614 articles for thisTarget
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Discovery of a Highly Selective Tankyrase Inhibitor Displaying Growth Inhibition Effects against a Diverse Range of Tumor Derived Cell Lines.
Glaxosmithkline
The discovery of potent and selective kynurenine 3-monooxygenase inhibitors for the treatment of acute pancreatitis.
Glaxosmithkline
Discovery of a Potent, Cell Penetrant, and Selective p300/CBP-Associated Factor (PCAF)/General Control Nonderepressible 5 (GCN5) Bromodomain Chemical Probe.
Glaxosmithkline
Discovery of GSK2193874: An Orally Active, Potent, and Selective Blocker of Transient Receptor Potential Vanilloid 4.
Glaxosmithkline
Exploration of phenylpropanoic acids as agonists of the free fatty acid receptor 4 (FFA4): Identification of an orally efficacious FFA4 agonist.
Glaxosmithkline
SB-656104-A: a novel 5-HT(7) receptor antagonist with improved in vivo properties.
Glaxosmithkline
Identification of potent and selective oxytocin antagonists. Part 1: indole and benzofuran derivatives.
Glaxosmithkline
Bicyclic piperazinylbenzenesulphonamides are potent and selective 5-HT6 receptor antagonists.
Glaxosmithkline
Novel (4-piperazin-1-ylquinolin-6-yl) arylsulfonamides with high affinity and selectivity for the 5-HT(6) receptor.
Glaxosmithkline
Synthesis of N-alkyl substituted indolocarbazoles as potent inhibitors of human cytomegalovirus replication.
Glaxosmithkline
1,3-Biarylureas as selective non-peptide antagonists of the orexin-1 receptor.
Glaxosmithkline
Structure-activity relationship investigations of a potent and selective benzodiazepine oxytocin antagonist.
Glaxosmithkline
Substituent Effects on Drug-Receptor H-bond Interactions: Correlations Useful for the Design of Kinase Inhibitors.
Glaxosmithkline
The Identification and Pharmacological Characterization of 6-(tert-Butylsulfonyl)-N-(5-fluoro-1H-indazol-3-yl)quinolin-4-amine (GSK583), a Highly Potent and Selective Inhibitor of RIP2 Kinase.
Glaxosmithkline
Optimizing Ligand Efficiency of Selective Androgen Receptor Modulators (SARMs).
Glaxosmithkline
GSK114: A selective inhibitor for elucidating the biological role of TNNI3K.
Glaxosmithkline
Discovery and Optimization of Potent, Selective, and in Vivo Efficacious 2-Aryl Benzimidazole BCATm Inhibitors.
Glaxosmithkline
The design of 8-hydroxyquinoline tetracyclic lactams as HIV-1 integrase strand transfer inhibitors.
Glaxosmithkline
Discovery of a Novel 2,6-Disubstituted Glucosamine Series of Potent and Selective Hexokinase 2 Inhibitors.
Glaxosmithkline
Structurally Diverse Mitochondrial Branched Chain Aminotransferase (BCATm) Leads with Varying Binding Modes Identified by Fragment Screening.
Glaxosmithkline
Identification of nonabsorbable inhibitors of the scavenger receptor-BI (SR-BI) for tissue-specific administration.
Glaxosmithkline
DNA-Encoded Library Screening Identifies Benzo[b][1,4]oxazepin-4-ones as Highly Potent and Monoselective Receptor Interacting Protein 1 Kinase Inhibitors.
Glaxosmithkline
Novel tricyclics (e.g., GSK945237) as potent inhibitors of bacterial type IIA topoisomerases.
Glaxosmithkline
Cell Penetrant Inhibitors of the KDM4 and KDM5 Families of Histone Lysine Demethylases. 1. 3-Amino-4-pyridine Carboxylate Derivatives.
Glaxosmithkline
Cell Penetrant Inhibitors of the KDM4 and KDM5 Families of Histone Lysine Demethylases. 2. Pyrido[3,4-d]pyrimidin-4(3H)-one Derivatives.
Glaxosmithkline
Discovery of Tetrahydropyrazolopyridine as Sphingosine 1-Phosphate Receptor 3 (S1P3)-Sparing S1P1 Agonists Active at Low Oral Doses.
Glaxosmithkline
Discovery and Characterization of GSK2801, a Selective Chemical Probe for the Bromodomains BAZ2A and BAZ2B.
Glaxosmithkline
Crystal structures of human RIP2 kinase catalytic domain complexed with ATP-competitive inhibitors: Foundations for understanding inhibitor selectivity.
Glaxosmithkline
Navigating CYP1A Induction and Arylhydrocarbon Receptor Agonism in Drug Discovery. A Case History with S1P1 Agonists.
Glaxosmithkline
Discovery, SAR, and X-ray Binding Mode Study of BCATm Inhibitors from a Novel DNA-Encoded Library.
Glaxosmithkline
Discovery of Potent and Selective Inhibitors for ADAMTS-4 through DNA-Encoded Library Technology (ELT).
Glaxosmithkline
The Discovery of in Vivo Active Mitochondrial Branched-Chain Aminotransferase (BCATm) Inhibitors by Hybridizing Fragment and HTS Hits.
Glaxosmithkline
Identification of Purines and 7-Deazapurines as Potent and Selective Type I Inhibitors of Troponin I-Interacting Kinase (TNNI3K).
Glaxosmithkline
Carbamoyl Triazoles, Known Serine Protease Inhibitors, Are a Potent New Class of Antimalarials.
Glaxosmithkline
Discovery of 4-Amino-8-quinoline Carboxamides as Novel, Submicromolar Inhibitors of NAD-Hydrolyzing Enzyme CD38.
Glaxosmithkline
Brain tissue binding of drugs: evaluation and validation of solid supported porcine brain membrane vesicles (TRANSIL) as a novel high-throughput method.
Glaxosmithkline
Structure-Based Optimization of Naphthyridones into Potent ATAD2 Bromodomain Inhibitors.
Glaxosmithkline
Fragment-Based Discovery of Low-Micromolar ATAD2 Bromodomain Inhibitors.
Glaxosmithkline
Discovery of a Potent Class of PI3Ka Inhibitors with Unique Binding Mode via Encoded Library Technology (ELT).
Glaxosmithkline
Metabolites of PPI-2458, a selective, irreversible inhibitor of methionine aminopeptidase-2: structure determination and in vivo activity.
Glaxosmithkline
Casopitant: in vitro data and SimCyp simulation to predict in vivo metabolic interactions involving cytochrome P450 3A4.
Glaxosmithkline
In vitro investigations into the roles of drug transporters and metabolizing enzymes in the disposition and drug interactions of dolutegravir, a HIV integrase inhibitor.
Glaxosmithkline
Discovery, Synthesis, and Biological Evaluation of Thiazoloquin(az)olin(on)es as Potent CD38 Inhibitors.
Glaxosmithkline
Structural requirements for TLR7-selective signaling by 9-(4-piperidinylalkyl)-8-oxoadenine derivatives.
Glaxosmithkline
Lead identification of benzimidazolone and azabenzimidazolone arylsulfonamides as CC-chemokine receptor 4 (CCR4) antagonists.
Glaxosmithkline
Naphthyridinone (NTD) integrase inhibitors 4. Investigating N1 acetamide substituent effects with C3 amide groups.
Glaxosmithkline
Identification of diarylsulfonamides as agonists of the free fatty acid receptor 4 (FFA4/GPR120).
Glaxosmithkline
Novel heterocyclic scaffolds of GW4064 as farnesoid X receptor agonists.
Glaxosmithkline
2-Aminopyrimidin-4(1H)-one as the novel bioisostere of urea: discovery of novel and potent CXCR2 antagonists.
Glaxosmithkline
Optimization of sphingosine-1-phosphate-1 receptor agonists: effects of acidic, basic, and zwitterionic chemotypes on pharmacokinetic and pharmacodynamic profiles.
Glaxosmithkline
1,3-Dimethyl Benzimidazolones Are Potent, Selective Inhibitors of the BRPF1 Bromodomain.
Glaxosmithkline
The discovery of I-BET726 (GSK1324726A), a potent tetrahydroquinoline ApoA1 up-regulator and selective BET bromodomain inhibitor.
Glaxosmithkline
Application of encoded library technology (ELT) to a protein-protein interaction target: discovery of a potent class of integrin lymphocyte function-associated antigen 1 (LFA-1) antagonists.
Glaxosmithkline
Diaryl substituted pyrrolidinones and pyrrolones as 5-HT2C inhibitors: synthesis and biological evaluation.
Glaxosmithkline
Biarylaniline phenethanolamines as potent and selective beta3 adrenergic receptor agonists.
Glaxosmithkline
2,5-diketopiperazines as potent, selective, and orally bioavailable oxytocin antagonists. 2. Synthesis, chirality, and pharmacokinetics.
Glaxosmithkline
Encoded library technology as a source of hits for the discovery and lead optimization of a potent and selective class of bactericidal direct inhibitors of Mycobacterium tuberculosis InhA.
Glaxosmithkline
Discovery of a rapidly metabolized, long-actingß(2) adrenergic receptor agonist with a short onset time incorporating a sulfone group suitable for once-daily dosing.
Glaxosmithkline
Novel spiroketal pyrrolidine GSK2336805 potently inhibits key hepatitis C virus genotype 1b mutants: from lead to clinical compound.
Glaxosmithkline
Discovery of selective small molecule type III phosphatidylinositol 4-kinase alpha (PI4KIIIa) inhibitors as anti hepatitis C (HCV) agents.
Glaxosmithkline
Discovery of novel indazole derivatives as dual angiotensin II antagonists and partial PPAR¿ agonists.
Glaxosmithkline
Discovery of Tertiary Amine and Indole Derivatives as Potent RORγt Inverse Agonists.
Glaxosmithkline
Discovery of Small Molecule RIP1 Kinase Inhibitors for the Treatment of Pathologies Associated with Necroptosis.
Glaxosmithkline
Discovery of novel N-(5-(arylcarbonyl)thiazol-2-yl)amides and N-(5-(arylcarbonyl)thiophen-2-yl)amides as potent ROR¿t inhibitors.
Glaxosmithkline
Identification of clinical candidates from the benzazepine class of histamine H3 receptor antagonists.
Glaxosmithkline
The discovery of the benzazepine class of histamine H3 receptor antagonists.
