469 articles for thisTarget
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Discovery of triazole aminopyrazines as a highly potent and selective series of PI3Kd inhibitors.
Astrazeneca
Discovery of indazole ethers as novel, potent, non-steroidal glucocorticoid receptor modulators.
Astrazeneca
Optimization of Highly Kinase Selective Bis-anilino Pyrimidine PAK1 Inhibitors.
Astrazeneca
Drug discovery strategies to outer membrane targets in Gram-negative pathogens.
Astrazeneca
Discovery of a Potent, Selective, Orally Bioavailable, and Efficacious Novel 2-(Pyrazol-4-ylamino)-pyrimidine Inhibitor of the Insulin-like Growth Factor-1 Receptor (IGF-1R).
Astrazeneca
Utilization of Structure-Based Design to Identify Novel, Irreversible Inhibitors of EGFR Harboring the T790M Mutation.
Astrazeneca
Potent and Selective CK2 Kinase Inhibitors with Effects on Wnt Pathway Signaling in Vivo.
Astrazeneca
Selective inhibitors of Bcl-2 and Bcl-xL: Balancing antitumor activity with on-target toxicity.
Astrazeneca
Isoindolinone compounds active as Kv1.5 blockers identified using a multicomponent reaction approach.
Astrazeneca
Discovery of (3-(4-(2-Oxa-6-azaspiro[3.3]heptan-6-ylmethyl)phenoxy)azetidin-1-yl)(5-(4-methoxyphenyl)-1,3,4-oxadiazol-2-yl)methanone (AZD1979), a Melanin Concentrating Hormone Receptor 1 (MCHr1) Antagonist with Favorable Physicochemical Properties.
Astrazeneca
Tetrahydroisoquinoline Phenols: Selective Estrogen Receptor Downregulator Antagonists with Oral Bioavailability in Rat.
Astrazeneca
Negishi cross-coupling enabled synthesis of novel NAD(+)-dependent DNA ligase inhibitors and SAR development.
Astrazeneca
Optimization of a Novel Binding Motif to (E)-3-(3,5-Difluoro-4-((1R,3R)-2-(2-fluoro-2-methylpropyl)-3-methyl-2,3,4,9-tetrahydro-1H-pyrido[3,4-b]indol-1-yl)phenyl)acrylic Acid (AZD9496), a Potent and Orally Bioavailable Selective Estrogen Receptor Downregulator and Antagonist.
Astrazeneca
Discovery and Evaluation of Clinical Candidate AZD3759, a Potent, Oral Active, Central Nervous System-Penetrant, Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitor.
Astrazeneca
Identification and Optimization of Benzimidazole Sulfonamides as Orally Bioavailable Sphingosine 1-Phosphate Receptor 1 Antagonists with in Vivo Activity.
Astrazeneca
Left-Hand Side Exploration of Novel Bacterial Topoisomerase Inhibitors to Improve Selectivity against hERG Binding.
Astrazeneca
Discovery of potent, selective small molecule inhibitors ofa-subtype of type III phosphatidylinositol-4-kinase (PI4KIIIa).
Astrazeneca
Circumventing seizure activity in a series of G protein coupled receptor 119 (GPR119) agonists.
Astrazeneca
Novel DNA gyrase inhibiting spiropyrimidinetriones with a benzisoxazole scaffold: SAR and in vivo characterization.
Astrazeneca
Rational design of inhibitors of the bacterial cell wall synthetic enzyme GlmU using virtual screening and lead-hopping.
Astrazeneca
N-aryl-2-aminobenzimidazoles: novel, efficacious, antimalarial lead compounds.
Astrazeneca
Design of selective PI3Ka inhibitors starting from a promiscuous pan kinase scaffold.
Astrazeneca
Amide hydrolysis of a novel chemical series of microsomal prostaglandin E synthase-1 inhibitors induces kidney toxicity in the rat.
Astrazeneca
In vitro inhibition of the bile salt export pump correlates with risk of cholestatic drug-induced liver injury in humans.
Astrazeneca
Investigation of (E)-3-[4-(2-Oxo-3-aryl-chromen-4-yl)oxyphenyl]acrylic Acids as Oral Selective Estrogen Receptor Down-Regulators.
