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614 articles for thisTarget


The following articles (labelled with PubMed ID or TBD) are for your review

PMID
Data
Article Title
Organization
Discovery of a Highly Selective Tankyrase Inhibitor Displaying Growth Inhibition Effects against a Diverse Range of Tumor Derived Cell Lines.EBI
Glaxosmithkline
The discovery of potent and selective kynurenine 3-monooxygenase inhibitors for the treatment of acute pancreatitis.EBI
Glaxosmithkline
Discovery of a Potent, Cell Penetrant, and Selective p300/CBP-Associated Factor (PCAF)/General Control Nonderepressible 5 (GCN5) Bromodomain Chemical Probe.EBI
Glaxosmithkline
Discovery of GSK2193874: An Orally Active, Potent, and Selective Blocker of Transient Receptor Potential Vanilloid 4.EBI
Glaxosmithkline
Exploration of phenylpropanoic acids as agonists of the free fatty acid receptor 4 (FFA4): Identification of an orally efficacious FFA4 agonist.EBI
Glaxosmithkline
Novel GSK-3 inhibitors with improved cellular activity.EBI
Glaxosmithkline
SB-656104-A: a novel 5-HT(7) receptor antagonist with improved in vivo properties.EBI
Glaxosmithkline
Identification of potent and selective oxytocin antagonists. Part 1: indole and benzofuran derivatives.EBI
Glaxosmithkline
Bicyclic piperazinylbenzenesulphonamides are potent and selective 5-HT6 receptor antagonists.EBI
Glaxosmithkline
Novel (4-piperazin-1-ylquinolin-6-yl) arylsulfonamides with high affinity and selectivity for the 5-HT(6) receptor.EBI
Glaxosmithkline
Synthesis of N-alkyl substituted indolocarbazoles as potent inhibitors of human cytomegalovirus replication.EBI
Glaxosmithkline
1,3-Biarylureas as selective non-peptide antagonists of the orexin-1 receptor.EBI
Glaxosmithkline
Structure-activity relationship investigations of a potent and selective benzodiazepine oxytocin antagonist.EBI
Glaxosmithkline
The discovery of quinoline based single-ligand human HEBI
Glaxosmithkline
Substituent Effects on Drug-Receptor H-bond Interactions: Correlations Useful for the Design of Kinase Inhibitors.EBI
Glaxosmithkline
GSK6853, a Chemical Probe for Inhibition of the BRPF1 Bromodomain.EBI
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.EBI
Glaxosmithkline
Optimizing Ligand Efficiency of Selective Androgen Receptor Modulators (SARMs).EBI
Glaxosmithkline
GSK114: A selective inhibitor for elucidating the biological role of TNNI3K.EBI
Glaxosmithkline
Discovery and Optimization of Potent, Selective, and in Vivo Efficacious 2-Aryl Benzimidazole BCATm Inhibitors.EBI
Glaxosmithkline
The design of 8-hydroxyquinoline tetracyclic lactams as HIV-1 integrase strand transfer inhibitors.EBI
Glaxosmithkline
Discovery of a Novel 2,6-Disubstituted Glucosamine Series of Potent and Selective Hexokinase 2 Inhibitors.EBI
Glaxosmithkline
Structurally Diverse Mitochondrial Branched Chain Aminotransferase (BCATm) Leads with Varying Binding Modes Identified by Fragment Screening.EBI
Glaxosmithkline
Identification of nonabsorbable inhibitors of the scavenger receptor-BI (SR-BI) for tissue-specific administration.EBI
Glaxosmithkline
DNA-Encoded Library Screening Identifies Benzo[b][1,4]oxazepin-4-ones as Highly Potent and Monoselective Receptor Interacting Protein 1 Kinase Inhibitors.EBI
Glaxosmithkline
Novel tricyclics (e.g., GSK945237) as potent inhibitors of bacterial type IIA topoisomerases.EBI
Glaxosmithkline
Cell Penetrant Inhibitors of the KDM4 and KDM5 Families of Histone Lysine Demethylases. 1. 3-Amino-4-pyridine Carboxylate Derivatives.EBI
Glaxosmithkline
Cell Penetrant Inhibitors of the KDM4 and KDM5 Families of Histone Lysine Demethylases. 2. Pyrido[3,4-d]pyrimidin-4(3H)-one Derivatives.EBI
Glaxosmithkline
Discovery of Tetrahydropyrazolopyridine as Sphingosine 1-Phosphate Receptor 3 (S1P3)-Sparing S1P1 Agonists Active at Low Oral Doses.EBI
Glaxosmithkline
Discovery and Characterization of GSK2801, a Selective Chemical Probe for the Bromodomains BAZ2A and BAZ2B.EBI
Glaxosmithkline
Crystal structures of human RIP2 kinase catalytic domain complexed with ATP-competitive inhibitors: Foundations for understanding inhibitor selectivity.EBI
Glaxosmithkline
Navigating CYP1A Induction and Arylhydrocarbon Receptor Agonism in Drug Discovery. A Case History with S1P1 Agonists.EBI
Glaxosmithkline
Discovery, SAR, and X-ray Binding Mode Study of BCATm Inhibitors from a Novel DNA-Encoded Library.EBI
Glaxosmithkline
Discovery of Potent and Selective Inhibitors for ADAMTS-4 through DNA-Encoded Library Technology (ELT).EBI
Glaxosmithkline
The Discovery of in Vivo Active Mitochondrial Branched-Chain Aminotransferase (BCATm) Inhibitors by Hybridizing Fragment and HTS Hits.EBI
Glaxosmithkline
Identification of Purines and 7-Deazapurines as Potent and Selective Type I Inhibitors of Troponin I-Interacting Kinase (TNNI3K).EBI
Glaxosmithkline
Carbamoyl Triazoles, Known Serine Protease Inhibitors, Are a Potent New Class of Antimalarials.EBI
Glaxosmithkline
Discovery of 4-Amino-8-quinoline Carboxamides as Novel, Submicromolar Inhibitors of NAD-Hydrolyzing Enzyme CD38.EBI
Glaxosmithkline
Brain tissue binding of drugs: evaluation and validation of solid supported porcine brain membrane vesicles (TRANSIL) as a novel high-throughput method.EBI
Glaxosmithkline
Structure-Based Optimization of Naphthyridones into Potent ATAD2 Bromodomain Inhibitors.EBI
Glaxosmithkline
Fragment-Based Discovery of Low-Micromolar ATAD2 Bromodomain Inhibitors.EBI
Glaxosmithkline
Discovery of a Potent Class of PI3Ka Inhibitors with Unique Binding Mode via Encoded Library Technology (ELT).EBI
Glaxosmithkline
Metabolites of PPI-2458, a selective, irreversible inhibitor of methionine aminopeptidase-2: structure determination and in vivo activity.EBI
Glaxosmithkline
Casopitant: in vitro data and SimCyp simulation to predict in vivo metabolic interactions involving cytochrome P450 3A4.EBI
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.EBI
Glaxosmithkline
Discovery, Synthesis, and Biological Evaluation of Thiazoloquin(az)olin(on)es as Potent CD38 Inhibitors.EBI
Glaxosmithkline
Structural requirements for TLR7-selective signaling by 9-(4-piperidinylalkyl)-8-oxoadenine derivatives.EBI
Glaxosmithkline
Lead identification of benzimidazolone and azabenzimidazolone arylsulfonamides as CC-chemokine receptor 4 (CCR4) antagonists.EBI
Glaxosmithkline
Naphthyridinone (NTD) integrase inhibitors 4. Investigating N1 acetamide substituent effects with C3 amide groups.EBI
Glaxosmithkline
Identification of diarylsulfonamides as agonists of the free fatty acid receptor 4 (FFA4/GPR120).EBI
Glaxosmithkline
Novel heterocyclic scaffolds of GW4064 as farnesoid X receptor agonists.EBI
Glaxosmithkline
2-Aminopyrimidin-4(1H)-one as the novel bioisostere of urea: discovery of novel and potent CXCR2 antagonists.EBI
Glaxosmithkline
Optimization of sphingosine-1-phosphate-1 receptor agonists: effects of acidic, basic, and zwitterionic chemotypes on pharmacokinetic and pharmacodynamic profiles.EBI
Glaxosmithkline
1,3-Dimethyl Benzimidazolones Are Potent, Selective Inhibitors of the BRPF1 Bromodomain.EBI
Glaxosmithkline
The discovery of I-BET726 (GSK1324726A), a potent tetrahydroquinoline ApoA1 up-regulator and selective BET bromodomain inhibitor.EBI
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.EBI
Glaxosmithkline
Pyridopyrimidinone inhibitors of HIV-1 RNase H.EBI
Glaxosmithkline
Diaryl substituted pyrrolidinones and pyrrolones as 5-HT2C inhibitors: synthesis and biological evaluation.EBI
Glaxosmithkline
Biarylaniline phenethanolamines as potent and selective beta3 adrenergic receptor agonists.EBI
Glaxosmithkline
2,5-diketopiperazines as potent, selective, and orally bioavailable oxytocin antagonists. 2. Synthesis, chirality, and pharmacokinetics.EBI
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.EBI
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.EBI
Glaxosmithkline
Hepatitis C replication inhibitors that target the viral NS4B protein.EBI
Glaxosmithkline
Novel spiroketal pyrrolidine GSK2336805 potently inhibits key hepatitis C virus genotype 1b mutants: from lead to clinical compound.EBI
Glaxosmithkline
Discovery of selective small molecule type III phosphatidylinositol 4-kinase alpha (PI4KIIIa) inhibitors as anti hepatitis C (HCV) agents.EBI
Glaxosmithkline
Discovery of novel indazole derivatives as dual angiotensin II antagonists and partial PPAR¿ agonists.EBI
Glaxosmithkline
Discovery of Tertiary Amine and Indole Derivatives as Potent RORγt Inverse Agonists.EBI
Glaxosmithkline
Discovery of Small Molecule RIP1 Kinase Inhibitors for the Treatment of Pathologies Associated with Necroptosis.EBI
Glaxosmithkline
Discovery of novel N-(5-(arylcarbonyl)thiazol-2-yl)amides and N-(5-(arylcarbonyl)thiophen-2-yl)amides as potent ROR¿t inhibitors.EBI
