Novartis Institutes For Biomedical Research
S1P receptor mediated activity of FTY720 phosphate mimics.
Novartis Institutes For Biomedical Research
2-Amino-aryl-7-aryl-benzoxazoles as potent, selective and orally available JAK2 inhibitors.
Novartis Institutes For Biomedical Research
Decahydroisoquinoline derivatives as novel non-peptidic, potent and subtype-selective somatostatin sst(3) receptor antagonists.
Novartis Institutes For Biomedical Research
Novel 3-aminopyrazole inhibitors of MK-2 discovered by scaffold hopping strategy.
Novartis Institutes For Biomedical Research
Synthesis and evaluation of two series of 4'-aza-carbocyclic nucleosides as adenosine A2A receptor agonists.
Novartis Institutes For Biomedical Research
1-Alkyl-4-phenyl-6-alkoxy-1H-quinazolin-2-ones: a novel series of potent calcium-sensing receptor antagonists.
Novartis Institutes For Biomedical Research
Macrocyclic BACE-1 inhibitors acutely reduce Abeta in brain after po application.
Novartis Institutes For Biomedical Research
Pyrazole derived from (+)-3-carene; a novel potent, selective scaffold for sphingosine-1-phosphate (S1P(1)) receptor agonists.
Novartis Institutes For Biomedical Research
The discovery of tetrahydro-beta-carbolines as inhibitors of the kinesin Eg5.
Novartis Institutes For Biomedical Research
Piperidyl amides as novel, potent and orally active mGlu5 receptor antagonists with anxiolytic-like activity.
Novartis Institutes For Biomedical Research
Special ergolines are highly selective, potent antagonists of the chemokine receptor CXCR3: discovery, characterization and preliminary SAR of a promising lead.
Novartis Institutes For Biomedical Research
Discovery of a new class of catalytic topoisomerase II inhibitors targeting the ATP-binding site by structure based design. Part I.
Novartis Institutes For Biomedical Research
Macrocyclic peptidomimetic beta-secretase (BACE-1) inhibitors with activity in vivo.
Novartis Institutes For Biomedical Research
1-amino-4-benzylphthalazines as orally bioavailable smoothened antagonists with antitumor activity.
Novartis Institutes For Biomedical Research
Discovery of novel non-peptidic beta-alanine piperazine amide derivatives and their optimization to achiral, easily accessible, potent and selective somatostatin sst1 receptor antagonists.
Novartis Institutes For Biomedical Research
Gamma-lactams--a novel scaffold for highly potent and selective alpha 7 nicotinic acetylcholine receptor agonists.
Novartis Institutes For Biomedical Research
Design, structure-activity relationships and in vivo characterization of 4-amino-3-benzimidazol-2-ylhydroquinolin-2-ones: a novel class of receptor tyrosine kinase inhibitors.
Novartis Institutes For Biomedical Research
Orally bioavailable isothioureas block function of the chemokine receptor CXCR4 in vitro and in vivo.
Novartis Institutes For Biomedical Research
Overcoming hERG issues for brain-penetrating cathepsin S inhibitors: 2-cyanopyrimidines. Part 2.
Novartis Institutes For Biomedical Research
Effect of cathepsin K inhibitors on bone resorption.
Novartis Institutes For Biomedical Research
4-Amino-2-cyanopyrimidines: novel scaffold for nonpeptidic cathepsin S inhibitors.
Novartis Institutes For Biomedical Research
Discovery of selective and nonpeptidic cathepsin S inhibitors.
Novartis Institutes For Biomedical Research
Entry into a new class of protein kinase inhibitors by pseudo ring design.
Novartis Institutes For Biomedical Research
Discovery of Ligands for TRIM58, a Novel Tissue-Selective E3 Ligase.
Novartis Institutes for Biomedical Research
Design of a Supersoft Topical JAK Inhibitor, Which Is Effective in Human Skin but Rapidly Deactivated in Blood.
Novartis Institutes For Biomedical Research
Discovery of the TLR7/8 Antagonist MHV370 for Treatment of Systemic Autoimmune Diseases.
Novartis Institutes for Biomedical Research
Discovery of New Binders for DCAF1, an Emerging Ligase Target in the Targeted Protein Degradation Field.
Novartis Institutes for Biomedical Research
Discovery and Structure-Based Design of Inhibitors of the WD Repeat-Containing Protein 5 (WDR5)-MYC Interaction.