Glaxosmithkline
Identification, biological characterization and pharmacophoric analysis of a new potent and selective NK1 receptor antagonist clinical candidate.
Glaxosmithkline
Novel complex crystal structure of prolyl hydroxylase domain-containing protein 2 (PHD2): 2,8-Diazaspiro[4.5]decan-1-ones as potent, orally bioavailable PHD2 inhibitors.
Glaxosmithkline
Discovery of GSK2656157: An Optimized PERK Inhibitor Selected for Preclinical Development.
Glaxosmithkline
Identification of a Novel and Selective Series of Itk Inhibitors via a Template-Hopping Strategy.
Glaxosmithkline
Discovery of epigenetic regulator I-BET762: lead optimization to afford a clinical candidate inhibitor of the BET bromodomains.
Glaxosmithkline
The discovery of potent blockers of the canonical transient receptor channels, TRPC3 and TRPC6, based on an anilino-thiazole pharmacophore.
Glaxosmithkline
Discovery of 1-(1,3,5-triazin-2-yl)piperidine-4-carboxamides as inhibitors of soluble epoxide hydrolase.
Glaxosmithkline
Discovery of a highly potent, nonabsorbable apical sodium-dependent bile acid transporter inhibitor (GSK2330672) for treatment of type 2 diabetes.
Glaxosmithkline
Selective 3-phosphoinositide-dependent kinase 1 (PDK1) inhibitors: dissecting the function and pharmacology of PDK1.
Glaxosmithkline
Discovery of Dabrafenib: A Selective Inhibitor of Raf Kinases with Antitumor Activity against B-Raf-Driven Tumors.
Glaxosmithkline
Optimization of a Novel Series of TRPV4 Antagonists with In Vivo Activity in a Model of Pulmonary Edema.
Glaxosmithkline
The discovery of potent and selective 4-aminothienopyridines as B-Raf kinase inhibitors.
Glaxosmithkline
New fused benzazepine as selective D3 receptor antagonists. Synthesis and biological evaluation. Part 2: [g]-fused and hetero-fused systems.
Glaxosmithkline
Novel substituted tetrahydrotriazaacenaphthylene derivatives as potent CRF1 receptor antagonists.
Glaxosmithkline
1,3-diaminopropan-2-ol sulfonamides as potent and selective inhibitors of the glycine transporter type 1.
Glaxosmithkline
Non-steroidal glucocorticoid agonists: the discovery of aryl pyrazoles as A-ring mimetics.
Glaxosmithkline
Discovery of novel, non-acidic 1,5-biaryl pyrrole EP1 receptor antagonists.
Glaxosmithkline
13C bis-labeled pyrroles: a tool for the identification of the rat metabolism of 3-methyl pyrrole-2,4-dicarboxylic acid 2-propyl ester 4-(1,2,2-trimethyl-propyl) ester.
Glaxosmithkline
1,5-Biaryl pyrrole derivatives as EP1 receptor antagonists: Structure-activity relationships of 4- and 5-substituted benzoic acid derivatives.
Glaxosmithkline
Co-crystal structure guided array synthesis of PPARgamma inverse agonists.
Glaxosmithkline
1,5-Biaryl pyrrole derivatives as EP1 receptor antagonists. Structure-activity relationships of 6-substituted and 5,6-disubstituted benzoic acid derivatives.
Glaxosmithkline
The discovery and optimization of pyrimidinone-containing MCH R1 antagonists.
Glaxosmithkline
Array synthesis of progesterone receptor antagonists: 3-aryl-1,2-diazepines.
Glaxosmithkline
Synthesis and SAR of substituted tetrahydrocarbazole derivatives as new NPY-1 antagonists.
Glaxosmithkline
From pyrroles to pyrrolo[1,2-a]pyrazinones: a new class of mGluR1 antagonists.
Glaxosmithkline
Design and synthesis of new nonsteroidal glucocorticoid modulators through application of an"agreement docking" method.
Glaxosmithkline
Aminoalkoxybenzyl pyrrolidines as novel human urotensin-II receptor antagonists.
Glaxosmithkline
Synthesis and evaluation of potent and selective beta(3) adrenergic receptor agonists containing acylsulfonamide, sulfonylsulfonamide, and sulfonylurea carboxylic acid isosteres.
Glaxosmithkline
2-(Anilinomethyl)imidazolines as alpha1 adrenergic receptor agonists: alpha1a subtype selective 2'-heteroaryl compounds.
Glaxosmithkline
2-(anilinomethyl)imidazolines as alpha1A adrenergic receptor agonists: 2'-heteroaryl and 2'-oxime ether series.
Glaxosmithkline
alpha(1)-Adrenoceptor agonists: the identification of novel alpha(1A )subtype selective 2'-heteroaryl-2-(phenoxymethyl)imidazolines.
Glaxosmithkline
Alpha(1)-adrenoceptor activation: a comparison of 4-(anilinomethyl)imidazoles and 4-(phenoxymethyl)imidazoles to related 2-imidazolines.
Glaxosmithkline
2-(Anilinomethyl)imidazolines as alpha(1)-adrenoceptor agonists: the identification of alpha(1A) subtype selective 2'-carboxylic acid esters and amides.
Glaxosmithkline
Indole-propionic acid derivatives as potent, S1P3-sparing and EAE efficacious sphingosine-1-phosphate 1 (S1P1) receptor agonists.
Glaxosmithkline
Discovery of a novel series of nonacidic benzofuran EP1 receptor antagonists.
Glaxosmithkline
Identification of novel NK1/NK3 dual antagonists for the potential treatment of schizophrenia.
Glaxosmithkline
The discovery of long-acting saligeninß2 adrenergic receptor agonists incorporating a urea group.
Glaxosmithkline
Discovery of GSK143, a highly potent, selective and orally efficacious spleen tyrosine kinase inhibitor.
Glaxosmithkline
Discovery process and pharmacological characterization of a novel dual orexin 1 and orexin 2 receptor antagonist useful for treatment of sleep disorders.
Glaxosmithkline
The discovery of long-acting saligeninß2 adrenergic receptor agonists incorporating hydantoin or uracil rings.
Glaxosmithkline
Synthesis and structure-activity relationship of new 1,5-dialkyl-1,5-benzodiazepines as cholecystokinin-2 receptor antagonists.
Glaxosmithkline
p38alpha mitogen-activated protein kinase inhibitors: optimization of a series of biphenylamides to give a molecule suitable for clinical progression.
Glaxosmithkline
Novel 4,4-disubstituted piperidine-based C-C chemokine receptor-5 inhibitors with high potency against human immunodeficiency virus-1 and an improved human ether-a-go-go related gene (hERG) profile.
Glaxosmithkline
3,5-Disubstituted-indole-7-carboxamides: the discovery of a novel series of potent, selective inhibitors of IKK-ß.
Glaxosmithkline
Phenoxyacetic acids as PPARd partial agonists: synthesis, optimization, and in vivo efficacy.
Glaxosmithkline
Discovery of a potent series of non-steroidal nona-trifluoromethyl carbinol glucocorticoid receptor agonists with reduced lipophilicity.
Glaxosmithkline
The identification of a series of novel, soluble non-peptidic neuropeptide Y Y2 receptor antagonists.
Glaxosmithkline
5-{2-[4-(2-methyl-5-quinolinyl)-1-piperazinyl]ethyl}-2(1H)-quinolinones and 3,4-dihydro-2(1H)-quinolinones: dual-acting 5-HT1 receptor antagonists and serotonin reuptake inhibitors. Part 3.
Glaxosmithkline
Design, synthesis and SAR of a novel series of benzimidazoles as potent NPY Y5 antagonists.
Glaxosmithkline
Identification of 2-oxo-N-(phenylmethyl)-4-imidazolidinecarboxamide antagonists of the P2X(7) receptor.
Glaxosmithkline
Discovery and structure-activity relationship of a novel spirocarbamate series of NPY Y5 antagonists.
Glaxosmithkline
The discovery of a series of N-substituted 3-(4-piperidinyl)-1,3-benzoxazolinones and oxindoles as highly brain penetrant, selective muscarinic M1 agonists.
Glaxosmithkline
[3-azabicyclo[3.1.0]hex-1-yl]phenyl-benzenesulfonamides as selective dopamine D3 antagonists.
Glaxosmithkline
Novel imidazobenzazepine derivatives as dual H1/5-HT2A antagonists for the treatment of sleep disorders.
Glaxosmithkline
Pyrrolo[1,2-a]pyrazine and pyrazolo[1,5-a]pyrazine: novel, potent, and selective series of Vasopressin 1b receptor antagonists.
Glaxosmithkline
Discovery and structure-activity relationships of a series of pyroglutamic acid amide antagonists of the P2X7 receptor.
Glaxosmithkline
Identification of novel alpha7 nAChR positive allosteric modulators with the use of pharmacophore in silico screening methods.
Glaxosmithkline
Structure-activity relationships and in vivo activity of (1H-pyrazol-4-yl)acetamide antagonists of the P2X(7) receptor.
Glaxosmithkline
ADMET rules of thumb II: A comparison of the effects of common substituents on a range of ADMET parameters.
Glaxosmithkline
2' biaryl amides as novel and subtype selective M1 agonists. Part I: Identification, synthesis, and initial SAR.
Glaxosmithkline
2' biaryl amides as novel and subtype selective M1 agonists. Part II: Further optimization and profiling.
Glaxosmithkline
Structure guided design of 5-arylindazole glucocorticoid receptor agonists and antagonists.
Glaxosmithkline
Synthesis and structure-activity relationships of long-acting beta2 adrenergic receptor agonists incorporating metabolic inactivation: an antedrug approach.
Glaxosmithkline
Synthesis and structure-activity relationships of a series of (1H-pyrazol-4-yl)acetamide antagonists of the P2X7 receptor.
Glaxosmithkline
Discovery of tertiary sulfonamides as potent liver X receptor antagonists.
Glaxosmithkline
Identification and characterization of 4-chloro-N-(2-{[5-trifluoromethyl)-2-pyridyl]sulfonyl}ethyl)benzamide (GSK3787), a selective and irreversible peroxisome proliferator-activated receptor delta (PPARdelta) antagonist.
Glaxosmithkline
Synthesis and structure-activity relationships of a series of 3-aryl-4-isoxazolecarboxamides as a new class of TGR5 agonists.
Glaxosmithkline
Potent oxadiazole CGRP receptor antagonists for the potential treatment of migraine.