Glaxosmithkline
Identification of clinical candidates from the benzazepine class of histamine H3 receptor antagonists.EBI
Glaxosmithkline
The discovery of the benzazepine class of histamine H3 receptor antagonists.EBI
Glaxosmithkline
Identification, biological characterization and pharmacophoric analysis of a new potent and selective NK1 receptor antagonist clinical candidate.EBI
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.EBI
Glaxosmithkline
Discovery of GSK2656157: An Optimized PERK Inhibitor Selected for Preclinical Development.EBI
Glaxosmithkline
Identification of a Novel and Selective Series of Itk Inhibitors via a Template-Hopping Strategy.EBI
Glaxosmithkline
Discovery of epigenetic regulator I-BET762: lead optimization to afford a clinical candidate inhibitor of the BET bromodomains.EBI
Glaxosmithkline
The discovery of potent blockers of the canonical transient receptor channels, TRPC3 and TRPC6, based on an anilino-thiazole pharmacophore.EBI
Glaxosmithkline
Discovery of 1-(1,3,5-triazin-2-yl)piperidine-4-carboxamides as inhibitors of soluble epoxide hydrolase.EBI
Glaxosmithkline
Discovery of a highly potent, nonabsorbable apical sodium-dependent bile acid transporter inhibitor (GSK2330672) for treatment of type 2 diabetes.EBI
Glaxosmithkline
Optimized chemical probes for REV-ERBa.EBI
Glaxosmithkline
Selective 3-phosphoinositide-dependent kinase 1 (PDK1) inhibitors: dissecting the function and pharmacology of PDK1.EBI
Glaxosmithkline
Discovery of Dabrafenib: A Selective Inhibitor of Raf Kinases with Antitumor Activity against B-Raf-Driven Tumors.EBI
Glaxosmithkline
Optimization of a Novel Series of TRPV4 Antagonists with In Vivo Activity in a Model of Pulmonary Edema.EBI
Glaxosmithkline
The discovery of potent and selective 4-aminothienopyridines as B-Raf kinase inhibitors.EBI
Glaxosmithkline
Macrolactonolides: a novel class of anti-inflammatory compounds.EBI
Glaxosmithkline
New fused benzazepine as selective D3 receptor antagonists. Synthesis and biological evaluation. Part 2: [g]-fused and hetero-fused systems.EBI
Glaxosmithkline
Novel methylene-linked heterocyclic EP1 receptor antagonists.EBI
Glaxosmithkline
Novel substituted tetrahydrotriazaacenaphthylene derivatives as potent CRF1 receptor antagonists.EBI
Glaxosmithkline
Oxazolidinones as novel human CCR8 antagonists.EBI
Glaxosmithkline
1,3-diaminopropan-2-ol sulfonamides as potent and selective inhibitors of the glycine transporter type 1.EBI
Glaxosmithkline
Non-steroidal glucocorticoid agonists: the discovery of aryl pyrazoles as A-ring mimetics.EBI
Glaxosmithkline
Discovery of novel, non-acidic 1,5-biaryl pyrrole EP1 receptor antagonists.EBI
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.EBI
Glaxosmithkline
1,5-Biaryl pyrrole derivatives as EP1 receptor antagonists: Structure-activity relationships of 4- and 5-substituted benzoic acid derivatives.EBI
Glaxosmithkline
Co-crystal structure guided array synthesis of PPARgamma inverse agonists.EBI
Glaxosmithkline
1,5-Biaryl pyrrole derivatives as EP1 receptor antagonists. Structure-activity relationships of 6-substituted and 5,6-disubstituted benzoic acid derivatives.EBI
Glaxosmithkline
The discovery and optimization of pyrimidinone-containing MCH R1 antagonists.EBI
Glaxosmithkline
Novel benzimidazole-based MCH R1 antagonists.EBI
Glaxosmithkline
Array synthesis of progesterone receptor antagonists: 3-aryl-1,2-diazepines.EBI
Glaxosmithkline
Synthesis and SAR of substituted tetrahydrocarbazole derivatives as new NPY-1 antagonists.EBI
Glaxosmithkline
From pyrroles to pyrrolo[1,2-a]pyrazinones: a new class of mGluR1 antagonists.EBI
Glaxosmithkline
Design and synthesis of new nonsteroidal glucocorticoid modulators through application of an"agreement docking" method.EBI
Glaxosmithkline
Aminoalkoxybenzyl pyrrolidines as novel human urotensin-II receptor antagonists.EBI
Glaxosmithkline
Synthesis and evaluation of potent and selective beta(3) adrenergic receptor agonists containing acylsulfonamide, sulfonylsulfonamide, and sulfonylurea carboxylic acid isosteres.EBI
Glaxosmithkline
2-(Anilinomethyl)imidazolines as alpha1 adrenergic receptor agonists: alpha1a subtype selective 2'-heteroaryl compounds.EBI
Glaxosmithkline
2-(anilinomethyl)imidazolines as alpha1A adrenergic receptor agonists: 2'-heteroaryl and 2'-oxime ether series.EBI
Glaxosmithkline
alpha(1)-Adrenoceptor agonists: the identification of novel alpha(1A )subtype selective 2'-heteroaryl-2-(phenoxymethyl)imidazolines.EBI
Glaxosmithkline
Alpha(1)-adrenoceptor activation: a comparison of 4-(anilinomethyl)imidazoles and 4-(phenoxymethyl)imidazoles to related 2-imidazolines.EBI
Glaxosmithkline
2-(Anilinomethyl)imidazolines as alpha(1)-adrenoceptor agonists: the identification of alpha(1A) subtype selective 2'-carboxylic acid esters and amides.EBI
Glaxosmithkline
Indole-propionic acid derivatives as potent, S1P3-sparing and EAE efficacious sphingosine-1-phosphate 1 (S1P1) receptor agonists.EBI
Glaxosmithkline
Discovery of a novel series of nonacidic benzofuran EP1 receptor antagonists.EBI
Glaxosmithkline
Identification of novel NK1/NK3 dual antagonists for the potential treatment of schizophrenia.EBI
Glaxosmithkline
The discovery of long-acting saligeninß2 adrenergic receptor agonists incorporating a urea group.EBI
Glaxosmithkline
Discovery of GSK143, a highly potent, selective and orally efficacious spleen tyrosine kinase inhibitor.EBI
Glaxosmithkline
Acylglycinamides as inhibitors of glycine transporter type 1.EBI
Glaxosmithkline
Discovery process and pharmacological characterization of a novel dual orexin 1 and orexin 2 receptor antagonist useful for treatment of sleep disorders.EBI
Glaxosmithkline
The discovery of long-acting saligeninß2 adrenergic receptor agonists incorporating hydantoin or uracil rings.EBI
Glaxosmithkline
Identification of 2-(4-pyridyl)thienopyridinones as GSK-3ß inhibitors.EBI
Glaxosmithkline
Synthesis and structure-activity relationship of new 1,5-dialkyl-1,5-benzodiazepines as cholecystokinin-2 receptor antagonists.EBI
Glaxosmithkline
p38alpha mitogen-activated protein kinase inhibitors: optimization of a series of biphenylamides to give a molecule suitable for clinical progression.EBI
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.EBI
Glaxosmithkline
3,5-Disubstituted-indole-7-carboxamides: the discovery of a novel series of potent, selective inhibitors of IKK-ß.EBI
Glaxosmithkline
Phenoxyacetic acids as PPARd partial agonists: synthesis, optimization, and in vivo efficacy.EBI
Glaxosmithkline
Discovery of a potent series of non-steroidal nona-trifluoromethyl carbinol glucocorticoid receptor agonists with reduced lipophilicity.EBI
Glaxosmithkline
The characterization of a novel V1b antagonist lead series.EBI
Glaxosmithkline
Tetrahydroquinoline derivatives as opioid receptor antagonists.EBI
Glaxosmithkline
The identification of a series of novel, soluble non-peptidic neuropeptide Y Y2 receptor antagonists.EBI
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.EBI
Glaxosmithkline
Design, synthesis and SAR of a novel series of benzimidazoles as potent NPY Y5 antagonists.EBI
Glaxosmithkline
Identification of 2-oxo-N-(phenylmethyl)-4-imidazolidinecarboxamide antagonists of the P2X(7) receptor.EBI
Glaxosmithkline
Discovery and structure-activity relationship of a novel spirocarbamate series of NPY Y5 antagonists.EBI
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.EBI
Glaxosmithkline
[3-azabicyclo[3.1.0]hex-1-yl]phenyl-benzenesulfonamides as selective dopamine D3 antagonists.EBI
Glaxosmithkline
Novel imidazobenzazepine derivatives as dual H1/5-HT2A antagonists for the treatment of sleep disorders.EBI
Glaxosmithkline
Pyrrolo[1,2-a]pyrazine and pyrazolo[1,5-a]pyrazine: novel, potent, and selective series of Vasopressin 1b receptor antagonists.EBI
Glaxosmithkline
Discovery and structure-activity relationships of a series of pyroglutamic acid amide antagonists of the P2X7 receptor.EBI
Glaxosmithkline
Identification of novel alpha7 nAChR positive allosteric modulators with the use of pharmacophore in silico screening methods.EBI
Glaxosmithkline
Structure-activity relationships and in vivo activity of (1H-pyrazol-4-yl)acetamide antagonists of the P2X(7) receptor.EBI
Glaxosmithkline
ADMET rules of thumb II: A comparison of the effects of common substituents on a range of ADMET parameters.EBI
Glaxosmithkline
Identification of a sulfonamide series of CCR2 antagonists.EBI
Glaxosmithkline
2' biaryl amides as novel and subtype selective M1 agonists. Part I: Identification, synthesis, and initial SAR.EBI
Glaxosmithkline
2' biaryl amides as novel and subtype selective M1 agonists. Part II: Further optimization and profiling.EBI
Glaxosmithkline