Novartis Institutes For Biomedical Research
Optimization of halopemide for phospholipase D2 inhibition.
Novartis Institutes For Biomedical Research
Identification of Brain-Penetrant ATP-Competitive mTOR Inhibitors for CNS Syndromes.
Novartis Institutes for Biomedical Research
Optimization of 3-Pyrimidin-4-yl-oxazolidin-2-ones as Allosteric and Mutant Specific Inhibitors of IDH1.
Novartis Institutes For Biomedical Research
Discovery of a brain-sparing GIRK1/4 inhibitor for pharmacological cardioversion of atrial fibrillation.
Novartis Institutes For Biomedical Research
A Novel Potent Oral Series of VEGFR2 Inhibitors Abrogate Tumor Growth by Inhibiting Angiogenesis.
Novartis Institutes For Biomedical Research
Novel Concept for Super-Soft Topical Drugs: Deactivation by an Enzyme-Induced Switch into an Inactive Conformation.
Novartis Institutes For Biomedical Research
JDQ443, a Structurally Novel, Pyrazole-Based, Covalent Inhibitor of KRAS
Novartis Institutes For Biomedical Research
Drug Hunting at the Nexus of Medicinal Chemistry and Chemical Biology and the Discovery of Novel Therapeutic Modalities.
Novartis Institutes For Biomedical Research
Progress in mechanistically novel treatments for schizophrenia.
Novartis Institutes For Biomedical Research
Discovery of the Clinical Candidate MAK683: An EED-Directed, Allosteric, and Selective PRC2 Inhibitor for the Treatment of Advanced Malignancies.
Novartis Institutes For Biomedical Research
Discovery and Preclinical Pharmacology of INE963, a Potent and Fast-Acting Blood-Stage Antimalarial with a High Barrier to Resistance and Potential for Single-Dose Cures in Uncomplicated Malaria.
Novartis Institutes For Biomedical Research
A cassette-dosing approach for improvement of oral bioavailability of dual TACE/MMP inhibitors.
Novartis Institutes For Biomedical Research
Identification and biological characterization of 6-aryl-7-isopropylquinazolinones as novel TRPV1 antagonists that are effective in models of chronic pain.
Novartis Institutes For Biomedical Research
Inhibition of DNA helicases with DNA-competitive inhibitors.
Novartis Institutes For Biomedical Research
Pyrazoloheteroaryls: novel p38alpha MAP kinase inhibiting scaffolds with oral activity.
Novartis Institutes For Biomedical Research
Design and preparation of 2-benzamido-pyrimidines as inhibitors of IKK.
Novartis Institutes For Biomedical Research
Biological evaluation of 1-alkyl-3-phenylthioureas as orally active HDL-elevating agents.
Novartis Institutes For Biomedical Research
Identification of NVP-CLR457 as an Orally Bioavailable Non-CNS-Penetrant pan-Class IA Phosphoinositol-3-Kinase Inhibitor.
Novartis Institutes For Biomedical Research
A kinase inhibitor which specifically targets the ABL myristate pocket (STAMP), but unlike asciminib crosses the blood-brain barrier.
Novartis Institutes For Biomedical Research
Novel immunomodulator FTY720 is phosphorylated in rats and humans to form a single stereoisomer. Identification, chemical proof, and biological characterization of the biologically active species and its enantiomer.
Novartis Institutes For Biomedical Research
Paradoxical Increase of Permeability and Lipophilicity with the Increasing Topological Polar Surface Area within a Series of PRMT5 Inhibitors.
Novartis Institutes For Biomedical Research
Discovery of Novel Quinoline-Based Proteasome Inhibitors for Human African Trypanosomiasis (HAT).
Novartis Institutes For Biomedical Research
Discovery of a novel 2-aminopyrazine-3-carboxamide as a potent and selective inhibitor of Activin Receptor-Like Kinase-2 (ALK2) for the treatment of fibrodysplasia ossificans progressiva.
Novartis Institutes For Biomedical Research
N-Acyl arylsulfonamides as novel, reversible inhibitors of human steroid sulfatase.
Novartis Institutes For Biomedical Research
1,4-Diazepane-2,5-diones as novel inhibitors of LFA-1.
Novartis Institutes For Biomedical Research
Novel purine nitrile derived inhibitors of the cysteine protease cathepsin K.
Novartis Institutes For Biomedical Research
Structure-Based Optimization of a Fragment-like TLR8 Binding Screening Hit to an
Novartis Institutes For Biomedical Research
Urea derivatives of STI571 as inhibitors of Bcr-Abl and PDGFR kinases.