Glaxosmithkline
Synthesis and evaluation of 3-amino-6-aryl-pyridazines as selective CB(2) agonists for the treatment of inflammatory pain.
Glaxosmithkline
The identification of structurally novel, selective, orally bioavailable positive modulators of mGluR2.
Glaxosmithkline
Synthesis and pharmacological characterization of constrained analogues of Vestipitant as in vitro potent and orally active NK(1) receptor antagonists.
Glaxosmithkline
Addressing species specific metabolism and solubility issues in a quinoline series of oral PDE4 inhibitors.
Glaxosmithkline
2-Amino-5-aryl-pyridines as selective CB2 agonists: synthesis and investigation of structure-activity relationships.
Glaxosmithkline
2-Amino-9-aryl-3-cyano-4-methyl-7-oxo-6,7,8,9-tetrahydropyrido[2',3':4,5]thieno[2,3-b]pyridine derivatives as selective progesterone receptor agonists.
Glaxosmithkline
Quinolines as a novel structural class of potent and selective PDE4 inhibitors. Optimisation for inhaled administration.
Glaxosmithkline
Highly tractable, sub-nanomolar non-steroidal glucocorticoid receptor agonists.
Glaxosmithkline
Dopamine D(3) receptor antagonists: The quest for a potentially selective PET ligand. Part two: Lead optimization.
Glaxosmithkline
Discovery process and pharmacological characterization of 2-(S)-(4-fluoro-2-methylphenyl)piperazine-1-carboxylic acid [1-(R)-(3,5-bis-trifluoromethylphenyl)ethyl]methylamide (vestipitant) as a potent, selective, and orally active NK1 receptor antagonist.
Glaxosmithkline
Discovery and optimisation of a potent and selective tertiary sulfonamide oxytocin antagonist.
Glaxosmithkline
Studies on a series of potent, orally bioavailable, 5-HT(1) receptor ligands--part II.
Glaxosmithkline
8-[2-(4-Aryl-1-piperazinyl)ethyl]-2H-1,4-benzoxazin-3(4H)-ones: dual-acting 5-HT1 receptor antagonists and serotonin reuptake inhibitors--part II.
Glaxosmithkline
Synthesis and structure-activity relationships of long-acting beta2 adrenergic receptor agonists incorporating arylsulfonamide groups.
Glaxosmithkline
M3 muscarinic acetylcholine receptor antagonists: SAR and optimization of bi-aryl amines.
Glaxosmithkline
Quinolines as a novel structural class of potent and selective PDE4 inhibitors: optimisation for oral administration.
Glaxosmithkline
Dihydropyrrole[2,3-d]pyridine derivatives as novel corticotropin-releasing factor-1 antagonists: mapping of the receptor binding pocket by in silico docking studies.
Glaxosmithkline
Muscarinic acetylcholine receptor antagonists: SAR and optimization of tyrosine ureas.
Glaxosmithkline
6-[2-(4-Aryl-1-piperazinyl)ethyl]-2H-1,4-benzoxazin-3(4H)-ones: dual-acting 5-HT1 receptor antagonists and serotonin reuptake inhibitors.
Glaxosmithkline
N-alkyl-5H-pyrido[4,3-b]indol-1-amines and derivatives as novel urotensin-II receptor antagonists.
Glaxosmithkline
The discovery of a selective, small molecule agonist for the MAS-related gene X1 receptor.
Glaxosmithkline
Aryl sulphonyl amides as potent agonists of the growth hormone secretagogue (ghrelin) receptor.
Glaxosmithkline
Synthesis and pharmacological characterization of novel druglike corticotropin-releasing factor 1 antagonists.
Glaxosmithkline
Discovery of bioavailable 4,4-disubstituted piperidines as potent ligands of the chemokine receptor 5 and inhibitors of the human immunodeficiency virus-1.
Glaxosmithkline
Discovery of biphenyl piperazines as novel and long acting muscarinic acetylcholine receptor antagonists.
Glaxosmithkline
The first X-ray crystal structure of the glucocorticoid receptor bound to a non-steroidal agonist.
Glaxosmithkline
Novel 5-HT(1A/1B/1D) receptors antagonists with potent 5-HT reuptake inhibitory activity.
Glaxosmithkline
Pyrazolopyridines as a novel structural class of potent and selective PDE4 inhibitors.
Glaxosmithkline
Discovery of novel and long acting muscarinic acetylcholine receptor antagonists.
Glaxosmithkline
Discovery of brain penetrant, soluble, pyrazole amide EP1 receptor antagonists.
Glaxosmithkline
Discovery of potent, orally bioavailable, selective 5-HT1A/B/D receptor antagonists.
Glaxosmithkline
Phenylethynyl-pyrrolo[1,2-a]pyrazine: a new potent and selective tool in the mGluR5 antagonists arena.
Glaxosmithkline
Thiol-based angiotensin-converting enzyme 2 inhibitors: P1 modifications for the exploration of the S1 subsite.
Glaxosmithkline
New fused benzazepine as selective D3 receptor antagonists. Synthesis and biological evaluation. Part one: [h]-fused tricyclic systems.
Glaxosmithkline
Identification of novel glycine sulfonamide antagonists for the EP1 receptor.
Glaxosmithkline
Nonsteroidal glucocorticoid agonists: tetrahydronaphthalenes with alternative steroidal A-ring mimetics possessing dissociated (transrepression/transactivation) efficacy selectivity.
Glaxosmithkline
N-(3-Cyano-4,5,6,7-tetrahydro-1-benzothien-2-yl)amides as potent, selective, inhibitors of JNK2 and JNK3.
Glaxosmithkline
Dissociated nonsteroidal glucocorticoid receptor modulators; discovery of the agonist trigger in a tetrahydronaphthalene-benzoxazine series.
Glaxosmithkline
A series of bisaryl imidazolidin-2-ones has shown to be selective and orally active 5-HT2C receptor antagonists.
Glaxosmithkline
8-Piperazinyl-2,3-dihydropyrrolo[3,2-g]isoquinolines: potent, selective, orally bioavailable 5-HT1 receptor ligands.
Glaxosmithkline
Tyrosine urea muscarinic acetylcholine receptor antagonists: achiral quaternary ammonium groups.
Glaxosmithkline
GSK2578215A; a potent and highly selective 2-arylmethyloxy-5-substitutent-N-arylbenzamide LRRK2 kinase inhibitor.
Glaxosmithkline
Discovery of 6,7-dihydro-5H-pyrrolo[2,3-a]pyrimidines as orally available G protein-coupled receptor 119 agonists.
Glaxosmithkline
Identification of a novel series of BET family bromodomain inhibitors: binding mode and profile of I-BET151 (GSK1210151A).
Glaxosmithkline
Fragment-based discovery of bromodomain inhibitors part 2: optimization of phenylisoxazole sulfonamides.
Glaxosmithkline
Discovery of 7-methyl-5-(1-{[3-(trifluoromethyl)phenyl]acetyl}-2,3-dihydro-1H-indol-5-yl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine (GSK2606414), a potent and selective first-in-class inhibitor of protein kinase R (PKR)-like endoplasmic reticulum kinase (PERK).
Glaxosmithkline
Discovery of highly potent and selective small molecule ADAMTS-5 inhibitors that inhibit human cartilage degradation via encoded library technology (ELT).
Glaxosmithkline
4-Phenyl-7-azaindoles as potent, selective and bioavailable IKK2 inhibitors demonstrating good in vivo efficacy.
Glaxosmithkline
N'-substituted-2'-O,3'-N-carbonimidoyl bridged macrolides: novel anti-inflammatory macrolides without antimicrobial activity.
Glaxosmithkline
Discovery and characterization of small molecule inhibitors of the BET family bromodomains.
Glaxosmithkline
Synthesis and pharmacological investigation of azaphthalazinone human histamine H(1) receptor antagonists.
Glaxosmithkline
Discovery of novel 1,2,4-thiadiazole derivatives as potent, orally active agonists of sphingosine 1-phosphate receptor subtype 1 (S1P(1)).
Glaxosmithkline
Pyridyl-2,5-diketopiperazines as potent, selective, and orally bioavailable oxytocin antagonists: synthesis, pharmacokinetics, and in vivo potency.
Glaxosmithkline
Identification of benzoxazole analogs as novel, S1P(3) sparing S1P(1) agonists.
Glaxosmithkline
Acylprolinamides: a new class of peptide deformylase inhibitors with in vivo antibacterial activity.
Glaxosmithkline
The discovery of 2-fluoro-N-(3-fluoro-4-(5-((4-morpholinobutyl)amino)-1,3,4-oxadiazol-2-yl)phenyl)benzamide, a full agonist of the alpha-7 nicotinic acetylcholine receptor showing efficacy in the novel object recognition model of cognition enhancement.
Glaxosmithkline
Identification of a series of 1,3,4-oxadiazol-2-amines as potent alpha-7 agonists with efficacy in the novel object recognition model of cognition.
Glaxosmithkline
Design, synthesis and structure-activity relationship of N-substituted tropane muscarinic acetylcholine receptor antagonists.
Glaxosmithkline
Synthesis and structure-activity relationships of 1,2,4-triazolo[1,5-a]pyrimidin-7(3H)-ones as novel series of potentß isoform selective phosphatidylinositol 3-kinase inhibitors.
Glaxosmithkline
Lead optimisation of the N1 substituent of a novel series of indazole arylsulfonamides as CCR4 antagonists and identification of a candidate for clinical investigation.
Glaxosmithkline
From ApoA1 upregulation to BET family bromodomain inhibition: discovery of I-BET151.
Glaxosmithkline
Discovery of thiadiazole amides as potent, S1P3-sparing agonists of sphingosine-1-phosphate 1 (S1P1) receptor.
Glaxosmithkline
A novel series of benzimidazole NR2B-selective NMDA receptor antagonists.
Glaxosmithkline
Design, synthesis, and structure-activity relationship of tropane muscarinic acetylcholine receptor antagonists.
Glaxosmithkline
Discovery of N-[(2S)-5-(6-fluoro-3-pyridinyl)-2,3-dihydro-1H-inden-2-yl]-2-propanesulfonamide, a novel clinical AMPA receptor positive modulator.
Glaxosmithkline
BACE-1 hydroxyethylamine inhibitors using novel edge-to-face interaction with Arg-296.