Astrazeneca
Identification of indole inhibitors of human hematopoietic prostaglandin D2 synthase (hH-PGDS).
Astrazeneca
Structure-Based Design of Potent and Selective Inhibitors of the Metabolic Kinase PFKFB3.
Astrazeneca
Discovery and optimization of a novel series of Dyrk1B kinase inhibitors to explore a MEK resistance hypothesis.
Astrazeneca
Discovery of AZD3147: a potent, selective dual inhibitor of mTORC1 and mTORC2.
Astrazeneca
Discovery of (R)-8-(1-(3,5-difluorophenylamino)ethyl)-N,N-dimethyl-2-morpholino-4-oxo-4H-chromene-6-carboxamide (AZD8186): a potent and selective inhibitor of PI3Kß and PI3Kd for the treatment of PTEN-deficient cancers.
Astrazeneca
Discovery of heterocyclic sulfonamides as sphingosine 1-phosphate receptor 1 (S1P1) antagonists.
Astrazeneca
Discovery and characterization of MAPK-activated protein kinase-2 prevention of activation inhibitors.
Astrazeneca
Benzimidazoles: novel mycobacterial gyrase inhibitors from scaffold morphing.
Astrazeneca
Discovery of 9-(1-phenoxyethyl)-2-morpholino-4-oxo-pyrido[1,2-a]pyrimidine-7-carboxamides as oral PI3Kß inhibitors, useful as antiplatelet agents.
Astrazeneca
Discovery of 9-(1-anilinoethyl)-2-morpholino-4-oxo-pyrido[1,2-a]pyrimidine-7-carboxamides as PI3Kß/d inhibitors for the treatment of PTEN-deficient tumours.
Astrazeneca
Diarylthiazole: an antimycobacterial scaffold potentially targeting PrrB-PrrA two-component system.
Astrazeneca
Identification, optimization, and pharmacology of acylurea GHS-R1a inverse agonists.
Astrazeneca
Optimization of pyrrolamide topoisomerase II inhibitors toward identification of an antibacterial clinical candidate (AZD5099).
Astrazeneca
GPR103 antagonists demonstrating anorexigenic activity in vivo: design and development of pyrrolo[2,3-c]pyridines that mimic the C-terminal Arg-Phe motif of QRFP26.
Astrazeneca
Discovery of a series of aryl-N-(3-(alkylamino)-5-(trifluoromethyl)phenyl)benzamides as TRPA1 antagonists.
Astrazeneca
Discovery of potent KIFC1 inhibitors using a method of integrated high-throughput synthesis and screening.
Astrazeneca
Discovery of a novel pyrazole series of group X secreted phospholipase A2 inhibitor (sPLA2X) via fragment based virtual screening.
Astrazeneca
Discovery of a potent and selective EGFR inhibitor (AZD9291) of both sensitizing and T790M resistance mutations that spares the wild type form of the receptor.
Astrazeneca
2-Phenylindole and Arylsulphonamide: Novel Scaffolds Bactericidal against Mycobacterium tuberculosis.
Astrazeneca
Optimization of physicochemical properties and safety profile of novel bacterial topoisomerase type II inhibitors (NBTIs) with activity against Pseudomonas aeruginosa.
Astrazeneca
Discovery of a 4-aryloxy-1H-pyrrolo[3,2-c]pyridine and a 1-aryloxyisoquinoline series of TRPA1 antagonists.
Astrazeneca
Discovery of the Fibrinolysis Inhibitor AZD6564, Acting via Interference of a Protein-Protein Interaction.
Astrazeneca
4-aminoquinolone piperidine amides: noncovalent inhibitors of DprE1 with long residence time and potent antimycobacterial activity.
Astrazeneca
Optimization of ketone-based P2Y(12) receptor antagonists as antithrombotic agents: pharmacodynamics and receptor kinetics considerations.
Astrazeneca
Novel N-linked aminopiperidine-based gyrase inhibitors with improved hERG and in vivo efficacy against Mycobacterium tuberculosis.
Astrazeneca
Efficacious inhaled PDE4 inhibitors with low emetic potential and long duration of action for the treatment of COPD.