Structure guided design of 5-arylindazole glucocorticoid receptor agonists and antagonists.EBI
Glaxosmithkline
Synthesis and structure-activity relationships of long-acting beta2 adrenergic receptor agonists incorporating metabolic inactivation: an antedrug approach.EBI
Glaxosmithkline
Synthesis and structure-activity relationships of a series of (1H-pyrazol-4-yl)acetamide antagonists of the P2X7 receptor.EBI
Glaxosmithkline
Discovery of tertiary sulfonamides as potent liver X receptor antagonists.EBI
Glaxosmithkline
1-Aryl-3,4-dihydroisoquinoline inhibitors of JNK3.EBI
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.EBI
Glaxosmithkline
Synthesis and structure-activity relationships of a series of 3-aryl-4-isoxazolecarboxamides as a new class of TGR5 agonists.EBI
Glaxosmithkline
Potent oxadiazole CGRP receptor antagonists for the potential treatment of migraine.EBI
Glaxosmithkline
Synthesis and evaluation of 3-amino-6-aryl-pyridazines as selective CB(2) agonists for the treatment of inflammatory pain.EBI
Glaxosmithkline
The identification of structurally novel, selective, orally bioavailable positive modulators of mGluR2.EBI
Glaxosmithkline
Synthesis and pharmacological characterization of constrained analogues of Vestipitant as in vitro potent and orally active NK(1) receptor antagonists.EBI
Glaxosmithkline
Addressing species specific metabolism and solubility issues in a quinoline series of oral PDE4 inhibitors.EBI
Glaxosmithkline
2-Amino-5-aryl-pyridines as selective CB2 agonists: synthesis and investigation of structure-activity relationships.EBI
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.EBI
Glaxosmithkline
Quinolines as a novel structural class of potent and selective PDE4 inhibitors. Optimisation for inhaled administration.EBI
Glaxosmithkline
Discovery of 3-aryl-4-isoxazolecarboxamides as TGR5 receptor agonists.EBI
Glaxosmithkline
Highly tractable, sub-nanomolar non-steroidal glucocorticoid receptor agonists.EBI
Glaxosmithkline
Dopamine D(3) receptor antagonists: The quest for a potentially selective PET ligand. Part two: Lead optimization.EBI
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.EBI
Glaxosmithkline
4-Phenyl-7-azaindoles as potent and selective IKK2 inhibitors.EBI
Glaxosmithkline
Discovery and optimisation of a potent and selective tertiary sulfonamide oxytocin antagonist.EBI
Glaxosmithkline
Studies on a series of potent, orally bioavailable, 5-HT(1) receptor ligands--part II.EBI
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.EBI
Glaxosmithkline
Synthesis and structure-activity relationships of long-acting beta2 adrenergic receptor agonists incorporating arylsulfonamide groups.EBI
Glaxosmithkline
M3 muscarinic acetylcholine receptor antagonists: SAR and optimization of bi-aryl amines.EBI
Glaxosmithkline
Quinolines as a novel structural class of potent and selective PDE4 inhibitors: optimisation for oral administration.EBI
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.EBI
Glaxosmithkline
Muscarinic acetylcholine receptor antagonists: SAR and optimization of tyrosine ureas.EBI
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.EBI
Glaxosmithkline
N-alkyl-5H-pyrido[4,3-b]indol-1-amines and derivatives as novel urotensin-II receptor antagonists.EBI
Glaxosmithkline
The discovery of a selective, small molecule agonist for the MAS-related gene X1 receptor.EBI
Glaxosmithkline
Aryl sulphonyl amides as potent agonists of the growth hormone secretagogue (ghrelin) receptor.EBI
Glaxosmithkline
Identification of small molecule agonists of the motilin receptor.EBI
Glaxosmithkline
Synthesis and pharmacological characterization of novel druglike corticotropin-releasing factor 1 antagonists.EBI
Glaxosmithkline
Discovery of bioavailable 4,4-disubstituted piperidines as potent ligands of the chemokine receptor 5 and inhibitors of the human immunodeficiency virus-1.EBI
Glaxosmithkline
Discovery of biphenyl piperazines as novel and long acting muscarinic acetylcholine receptor antagonists.EBI
Glaxosmithkline
The first X-ray crystal structure of the glucocorticoid receptor bound to a non-steroidal agonist.EBI
Glaxosmithkline
Novel 5-HT(1A/1B/1D) receptors antagonists with potent 5-HT reuptake inhibitory activity.EBI
Glaxosmithkline
Pyrazolopyridines as a novel structural class of potent and selective PDE4 inhibitors.EBI
Glaxosmithkline
Discovery of novel and long acting muscarinic acetylcholine receptor antagonists.EBI
Glaxosmithkline
Discovery of brain penetrant, soluble, pyrazole amide EP1 receptor antagonists.EBI
Glaxosmithkline
Discovery of potent, orally bioavailable, selective 5-HT1A/B/D receptor antagonists.EBI
Glaxosmithkline
Phenylethynyl-pyrrolo[1,2-a]pyrazine: a new potent and selective tool in the mGluR5 antagonists arena.EBI
Glaxosmithkline
Thiol-based angiotensin-converting enzyme 2 inhibitors: P1 modifications for the exploration of the S1 subsite.EBI
Glaxosmithkline
New fused benzazepine as selective D3 receptor antagonists. Synthesis and biological evaluation. Part one: [h]-fused tricyclic systems.EBI
Glaxosmithkline
Identification of novel glycine sulfonamide antagonists for the EP1 receptor.EBI
Glaxosmithkline
Nonsteroidal glucocorticoid agonists: tetrahydronaphthalenes with alternative steroidal A-ring mimetics possessing dissociated (transrepression/transactivation) efficacy selectivity.EBI
Glaxosmithkline
N-(3-Cyano-4,5,6,7-tetrahydro-1-benzothien-2-yl)amides as potent, selective, inhibitors of JNK2 and JNK3.EBI
Glaxosmithkline
Dissociated nonsteroidal glucocorticoid receptor modulators; discovery of the agonist trigger in a tetrahydronaphthalene-benzoxazine series.EBI
Glaxosmithkline
A series of bisaryl imidazolidin-2-ones has shown to be selective and orally active 5-HT2C receptor antagonists.EBI
Glaxosmithkline
8-Piperazinyl-2,3-dihydropyrrolo[3,2-g]isoquinolines: potent, selective, orally bioavailable 5-HT1 receptor ligands.EBI
Glaxosmithkline
Tyrosine urea muscarinic acetylcholine receptor antagonists: achiral quaternary ammonium groups.EBI
Glaxosmithkline
In vivo activity of an azole series of CCR2 antagonists.EBI
Glaxosmithkline
GSK2578215A; a potent and highly selective 2-arylmethyloxy-5-substitutent-N-arylbenzamide LRRK2 kinase inhibitor.EBI
Glaxosmithkline
Discovery of 6,7-dihydro-5H-pyrrolo[2,3-a]pyrimidines as orally available G protein-coupled receptor 119 agonists.EBI
Glaxosmithkline
Identification of a novel series of BET family bromodomain inhibitors: binding mode and profile of I-BET151 (GSK1210151A).EBI
Glaxosmithkline
Fragment-based discovery of bromodomain inhibitors part 2: optimization of phenylisoxazole sulfonamides.EBI
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).EBI
Glaxosmithkline
Discovery of highly potent and selective small molecule ADAMTS-5 inhibitors that inhibit human cartilage degradation via encoded library technology (ELT).EBI
Glaxosmithkline
4-Phenyl-7-azaindoles as potent, selective and bioavailable IKK2 inhibitors demonstrating good in vivo efficacy.EBI
Glaxosmithkline
N'-substituted-2'-O,3'-N-carbonimidoyl bridged macrolides: novel anti-inflammatory macrolides without antimicrobial activity.EBI
Glaxosmithkline
Discovery and characterization of small molecule inhibitors of the BET family bromodomains.EBI
Glaxosmithkline
Synthesis and pharmacological investigation of azaphthalazinone human histamine H(1) receptor antagonists.EBI
Glaxosmithkline
Discovery of novel 1,2,4-thiadiazole derivatives as potent, orally active agonists of sphingosine 1-phosphate receptor subtype 1 (S1P(1)).EBI
Glaxosmithkline
Pyridyl-2,5-diketopiperazines as potent, selective, and orally bioavailable oxytocin antagonists: synthesis, pharmacokinetics, and in vivo potency.EBI
Glaxosmithkline
Identification of benzoxazole analogs as novel, S1P(3) sparing S1P(1) agonists.EBI
Glaxosmithkline
Acylprolinamides: a new class of peptide deformylase inhibitors with in vivo antibacterial activity.EBI
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.EBI
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.EBI
Glaxosmithkline
Design, synthesis and structure-activity relationship of N-substituted tropane muscarinic acetylcholine receptor antagonists.EBI
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.EBI
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.EBI
Glaxosmithkline
From ApoA1 upregulation to BET family bromodomain inhibition: discovery of I-BET151.EBI
Glaxosmithkline
Discovery of thiadiazole amides as potent, S1P3-sparing agonists of sphingosine-1-phosphate 1 (S1P1) receptor.EBI
Glaxosmithkline
A novel series of benzimidazole NR2B-selective NMDA receptor antagonists.EBI
Glaxosmithkline
Design, synthesis, and structure-activity relationship of tropane muscarinic acetylcholine receptor antagonists.EBI
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.EBI