Glaxosmithkline
6-(3,4-dichlorophenyl)-1-[(methyloxy)methyl]-3-azabicyclo[4.1.0]heptane: a new potent and selective triple reuptake inhibitor.
Glaxosmithkline
Benzofuran-substituted urea derivatives as novel P2Y(1) receptor antagonists.
Glaxosmithkline
The discovery and initial optimisation of pyrrole-2-carboxamides as inhibitors of p38alpha MAP kinase.
Glaxosmithkline
Discovery of GSK1070916, a potent and selective inhibitor of Aurora B/C kinase.
Glaxosmithkline
A concise synthesis of 1,4-dihydro-[1,4]diazepine-5,7-dione, a novel 7-TM receptor ligand core structure with melanocortin receptor agonist activity.
Glaxosmithkline
Antagonists of the calcium receptor. 2. Amino alcohol-based parathyroid hormone secretagogues.
Glaxosmithkline
Discovery of 3,5-disubstituted-1H-pyrrolo[2,3-b]pyridines as potent inhibitors of the insulin-like growth factor-1 receptor (IGF-1R) tyrosine kinase.
Glaxosmithkline
Optimization of a series of 4,6-bis-anilino-1H-pyrrolo[2,3-d]pyrimidine inhibitors of IGF-1R: elimination of an acid-mediated decomposition pathway.
Glaxosmithkline
Discovery and optimization of highly ligand-efficient oxytocin receptor antagonists using structure-based drug design.
Glaxosmithkline
Discovery of N-(3-fluorophenyl)-1-[(4-([(3S)-3-methyl-1-piperazinyl]methyl)phenyl)acetyl]-4-piperidinamine (GSK962040), the first small molecule motilin receptor agonist clinical candidate.
Glaxosmithkline
Development of potent and selective small-molecule human Urotensin-II antagonists.
Glaxosmithkline
Discovery of a novel indole series of EP1 receptor antagonists by scaffold hopping.
Glaxosmithkline
Structure and property based design of factor Xa inhibitors: biaryl pyrrolidin-2-ones incorporating basic heterocyclic motifs.
Glaxosmithkline
BACE-1 inhibitors part 1: identification of novel hydroxy ethylamines (HEAs).
Glaxosmithkline
Non-acidic pyrazole EP1 receptor antagonists with in vivo analgesic efficacy.
Glaxosmithkline
Rational design of 4-amino-5,6-diaryl-furo[2,3-d]pyrimidines as potent glycogen synthase kinase-3 inhibitors.
Glaxosmithkline
The discovery of GSK221149A: a potent and selective oxytocin antagonist.
Glaxosmithkline
Comparison of N,N'-diarylsquaramides and N,N'-diarylureas as antagonists of the CXCR2 chemokine receptor.
Glaxosmithkline
4-acyl-1-(4-aminoalkoxyphenyl)-2-ketopiperazines as a novel class of non-brain-penetrant histamine H3 receptor antagonists.
Glaxosmithkline
Homology modeling of human Fyn kinase structure: discovery of rosmarinic acid as a new Fyn kinase inhibitor and in silico study of its possible binding modes.
Glaxosmithkline
Optimization and SAR for dual ErbB-1/ErbB-2 tyrosine kinase inhibition in the 6-furanylquinazoline series.
Glaxosmithkline
Ultra-potent P1 modified arylsulfonamide HIV protease inhibitors: the discovery of GW0385.
Glaxosmithkline
Discovery of 4-{4-[3-(pyridin-2-yl)-1H-pyrazol-4-yl]pyridin-2-yl}-N-(tetrahydro-2H- pyran-4-yl)benzamide (GW788388): a potent, selective, and orally active transforming growth factor-beta type I receptor inhibitor.
Glaxosmithkline
The identification of potent and selective imidazole-based inhibitors of B-Raf kinase.
Glaxosmithkline
Discovery of potent and orally bioavailable N,N'-diarylurea antagonists for the CXCR2 chemokine receptor.
Glaxosmithkline
Novel benzophenones as non-nucleoside reverse transcriptase inhibitors of HIV-1.
Glaxosmithkline
3-(alphaR)-alpha-((2S,5R)-4-allyl-2,5-dimethyl-1-piperazinyl)-3-hydroxybenzyl)-N-alkyl-N-arylbenzamides: potent, non-peptidic agonists of both the micro and delta opioid receptors.
Glaxosmithkline
The discovery of tadalafil: a novel and highly selective PDE5 inhibitor. 1: 5,6,11,11a-tetrahydro-1H-imidazo[1',5':1,6]pyrido[3,4-b]indole-1,3(2H)-dione analogues.
Glaxosmithkline
Discovery and in vitro evaluation of potent TrkA kinase inhibitors: oxindole and aza-oxindoles.
Glaxosmithkline
Synthesis and structure-activity relationships of imidazo[1,2-a]pyrimidin-5(1H)-ones as a novel series of beta isoform selective phosphatidylinositol 3-kinase inhibitors.
Glaxosmithkline
5-Aryl-4-carboxamide-1,3-oxazoles: potent and selective GSK-3 inhibitors.
Glaxosmithkline
Structure-guided lead optimization of triazolopyrimidine-ring substituents identifies potent Plasmodium falciparum dihydroorotate dehydrogenase inhibitors with clinical candidate potential.
Glaxosmithkline
Novel Rho kinase inhibitors with anti-inflammatory and vasodilatory activities.
Glaxosmithkline
Inhibition of colony-stimulating-factor-1 signaling in vivo with the orally bioavailable cFMS kinase inhibitor GW2580.
Glaxosmithkline
Fragment-based discovery of bromodomain inhibitors part 1: inhibitor binding modes and implications for lead discovery.
Glaxosmithkline
Novel amino-piperidines as potent antibacterials targeting bacterial type IIA topoisomerases.
Glaxosmithkline
Novel cyclohexyl-amides as potent antibacterials targeting bacterial type IIA topoisomerases.
Glaxosmithkline
CCR2 receptor antagonists: optimization of biaryl sulfonamides to increase activity in whole blood.
Glaxosmithkline
Conformationally constrained farnesoid X receptor (FXR) agonists: alternative replacements of the stilbene.
Glaxosmithkline
Discovery of a brain-penetrant S1P3-sparing direct agonist of the S1P¿? and S1P5 receptors efficacious at low oral dose.
Glaxosmithkline
Discovery of GSK1997132B a novel centrally penetrant benzimidazole PPAR¿ partial agonist.
Glaxosmithkline
1-Heteroaryl-6-(3,4-dichlorophenyl)-3-azabicyclo[4.1.0]heptane: further insights into a class of triple re-uptake inhibitors.
Glaxosmithkline
Development of potent B-RafV600E inhibitors containing an arylsulfonamide headgroup.
Glaxosmithkline
Azepanone-based inhibitors of human cathepsin S: optimization of selectivity via the P2 substituent.
Glaxosmithkline
Synthesis and biological activity of a series of tetrasubstituted-imidazoles as P2X(7) antagonists.
Glaxosmithkline
Pyrazolopyridazine alpha-2-delta-1 ligands for the treatment of neuropathic pain.
Glaxosmithkline
Heteroalicyclic carboxamidines as inhibitors of inducible nitric oxide synthase; the identification of (2R)-2-pyrrolidinecarboxamidine as a potent and selective haem-co-ordinating inhibitor.
Glaxosmithkline
The discovery of phthalazinone-based human H1 and H3 single-ligand antagonists suitable for intranasal administration for the treatment of allergic rhinitis.
Glaxosmithkline
Structure-based design of potent and selective 3-phosphoinositide-dependent kinase-1 (PDK1) inhibitors.
Glaxosmithkline
The discovery of potent and long-acting oral factor Xa inhibitors with tetrahydroisoquinoline and benzazepine P4 motifs.
Glaxosmithkline
Structure and property based design of factor Xa inhibitors: pyrrolidin-2-ones with aminoindane and phenylpyrrolidine P4 motifs.
Glaxosmithkline
Conformationally constrained farnesoid X receptor (FXR) agonists: heteroaryl replacements of the naphthalene.
Glaxosmithkline
Discovery and biological characterization of (2R,4S)-1'-acetyl-N-{(1R)-1-[3,5-bis(trifluoromethyl)phenyl]ethyl}-2-(4-fluoro-2-methylphenyl)-N-methyl-4,4'-bipiperidine-1-carboxamide as a new potent and selective neurokinin 1 (NK1) receptor antagonist clinical candidate.
Glaxosmithkline
Stereospecific synthesis and structure-activity relationships of unsymmetrical 4,4-diphenylbut-3-enyl derivatives of nipecotic acid as GAT-1 inhibitors.
Glaxosmithkline
Synthesis and pharmacological characterization of 5-phenyl-2-[2-(1-piperidinylcarbonyl)phenyl]-2,3-dihydro-1H-pyrrolo[1,2-c]imidazol-1-ones: a new class of Neuropeptide S antagonists.
Glaxosmithkline
Discovery of N-benzyl-N'-(4-pipyridinyl)urea CCR5 antagonists as anti-HIV-1 agents (II): modification of the acyl portion.
Glaxosmithkline
Discovery of N-benzyl-N'-(4-pipyridinyl)urea CCR5 antagonists as anti-HIV-1 agents (I): optimization of the amine portion.
Glaxosmithkline
Substituted N-{3-[(1,1-dioxido-1,2-benzothiazol-3-yl)(phenyl)amino]propyl}benzamide analogs as potent Kv1.3 ion channel blockers. Part 2.
Glaxosmithkline
N-{3-[(1,1-dioxido-1,2-benzothiazol-3-yl)(phenyl)amino]propyl}benzamide analogs as potent Kv1.3 inhibitors. Part 1.
Glaxosmithkline
N-substituted pyrrolidines and tetrahydrofurans as novel AMPAR positive modulators.
Glaxosmithkline
Novel spirotetracyclic zwitterionic dual H(1)/5-HT(2A) receptor antagonists for the treatment of sleep disorders.
Glaxosmithkline
2-Methyl-3-furanyl-4H-1,2,4-triazol-3-ylthioamides: a new class of selective orexin 2 antagonists.
Glaxosmithkline
3-Urea-1-(phenylmethyl)-pyridones as novel, potent, and selective EP3 receptor antagonists.
Glaxosmithkline
Exploration of the amine terminus in a novel series of 1,2,4-triazolo-3-yl-azabicyclo[3.1.0]hexanes as selective dopamine D3 receptor antagonists.