Novartis Institutes For Biomedical Research
Discovery of Icenticaftor (QBW251), a Cystic Fibrosis Transmembrane Conductance Regulator Potentiator with Clinical Efficacy in Cystic Fibrosis and Chronic Obstructive Pulmonary Disease.
Novartis Institutes For Biomedical Research
Novel p38 inhibitors with potent oral efficacy in several models of rheumatoid arthritis.
Novartis Institutes For Biomedical Research
Statin-derived 1,3-oxazinan-2-ones as submicromolar inhibitors of LFA-1/ICAM-1 interaction: stabilization of the metabolically labile vanillyl side chain.
Novartis Institutes For Biomedical Research
Orally bioavailable competitive CCR5 antagonists.
Novartis Institutes For Biomedical Research
Discovery and Toxicological Profiling of Aminopyridines as Orally Bioavailable Selective Inhibitors of PI3-Kinase γ.
Novartis Institutes For Biomedical Research
Discovery and Optimization of DNA Gyrase and Topoisomerase IV Inhibitors with Potent Activity against Fluoroquinolone-Resistant Gram-Positive Bacteria.
Novartis Institutes For Biomedical Research
Discovery and Optimization of Novel SUCNR1 Inhibitors: Design of Zwitterionic Derivatives with a Salt Bridge for the Improvement of Oral Exposure.
Novartis Institutes For Biomedical Research
Synthesis and Structure-Activity Relationship of Tetra-Substituted Cyclohexyl Diol Inhibitors of Proviral Insertion of Moloney Virus (PIM) Kinases.
Novartis Institutes For Biomedical Research
Discovery of Roblitinib (FGF401) as a Reversible-Covalent Inhibitor of the Kinase Activity of Fibroblast Growth Factor Receptor 4.
Novartis Institutes For Biomedical Research
Fragment-to-Lead Medicinal Chemistry Publications in 2019.
Novartis Institutes For Biomedical Research
Development of autotaxin inhibitors: A series of tetrazole cinnamides.
Novartis Institutes For Biomedical Research
Design of Potent and Selective Covalent Inhibitors of Bruton's Tyrosine Kinase Targeting an Inactive Conformation.
Novartis Institutes For Biomedical Research
Discovery of Orally Active Hydroxyethylamine Based SPPL2a Inhibitors.
Novartis Institutes For Biomedical Research
Discovery of a novel indole pharmacophore for the irreversible inhibition of myeloperoxidase (MPO).
Novartis Institutes For Biomedical Research
Structure-Based Design and Preclinical Characterization of Selective and Orally Bioavailable Factor XIa Inhibitors: Demonstrating the Power of an Integrated S1 Protease Family Approach.
Novartis Institutes For Biomedical Research
Topoisomerase Inhibitors Addressing Fluoroquinolone Resistance in Gram-Negative Bacteria.
Novartis Institutes For Biomedical Research
Discovery of 4-((2 S,4 S)-4-Ethoxy-1-((5-methoxy-7-methyl-1 H-indol-4-yl)methyl)piperidin-2-yl)benzoic Acid (LNP023), a Factor B Inhibitor Specifically Designed To Be Applicable to Treating a Diverse Array of Complement Mediated Diseases
Novartis Institutes For Biomedical Research
Discovery of Novel Dot1L Inhibitors through a Structure-Based Fragmentation Approach.
Novartis Institutes For Biomedical Research
Structure-based design of potent linear peptide inhibitors of the YAP-TEAD protein-protein interaction derived from the YAP omega-loop sequence.
Novartis Institutes For Biomedical Research
Optimization of a Fragment-Based Screening Hit toward Potent DOT1L Inhibitors Interacting in an Induced Binding Pocket.
Novartis Institutes For Biomedical Research
Allosteric Inhibition of SHP2: Identification of a Potent, Selective, and Orally Efficacious Phosphatase Inhibitor.
Novartis Institutes For Biomedical Research
Discovery and Pharmacological Characterization of Novel Quinazoline-Based PI3K Delta-Selective Inhibitors.
Novartis Institutes For Biomedical Research
Uncoupling the Structure-Activity Relationships of β2 Adrenergic Receptor Ligands from Membrane Binding.
Novartis Institutes For Biomedical Research
Discovery of a small molecule RXFP3/4 agonist that increases food intake in rats upon acute central administration.