Glaxosmithkline
BACE-1 hydroxyethylamine inhibitors using novel edge-to-face interaction with Arg-296.EBI
Glaxosmithkline
6-(3,4-dichlorophenyl)-1-[(methyloxy)methyl]-3-azabicyclo[4.1.0]heptane: a new potent and selective triple reuptake inhibitor.EBI
Glaxosmithkline
Benzofuran-substituted urea derivatives as novel P2Y(1) receptor antagonists.EBI
Glaxosmithkline
The discovery and initial optimisation of pyrrole-2-carboxamides as inhibitors of p38alpha MAP kinase.EBI
Glaxosmithkline
Discovery of GSK1070916, a potent and selective inhibitor of Aurora B/C kinase.EBI
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.EBI
Glaxosmithkline
Antagonists of the calcium receptor. 2. Amino alcohol-based parathyroid hormone secretagogues.EBI
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.EBI
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.EBI
Glaxosmithkline
Kinase array design, back to front: biaryl amides.EBI
Glaxosmithkline
Thienopyrimidine-based dual EGFR/ErbB-2 inhibitors.EBI
Glaxosmithkline
Discovery and optimization of highly ligand-efficient oxytocin receptor antagonists using structure-based drug design.EBI
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.EBI
Glaxosmithkline
Knowledge-based design of 7-azaindoles as selective B-Raf inhibitors.EBI
Glaxosmithkline
2-Aminomethyl piperidines as novel urotensin-II receptor antagonists.EBI
Glaxosmithkline
Development of potent and selective small-molecule human Urotensin-II antagonists.EBI
Glaxosmithkline
Discovery of a novel indole series of EP1 receptor antagonists by scaffold hopping.EBI
Glaxosmithkline
Structure and property based design of factor Xa inhibitors: biaryl pyrrolidin-2-ones incorporating basic heterocyclic motifs.EBI
Glaxosmithkline
BACE-1 inhibitors part 1: identification of novel hydroxy ethylamines (HEAs).EBI
Glaxosmithkline
Non-acidic pyrazole EP1 receptor antagonists with in vivo analgesic efficacy.EBI
Glaxosmithkline
Rational design of 4-amino-5,6-diaryl-furo[2,3-d]pyrimidines as potent glycogen synthase kinase-3 inhibitors.EBI
Glaxosmithkline
The discovery of GSK221149A: a potent and selective oxytocin antagonist.EBI
Glaxosmithkline
Comparison of N,N'-diarylsquaramides and N,N'-diarylureas as antagonists of the CXCR2 chemokine receptor.EBI
Glaxosmithkline
4-acyl-1-(4-aminoalkoxyphenyl)-2-ketopiperazines as a novel class of non-brain-penetrant histamine H3 receptor antagonists.EBI
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.EBI
Glaxosmithkline
Optimization and SAR for dual ErbB-1/ErbB-2 tyrosine kinase inhibition in the 6-furanylquinazoline series.EBI
Glaxosmithkline
Ultra-potent P1 modified arylsulfonamide HIV protease inhibitors: the discovery of GW0385.EBI
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.EBI
Glaxosmithkline
The identification of potent and selective imidazole-based inhibitors of B-Raf kinase.EBI
Glaxosmithkline
Discovery of potent and orally bioavailable N,N'-diarylurea antagonists for the CXCR2 chemokine receptor.EBI
Glaxosmithkline
Novel benzophenones as non-nucleoside reverse transcriptase inhibitors of HIV-1.EBI
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.EBI
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.EBI
Glaxosmithkline
Discovery and in vitro evaluation of potent TrkA kinase inhibitors: oxindole and aza-oxindoles.EBI
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.EBI
Glaxosmithkline
5-Aryl-4-carboxamide-1,3-oxazoles: potent and selective GSK-3 inhibitors.EBI
Glaxosmithkline
Structure-guided lead optimization of triazolopyrimidine-ring substituents identifies potent Plasmodium falciparum dihydroorotate dehydrogenase inhibitors with clinical candidate potential.EBI
Glaxosmithkline
Novel Rho kinase inhibitors with anti-inflammatory and vasodilatory activities.EBI
Glaxosmithkline
Inhibition of colony-stimulating-factor-1 signaling in vivo with the orally bioavailable cFMS kinase inhibitor GW2580.EBI
Glaxosmithkline
Fragment-based discovery of bromodomain inhibitors part 1: inhibitor binding modes and implications for lead discovery.EBI
Glaxosmithkline
Novel amino-piperidines as potent antibacterials targeting bacterial type IIA topoisomerases.EBI
Glaxosmithkline
Novel cyclohexyl-amides as potent antibacterials targeting bacterial type IIA topoisomerases.EBI
Glaxosmithkline
CCR2 receptor antagonists: optimization of biaryl sulfonamides to increase activity in whole blood.EBI
Glaxosmithkline
Conformationally constrained farnesoid X receptor (FXR) agonists: alternative replacements of the stilbene.EBI
Glaxosmithkline
Discovery of a brain-penetrant S1P3-sparing direct agonist of the S1P¿? and S1P5 receptors efficacious at low oral dose.EBI
Glaxosmithkline
Discovery of GSK1997132B a novel centrally penetrant benzimidazole PPAR¿ partial agonist.EBI
Glaxosmithkline
Selectivity of kinase inhibitor fragments.EBI
Glaxosmithkline
1-Heteroaryl-6-(3,4-dichlorophenyl)-3-azabicyclo[4.1.0]heptane: further insights into a class of triple re-uptake inhibitors.EBI
Glaxosmithkline
Development of potent B-RafV600E inhibitors containing an arylsulfonamide headgroup.EBI
Glaxosmithkline
Azepanone-based inhibitors of human cathepsin S: optimization of selectivity via the P2 substituent.EBI
Glaxosmithkline
Synthesis and biological activity of a series of tetrasubstituted-imidazoles as P2X(7) antagonists.EBI
Glaxosmithkline
Pyrazolopyridazine alpha-2-delta-1 ligands for the treatment of neuropathic pain.EBI
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.EBI
Glaxosmithkline
The discovery of phthalazinone-based human H1 and H3 single-ligand antagonists suitable for intranasal administration for the treatment of allergic rhinitis.EBI
Glaxosmithkline
Structure-based design of potent and selective 3-phosphoinositide-dependent kinase-1 (PDK1) inhibitors.EBI
Glaxosmithkline
The discovery of potent and long-acting oral factor Xa inhibitors with tetrahydroisoquinoline and benzazepine P4 motifs.EBI
Glaxosmithkline
Structure and property based design of factor Xa inhibitors: pyrrolidin-2-ones with aminoindane and phenylpyrrolidine P4 motifs.EBI
Glaxosmithkline
Conformationally constrained farnesoid X receptor (FXR) agonists: heteroaryl replacements of the naphthalene.EBI
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.EBI
Glaxosmithkline
Stereospecific synthesis and structure-activity relationships of unsymmetrical 4,4-diphenylbut-3-enyl derivatives of nipecotic acid as GAT-1 inhibitors.EBI
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.EBI
Glaxosmithkline
Discovery of N-benzyl-N'-(4-pipyridinyl)urea CCR5 antagonists as anti-HIV-1 agents (II): modification of the acyl portion.EBI
Glaxosmithkline
Discovery of N-benzyl-N'-(4-pipyridinyl)urea CCR5 antagonists as anti-HIV-1 agents (I): optimization of the amine portion.EBI
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.EBI
Glaxosmithkline
N-{3-[(1,1-dioxido-1,2-benzothiazol-3-yl)(phenyl)amino]propyl}benzamide analogs as potent Kv1.3 inhibitors. Part 1.EBI
Glaxosmithkline
N-substituted pyrrolidines and tetrahydrofurans as novel AMPAR positive modulators.EBI
Glaxosmithkline
Novel spirotetracyclic zwitterionic dual H(1)/5-HT(2A) receptor antagonists for the treatment of sleep disorders.EBI
Glaxosmithkline
2-Methyl-3-furanyl-4H-1,2,4-triazol-3-ylthioamides: a new class of selective orexin 2 antagonists.EBI
Glaxosmithkline
3-Urea-1-(phenylmethyl)-pyridones as novel, potent, and selective EP3 receptor antagonists.EBI
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.EBI
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).EBI
Glaxosmithkline
Blockade of X4-tropic HIV-1 cellular entry by GSK812397, a potent noncompetitive CXCR4 receptor antagonist.EBI
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.EBI
Glaxosmithkline
Heteroaryl-linked 5-(1H-benzimidazol-1-yl)-2-thiophenecarboxamides: potent inhibitors of polo-like kinase 1 (PLK1) with improved drug-like properties.EBI
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.EBI
Glaxosmithkline
Synthesis and SAR of novel isoquinoline CXCR4 antagonists with potent anti-HIV activity.EBI
Glaxosmithkline
Aminofurazans as potent inhibitors of AKT kinase.EBI
Glaxosmithkline
Discovery of a new series of Aurora inhibitors through truncation of GSK1070916.EBI
Glaxosmithkline
2,5-Disubstituted pyridines as potent GPR119 agonists.EBI
Glaxosmithkline
Novel N-substituted benzimidazole CXCR4 antagonists as potential anti-HIV agents.EBI
Glaxosmithkline
The identification of a selective dopamine D2 partial agonist, D3 antagonist displaying high levels of brain exposure.EBI
Glaxosmithkline
1,2,4-Triazolyl azabicyclo[3.1.0]hexanes: a new series of potent and selective dopamine D(3) receptor antagonists.EBI
Glaxosmithkline