Astrazeneca
Medicinal chemistry of inhibitors of 11ß-hydroxysteroid dehydrogenase type 1 (11ß-HSD1).
Astrazeneca
The discovery of potent and selective non-steroidal glucocorticoid receptor modulators, suitable for inhalation.
Astrazeneca
Cathepsin C inhibitors: property optimization and identification of a clinical candidate.
Astrazeneca
Discovery of AZD3199, An Inhaled Ultralong Actingβ2 Receptor Agonist with Rapid Onset of Action.
Astrazeneca
Design and synthesis of conformationally restricted inhibitors of active thrombin activatable fibrinolysis inhibitor (TAFIa).
Astrazeneca
Structure-based design and synthesis of tricyclic IAP (Inhibitors of Apoptosis Proteins) inhibitors.
Astrazeneca
HTS followed by NMR based counterscreening. Discovery and optimization of pyrimidones as reversible and competitive inhibitors of xanthine oxidase.
Astrazeneca
Optimization of brain penetrant 11ß-hydroxysteroid dehydrogenase type I inhibitors and in vivo testing in diet-induced obese mice.
Astrazeneca
Design, synthesis, and SAR of a series of activated protein C (APC) inhibitors with selectivity against thrombin for the treatment of haemophilia.
Astrazeneca
Thiazolopyridone ureas as DNA gyrase B inhibitors: optimization of antitubercular activity and efficacy.
Astrazeneca
Stapled Vasoactive Intestinal Peptide (VIP) Derivatives Improve VPAC2 Agonism and Glucose-Dependent Insulin Secretion.
Astrazeneca
Structure activity relationships of fused bicyclic and urea derivatives of spirocyclic compounds as potent CCR1 antagonists.
Astrazeneca
Identification through structure-based methods of a bacterial NAD(+)-dependent DNA ligase inhibitor that avoids known resistance mutations.
Astrazeneca
Lead optimization of ethyl 6-aminonicotinate acyl sulfonamides as antagonists of the P2Y12 receptor. separation of the antithrombotic effect and bleeding for candidate drug AZD1283.
Astrazeneca
Structure and Property Based Design of Pyrazolo[1,5-a]pyrimidine Inhibitors of CK2 Kinase with Activity in Vivo.
Astrazeneca
Discovery of AZD8931, an Equipotent, Reversible Inhibitor of Signaling by EGFR, HER2, and HER3 Receptors.
Astrazeneca
Design, synthesis and structure-activity relationships of zwitterionic spirocyclic compounds as potent CCR1 antagonists.
Astrazeneca
Synthesis, structure-property relationships and pharmacokinetic evaluation of ethyl 6-aminonicotinate sulfonylureas as antagonists of the P2Y12 receptor.
Astrazeneca
Design, synthesis and structure activity relationships of spirocyclic compounds as potent CCR1 antagonists.
Astrazeneca
Conformational restriction in a series of GPR119 agonists: differences in pharmacology between mouse and human.
Astrazeneca
Discovery of novel Jak2-Stat pathway inhibitors with extended residence time on target.
Astrazeneca
Substituted 7-amino-5-thio-thiazolo[4,5-d]pyrimidines as potent and selective antagonists of the fractalkine receptor (CX3CR1).
Astrazeneca
Discovery of AZD3514, a small-molecule androgen receptor downregulator for treatment of advanced prostate cancer.
Astrazeneca
Development of a plate-based optical biosensor fragment screening methodology to identify phosphodiesterase 10A inhibitors.
Astrazeneca
Discovery and optimization of a novel series of potent mutant B-Raf(V600E) selective kinase inhibitors.
Astrazeneca
Optimization of potent and selective dual mTORC1 and mTORC2 inhibitors: the discovery of AZD8055 and AZD2014.
Astrazeneca
Sulfonylpiperidines as novel, antibacterial inhibitors of Gram-positive thymidylate kinase (TMK).
Astrazeneca
Discovery of N-[[1-[2-(tert-butylcarbamoylamino)ethyl]-4-(hydroxymethyl)-4-piperidyl]methyl]-3,5-dichloro-benzamide as a selective T-type calcium channel (Cav3.2) inhibitor.