Glaxosmithkline
Design and synthesis of novel tricyclic benzoxazines as potent 5-HT(1A/B/D) receptor antagonists leading to the discovery of 6-{2-[4-(2-methyl-5-quinolinyl)-1-piperazinyl]ethyl}-4H-imidazo[5,1-c][1,4]benzoxazine-3-carboxamide (GSK588045).
Glaxosmithkline
Blockade of X4-tropic HIV-1 cellular entry by GSK812397, a potent noncompetitive CXCR4 receptor antagonist.
Glaxosmithkline
Synthesis and structure-activity relationship of N-(3-azabicyclo[3.1.0]hex-6-ylmethyl)-5-(2-pyridinyl)-1,3-thiazol-2-amines derivatives as NPY Y5 antagonists.
Glaxosmithkline
Heteroaryl-linked 5-(1H-benzimidazol-1-yl)-2-thiophenecarboxamides: potent inhibitors of polo-like kinase 1 (PLK1) with improved drug-like properties.
Glaxosmithkline
A specific and direct comparison of the trifluoromethyl and pentafluoro sulfanyl groups on the selective dopamine D(3) antagonist 3-(3-{[4-methyl-5-(4-methyl-1,3-oxazol-5-yl)-4H-1,2,4-triazol-3-yl]thio}propyl)-1-phenyl-3-azabicyclo[3.1.0]hexane template.
Glaxosmithkline
Synthesis and SAR of novel isoquinoline CXCR4 antagonists with potent anti-HIV activity.
Glaxosmithkline
Discovery of a new series of Aurora inhibitors through truncation of GSK1070916.
Glaxosmithkline
Novel N-substituted benzimidazole CXCR4 antagonists as potential anti-HIV agents.
Glaxosmithkline
The identification of a selective dopamine D2 partial agonist, D3 antagonist displaying high levels of brain exposure.
Glaxosmithkline
1,2,4-Triazolyl azabicyclo[3.1.0]hexanes: a new series of potent and selective dopamine D(3) receptor antagonists.
Glaxosmithkline
Evaluation of basic, heterocyclic ring systems as templates for use as potassium competitive acid blockers (pCABs).
Glaxosmithkline
The discovery and optimisation of benzazepine sulfonamide and sulfones as potent agonists of the motilin receptor.
Glaxosmithkline
1-(Aryl)-6-[alkoxyalkyl]-3-azabicyclo[3.1.0]hexanes and 6-(aryl)-6-[alkoxyalkyl]-3-azabicyclo[3.1.0]hexanes: a new series of potent and selective triple reuptake inhibitors.
Glaxosmithkline
Synthesis and biological activities of novel indole derivatives as potent and selective PPARgamma modulators.
Glaxosmithkline
Tetrasubstituted pyridines as potent and selective AKT inhibitors: Reduced CYP450 and hERG inhibition of aminopyridines.
Glaxosmithkline
Structure and property based design of factor Xa inhibitors: pyrrolidin-2-ones with monoaryl P4 motifs.
Glaxosmithkline
2,3,5-Trisubstituted pyridines as selective AKT inhibitors-Part I: Substitution at 2-position of the core pyridine for ROCK1 selectivity.
Glaxosmithkline
2,3,5-Trisubstituted pyridines as selective AKT inhibitors. Part II: Improved drug-like properties and kinase selectivity from azaindazoles.
Glaxosmithkline
Improving the developability profile of pyrrolidine progesterone receptor partial agonists.
Glaxosmithkline
Discovery of 1-[4-(3-chlorophenylamino)-1-methyl-1H-pyrrolo[3,2-c]pyridin-7-yl]-1-morpholin-4-ylmethanone (GSK554418A), a brain penetrant 5-azaindole CB2 agonist for the treatment of chronic pain.
Glaxosmithkline
The discovery of tertiary-amine LXR agonists with potent cholesterol efflux activity in macrophages.
Glaxosmithkline
Discovery of orally active, pyrrolidinone-based progesterone receptor partial agonists.
Glaxosmithkline
Rational design of orally-active, pyrrolidine-based progesterone receptor partial agonists.
Glaxosmithkline
FXR agonist activity of conformationally constrained analogs of GW 4064.
Glaxosmithkline
Identification and optimisation of a novel series of pyrimidine based cyclooxygenase-2 (COX-2) inhibitors. Utilisation of a biotransformation approach.
Glaxosmithkline
Identification of [4-[4-(methylsulfonyl)phenyl]-6-(trifluoromethyl)-2-pyrimidinyl] amines and ethers as potent and selective cyclooxygenase-2 inhibitors.
Glaxosmithkline
Discovery of (3-endo)-3-(2-cyano-2,2-diphenylethyl)-8,8-dimethyl-8-azoniabicyclo[3.2.1]octane bromide as an efficacious inhaled muscarinic acetylcholine receptor antagonist for the treatment of COPD.
Glaxosmithkline
Discovery of novel aminothiadiazole amides as selective EP(3) receptor antagonists.
Glaxosmithkline
Design and synthesis of orally bioavailable serum and glucocorticoid-regulated kinase 1 (SGK1) inhibitors.
Glaxosmithkline
The identification and optimisation of novel and selective diamide neuropeptide Y Y2 receptor antagonists.
Glaxosmithkline
Tetrahydrocarbazole amides with potent activity against human papillomaviruses.
Glaxosmithkline
Synthesis and SAR of amino acid-derived heterocyclic progesterone receptor full and partial agonists.
Glaxosmithkline
Design of novel quinazoline derivatives and related analogues as potent and selective ALK5 inhibitors.
Glaxosmithkline
Dual EGFR/ErbB-2 inhibitors from novel pyrrolidinyl-acetylenic thieno[3,2-d]pyrimidines.
Glaxosmithkline
Synthesis and evaluation of pyrazolo[1,5-b]pyridazines as selective cyclin dependent kinase inhibitors.
Glaxosmithkline
Antagonists of the calcium receptor I. Amino alcohol-based parathyroid hormone secretagogues.
Glaxosmithkline
Orally active C-6 heteroaryl- and heterocyclyl-substituted imidazo[1,2-a]pyridine acid pump antagonists (APAs).
Glaxosmithkline
Substituted isoxazole analogs of farnesoid X receptor (FXR) agonist GW4064.
Glaxosmithkline
Discovery of sodium 6-[(5-chloro-2-{[(4-chloro-2-fluorophenyl)methyl]oxy}phenyl)methyl]-2-pyridinecarboxylate (GSK269984A) an EP(1) receptor antagonist for the treatment of inflammatory pain.
Glaxosmithkline
Discovery of novel 1-azoniabicyclo[2.2.2]octane muscarinic acetylcholine receptor antagonists.
Glaxosmithkline
Discovery of 5-pyrrolopyridinyl-2-thiophenecarboxamides as potent AKT kinase inhibitors.
Glaxosmithkline
[2-(4-Phenyl-4-piperidinyl)ethyl]amine based CCR5 antagonists: derivatizations at the N-terminal of the piperidine ring.
Glaxosmithkline
Discovery and optimization of imidazo[1,2-a]pyridine inhibitors of insulin-like growth factor-1 receptor (IGF-1R).
Glaxosmithkline
Anthranilimide-based glycogen phosphorylase inhibitors for the treatment of Type 2 diabetes: 2. Optimization of serine and threonine ether amino acid residues.
Glaxosmithkline
Anthranilimide-based glycogen phosphorylase inhibitors for the treatment of type 2 diabetes: 1. Identification of 1-amino-1-cycloalkyl carboxylic acid headgroups.
Glaxosmithkline
Discovery of potent, selective sulfonylfuran urea endothelial lipase inhibitors.
Glaxosmithkline
Discovery of GSK345931A: An EP(1) receptor antagonist with efficacy in preclinical models of inflammatory pain.
Glaxosmithkline
Assessment of chemical coverage of kinome space and its implications for kinase drug discovery.
Glaxosmithkline
Camphor sulfonamide derivatives as novel, potent and selective CXCR3 antagonists.
Glaxosmithkline
The discovery of biaryl carboxamides as novel small molecule agonists of the motilin receptor.
Glaxosmithkline
Imidazo[5,1-f][1,2,4]triazin-2-amines as novel inhibitors of polo-like kinase 1.
Glaxosmithkline
Tetrahydro-4-quinolinamines identified as novel P2Y(1) receptor antagonists.
Glaxosmithkline
The 'Ethereal' nature of TLR4 agonism and antagonism in the AGP class of lipid A mimetics.
Glaxosmithkline
The identification of pyrazolo[1,5-a]pyridines as potent p38 kinase inhibitors.
Glaxosmithkline
Discovery of small molecule agonists for the bombesin receptor subtype 3 (BRS-3) based on an omeprazole lead.
Glaxosmithkline
Design and synthesis of 6-phenylnicotinamide derivatives as antagonists of TRPV1.
Glaxosmithkline
Structure-guided design of N-phenyl tertiary amines as transrepression-selective liver X receptor modulators with anti-inflammatory activity.
Glaxosmithkline
Tricyclic azepine derivatives as selective brain penetrant 5-HT6 receptor antagonists.
Glaxosmithkline
Biphenyl amide p38 kinase inhibitors 3: Improvement of cellular and in vivo activity.
Glaxosmithkline
Biphenyl amide p38 kinase inhibitors 4: DFG-in and DFG-out binding modes.
Glaxosmithkline
Urotensin-II receptor antagonists: synthesis and SAR of N-cyclic azaalkyl benzamides.
Glaxosmithkline
Amino acid anthranilamide derivatives as a new class of glycogen phosphorylase inhibitors.
Glaxosmithkline
Potent and selective small-molecule human urotensin-II antagonists with improved pharmacokinetic profiles.
Glaxosmithkline
Isolation, structure elucidation, and biological evaluation of 15-amido-3-demethoxy-2alpha,3alpha-methylenedioxyerythroculine, a new alkaloid from Hyperbaena valida.
Glaxosmithkline
Thiol-based angiotensin-converting enzyme 2 inhibitors: P1' modifications for the exploration of the S1' subsite.
Glaxosmithkline
BACE-1 inhibitors part 2: identification of hydroxy ethylamines (HEAs) with reduced peptidic character.