Evaluation of basic, heterocyclic ring systems as templates for use as potassium competitive acid blockers (pCABs).EBI
Glaxosmithkline
The discovery and optimisation of benzazepine sulfonamide and sulfones as potent agonists of the motilin receptor.EBI
Glaxosmithkline
Substituted benzothiadizine inhibitors of Hepatitis C virus polymerase.EBI
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.EBI
Glaxosmithkline
Synthesis and biological activities of novel indole derivatives as potent and selective PPARgamma modulators.EBI
Glaxosmithkline
Tetrasubstituted pyridines as potent and selective AKT inhibitors: Reduced CYP450 and hERG inhibition of aminopyridines.EBI
Glaxosmithkline
Structure and property based design of factor Xa inhibitors: pyrrolidin-2-ones with monoaryl P4 motifs.EBI
Glaxosmithkline
2,3,5-Trisubstituted pyridines as selective AKT inhibitors-Part I: Substitution at 2-position of the core pyridine for ROCK1 selectivity.EBI
Glaxosmithkline
2,3,5-Trisubstituted pyridines as selective AKT inhibitors. Part II: Improved drug-like properties and kinase selectivity from azaindazoles.EBI
Glaxosmithkline
Improving the developability profile of pyrrolidine progesterone receptor partial agonists.EBI
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.EBI
Glaxosmithkline
The discovery of tertiary-amine LXR agonists with potent cholesterol efflux activity in macrophages.EBI
Glaxosmithkline
Discovery of orally active, pyrrolidinone-based progesterone receptor partial agonists.EBI
Glaxosmithkline
Rational design of orally-active, pyrrolidine-based progesterone receptor partial agonists.EBI
Glaxosmithkline
FXR agonist activity of conformationally constrained analogs of GW 4064.EBI
Glaxosmithkline
Identification and optimisation of a novel series of pyrimidine based cyclooxygenase-2 (COX-2) inhibitors. Utilisation of a biotransformation approach.EBI
Glaxosmithkline
Identification of [4-[4-(methylsulfonyl)phenyl]-6-(trifluoromethyl)-2-pyrimidinyl] amines and ethers as potent and selective cyclooxygenase-2 inhibitors.EBI
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.EBI
Glaxosmithkline
Discovery of novel aminothiadiazole amides as selective EP(3) receptor antagonists.EBI
Glaxosmithkline
Design and synthesis of orally bioavailable serum and glucocorticoid-regulated kinase 1 (SGK1) inhibitors.EBI
Glaxosmithkline
The identification and optimisation of novel and selective diamide neuropeptide Y Y2 receptor antagonists.EBI
Glaxosmithkline
Tetrahydrocarbazole amides with potent activity against human papillomaviruses.EBI
Glaxosmithkline
Synthesis and SAR of amino acid-derived heterocyclic progesterone receptor full and partial agonists.EBI
Glaxosmithkline
Design of novel quinazoline derivatives and related analogues as potent and selective ALK5 inhibitors.EBI
Glaxosmithkline
Dual EGFR/ErbB-2 inhibitors from novel pyrrolidinyl-acetylenic thieno[3,2-d]pyrimidines.EBI
Glaxosmithkline
Synthesis and evaluation of pyrazolo[1,5-b]pyridazines as selective cyclin dependent kinase inhibitors.EBI
Glaxosmithkline
Antagonists of the calcium receptor I. Amino alcohol-based parathyroid hormone secretagogues.EBI
Glaxosmithkline
Orally active C-6 heteroaryl- and heterocyclyl-substituted imidazo[1,2-a]pyridine acid pump antagonists (APAs).EBI
Glaxosmithkline
Substituted isoxazole analogs of farnesoid X receptor (FXR) agonist GW4064.EBI
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.EBI
Glaxosmithkline
Discovery of novel 1-azoniabicyclo[2.2.2]octane muscarinic acetylcholine receptor antagonists.EBI
Glaxosmithkline
Discovery of 5-pyrrolopyridinyl-2-thiophenecarboxamides as potent AKT kinase inhibitors.EBI
Glaxosmithkline
[2-(4-Phenyl-4-piperidinyl)ethyl]amine based CCR5 antagonists: derivatizations at the N-terminal of the piperidine ring.EBI
Glaxosmithkline
Discovery and optimization of imidazo[1,2-a]pyridine inhibitors of insulin-like growth factor-1 receptor (IGF-1R).EBI
Glaxosmithkline
Anthranilimide-based glycogen phosphorylase inhibitors for the treatment of Type 2 diabetes: 2. Optimization of serine and threonine ether amino acid residues.EBI
Glaxosmithkline
Anthranilimide-based glycogen phosphorylase inhibitors for the treatment of type 2 diabetes: 1. Identification of 1-amino-1-cycloalkyl carboxylic acid headgroups.EBI
Glaxosmithkline
Discovery of potent, selective sulfonylfuran urea endothelial lipase inhibitors.EBI
Glaxosmithkline
Discovery of GSK345931A: An EP(1) receptor antagonist with efficacy in preclinical models of inflammatory pain.EBI
Glaxosmithkline
Assessment of chemical coverage of kinome space and its implications for kinase drug discovery.EBI
Glaxosmithkline
Camphor sulfonamide derivatives as novel, potent and selective CXCR3 antagonists.EBI
Glaxosmithkline
Pyridine-3-carboxamides as novel CB(2) agonists for analgesia.EBI
Glaxosmithkline
The discovery of biaryl carboxamides as novel small molecule agonists of the motilin receptor.EBI
Glaxosmithkline
The discovery of equipotent PPARalpha/gamma dual activators.EBI
Glaxosmithkline
Imidazo[5,1-f][1,2,4]triazin-2-amines as novel inhibitors of polo-like kinase 1.EBI
Glaxosmithkline
Tetrahydro-4-quinolinamines identified as novel P2Y(1) receptor antagonists.EBI
Glaxosmithkline
The 'Ethereal' nature of TLR4 agonism and antagonism in the AGP class of lipid A mimetics.EBI
Glaxosmithkline
The identification of pyrazolo[1,5-a]pyridines as potent p38 kinase inhibitors.EBI
Glaxosmithkline
Discovery of small molecule agonists for the bombesin receptor subtype 3 (BRS-3) based on an omeprazole lead.EBI
Glaxosmithkline
Design and synthesis of 6-phenylnicotinamide derivatives as antagonists of TRPV1.EBI
Glaxosmithkline
Structure-guided design of N-phenyl tertiary amines as transrepression-selective liver X receptor modulators with anti-inflammatory activity.EBI
Glaxosmithkline
Tricyclic azepine derivatives as selective brain penetrant 5-HT6 receptor antagonists.EBI
Glaxosmithkline
Synthesis of 3-alkyl naphthalenes as novel estrogen receptor ligands.EBI
Glaxosmithkline
Aminomethylpiperazines as selective urotensin antagonists.EBI
Glaxosmithkline
Biphenyl amide p38 kinase inhibitors 3: Improvement of cellular and in vivo activity.EBI
Glaxosmithkline
Biphenyl amide p38 kinase inhibitors 4: DFG-in and DFG-out binding modes.EBI
Glaxosmithkline
Urotensin-II receptor antagonists: synthesis and SAR of N-cyclic azaalkyl benzamides.EBI
Glaxosmithkline
Amino acid anthranilamide derivatives as a new class of glycogen phosphorylase inhibitors.EBI
Glaxosmithkline
Potent and selective small-molecule human urotensin-II antagonists with improved pharmacokinetic profiles.EBI
Glaxosmithkline
Isolation, structure elucidation, and biological evaluation of 15-amido-3-demethoxy-2alpha,3alpha-methylenedioxyerythroculine, a new alkaloid from Hyperbaena valida.EBI
Glaxosmithkline
Thiol-based angiotensin-converting enzyme 2 inhibitors: P1' modifications for the exploration of the S1' subsite.EBI
Glaxosmithkline
BACE-1 inhibitors part 2: identification of hydroxy ethylamines (HEAs) with reduced peptidic character.EBI
Glaxosmithkline
Design, synthesis and evaluation of trifluoromethane sulfonamide derivatives as new potent and selective peroxisome proliferator-activated receptor alpha agonists.EBI
Glaxosmithkline
Structure and property based design of factor Xa inhibitors: pyrrolidin-2-ones with biaryl P4 motifs.EBI
Glaxosmithkline
Discovery of novel 8-azoniabicyclo[3.2.1]octane carbamates as muscarinic acetylcholine receptor antagonists.EBI
Glaxosmithkline
Synthesis of novel anilinoquinolines as c-fms inhibitors.EBI
Glaxosmithkline
1,2,4-triazol-3-yl-thiopropyl-tetrahydrobenzazepines: a series of potent and selective dopamine D(3) receptor antagonists.EBI
Glaxosmithkline
Optimization of triarylimidazoles for Tie2: influence of conformation on potency.EBI
Glaxosmithkline
Novel ATP-competitive kinesin spindle protein inhibitors.EBI
Glaxosmithkline
Studies on a series of potent, orally bioavailable, 5-HT(1) receptor ligands.EBI
Glaxosmithkline
Pyridinylimidazole inhibitors of Tie2 kinase.EBI
Glaxosmithkline
Identification and optimization of novel 1,3,4-oxadiazole EP1 receptor antagonists.EBI
Glaxosmithkline
3-Arylamino-2H-1,2,4-benzothiadiazin-5-ol 1,1-dioxides as novel and selective CXCR2 antagonists.EBI
Glaxosmithkline
The potential of transient receptor potential vanilloid type 1 channel modulators for the treatment of pain.EBI
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.EBI
Glaxosmithkline
Selective and dual action orally active inhibitors of thrombin and factor Xa.EBI
Glaxosmithkline
Sulfonamide-related conformational effects and their importance in structure-based design.EBI
Glaxosmithkline
From pyrroles to 1-oxo-2,3,4,9-tetrahydro-1H-beta-carbolines: a new class of orally bioavailable mGluR1 antagonists.EBI