Astrazeneca
Potent fibrinolysis inhibitor discovered by shape and electrostatic complementarity to the drug tranexamic acid.
Astrazeneca
Discovery of 4-amino-N-[(1S)-1-(4-chlorophenyl)-3-hydroxypropyl]-1-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)piperidine-4-carboxamide (AZD5363), an orally bioavailable, potent inhibitor of Akt kinases.
Astrazeneca
Discovery of 4-{4-[(3R)-3-Methylmorpholin-4-yl]-6-[1-(methylsulfonyl)cyclopropyl]pyrimidin-2-yl}-1H-indole (AZ20): a potent and selective inhibitor of ATR protein kinase with monotherapy in vivo antitumor activity.
Astrazeneca
Synthesis and SAR of aminothiazole fused benzazepines as selective dopamine D2 partial agonists.
Astrazeneca
Azepines and piperidines with dual norepinephrine dopamine uptake inhibition and antidepressant activity.
Astrazeneca
Systematic exploration of dual-acting modulators from a combined medicinal chemistry and biology perspective.
Astrazeneca
Synthesis and evaluation of diphenylphosphinic amides and diphenylphosphine oxides as inhibitors of Kv1.5.
Astrazeneca
Discovery of agonists of cannabinoid receptor 1 with restricted central nervous system penetration aimed for treatment of gastroesophageal reflux disease.
Astrazeneca
From ATP to AZD6140: the discovery of an orally active reversible P2Y12 receptor antagonist for the prevention of thrombosis.
Astrazeneca
Structure-driven HtL: design and synthesis of novel aminoindazole inhibitors of c-Jun N-terminal kinase activity.
Astrazeneca
Statistical molecular design, parallel synthesis, and biological evaluation of a library of thrombin inhibitors.
Astrazeneca
Design of inhibitors of Helicobacter pylori glutamate racemase as selective antibacterial agents: incorporation of imidazoles onto a core pyrazolopyrimidinedione scaffold to improve bioavailabilty.
Astrazeneca
Protein-ligand crystal structures can guide the design of selective inhibitors of the FGFR tyrosine kinase.
Astrazeneca
Use of small-molecule crystal structures to address solubility in a novel series of G protein coupled receptor 119 agonists: optimization of a lead and in vivo evaluation.
Astrazeneca
Aminoimidazoles as BACE-1 inhibitors: the challenge to achieve in vivo brain efficacy.
Astrazeneca
From libraries to candidate: the discovery of new ultra long-acting dibasicß2-adrenoceptor agonists.
Astrazeneca
Effect of lipophilicity modulation on inhibition of human rhinovirus capsid binders.
Astrazeneca
The discovery of benzanilides as c-Met receptor tyrosine kinase inhibitors by a directed screening approach.
Astrazeneca
Design-driven LO: the discovery of new ultra long acting dibasicß2-adrenoceptor agonists.
Astrazeneca
Design driven HtL: The discovery and synthesis of new high efficacyß2-agonists.
Astrazeneca
Phenyl isoxazole voltage-gated sodium channel blockers: structure and activity relationship.
Astrazeneca
Development and SAR of functionally selective allosteric modulators of GABAA receptors.
Astrazeneca
Increasing selectivity of CC chemokine receptor 8 antagonists by engineering nondesolvation related interactions with the intended and off-target binding sites.
Astrazeneca
Antagonists of the P2X(7) receptor. From lead identification to drug development.
Astrazeneca
Overcoming undesirable HERG potency of chemokine receptor antagonists using baseline lipophilicity relationships.
Astrazeneca
The discovery of a novel series of glucokinase activators based on a pyrazolopyrimidine scaffold.
Astrazeneca
Discovery and evolution of phenoxypiperidine hydroxyamide dual CCR3/H1 antagonists. Part I.
Astrazeneca
Discovery and evolution of phenoxypiperidine hydroxyamide dual CCR3/H1 antagonists. Part II: optimising in vivo clearance.
Astrazeneca
Free-Wilson and structural approaches to co-optimizing human and rodent isoform potency for 11ß-hydroxysteroid dehydrogenase type 1 (11ß-HSD1) inhibitors.