Glaxosmithkline
Design, synthesis and evaluation of trifluoromethane sulfonamide derivatives as new potent and selective peroxisome proliferator-activated receptor alpha agonists.
Glaxosmithkline
Structure and property based design of factor Xa inhibitors: pyrrolidin-2-ones with biaryl P4 motifs.
Glaxosmithkline
Discovery of novel 8-azoniabicyclo[3.2.1]octane carbamates as muscarinic acetylcholine receptor antagonists.
Glaxosmithkline
1,2,4-triazol-3-yl-thiopropyl-tetrahydrobenzazepines: a series of potent and selective dopamine D(3) receptor antagonists.
Glaxosmithkline
Optimization of triarylimidazoles for Tie2: influence of conformation on potency.
Glaxosmithkline
Studies on a series of potent, orally bioavailable, 5-HT(1) receptor ligands.
Glaxosmithkline
Identification and optimization of novel 1,3,4-oxadiazole EP1 receptor antagonists.
Glaxosmithkline
3-Arylamino-2H-1,2,4-benzothiadiazin-5-ol 1,1-dioxides as novel and selective CXCR2 antagonists.
Glaxosmithkline
The potential of transient receptor potential vanilloid type 1 channel modulators for the treatment of pain.
Glaxosmithkline
Discovery of 2-[(2,4-dichlorophenyl)amino]-N-[(tetrahydro- 2H-pyran-4-yl)methyl]-4-(trifluoromethyl)- 5-pyrimidinecarboxamide, a selective CB2 receptor agonist for the treatment of inflammatory pain.
Glaxosmithkline
Selective and dual action orally active inhibitors of thrombin and factor Xa.
Glaxosmithkline
Sulfonamide-related conformational effects and their importance in structure-based design.
Glaxosmithkline
From pyrroles to 1-oxo-2,3,4,9-tetrahydro-1H-beta-carbolines: a new class of orally bioavailable mGluR1 antagonists.
Glaxosmithkline
The exploration of aza-quinolines as hematopoietic prostaglandin D synthase (H-PGDS) inhibitors with low brain exposure.
Glaxosmithkline
6-(4-chlorophenyl)-3-substituted-thieno[3,2-d]pyrimidin-4(3H)-one-based melanin-concentrating hormone receptor 1 antagonist.
Glaxosmithkline
Potent, selective, and orally efficacious antagonists of melanin-concentrating hormone receptor 1.
Glaxosmithkline
Design and effective synthesis of novel templates, 3,7-diphenyl-4-amino-thieno and furo-[3,2-c]pyridines as protein kinase inhibitors and in vitro evaluation targeting angiogenetic kinases.
Glaxosmithkline
Synthesis and structure-activity relationships of 3-phenyl-2-propenamides as inhibitors of glycogen phosphorylase a.
Glaxosmithkline
N,N'-Diarylcyanoguanidines as antagonists of the CXCR2 and CXCR1 chemokine receptors.
Glaxosmithkline
Discovery of Proline-Based p300/CBP Inhibitors Using DNA-Encoded Library Technology in Combination with High-Throughput Screening.
Glaxosmithkline
N-Tetrahydroquinolinyl, N-quinolinyl and N-isoquinolinyl biaryl carboxamides as antagonists of TRPV1.
Glaxosmithkline
Structure-activity relationships of 1,5-biaryl pyrroles as EP1 receptor antagonists.
Glaxosmithkline
An efficient, asymmetric solid-phase synthesis of benzothiadiazine-substituted tetramic acids: potent inhibitors of the hepatitis C virus RNA-dependent RNA polymerase.
Glaxosmithkline
3-(1,1-dioxo-2H-(1,2,4)-benzothiadiazin-3-yl)-4-hydroxy-2(1H)-quinolinones, potent inhibitors of hepatitis C virus RNA-dependent RNA polymerase.
Glaxosmithkline
Novel, potent P2-P3 pyrrolidine derivatives of ketoamide-based cathepsin K inhibitors.
Glaxosmithkline
Semicarbazone-based inhibitors of cathepsin K, are they prodrugs for aldehyde inhibitors?
Glaxosmithkline
2-Cyano-4-fluoro-1-thiovalylpyrrolidine analogues as potent inhibitors of DPP-IV.
Glaxosmithkline
Ketoheterocycle-based inhibitors of cathepsin K: a novel entry into the synthesis of peptidic ketoheterocycles.
Glaxosmithkline
Discovery and in vitro evaluation of potent kinase inhibitors: Pyrido[1',2':1,5]pyrazolo[3,4-d]pyrimidines.
Glaxosmithkline
P2-P3 conformationally constrained ketoamide-based inhibitors of cathepsin K.
Glaxosmithkline
(1H-imidazo[4,5-c]pyridin-2-yl)-1,2,5-oxadiazol-3-ylamine derivatives: further optimisation as highly potent and selective MSK-1-inhibitors.
Glaxosmithkline
(1H-imidazo[4,5-c]pyridin-2-yl)-1,2,5-oxadiazol-3-ylamine derivatives: a novel class of potent MSK-1-inhibitors.
Glaxosmithkline
A structural screening approach to ketoamide-based inhibitors of cathepsin K.
Glaxosmithkline
Dimeric zanamivir conjugates with various linking groups are potent, long-lasting inhibitors of influenza neuraminidase including H5N1 avian influenza.
Glaxosmithkline
Identification of small molecule inhibitors of the hepatitis C virus RNA-dependent RNA polymerase from a pyrrolidine combinatorial mixture.
Glaxosmithkline
Ketoamide-based inhibitors of cysteine protease, cathepsin K: P3 modifications.
Glaxosmithkline
Potent and selective ketoamide-based inhibitors of cysteine protease, cathepsin K.
Glaxosmithkline
Identification of 2,3-diaryl-pyrazolo[1,5-b]pyridazines as potent and selective cyclooxygenase-2 inhibitors.
Glaxosmithkline
Potent and selective P2-P3 ketoamide inhibitors of cathepsin K with good pharmacokinetic properties via favorable P1', P1, and/or P3 substitutions.
Glaxosmithkline
Identification of 1,5-naphthyridine derivatives as a novel series of potent and selective TGF-beta type I receptor inhibitors.
Glaxosmithkline
Peroxisome proliferator-activated receptor alpha/gamma dual agonists for the treatment of type 2 diabetes.
Glaxosmithkline
Definition of the heterocyclic pharmacophore of bacterial methionyl tRNA synthetase inhibitors: potent antibacterially active non-quinolone analogues.
Glaxosmithkline
Progesterone receptor ligand binding pocket flexibility: crystal structures of the norethindrone and mometasone furoate complexes.
Glaxosmithkline
Discovery of a Novel Bromodomain and Extra Terminal Domain (BET) Protein Inhibitor, I-BET282E, Suitable for Clinical Progression.
Glaxosmithkline
Orally bioavailable small molecule ketoamide-based inhibitors of cathepsin K.
Glaxosmithkline
Identification of Diarylurea Inhibitors of the Cardiac-Specific Kinase TNNI3K by Designing Selectivity Against VEGFR2, p38α, and B-Raf.
Glaxosmithkline
Overcoming the Pregnane X Receptor Liability: Rational Design to Eliminate PXR-Mediated CYP Induction.
Glaxosmithkline
Optimization of a Series of 2,3-Dihydrobenzofurans as Highly Potent, Second Bromodomain (BD2)-Selective, Bromo and Extra-Terminal Domain (BET) Inhibitors.
Glaxosmithkline
Fragment-based Scaffold Hopping: Identification of Potent, Selective, and Highly Soluble Bromo and Extra Terminal Domain (BET) Second Bromodomain (BD2) Inhibitors.
Glaxosmithkline
A knowledge-based, structural-aided discovery of a novel class of 2-phenylimidazo[1,2-a]pyridine-6-carboxamide H-PGDS inhibitors.
Glaxosmithkline
Template-Hopping Approach Leads to Potent, Selective, and Highly Soluble Bromo and Extraterminal Domain (BET) Second Bromodomain (BD2) Inhibitors.
Glaxosmithkline
Evaluation of potent and selective small-molecule antagonists for the CXCR2 chemokine receptor.
Glaxosmithkline
3-trifluoromethyl-4-nitro-5-arylpyrazoles are novel K(ATP) channel agonists.
Glaxosmithkline
DNA-Encoded Library Hit Confirmation: Bridging the Gap Between On-DNA and Off-DNA Chemistry.
Glaxosmithkline
The Discovery of Conformationally Constrained Bicyclic Peptidomimetics as Potent Hepatitis C NS5A Inhibitors.
Glaxosmithkline
Identification, Synthesis, and Characterization of a Major Circulating Human Metabolite of TRPV4 Antagonist GSK2798745.
Glaxosmithkline
Design of potent, selective, and orally bioavailable inhibitors of cysteine protease cathepsin k.
Glaxosmithkline
Discovery of a Highly Selective BET BD2 Inhibitor from a DNA-Encoded Library Technology Screening Hit.
Glaxosmithkline
The discovery of tadalafil: a novel and highly selective PDE5 inhibitor. 2: 2,3,6,7,12,12a-hexahydropyrazino[1',2':1,6]pyrido[3,4-b]indole-1,4-dione analogues.
Glaxosmithkline
Design and synthesis of pyrrolidine-5,5'-trans-lactams (5-oxo-hexahydropyrrolo[3,2-b]pyrroles) as novel mechanism-based inhibitors of human cytomegalovirus protease. 4. Antiviral activity and plasma stability.
Glaxosmithkline
CCR2: characterization of the antagonist binding site from a combined receptor modeling/mutagenesis approach.
Glaxosmithkline
Drug rings database with web interface. A tool for identifying alternative chemical rings in lead discovery programs.
Glaxosmithkline
2,4-Dicarboxy-pyrroles as selective non-competitive mGluR1 antagonists: further characterization of 3,5-dimethyl pyrrole-2,4-dicarboxylic acid 2-propyl ester 4-(1,2,2-trimethyl-propyl) ester and structure-activity relationships.
Glaxosmithkline
Novel selective small molecule agonists for peroxisome proliferator-activated receptor delta (PPARdelta)--synthesis and biological activity.
Glaxosmithkline
Phenylbutyrates as potent, orally bioavailable vitronectin receptor (integrin alphavbeta3) antagonists.
Glaxosmithkline
N-Phenyl-N-purin-6-yl ureas: the design and synthesis of p38alpha MAP kinase inhibitors.