Glaxosmithkline
The exploration of aza-quinolines as hematopoietic prostaglandin D synthase (H-PGDS) inhibitors with low brain exposure.EBI
Glaxosmithkline
Design of Phthalazinone Amide Histamine HEBI
Glaxosmithkline
Novel carbazole derivatives as NPY Y1 antagonists.EBI
Glaxosmithkline
6-(4-chlorophenyl)-3-substituted-thieno[3,2-d]pyrimidin-4(3H)-one-based melanin-concentrating hormone receptor 1 antagonist.EBI
Glaxosmithkline
Potent, selective, and orally efficacious antagonists of melanin-concentrating hormone receptor 1.EBI
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.EBI
Glaxosmithkline
Synthesis and structure-activity relationships of 3-phenyl-2-propenamides as inhibitors of glycogen phosphorylase a.EBI
Glaxosmithkline
N,N'-Diarylcyanoguanidines as antagonists of the CXCR2 and CXCR1 chemokine receptors.EBI
Glaxosmithkline
Aza-stilbenes as potent and selective c-RAF inhibitors.EBI
Glaxosmithkline
Identification of novel pyrazole acid antagonists for the EP1 receptor.EBI
Glaxosmithkline
Discovery of Proline-Based p300/CBP Inhibitors Using DNA-Encoded Library Technology in Combination with High-Throughput Screening.EBI
Glaxosmithkline
N-Tetrahydroquinolinyl, N-quinolinyl and N-isoquinolinyl biaryl carboxamides as antagonists of TRPV1.EBI
Glaxosmithkline
Structure-activity relationships of 1,5-biaryl pyrroles as EP1 receptor antagonists.EBI
Glaxosmithkline
Discovery of novel biaryl heterocyclic EP1 receptor antagonists.EBI
Glaxosmithkline
Alkynyl pyrimidines as dual EGFR/ErbB2 kinase inhibitors.EBI
Glaxosmithkline
An efficient, asymmetric solid-phase synthesis of benzothiadiazine-substituted tetramic acids: potent inhibitors of the hepatitis C virus RNA-dependent RNA polymerase.EBI
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.EBI
Glaxosmithkline
New benzimidazoles as thrombopoietin receptor agonists.EBI
Glaxosmithkline
Novel, potent P2-P3 pyrrolidine derivatives of ketoamide-based cathepsin K inhibitors.EBI
Glaxosmithkline
Semicarbazone-based inhibitors of cathepsin K, are they prodrugs for aldehyde inhibitors?EBI
Glaxosmithkline
Azepanone-based inhibitors of human cathepsin L.EBI
Glaxosmithkline
2-Cyano-4-fluoro-1-thiovalylpyrrolidine analogues as potent inhibitors of DPP-IV.EBI
Glaxosmithkline
Ketoheterocycle-based inhibitors of cathepsin K: a novel entry into the synthesis of peptidic ketoheterocycles.EBI
Glaxosmithkline
Discovery and in vitro evaluation of potent kinase inhibitors: Pyrido[1',2':1,5]pyrazolo[3,4-d]pyrimidines.EBI
Glaxosmithkline
P2-P3 conformationally constrained ketoamide-based inhibitors of cathepsin K.EBI
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.EBI
Glaxosmithkline
(1H-imidazo[4,5-c]pyridin-2-yl)-1,2,5-oxadiazol-3-ylamine derivatives: a novel class of potent MSK-1-inhibitors.EBI
Glaxosmithkline
Acyclic cyanamide-based inhibitors of cathepsin K.EBI
Glaxosmithkline
A structural screening approach to ketoamide-based inhibitors of cathepsin K.EBI
Glaxosmithkline
Dimeric zanamivir conjugates with various linking groups are potent, long-lasting inhibitors of influenza neuraminidase including H5N1 avian influenza.EBI
Glaxosmithkline
Novel and potent cyclic cyanamide-based cathepsin K inhibitors.EBI
Glaxosmithkline
Identification of small molecule inhibitors of the hepatitis C virus RNA-dependent RNA polymerase from a pyrrolidine combinatorial mixture.EBI
Glaxosmithkline
Ketoamide-based inhibitors of cysteine protease, cathepsin K: P3 modifications.EBI
Glaxosmithkline
Potent and selective ketoamide-based inhibitors of cysteine protease, cathepsin K.EBI
Glaxosmithkline
Identification of 2,3-diaryl-pyrazolo[1,5-b]pyridazines as potent and selective cyclooxygenase-2 inhibitors.EBI
Glaxosmithkline
Potent and selective P2-P3 ketoamide inhibitors of cathepsin K with good pharmacokinetic properties via favorable P1', P1, and/or P3 substitutions.EBI
Glaxosmithkline
Identification of 1,5-naphthyridine derivatives as a novel series of potent and selective TGF-beta type I receptor inhibitors.EBI
Glaxosmithkline
Peroxisome proliferator-activated receptor alpha/gamma dual agonists for the treatment of type 2 diabetes.EBI
Glaxosmithkline
Definition of the heterocyclic pharmacophore of bacterial methionyl tRNA synthetase inhibitors: potent antibacterially active non-quinolone analogues.EBI
Glaxosmithkline
Progesterone receptor ligand binding pocket flexibility: crystal structures of the norethindrone and mometasone furoate complexes.EBI
Glaxosmithkline
Exploration of the P2-P3 SAR of aldehyde cathepsin K inhibitors.EBI
Glaxosmithkline
Discovery of a Novel Bromodomain and Extra Terminal Domain (BET) Protein Inhibitor, I-BET282E, Suitable for Clinical Progression.EBI
Glaxosmithkline
Orally bioavailable small molecule ketoamide-based inhibitors of cathepsin K.EBI
Glaxosmithkline
Identification of Diarylurea Inhibitors of the Cardiac-Specific Kinase TNNI3K by Designing Selectivity Against VEGFR2, p38α, and B-Raf.EBI
Glaxosmithkline
Overcoming the Pregnane X Receptor Liability: Rational Design to Eliminate PXR-Mediated CYP Induction.EBI
Glaxosmithkline
Structure-based design of potent retinoid X receptor alpha agonists.EBI
Glaxosmithkline
Optimization of a Series of 2,3-Dihydrobenzofurans as Highly Potent, Second Bromodomain (BD2)-Selective, Bromo and Extra-Terminal Domain (BET) Inhibitors.EBI
Glaxosmithkline
Fragment-based Scaffold Hopping: Identification of Potent, Selective, and Highly Soluble Bromo and Extra Terminal Domain (BET) Second Bromodomain (BD2) Inhibitors.EBI
Glaxosmithkline
A knowledge-based, structural-aided discovery of a novel class of 2-phenylimidazo[1,2-a]pyridine-6-carboxamide H-PGDS inhibitors.EBI
Glaxosmithkline
Template-Hopping Approach Leads to Potent, Selective, and Highly Soluble Bromo and Extraterminal Domain (BET) Second Bromodomain (BD2) Inhibitors.EBI
Glaxosmithkline
Optimization of a Series of RIPK2 PROTACs.EBI
Glaxosmithkline
Evaluation of potent and selective small-molecule antagonists for the CXCR2 chemokine receptor.EBI
Glaxosmithkline
3-trifluoromethyl-4-nitro-5-arylpyrazoles are novel K(ATP) channel agonists.EBI
Glaxosmithkline
DNA-Encoded Library Hit Confirmation: Bridging the Gap Between On-DNA and Off-DNA Chemistry.EBI
Glaxosmithkline
Design of small molecule ketoamide-based inhibitors of cathepsin K.EBI
Glaxosmithkline
The Discovery of Conformationally Constrained Bicyclic Peptidomimetics as Potent Hepatitis C NS5A Inhibitors.EBI
Glaxosmithkline
Identification, Synthesis, and Characterization of a Major Circulating Human Metabolite of TRPV4 Antagonist GSK2798745.EBI
Glaxosmithkline
Design of potent, selective, and orally bioavailable inhibitors of cysteine protease cathepsin k.EBI
Glaxosmithkline
Discovery of a Highly Selective BET BD2 Inhibitor from a DNA-Encoded Library Technology Screening Hit.EBI
Glaxosmithkline
Exploration of the P1 SAR of aldehyde cathepsin K inhibitors.EBI
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.EBI
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.EBI
Glaxosmithkline
CCR2: characterization of the antagonist binding site from a combined receptor modeling/mutagenesis approach.EBI
Glaxosmithkline
Identification of a Series of EBI
Glaxosmithkline
Drug rings database with web interface. A tool for identifying alternative chemical rings in lead discovery programs.EBI
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.EBI
Glaxosmithkline
Novel selective small molecule agonists for peroxisome proliferator-activated receptor delta (PPARdelta)--synthesis and biological activity.EBI
Glaxosmithkline
Phenylbutyrates as potent, orally bioavailable vitronectin receptor (integrin alphavbeta3) antagonists.EBI
Glaxosmithkline
N-Phenyl-N-purin-6-yl ureas: the design and synthesis of p38alpha MAP kinase inhibitors.EBI
Glaxosmithkline
The identification of clinical candidate SB-480848: a potent inhibitor of lipoprotein-associated phospholipase A2.EBI
Glaxosmithkline
Identification of a novel series of selective 5-HT7 receptor antagonists.EBI
Glaxosmithkline
Optimisation of aryl substitution leading to potent methionyl tRNA synthetase inhibitors with excellent gram-positive antibacterial activity.EBI
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.EBI
Glaxosmithkline
GSK789: A Selective Inhibitor of the First Bromodomains (BD1) of the Bromo and Extra Terminal Domain (BET) Proteins.EBI
Glaxosmithkline
A new series of estrogen receptor modulators that display selectivity for estrogen receptor beta.EBI
Glaxosmithkline
Design and synthesis of ethyl pyrrolidine-5,5-trans-lactams as inhibitors of hepatitis C virus NS3/4A protease.EBI
Glaxosmithkline
Relating the structure, activity, and physical properties of ultrashort-acting benzodiazepine receptor agonists.EBI
Glaxosmithkline