Novartis Institutes For Biomedical Research
Design, Synthesis, and Preclinical Characterization of Selective Factor D Inhibitors Targeting the Alternative Complement Pathway.
Novartis Institutes For Biomedical Research
Application of Virtual Screening to the Identification of New LpxC Inhibitor Chemotypes, Oxazolidinone and Isoxazoline.
Novartis Institutes For Biomedical Research
Discovery of a Brain-Penetrant ATP-Competitive Inhibitor of the Mechanistic Target of Rapamycin (mTOR) for CNS Disorders.
Novartis Institutes For Biomedical Research
Structure-Guided Design of Substituted Biphenyl Butanoic Acid Derivatives as Neprilysin Inhibitors.
Novartis Institutes For Biomedical Research
Successful Strategies for Mitigation of a Preclinical Signal for Phototoxicity in a DGAT1 Inhibitor.
Novartis Institutes For Biomedical Research
Discovery of a Selective and Potent Inhibitor of Mitogen-Activated Protein Kinase-Interacting Kinases 1 and 2 (MNK1/2) Utilizing Structure-Based Drug Design.
Novartis Institutes For Biomedical Research
Discovery of Oral VEGFR-2 Inhibitors with Prolonged Ocular Retention That Are Efficacious in Models of Wet Age-Related Macular Degeneration.
Novartis Institutes For Biomedical Research
Discovery of N-[5-(6-Chloro-3-cyano-1-methyl-1H-indol-2-yl)-pyridin-3-ylmethyl]-ethanesulfonamide, a Cortisol-Sparing CYP11B2 Inhibitor that Lowers Aldosterone in Human Subjects.
Novartis Institutes For Biomedical Research
Identification of N-(4-((1R,3S,5S)-3-Amino-5-methylcyclohexyl)pyridin-3-yl)-6-(2,6-difluorophenyl)-5-fluoropicolinamide (PIM447), a Potent and Selective Proviral Insertion Site of Moloney Murine Leukemia (PIM) 1, 2, and 3 Kinase Inhibitor in Clinical Trials for Hematological Malignancies.
Novartis Institutes For Biomedical Research
Identification and optimisation of a 4',5-bisthiazole series of selective phosphatidylinositol-3 kinase alpha inhibitors.
Novartis Institutes For Biomedical Research
The discovery of potent, orally bioavailable pyrazolo and triazolopyrimidine CXCR2 receptor antagonists.
Novartis Institutes For Biomedical Research
An effective prodrug strategy to selectively enhance ocular exposure of a cannabinoid receptor (CB1/2) agonist.
Novartis Institutes For Biomedical Research
Lipophilic Isosteres of a π-π Stacking Interaction: New Inhibitors of the Bcl-2-Bak Protein-Protein Interaction.
Novartis Institutes For Biomedical Research
Design and synthesis of 6,6-fused heterocyclic amides as raf kinase inhibitors.
Novartis Institutes For Biomedical Research
Synthesis and characterization of a BODIPY-labeled derivative of Soraphen A that binds to acetyl-CoA carboxylase.
Novartis Institutes For Biomedical Research
Structure-activity relationship studies on a novel class of antiproliferative agents derived from Lavendustin A. Part I: Ring A modifications.
Novartis Institutes For Biomedical Research
Syntheses and optimization of new GS39783 analogues as positive allosteric modulators of GABA B receptors.
Novartis Institutes For Biomedical Research
NBD-labeled derivatives of the immunomodulatory drug FTY720 as tools for metabolism and mode of action studies.
Novartis Institutes For Biomedical Research
Discovery of Orally Active Inhibitors of Brahma Homolog (BRM)/SMARCA2 ATPase Activity for the Treatment of Brahma Related Gene 1 (BRG1)/SMARCA4-Mutant Cancers.
Novartis Institutes For Biomedical Research
In vitro and in vivo characterization of a novel, highly potent p53-MDM2 inhibitor.
Novartis Institutes For Biomedical Research
Design and synthesis of potent RSK inhibitors.
Novartis Institutes For Biomedical Research
Discovery of Small Molecule Splicing Modulators of Survival Motor Neuron-2 (SMN2) for the Treatment of Spinal Muscular Atrophy (SMA).
Novartis Institutes For Biomedical Research
Modulating ADME Properties by Fluorination: MK2 Inhibitors with Improved Oral Exposure.