Glaxosmithkline
The identification of clinical candidate SB-480848: a potent inhibitor of lipoprotein-associated phospholipase A2.
Glaxosmithkline
Identification of a novel series of selective 5-HT7 receptor antagonists.
Glaxosmithkline
Optimisation of aryl substitution leading to potent methionyl tRNA synthetase inhibitors with excellent gram-positive antibacterial activity.
Glaxosmithkline
Indanylidenes. 1. Design and synthesis of (E)-2-(4,6-difluoro-1-indanylidene)acetamide, a potent, centrally acting muscle relaxant with antiinflammatory and analgesic activity.
Glaxosmithkline
GSK789: A Selective Inhibitor of the First Bromodomains (BD1) of the Bromo and Extra Terminal Domain (BET) Proteins.
Glaxosmithkline
A new series of estrogen receptor modulators that display selectivity for estrogen receptor beta.
Glaxosmithkline
Design and synthesis of ethyl pyrrolidine-5,5-trans-lactams as inhibitors of hepatitis C virus NS3/4A protease.
Glaxosmithkline
Relating the structure, activity, and physical properties of ultrashort-acting benzodiazepine receptor agonists.
Glaxosmithkline
Discovery of Orally Bioavailable Ligand Efficient Quinazolindiones as Potent and Selective Tankyrases Inhibitors.
Glaxosmithkline
Synthesis and evaluation of 7-substituted-3-cyclobutylamino-4H-1,2,4-benzothiadiazine-1,1-dioxide derivatives as K(ATP) channel agonists.
Glaxosmithkline
The discovery of SB-435495. A potent, orally active inhibitor of lipoprotein-associated phospholipase A(2) for evaluation in man.
Glaxosmithkline
Design and Optimization of an Acyclic Amine Series of TRPV4 Antagonists by Electronic Modulation of Hydrogen Bond Interactions.
Glaxosmithkline
Pyrrolidine-5,5-trans-lactams as novel mechanism-based inhibitors of human cytomegalovirus protease. Part 3: potency and plasma stability.
Glaxosmithkline
Identification of potent and selective oxytocin antagonists. Part 2: further investigation of benzofuran derivatives.
Glaxosmithkline
Identification of novel inhibitors of the transforming growth factor beta1 (TGF-beta1) type 1 receptor (ALK5).
Glaxosmithkline
Design and synthesis of pyrrolidine-5,5-trans-lactams (5-oxohexahydropyrrolo[3,2-b]pyrroles) as novel mechanism-based inhibitors of human cytomegalovirus protease. 2. Potency and chirality.
Glaxosmithkline
Potent, orally active inhibitors of lipoprotein-associated phospholipase A(2): 1-(biphenylmethylamidoalkyl)-pyrimidones.
Glaxosmithkline
Synthesis and biological activity of L-tyrosine-based PPARgamma agonists with reduced molecular weight.
Glaxosmithkline
Design of selective and soluble inhibitors of tumor necrosis factor-alpha converting enzyme (TACE).
Glaxosmithkline
Identification of a series of PPAR gamma/delta dual agonists via solid-phase parallel synthesis.
Glaxosmithkline
Hydrazinonaphthalene and azonaphthalene thrombopoietin mimics are nonpeptidyl promoters of megakaryocytopoiesis.
Glaxosmithkline
Pyrimidinylimidazole inhibitors of p38: cyclic N-1 imidazole substituents enhance p38 kinase inhibition and oral activity.
Glaxosmithkline
Structure-based optimisation of orally active & reversible MetAP-2 inhibitors maintaining a tight 'molecular budget'.
Glaxosmithkline
Inhibitors of bacterial tyrosyl tRNA synthetase: synthesis of carbocyclic analogues of the natural product SB-219383.
Glaxosmithkline
Identification of a series of oxadiazole-substituted alpha-isopropoxy phenylpropanoic acids with activity on PPARalpha, PPARgamma, and PPARdelta.
Glaxosmithkline
Conformationally restricted indolopiperidine derivatives as potent CCR2B receptor antagonists.
Glaxosmithkline
N-hydroxyformamide peptidomimetics as TACE/matrix metalloprotease inhibitors: oral activity via P1' isobutyl substitution.
Glaxosmithkline
Selective CDK6 degradation mediated by cereblon, VHL, and novel IAP-recruiting PROTACs.
Glaxosmithkline
1-(Arylpiperazinylamidoalkyl)-pyrimidones: orally active inhibitors of lipoprotein-associated phospholipase A(2).
Glaxosmithkline
The Optimization of a Novel, Weak Bromo and Extra Terminal Domain (BET) Bromodomain Fragment Ligand to a Potent and Selective Second Bromodomain (BD2) Inhibitor.
Glaxosmithkline
Identification of a potent and selective oxytocin antagonist, from screening a fully encoded differential release combinatorial chemical library.
Glaxosmithkline
Identification of a subtype selective human PPARalpha agonist through parallel-array synthesis.
Glaxosmithkline
Phenoxypyrimidine inhibitors of p38alpha kinase: synthesis and statistical evaluation of the p38 inhibitory potencies of a series of 1-(piperidin-4-yl)-4-(4-fluorophenyl)-5-(2-phenoxypyrimidin-4-yl) imidazoles.
Glaxosmithkline
Potent synthetic inhibitors of tyrosyl tRNA synthetase derived from C-pyranosyl analogues of SB-219383.
Glaxosmithkline
Synthetic analogues of SB-219383. Novel C-glycosyl peptides as inhibitors of tyrosyl tRNA synthetase.
Glaxosmithkline
The identification of a potent, water soluble inhibitor of lipoprotein-associated phospholipase A2.
Glaxosmithkline
Discovery of piperazic acid peptide deformylase inhibitors with in vivo activity for respiratory tract and skin infections.
Glaxosmithkline
Discovery and Characterization of a Class of Pyrazole Inhibitors of Bacterial Undecaprenyl Pyrophosphate Synthase.
Glaxosmithkline
Development of Chemical Entities Endowed with Potent Fast-Killing Properties against
Glaxosmithkline
The discovery of quinoline-3-carboxamides as hematopoietic prostaglandin D synthase (H-PGDS) inhibitors.
Glaxosmithkline
Design and development of a series of borocycles as selective, covalent kallikrein 5 inhibitors.
Glaxosmithkline
Design of N-Benzoxaborole Benzofuran GSK8175-Optimization of Human Pharmacokinetics Inspired by Metabolites of a Failed Clinical HCV Inhibitor.
Glaxosmithkline
Discovery of a First-in-Class Receptor Interacting Protein 2 (RIP2) Kinase Specific Clinical Candidate, 2-((4-(Benzo[
Glaxosmithkline
GSK2818713, a Novel Biphenylene Scaffold-Based Hepatitis C NS5A Replication Complex Inhibitor with Broad Genotype Coverage.
Glaxosmithkline
Targeting the Regulatory Site of ER Aminopeptidase 1 Leads to the Discovery of a Natural Product Modulator of Antigen Presentation.
Glaxosmithkline
DNA-Encoded Library Technology-Based Discovery, Lead Optimization, and Prodrug Strategy toward Structurally Unique Indoleamine 2,3-Dioxygenase-1 (IDO1) Inhibitors.
Glaxosmithkline
Discovery and Lead-Optimization of 4,5-Dihydropyrazoles as Mono-Kinase Selective, Orally Bioavailable and Efficacious Inhibitors of Receptor Interacting Protein 1 (RIP1) Kinase.
Glaxosmithkline
Structure-guided design of antibacterials that allosterically inhibit DNA gyrase.
Glaxosmithkline
Discovery of Isoxazole Amides as Potent and Selective SMYD3 Inhibitors.
Glaxosmithkline
Discovery of a crystalline sulforaphane analog with good solid-state stability and engagement of the Nrf2 pathway in vitro and in vivo.
Glaxosmithkline
3,5-Disubstituted-indole-7-carboxamides as IKKβ Inhibitors: Optimization of Oral Activity via the C3 Substituent.
Glaxosmithkline
Optimization of Orally Bioavailable PI3Kδ Inhibitors and Identification of Vps34 as a Key Selectivity Target.
Glaxosmithkline
Discovery of GSK3527497: A Candidate for the Inhibition of Transient Receptor Potential Vanilloid-4 (TRPV4).
Glaxosmithkline
Discovery of Pyrazolocarboxamides as Potent and Selective Receptor Interacting Protein 2 (RIP2) Kinase Inhibitors.
Glaxosmithkline
Discovery of GSK2798745: A Clinical Candidate for Inhibition of Transient Receptor Potential Vanilloid 4 (TRPV4).
Glaxosmithkline
Identification of a RIP1 Kinase Inhibitor Clinical Candidate (GSK3145095) for the Treatment of Pancreatic Cancer.
Glaxosmithkline
Discovery of a potent boronic acid derived inhibitor of the HCV RNA-dependent RNA polymerase.
Glaxosmithkline
Novel hydroxyl tricyclics (e.g., GSK966587) as potent inhibitors of bacterial type IIA topoisomerases.
Glaxosmithkline
Synthesis and structure-activity relationships of indazole arylsulfonamides as allosteric CC-chemokine receptor 4 (CCR4) antagonists.
Glaxosmithkline
[3a,4]-Dihydropyrazolo[1,5a]pyrimidines: Novel, Potent, and Selective Phosphatidylinositol-3-kinase β Inhibitors.
Glaxosmithkline
Structure-activity relationship studies of novel 3-oxazolidinedione-6-naphthyl-2-pyridinones as potent and orally bioavailable EP3 receptor antagonists.
Glaxosmithkline
The naphthyridinone GSK364735 is a novel, potent human immunodeficiency virus type 1 integrase inhibitor and antiretroviral.
Glaxosmithkline
In vitro antiviral activity of the novel, tyrosyl-based human immunodeficiency virus (HIV) type 1 protease inhibitor brecanavir (GW640385) in combination with other antiretrovirals and against a panel of protease inhibitor-resistant HIV.
Glaxosmithkline
Pyrrolidinyl pyridone and pyrazinone analogues as potent inhibitors of prolyl oligopeptidase (POP).
Glaxosmithkline
Potent achiral agonists of the growth hormone secretagogue (ghrelin) receptor. Part 2: Lead optimisation.
Glaxosmithkline
Potent achiral agonists of the ghrelin (growth hormone secretagogue) receptor. Part I: Lead identification.