Discovery of Orally Bioavailable Ligand Efficient Quinazolindiones as Potent and Selective Tankyrases Inhibitors.EBI
Glaxosmithkline
Synthesis and evaluation of 7-substituted-3-cyclobutylamino-4H-1,2,4-benzothiadiazine-1,1-dioxide derivatives as K(ATP) channel agonists.EBI
Glaxosmithkline
The discovery of SB-435495. A potent, orally active inhibitor of lipoprotein-associated phospholipase A(2) for evaluation in man.EBI
Glaxosmithkline
Design and Optimization of an Acyclic Amine Series of TRPV4 Antagonists by Electronic Modulation of Hydrogen Bond Interactions.EBI
Glaxosmithkline
Pyrrolidine-5,5-trans-lactams as novel mechanism-based inhibitors of human cytomegalovirus protease. Part 3: potency and plasma stability.EBI
Glaxosmithkline
Identification of potent and selective oxytocin antagonists. Part 2: further investigation of benzofuran derivatives.EBI
Glaxosmithkline
Identification of novel inhibitors of the transforming growth factor beta1 (TGF-beta1) type 1 receptor (ALK5).EBI
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.EBI
Glaxosmithkline
Potent, orally active inhibitors of lipoprotein-associated phospholipase A(2): 1-(biphenylmethylamidoalkyl)-pyrimidones.EBI
Glaxosmithkline
Synthesis and biological activity of L-tyrosine-based PPARgamma agonists with reduced molecular weight.EBI
Glaxosmithkline
Design of selective and soluble inhibitors of tumor necrosis factor-alpha converting enzyme (TACE).EBI
Glaxosmithkline
Identification of a series of PPAR gamma/delta dual agonists via solid-phase parallel synthesis.EBI
Glaxosmithkline
Hydrazinonaphthalene and azonaphthalene thrombopoietin mimics are nonpeptidyl promoters of megakaryocytopoiesis.EBI
Glaxosmithkline
Pyrimidinylimidazole inhibitors of p38: cyclic N-1 imidazole substituents enhance p38 kinase inhibition and oral activity.EBI
Glaxosmithkline
Structure-based optimisation of orally active & reversible MetAP-2 inhibitors maintaining a tight 'molecular budget'.EBI
Glaxosmithkline
Design and Synthesis of a Highly Selective and EBI
Glaxosmithkline
Inhibitors of bacterial tyrosyl tRNA synthetase: synthesis of carbocyclic analogues of the natural product SB-219383.EBI
Glaxosmithkline
Identification of a series of oxadiazole-substituted alpha-isopropoxy phenylpropanoic acids with activity on PPARalpha, PPARgamma, and PPARdelta.EBI
Glaxosmithkline
Conformationally restricted indolopiperidine derivatives as potent CCR2B receptor antagonists.EBI
Glaxosmithkline
N-hydroxyformamide peptidomimetics as TACE/matrix metalloprotease inhibitors: oral activity via P1' isobutyl substitution.EBI
Glaxosmithkline
Selective CDK6 degradation mediated by cereblon, VHL, and novel IAP-recruiting PROTACs.EBI
Glaxosmithkline
Recent advances in TRPV4 agonists and antagonists.EBI
Glaxosmithkline
1-(Arylpiperazinylamidoalkyl)-pyrimidones: orally active inhibitors of lipoprotein-associated phospholipase A(2).EBI
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.EBI
Glaxosmithkline
Identification of a potent and selective oxytocin antagonist, from screening a fully encoded differential release combinatorial chemical library.EBI
Glaxosmithkline
Identification of a subtype selective human PPARalpha agonist through parallel-array synthesis.EBI
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.EBI
Glaxosmithkline
Azepanone-based inhibitors of human and rat cathepsin K.EBI
Glaxosmithkline
Potent synthetic inhibitors of tyrosyl tRNA synthetase derived from C-pyranosyl analogues of SB-219383.EBI
Glaxosmithkline
Synthetic analogues of SB-219383. Novel C-glycosyl peptides as inhibitors of tyrosyl tRNA synthetase.EBI
Glaxosmithkline
The identification of a potent, water soluble inhibitor of lipoprotein-associated phospholipase A2.EBI
Glaxosmithkline
Discovery of piperazic acid peptide deformylase inhibitors with in vivo activity for respiratory tract and skin infections.EBI
Glaxosmithkline
Discovery and Characterization of a Class of Pyrazole Inhibitors of Bacterial Undecaprenyl Pyrophosphate Synthase.EBI
Glaxosmithkline
Development of Chemical Entities Endowed with Potent Fast-Killing Properties against EBI
Glaxosmithkline
The discovery of quinoline-3-carboxamides as hematopoietic prostaglandin D synthase (H-PGDS) inhibitors.EBI
Glaxosmithkline
Design and development of a series of borocycles as selective, covalent kallikrein 5 inhibitors.EBI
Glaxosmithkline
Design of N-Benzoxaborole Benzofuran GSK8175-Optimization of Human Pharmacokinetics Inspired by Metabolites of a Failed Clinical HCV Inhibitor.EBI
Glaxosmithkline
Discovery of a First-in-Class Receptor Interacting Protein 2 (RIP2) Kinase Specific Clinical Candidate, 2-((4-(Benzo[EBI
Glaxosmithkline
MymA Bioactivated Thioalkylbenzoxazole Prodrug Family Active against EBI
Glaxosmithkline
GSK2818713, a Novel Biphenylene Scaffold-Based Hepatitis C NS5A Replication Complex Inhibitor with Broad Genotype Coverage.EBI
Glaxosmithkline
Targeting the Regulatory Site of ER Aminopeptidase 1 Leads to the Discovery of a Natural Product Modulator of Antigen Presentation.EBI
Glaxosmithkline
DNA-Encoded Library Technology-Based Discovery, Lead Optimization, and Prodrug Strategy toward Structurally Unique Indoleamine 2,3-Dioxygenase-1 (IDO1) Inhibitors.EBI
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.EBI
Glaxosmithkline
Structure-guided design of antibacterials that allosterically inhibit DNA gyrase.EBI
Glaxosmithkline
Discovery of Isoxazole Amides as Potent and Selective SMYD3 Inhibitors.EBI
Glaxosmithkline
Discovery of a crystalline sulforaphane analog with good solid-state stability and engagement of the Nrf2 pathway in vitro and in vivo.EBI
Glaxosmithkline
3,5-Disubstituted-indole-7-carboxamides as IKKβ Inhibitors: Optimization of Oral Activity via the C3 Substituent.EBI
Glaxosmithkline
Optimization of Orally Bioavailable PI3Kδ Inhibitors and Identification of Vps34 as a Key Selectivity Target.EBI
Glaxosmithkline
Discovery of GSK3527497: A Candidate for the Inhibition of Transient Receptor Potential Vanilloid-4 (TRPV4).EBI
Glaxosmithkline
Discovery of Pyrazolocarboxamides as Potent and Selective Receptor Interacting Protein 2 (RIP2) Kinase Inhibitors.EBI
Glaxosmithkline
Discovery of GSK2798745: A Clinical Candidate for Inhibition of Transient Receptor Potential Vanilloid 4 (TRPV4).EBI
Glaxosmithkline
Identification of a RIP1 Kinase Inhibitor Clinical Candidate (GSK3145095) for the Treatment of Pancreatic Cancer.EBI
Glaxosmithkline
Discovery of a potent boronic acid derived inhibitor of the HCV RNA-dependent RNA polymerase.EBI
Glaxosmithkline
Novel hydroxyl tricyclics (e.g., GSK966587) as potent inhibitors of bacterial type IIA topoisomerases.EBI
Glaxosmithkline
Synthesis and structure-activity relationships of indazole arylsulfonamides as allosteric CC-chemokine receptor 4 (CCR4) antagonists.EBI
Glaxosmithkline
[3a,4]-Dihydropyrazolo[1,5a]pyrimidines: Novel, Potent, and Selective Phosphatidylinositol-3-kinase β Inhibitors.EBI
Glaxosmithkline
Structure-activity relationship studies of novel 3-oxazolidinedione-6-naphthyl-2-pyridinones as potent and orally bioavailable EP3 receptor antagonists.EBI
Glaxosmithkline
The naphthyridinone GSK364735 is a novel, potent human immunodeficiency virus type 1 integrase inhibitor and antiretroviral.EBI
Glaxosmithkline
Piperidine-derived gamma-secretase modulators.EBI
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.EBI
Glaxosmithkline
Pyrrolidinyl pyridone and pyrazinone analogues as potent inhibitors of prolyl oligopeptidase (POP).EBI
Glaxosmithkline
Potent achiral agonists of the growth hormone secretagogue (ghrelin) receptor. Part 2: Lead optimisation.EBI
Glaxosmithkline
Potent achiral agonists of the ghrelin (growth hormone secretagogue) receptor. Part I: Lead identification.EBI
Glaxosmithkline
Synthesis and evaluation of potent and selective beta3 adrenergic receptor agonists containing heterobiaryl carboxylic acids.EBI
Glaxosmithkline
3,4-Dihydro-2H-benzoxazinones as dual-acting 5-HT1A receptor antagonists and serotonin reuptake inhibitors.EBI
Glaxosmithkline
5-HT2C antagonists based on fused heterotricyclic templates: design, synthesis and biological evaluation.EBI
Glaxosmithkline
Discovery of potent and stable conformationally constrained analogues of the MCH R1 antagonist SB-568849.EBI
Glaxosmithkline
SAR of biphenyl carboxamide ligands of the human melanin-concentrating hormone receptor 1 (MCH R1): discovery of antagonist SB-568849.EBI
Glaxosmithkline
Bicyclic heteroarylpiperazines as selective brain penetrant 5-HT6 receptor antagonists.EBI
Glaxosmithkline
Identification of a potent and selective 5-HT1B receptor antagonist.EBI
Glaxosmithkline
Discovery of the first potent, selective 5-hydroxytryptamine1D receptor antagonist.EBI
Glaxosmithkline