Novartis Institutes For Biomedical Research
2-Formylpyridyl Ureas as Highly Selective Reversible-Covalent Inhibitors of Fibroblast Growth Factor Receptor 4.
Novartis Institutes For Biomedical Research
Discovery of Asciminib (ABL001), an Allosteric Inhibitor of the Tyrosine Kinase Activity of BCR-ABL1.
Novartis Institutes For Biomedical Research
Optimization of 3-Pyrimidin-4-yl-oxazolidin-2-ones as Orally Bioavailable and Brain Penetrant Mutant IDH1 Inhibitors.
Novartis Institutes For Biomedical Research
Structure-based design and synthesis of macrocyclic human rhinovirus 3C protease inhibitors.
Novartis Institutes For Biomedical Research
Optimization of novel monobactams with activity against carbapenem-resistant Enterobacteriaceae - Identification of LYS228.
Novartis Institutes For Biomedical Research
Imidazo[1,2-a]pyridin-6-yl-benzamide analogs as potent RAF inhibitors.
Novartis Institutes For Biomedical Research
Development of Selective, Orally Active GPR4 Antagonists with Modulatory Effects on Nociception, Inflammation, and Angiogenesis.
Novartis Institutes For Biomedical Research
Discovery of CDZ173 (Leniolisib), Representing a Structurally Novel Class of PI3K Delta-Selective Inhibitors.
Novartis Institutes For Biomedical Research
Development of autotaxin inhibitors: A series of zinc binding triazoles.
Novartis Institutes For Biomedical Research
Discovery of amino-1,4-oxazines as potent BACE-1 inhibitors.
Novartis Institutes For Biomedical Research
N-aryl-piperidine-4-carboxamides as a novel class of potent inhibitors of MALT1 proteolytic activity.
Novartis Institutes For Biomedical Research
The Discovery of N-(1-Methyl-5-(trifluoromethyl)-1H-pyrazol-3-yl)-5-((6- ((methylamino)methyl)pyrimidin-4-yl)oxy)-1H-indole-1-carboxamide (Acrizanib), a VEGFR-2 Inhibitor Specifically Designed for Topical Ocular Delivery, as a Therapy for Neovascular Age-Related Macular Degeneration.
Novartis Institutes For Biomedical Research
Fragment-Based Drug Discovery of Inhibitors of Phosphopantetheine Adenylyltransferase from Gram-Negative Bacteria.
Novartis Institutes For Biomedical Research
Design and synthesis of potent and orally active GPR4 antagonists with modulatory effects on nociception, inflammation, and angiogenesis.
Novartis Institutes For Biomedical Research
Structure-Guided Design of EED Binders Allosterically Inhibiting the Epigenetic Polycomb Repressive Complex 2 (PRC2) Methyltransferase.
Novartis Institutes For Biomedical Research
Optimization of Allosteric With-No-Lysine (WNK) Kinase Inhibitors and Efficacy in Rodent Hypertension Models.
Novartis Institutes For Biomedical Research
F-NMR-Based Dual-Site Reporter Assay for the Discovery and Distinction of Catalytic and Allosteric Kinase Inhibitors.
Novartis Institutes For Biomedical Research
Discovery of a Novel Piperidine-Based Inhibitor of Cholesteryl Ester Transfer Protein (CETP) That Retains Activity in Hypertriglyceridemic Plasma.
Novartis Institutes For Biomedical Research
Design, Synthesis, and Properties of a Potent Inhibitor of Pseudomonas aeruginosa Deacetylase LpxC.
Novartis Institutes For Biomedical Research
Discovery of LSZ102, a Potent, Orally Bioavailable Selective Estrogen Receptor Degrader (SERD) for the Treatment of Estrogen Receptor Positive Breast Cancer.
Novartis Institutes For Biomedical Research
Synthesis, Binding Mode, and Antihyperglycemic Activity of Potent and Selective (5-Imidazol-2-yl-4-phenylpyrimidin-2-yl)[2-(2-pyridylamino)ethyl]amine Inhibitors of Glycogen Synthase Kinase 3.
Novartis Institutes For Biomedical Research
Discovery of an Orally Bioavailable Benzimidazole Diacylglycerol Acyltransferase 1 (DGAT1) Inhibitor That Suppresses Body Weight Gain in Diet-Induced Obese Dogs and Postprandial Triglycerides in Humans.
Novartis Institutes For Biomedical Research
Imidazopyrimidine and imidazotriazine derivative, and pharmaceutical composition comprising the same
Sk Biopharmaceuticals