Glaxosmithkline
Synthesis and evaluation of potent and selective beta3 adrenergic receptor agonists containing heterobiaryl carboxylic acids.
Glaxosmithkline
3,4-Dihydro-2H-benzoxazinones as dual-acting 5-HT1A receptor antagonists and serotonin reuptake inhibitors.
Glaxosmithkline
5-HT2C antagonists based on fused heterotricyclic templates: design, synthesis and biological evaluation.
Glaxosmithkline
Discovery of potent and stable conformationally constrained analogues of the MCH R1 antagonist SB-568849.
Glaxosmithkline
SAR of biphenyl carboxamide ligands of the human melanin-concentrating hormone receptor 1 (MCH R1): discovery of antagonist SB-568849.
Glaxosmithkline
Bicyclic heteroarylpiperazines as selective brain penetrant 5-HT6 receptor antagonists.
Glaxosmithkline
Discovery of the first potent, selective 5-hydroxytryptamine1D receptor antagonist.
Glaxosmithkline
3,4-Dihydro-2H-benzoxazinones are 5-HT(1A) receptor antagonists with potent 5-HT reuptake inhibitory activity.
Glaxosmithkline
Discovery of a potent and selective 5-ht5A receptor antagonist by high-throughput chemistry.
Glaxosmithkline
Discovery of non-steroidal mifepristone mimetics: pyrazoline-based PR antagonists.
Glaxosmithkline
Identification of Quinoline-Based RIP2 Kinase Inhibitors with an Improved Therapeutic Index to the hERG Ion Channel.
Glaxosmithkline
Easy-To-Synthesize Spirocyclic Compounds Possess Remarkable in Vivo Activity against Mycobacterium tuberculosis.
Glaxosmithkline
Aiming to Miss a Moving Target: Bromo and Extra Terminal Domain (BET) Selectivity in Constrained ATAD2 Inhibitors.
Glaxosmithkline
Discovery of {4-[4,9-bis(ethyloxy)-1-oxo-1,3-dihydro-2H-benzo[f]isoindol-2-yl]-2-fluorophenyl}acetic acid (GSK726701A), a novel EP
Glaxosmithkline
Discovery of a First-in-Class Gut-Restricted RET Kinase Inhibitor as a Clinical Candidate for the Treatment of IBS.
Glaxosmithkline
Mapping the Efficiency and Physicochemical Trajectories of Successful Optimizations.
Glaxosmithkline
Discovery of renin inhibitors containing a simple aspartate binding moiety that imparts reduced P450 inhibition.
Glaxosmithkline
Discovery of Tetralones as Potent and Selective Inhibitors of Acyl-CoA:Diacylglycerol Acyltransferase 1.
Glaxosmithkline
An orally available, brain-penetrant CAMKK2 inhibitor reduces food intake in rodent model.
Glaxosmithkline
Development of a Series of Kynurenine 3-Monooxygenase Inhibitors Leading to a Clinical Candidate for the Treatment of Acute Pancreatitis.
Glaxosmithkline
Identification of selective 8-(piperidin-4-yloxy)quinoline sulfone and sulfonamide histamine H
Glaxosmithkline
Identification of potent, nonabsorbable agonists of the calcium-sensing receptor for GI-specific administration.
Glaxosmithkline
Identification of pyrazolopyrimidine arylsulfonamides as CC-chemokine receptor 4 (CCR4) antagonists.
Glaxosmithkline
A Quick Route to Multiple Highly Potent SARS-CoV-2 Main Protease Inhibitors
Texas A&M University
Indazole and indole derivatives as inhibitors of retinoic acid related orphan receptor gamma (ROR gamma) for the treatment of immune-related diseases
Orca Pharmaceuticals
Bicyclic urea, thiourea, guanidine and cyanoguanidine compounds useful for the treatment of pain
Array Biopharma
Phosphonate derivatives and methods of use thereof in the treatment of Alzheimer's disease
University of Kansas
Antibacterial piperidinyl substituted 3,4-dihydro-1H-[1,8]naphthyridinones
Janssen Ireland
Thiazole-substituted aminopyridines as spleen tyrosine kinase inhibitors
Merck Sharp & Dohme
Histone deacetylase inhibitors and compositions and methods of use thereof
Chdi Foundation
Cannabinoid receptor antagonists/inverse agonists useful for treating metabolic disorders, including obesity and diabetes
Jenrin Discovery
Substituted N-(pyrrolidine-3-yl)-7H-pyrrolo[2,3-D]pyrimidine-4-amine as janus kinase inhibitor
Yang Ji Chemical
Substituted aza-bicyclic imidazole derivatives useful TRPM8 receptor modulators
Janssen Pharmaceutica
Aniline derivative, pharmaceutical composition containing same, and use thereof
Kissei Pharmaceutical
Estra-1,3,5(10),16-tetraene-3-carboxamides for inhibition of 17.beta.-hydroxysteroid dehydrogenase (AKR1C3)
Bayer Pharma Aktiengesellschaft
Azabicyclic carbamates and their use as alpha-7 nicotinic acetylcholine receptor agonists
Bayer Intellectual Property
Sulfoximine substituted quinazolines for pharmaceutical compositions
Evotec International
Synthesis and use of dual tyrosyl-DNA phosphodiesterase I (Tdp1)—topoisomerase I (Top1) inhibitors
Purdue Research Foundation
Disubstituted 3,4-diamino-3-cyclobutene-1,2-dione compounds for use in the treatment of chemokine-mediated diseases
Galderma Research & Development
A3 adenosine receptor allosteric modulators
The United States of America, Represented By The Secretary, Dept. of Health and Human Services
Guanidine substituted tetrahydroisoquinoline compounds as factor XIa inhibitors
Bristol-Myers Squibb
Discovery of novel 2-substituted-4-(2-fluorophenoxy) pyridine derivatives possessing pyrazolone and triazole moieties as dual c-Met/VEGFR-2 receptor tyrosine kinase inhibitors
China Pharmaceutical University
Structural, functional, and inhibition studies of a Gcn5-related N-acetyltransferase (GNAT) superfamily protein PA4794: a new C-terminal lysine protein acetyltransferase from pseudomonas aeruginosa.
University of Virginia
Physiological Mg(2+) Conditions Significantly Alter the Inhibition of HIV-1 and HIV-2 Reverse Transcriptases by Nucleoside and Non-Nucleoside Inhibitors in Vitro.
University of Maryland
Method of treatment using substituted imidazo[1,2B]pyridazine compounds
Array Biopharma
Use of 1H-indazole-3-carboxamide compounds as glycogen synthase kinase 3 beta inhibitors
Aziende Chimiche Riunite Angelini Francesco A.C.R.A.F.
Arylaminoalcohol-substituted 2,3-dihydroimidazo[1,2-C]quinolines
Bayer Intellectual Property
Design, synthesis, biological screening, and molecular docking studies of piperazine-derived constrained inhibitors of DPP-IV for the treatment of type 2 diabetes.
Csir-Central Drug Research Institute
Spiro-amino-imidazo-fused heterocyclic compounds as beta-secretase modulators and methods of use
Amgen
Neurochemical characteristics of amisulpride, an atypical dopamine D2/D3 receptor antagonist with both presynaptic and limbic selectivity.
SynthÉLabo Recherche
Chemical library screens targeting an HIV-1 accessory factor/host cell kinase complex identify novel antiretroviral compounds.
University of Pittsburgh
Small-molecule kinase inhibitors provide insight into Mps1 cell cycle function.
Dana-Farber Cancer Institute
Identification of potent and novel small-molecule inhibitors of caspase-3.
Sunesis Pharmaceuticals
Cyclic HIV protease inhibitors: synthesis, conformational analysis, P2/P2' structure-activity relationship, and molecular recognition of cyclic ureas.
Dupont Pharmaceuticals
Potent N-(1,3-thiazol-2-yl)pyridin-2-amine vascular endothelial growth factor receptor tyrosine kinase inhibitors with excellent pharmacokinetics and low affinity for the hERG ion channel.
Merck Research Laboratories
Tyrosine kinase inhibitors. 18. 6-Substituted 4-anilinoquinazolines and 4-anilinopyrido[3,4-d]pyrimidines as soluble, irreversible inhibitors of the epidermal growth factor receptor.
University of Auckland
Identification of tricyclic analogs related to ellagic acid as potent/selective tyrosine protein kinase inhibitors.
Pfizer
Inhibition of clinically relevant mutant variants of HIV-1 by quinazolinone non-nucleoside reverse transcriptase inhibitors.
Dupont Pharmaceuticals
Phenethylthiazolylthiourea (PETT) compounds as a new class of HIV-1 reverse transcriptase inhibitors. 2. Synthesis and further structure-activity relationship studies of PETT analogs.
Eli Lilly
2-Amino-6-arylsulfonylbenzonitriles as non-nucleoside reverse transcriptase inhibitors of HIV-1.
Glaxosmithkline
Nonpeptide cyclic cyanoguanidines as HIV-1 protease inhibitors: synthesis, structure-activity relationships, and X-ray crystal structure studies.
Dupont Pharmaceuticals
Stereoisomers of cyclic urea HIV-1 protease inhibitors: synthesis and binding affinities.
Dupont Pharmaceuticals
Novel non-nucleoside inhibitors of HIV-1 reverse transcriptase. 1. Tricyclic pyridobenzo- and dipyridodiazepinones.
Boehringer Ingelheim Pharmaceuticals
Structure-based design of nonpeptidic HIV protease inhibitors: the sulfonamide-substituted cyclooctylpyramones.
Upjohn
Selective non-nucleoside HIV-1 reverse transcriptase inhibitors. New 2,3-dihydrothiazolo[2,3-a]isoindol-5(9bH)-ones and related compounds with anti-HIV-1 activity.
Boehringer Mannheim
Synthesis and evaluation of 2-pyridinone derivatives as HIV-1-specific reverse transcriptase inhibitors. 2. Analogues of 3-aminopyridin-2(1H)-one.
Merck Research Laboratories
Inhibitors of HIV-1 proteinase containing 2-heterosubstituted 4-amino-3-hydroxy-5-phenylpentanoic acid: synthesis, enzyme inhibition, and antiviral activity.
Sandoz Forschungsinstitut Ges.M.B.H.
A novel, picomolar inhibitor of human immunodeficiency virus type 1 protease.
Abbott Laboratories