3,4-Dihydro-2H-benzoxazinones are 5-HT(1A) receptor antagonists with potent 5-HT reuptake inhibitory activity.EBI
Glaxosmithkline
Discovery of a potent and selective 5-ht5A receptor antagonist by high-throughput chemistry.EBI
Glaxosmithkline
Discovery of non-steroidal mifepristone mimetics: pyrazoline-based PR antagonists.EBI
Glaxosmithkline
Identification of Quinoline-Based RIP2 Kinase Inhibitors with an Improved Therapeutic Index to the hERG Ion Channel.EBI
Glaxosmithkline
Easy-To-Synthesize Spirocyclic Compounds Possess Remarkable in Vivo Activity against Mycobacterium tuberculosis.EBI
Glaxosmithkline
Novel KEBI
Glaxosmithkline
Aiming to Miss a Moving Target: Bromo and Extra Terminal Domain (BET) Selectivity in Constrained ATAD2 Inhibitors.EBI
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 EPEBI
Glaxosmithkline
Discovery of a First-in-Class Gut-Restricted RET Kinase Inhibitor as a Clinical Candidate for the Treatment of IBS.EBI
Glaxosmithkline
Mapping the Efficiency and Physicochemical Trajectories of Successful Optimizations.EBI
Glaxosmithkline
Discovery of renin inhibitors containing a simple aspartate binding moiety that imparts reduced P450 inhibition.EBI
Glaxosmithkline
Discovery of Tetralones as Potent and Selective Inhibitors of Acyl-CoA:Diacylglycerol Acyltransferase 1.EBI
Glaxosmithkline
From PIM1 to PI3Kδ via GSK3β: Target Hopping through the Kinome.EBI
Glaxosmithkline
An orally available, brain-penetrant CAMKK2 inhibitor reduces food intake in rodent model.EBI
Glaxosmithkline
Development of a Series of Kynurenine 3-Monooxygenase Inhibitors Leading to a Clinical Candidate for the Treatment of Acute Pancreatitis.EBI
Glaxosmithkline
Identification of selective 8-(piperidin-4-yloxy)quinoline sulfone and sulfonamide histamine HEBI
Glaxosmithkline
Identification of potent, nonabsorbable agonists of the calcium-sensing receptor for GI-specific administration.EBI
Glaxosmithkline
Identification of pyrazolopyrimidine arylsulfonamides as CC-chemokine receptor 4 (CCR4) antagonists.EBI
Glaxosmithkline
A Quick Route to Multiple Highly Potent SARS-CoV-2 Main Protease InhibitorsBDB
Texas A&M University
Mixed lineage kinase inhibitors for HIV/AIDS therapiesBDB
The University of Rochester
Indazole and indole derivatives as inhibitors of retinoic acid related orphan receptor gamma (ROR gamma) for the treatment of immune-related diseasesBDB
Orca Pharmaceuticals
Bicyclic urea, thiourea, guanidine and cyanoguanidine compounds useful for the treatment of painBDB
Array Biopharma
Phosphonate derivatives and methods of use thereof in the treatment of Alzheimer's diseaseBDB
University of Kansas
Substituted bicyclic compoundsBDB
Bristol-Myers Squibb
Antibacterial piperidinyl substituted 3,4-dihydro-1H-[1,8]naphthyridinonesBDB
Janssen Ireland
Thiazole-substituted aminopyridines as spleen tyrosine kinase inhibitorsBDB
Merck Sharp & Dohme
Histone deacetylase inhibitors and compositions and methods of use thereofBDB
Chdi Foundation
Histone demethylase inhibitorsBDB
Celgene Quanticel Research
Isoquinolin-3-yl carboxamides and preparation and use thereofBDB
Samumed
Cannabinoid receptor antagonists/inverse agonists useful for treating metabolic disorders, including obesity and diabetesBDB
Jenrin Discovery
Substituted N-(pyrrolidine-3-yl)-7H-pyrrolo[2,3-D]pyrimidine-4-amine as janus kinase inhibitorBDB
Yang Ji Chemical
Disubstituted 1, 2, 4-triazine compoundBDB
Mitsubishi Tanabe Pharma
Pyrimidine compounds as JAK kinase inhibitorsBDB
Theravance Biopharma R&D Ip
Selective glycosidase inhibitors and uses thereofBDB
Alectos Therapeutics
BTK InhibitorsBDB
Merck Sharp & Dohme
Macrocyclic compounds as Trk kinase inhibitorsBDB
Array Biopharma
Substituted aza-bicyclic imidazole derivatives useful TRPM8 receptor modulatorsBDB
Janssen Pharmaceutica
Non-nucleoside reverse transcriptase inhibitorsBDB
Merck Sharp & Dohme
Aniline derivative, pharmaceutical composition containing same, and use thereofBDB
Kissei Pharmaceutical
Estra-1,3,5(10),16-tetraene-3-carboxamides for inhibition of 17.beta.-hydroxysteroid dehydrogenase (AKR1C3)BDB
Bayer Pharma Aktiengesellschaft
Azabicyclic carbamates and their use as alpha-7 nicotinic acetylcholine receptor agonistsBDB
Bayer Intellectual Property
Cyclopropanamine compound and use thereofBDB
Takeda Pharmaceutical
Compounds and methods for inhibiting JAKBDB
Astrazeneca
Sulfoximine substituted quinazolines for pharmaceutical compositionsBDB
Evotec International
Inhibitors of α-amino-β-carboxymuconic acid semialdehyde decarboxylaseBDB
Tes Pharma
Androgen receptor antagonistsBDB
University of California
Tetrahydro-benzodiazepinonesBDB
Hoffmann-La Roche
Dihydropyridone p1 as factor XIa inhibitorsBDB
Bristol-Myers Squibb
Synthesis and use of dual tyrosyl-DNA phosphodiesterase I (Tdp1)—topoisomerase I (Top1) inhibitorsBDB
Purdue Research Foundation
Disubstituted 3,4-diamino-3-cyclobutene-1,2-dione compounds for use in the treatment of chemokine-mediated diseasesBDB
Galderma Research & Development
A3 adenosine receptor allosteric modulatorsBDB
The United States of America, Represented By The Secretary, Dept. of Health and Human Services
Guanidine substituted tetrahydroisoquinoline compounds as factor XIa inhibitorsBDB
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 inhibitorsBDB
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.BDB
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.BDB
University of Maryland
Method of treatment using substituted imidazo[1,2B]pyridazine compoundsBDB
Array Biopharma
4-(4-cyano-2-thioaryl)dihydropyrimidinones and use thereofBDB
Bayer Intellectual Property
Use of 1H-indazole-3-carboxamide compounds as glycogen synthase kinase 3 beta inhibitorsBDB
Aziende Chimiche Riunite Angelini Francesco A.C.R.A.F.
Heterocyclic carboxamides as modulators of kinase activityBDB
Merck Patent
Arylaminoalcohol-substituted 2,3-dihydroimidazo[1,2-C]quinolinesBDB
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.BDB
Csir-Central Drug Research Institute
Spiro-amino-imidazo-fused heterocyclic compounds as beta-secretase modulators and methods of useBDB
Amgen
Benzotriazine inhibitors of kinasesBDB
Targegen
Neurochemical characteristics of amisulpride, an atypical dopamine D2/D3 receptor antagonist with both presynaptic and limbic selectivity.BDB
SynthÉLabo Recherche
Chemical library screens targeting an HIV-1 accessory factor/host cell kinase complex identify novel antiretroviral compounds.BDB
University of Pittsburgh
Small-molecule kinase inhibitors provide insight into Mps1 cell cycle function.BDB
Dana-Farber Cancer Institute
N-acylpolyamine inhibitors of HDM2 and HDMX binding to p53.BDB
Nih
Identification of potent and novel small-molecule inhibitors of caspase-3.BDB
Sunesis Pharmaceuticals
Cyclic HIV protease inhibitors: synthesis, conformational analysis, P2/P2' structure-activity relationship, and molecular recognition of cyclic ureas.BDB
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.BDB
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.BDB
University of Auckland
Identification of tricyclic analogs related to ellagic acid as potent/selective tyrosine protein kinase inhibitors.BDB
Pfizer
Inhibition of clinically relevant mutant variants of HIV-1 by quinazolinone non-nucleoside reverse transcriptase inhibitors.BDB
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.BDB
Eli Lilly
2-Amino-6-arylsulfonylbenzonitriles as non-nucleoside reverse transcriptase inhibitors of HIV-1.BDB
Glaxosmithkline
Nonpeptide cyclic cyanoguanidines as HIV-1 protease inhibitors: synthesis, structure-activity relationships, and X-ray crystal structure studies.BDB
Dupont Pharmaceuticals
Stereoisomers of cyclic urea HIV-1 protease inhibitors: synthesis and binding affinities.BDB
Dupont Pharmaceuticals
Novel non-nucleoside inhibitors of HIV-1 reverse transcriptase. 1. Tricyclic pyridobenzo- and dipyridodiazepinones.BDB
Boehringer Ingelheim Pharmaceuticals
Structure-based design of nonpeptidic HIV protease inhibitors: the sulfonamide-substituted cyclooctylpyramones.BDB
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.BDB
Boehringer Mannheim
Synthesis and evaluation of 2-pyridinone derivatives as HIV-1-specific reverse transcriptase inhibitors. 2. Analogues of 3-aminopyridin-2(1H)-one.BDB
Merck Research Laboratories
Inhibitors of HIV-1 proteinase containing 2-heterosubstituted 4-amino-3-hydroxy-5-phenylpentanoic acid: synthesis, enzyme inhibition, and antiviral activity.BDB
Sandoz Forschungsinstitut Ges.M.B.H.
A novel, picomolar inhibitor of human immunodeficiency virus type 1 protease.BDB
Abbott Laboratories
The vnd/NK-2 homeodomain: thermodynamics of reversible unfolding and DNA binding for wild-type and with residue replacements H52R and H52R/T56W in helix III.BDB
National Institutes of Health