Astrazeneca
Design and optimization of pyrazinecarboxamide-based inhibitors of diacylglycerol acyltransferase 1 (DGAT1) leading to a clinical candidate dimethylpyrazinecarboxamide phenylcyclohexylacetic acid (AZD7687).
Astrazeneca
Novel acidic 11ß-hydroxysteroid dehydrogenase type 1 (11ß-HSD1) inhibitor with reduced acyl glucuronide liability: the discovery of 4-[4-(2-adamantylcarbamoyl)-5-tert-butyl-pyrazol-1-yl]benzoic acid (AZD8329).
Astrazeneca
Discovery of selective and potent inhibitors of gram-positive bacterial thymidylate kinase (TMK).
Astrazeneca
New aminoimidazoles asß-secretase (BACE-1) inhibitors showing amyloid-ß (Aß) lowering in brain.
Astrazeneca
Design and synthesis ofß-site amyloid precursor protein cleaving enzyme (BACE1) inhibitors with in vivo brain reduction ofß-amyloid peptides.
Astrazeneca
Modulation of DNA repair by pharmacological inhibitors of the PIKK protein kinase family.
Astrazeneca
Discovery of novel potent and highly selective glycogen synthase kinase-3ß (GSK3ß) inhibitors for Alzheimer's disease: design, synthesis, and characterization of pyrazines.
Astrazeneca
Pharmacokinetic benefits of 3,4-dimethoxy substitution of a phenyl ring and design of isosteres yielding orally available cathepsin K inhibitors.
Astrazeneca
Discovery of novel pyrrolopyridazine scaffolds as transient receptor potential vanilloid (TRPV1) antagonists.
Astrazeneca
Discovery and characterization of AZD9272 and AZD6538-Two novel mGluR5 negative allosteric modulators selected for clinical development.
Astrazeneca
Discovery of phosphoinositide 3-kinases (PI3K) p110ß isoform inhibitor 4-[2-hydroxyethyl(1-naphthylmethyl)amino]-6-[(2S)-2-methylmorpholin-4-yl]-1H-pyrimidin-2-one, an effective antithrombotic agent without associated bleeding and insulin resistance.
Astrazeneca
Novel N-linked aminopiperidine inhibitors of bacterial topoisomerase type II with reduced pK(a): antibacterial agents with an improved safety profile.
Astrazeneca
3-Oxoisoindoline-1-carboxamides: potent, state-dependent blockers of voltage-gated sodium channel Na(V)1.7 with efficacy in rat pain models.
Astrazeneca
(1R,2R)-N-(1-cyanocyclopropyl)-2-(6-methoxy-1,3,4,5-tetrahydropyrido[4,3-b]indole-2-carbonyl)cyclohexanecarboxamide (AZD4996): a potent and highly selective cathepsin K inhibitor for the treatment of osteoarthritis.
Astrazeneca
Scaffold-hopping with zwitterionic CCR3 antagonists: identification and optimisation of a series with good potency and pharmacokinetics leading to the discovery of AZ12436092.
Astrazeneca
Optimisation of pharmacokinetic properties in a neutral series of 11ß-HSD1 inhibitors.
Astrazeneca
Discovery of 4-morpholino-pyrimidin-6-one and 4-morpholino-pyrimidin-2-one-containing Phosphoinositide 3-kinase (PI3K) p110ß isoform inhibitors through structure-based fragment optimisation.
Astrazeneca
Discovery of a potent, selective, and orally bioavailable acidic 11ß-hydroxysteroid dehydrogenase type 1 (11ß-HSD1) inhibitor: discovery of 2-[(3S)-1-[5-(cyclohexylcarbamoyl)-6-propylsulfanylpyridin-2-yl]-3-piperidyl]acetic acid (AZD4017).
Astrazeneca
Phenethyl nicotinamides, a novel class of Na(V)1.7 channel blockers: structure and activity relationship.
Astrazeneca
Synthesis and structure-activity relationship of 4-(1,3-benzothiazol-2-yl)-thiophene-2-sulfonamides as cyclin-dependent kinase 5 (cdk5)/p25 inhibitors.
Astrazeneca
Isosteric replacements for benzothiazoles and optimisation to potent Cathepsin K inhibitors free from hERG channel inhibition.
Astrazeneca
Structure and activity relationship in the (S)-N-chroman-3-ylcarboxamide series of voltage-gated sodium channel blockers.
Astrazeneca
Discovery of checkpoint kinase inhibitor (S)-5-(3-fluorophenyl)-N-(piperidin-3-yl)-3-ureidothiophene-2-carboxamide (AZD7762) by structure-based design and optimization of thiophenecarboxamide ureas.
Astrazeneca
Discovery of novel hedgehog antagonists from cell-based screening: Isosteric modification of p38 bisamides as potent inhibitors of SMO.
Astrazeneca
Discovery of a novel azaindole class of antibacterial agents targeting the ATPase domains of DNA gyrase and Topoisomerase IV.
Astrazeneca
Discovery of novel benzylidene-1,3-thiazolidine-2,4-diones as potent and selective inhibitors of the PIM-1, PIM-2, and PIM-3 protein kinases.
Astrazeneca
Discovery of benzothiazole guanidines as novel inhibitors of thrombin and trypsin IV.
Astrazeneca
The design and synthesis of novel, potent and orally bioavailable N-aryl piperazine-1-carboxamide CCR2 antagonists with very high hERG selectivity.
Astrazeneca
Identification, optimisation and in vivo evaluation of oxadiazole DGAT-1 inhibitors for the treatment of obesity and diabetes.
Astrazeneca
The discovery of N-cyclopropyl-4-methyl-3-[6-(4-methylpiperazin-1-yl)-4-oxoquinazolin-3(4H)-yl]benzamide (AZD6703), a clinical p38a MAP kinase inhibitor for the treatment of inflammatory diseases.
Astrazeneca
Sulfonyl-morpholino-pyrimidines: SAR and development of a novel class of selective mTOR kinase inhibitor.
Astrazeneca
N-Methyl-3-(tetrahydro-2H-pyran-4-yl)-2,3,4,9-tetrahydro-1H-carbazole-6-carboxamides as a novel class of cannabinoid receptors agonists with low CNS penetration.
Astrazeneca
Structure-activity relationship of a series of non peptidic RGD integrin antagonists targetinga5ß1: part 1.
Astrazeneca
Structure-activity relationship of a series of non peptidic RGD integrin antagonists targetinga5ß1: part 2.
Astrazeneca
Discovery of new quinoline ether inhibitors with high affinity and selectivity for PDGFR tyrosine kinases.
Astrazeneca
Side chain flexibilities in the human ether-a-go-go related gene potassium channel (hERG) together with matched-pair binding studies suggest a new binding mode for channel blockers.
Astrazeneca
Novel 3-alkoxy-1H-pyrazolo[3,4-d]pyrimidines as EGFR and erbB2 receptor tyrosine kinase inhibitors.
Astrazeneca
A new series of neutral 5-substituted 4-anilinoquinazolines as potent, orally active inhibitors of erbB2 receptor tyrosine kinase.
Astrazeneca
Discovery of novel and potent thiazoloquinazolines as selective Aurora A and B kinase inhibitors.
Astrazeneca
The 5-HT3 antagonist tropisetron (ICS 205-930) is a potent and selective alpha7 nicotinic receptor partial agonist.
Astrazeneca
Studies leading to the identification of ZD1839 (IRESSA): an orally active, selective epidermal growth factor receptor tyrosine kinase inhibitor targeted to the treatment of cancer.
Astrazeneca
Discovery of 4-hydroxy-1,6-naphthyridine-3-carbonitrile derivatives as novel PDE10A inhibitors.
Astrazeneca
Balancing hERG affinity and absorption in the discovery of AZD5672, an orally active CCR5 antagonist for the treatment of rheumatoid arthritis.
Astrazeneca
Lead optimisation of selective non-zinc binding inhibitors of MMP13. Part 2.
Astrazeneca
Discovery of AZD2932, a new Quinazoline Ether Inhibitor with high affinity for VEGFR-2 and PDGFR tyrosine kinases.
Astrazeneca
Discovery of (+)-N-(3-aminopropyl)-N-[1-(5-benzyl-3-methyl-4-oxo-[1,2]thiazolo[5,4-d]pyrimidin-6-yl)-2-methylpropyl]-4-methylbenzamide (AZD4877), a kinesin spindle protein inhibitor and potential anticancer agent.
Astrazeneca
Discovery of novel imidazo[1,2-a]pyridines as inhibitors of the insulin-like growth factor-1 receptor tyrosine kinase.
Astrazeneca
Novel imidazo[1,2-a]pyridine based inhibitors of the IGF-1 receptor tyrosine kinase: optimization of the aniline.
Astrazeneca
Orally active achiral N-hydroxyformamide inhibitors of ADAM-TS4 (aggrecanase-1) and ADAM-TS5 (aggrecanase-2) for the treatment of osteoarthritis.
Astrazeneca
Inhibitors of the tyrosine kinase EphB4. Part 4: Discovery and optimization of a benzylic alcohol series.
Astrazeneca
The design and synthesis of novel N-hydroxyformamide inhibitors of ADAM-TS4 for the treatment of osteoarthritis.
Astrazeneca
Inhibitors of the tyrosine kinase EphB4. Part 3: identification of non-benzodioxole-based kinase inhibitors.
Astrazeneca
A statistical analysis of in vitro human microsomal metabolic stability of small phenyl group substituents, leading to improved design sets for parallel SAR exploration of a chemical series.
Astrazeneca
Discovery of a series of indan carboxylic acid glycogen phosphorylase inhibitors.
Astrazeneca
Novel thienopyrimidine and thiazolopyrimidine kinase inhibitors with activity against Tie-2 in vitro and in vivo.
Astrazeneca
Inhibitors of the tyrosine kinase EphB4. Part 2: structure-based discovery and optimisation of 3,5-bis substituted anilinopyrimidines.
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Imidazoles: SAR and development of a potent class of cyclin-dependent kinase inhibitors.
Astrazeneca
Discovery of imidazole vinyl pyrimidines as a novel class of kinase inhibitors which inhibit Tie-2 and are orally bioavailable.
Astrazeneca
Neutral 5-substituted 4-indazolylaminoquinazolines as potent, orally active inhibitors of erbB2 receptor tyrosine kinase.
Astrazeneca
Synthesis and structure-activity relationships of thieno[2,3-b]pyrroles as antagonists of the GnRH receptor.
Astrazeneca
Neutral 5-substituted 4-anilinoquinazolines as potent, orally active inhibitors of erbB2 receptor tyrosine kinase.
Astrazeneca
Discovery of a Novel Benzodiazepine Series of Cbl-b Inhibitors for the Enhancement of Antitumor Immunity.
Astrazeneca
Discovery and characterisation of quinazolines and 8-Azaquinazolines as NLRP3 agonists with oral bioavailability in mice.
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Screening Ultra-Large Encoded Compound Libraries Leads to Novel Protein-Ligand Interactions and High Selectivity.
Astrazeneca
Selective and Bioavailable HDAC6 2-(Difluoromethyl)-1,3,4-oxadiazole Substrate Inhibitors and Modeling of Their Bioactivation Mechanism.
Astrazeneca
Discovery of the Potent and Selective Inhaled Janus Kinase 1 Inhibitor AZD4604 and Its Preclinical Characterization.
Astrazeneca
Optimization of a series of novel, potent and selective Macrocyclic SYK inhibitors.
Astrazeneca
Discovery and Optimization of the First ATP Competitive Type-III c-MET Inhibitor.
Astrazeneca
The Role of Allylic Strain for Conformational Control in Medicinal Chemistry.
Astrazeneca
E3 Ligases Meet Their Match: Fragment-Based Approaches to Discover New E3 Ligands and to Unravel E3 Biology.
Astrazeneca
Discovery of AZD4747, a Potent and Selective Inhibitor of Mutant GTPase KRAS
Astrazeneca
Discovery of Clinical Candidate AZD0095, a Selective Inhibitor of Monocarboxylate Transporter 4 (MCT4) for Oncology.
Astrazeneca
Structure Based Design of Non-Natural Peptidic Macrocyclic Mcl-1 Inhibitors.
Astrazeneca
Improving metabolic stability and removing aldehyde oxidase liability in a 5-azaquinazoline series of IRAK4 inhibitors.
Astrazeneca
Novel thienopyrrole glycogen phosphorylase inhibitors: synthesis, in vitro SAR and crystallographic studies.
Astrazeneca
Inhibitors of epidermal growth factor receptor tyrosine kinase: optimisation of potency and in vivo pharmacokinetics.
Astrazeneca
Discovery of AZD4625, a Covalent Allosteric Inhibitor of the Mutant GTPase KRAS
Astrazeneca
Modulators of the human CCR5 receptor. Part 3: SAR of substituted 1-[3-(4-methanesulfonylphenyl)-3-phenylpropyl]-piperidinyl phenylacetamides.
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Novel 4-anilinoquinazolines with C-6 carbon-linked side chains: synthesis and structure-activity relationship of a series of potent, orally active, EGF receptor tyrosine kinase inhibitors.
Astrazeneca
Discovery of 5-{4-[(7-Ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl]piperazin-1-yl}-
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Inhibitors of epidermal growth factor receptor tyrosine kinase: Novel C-5 substituted anilinoquinazolines designed to target the ribose pocket.
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Identification and optimization of a novel series of selective PIP5K inhibitors.
Astrazeneca
Discovery and optimization of cyclohexane-1,4-diamines as allosteric MALT1 inhibitors.
Astrazeneca
New heterocyclic analogues of 4-(2-chloro-5-methoxyanilino)quinazolines as potent and selective c-Src kinase inhibitors.
Astrazeneca
Modulators of the human CCR5 receptor. Part 2: SAR of substituted 1-(3,3-diphenylpropyl)-piperidinyl phenylacetamides.
Astrazeneca
5-Substituted 4-anilinoquinazolines as potent, selective and orally active inhibitors of erbB2 receptor tyrosine kinase.
Astrazeneca
Discovery of AZD4831, a Mechanism-Based Irreversible Inhibitor of Myeloperoxidase, As a Potential Treatment for Heart Failure with Preserved Ejection Fraction.
Astrazeneca
Identification and optimisation of a pyrimidopyridone series of IRAK4 inhibitors.
Astrazeneca
Discovery, synthesis and biological evaluation of novel glucokinase activators.
Astrazeneca
Discovery of a Series of 7-Azaindoles as Potent and Highly Selective CDK9 Inhibitors for Transient Target Engagement.
Astrazeneca
Modulators of the human CCR5 receptor. Part 1: Discovery and initial SAR of 1-(3,3-diphenylpropyl)-piperidinyl amides and ureas.
Astrazeneca
Discovery by Virtual Screening of an Inhibitor of CDK5-Mediated PPARγ Phosphorylation.
Astrazeneca
Novel, potent and selective anilinoquinazoline and anilinopyrimidine inhibitors of p38 MAP kinase.
Astrazeneca
A novel series of p38 MAP kinase inhibitors for the potential treatment of rheumatoid arthritis.
Astrazeneca
Discovery of a Potent and Selective ATAD2 Bromodomain Inhibitor with Antiproliferative Activity in Breast Cancer Models.
Astrazeneca
Potent and Selective Inhibitors of the Epidermal Growth Factor Receptor to Overcome C797S-Mediated Resistance.
Astrazeneca
Diverse, Potent, and Efficacious Inhibitors That Target the EED Subunit of the Polycomb Repressive Complex 2 Methyltransferase.
Astrazeneca
AZD0284, a Potent, Selective, and Orally Bioavailable Inverse Agonist of Retinoic Acid Receptor-Related Orphan Receptor C2.
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N-Benzylindole-2-carboxylic acids: potent functional antagonists of the CCR2b chemokine receptor.
Astrazeneca
Free energy perturbation in the design of EED ligands as inhibitors of polycomb repressive complex 2 (PRC2) methyltransferase.
Astrazeneca
Generating Selective Leads for Mer Kinase Inhibitors-Example of a Comprehensive Lead-Generation Strategy.
Astrazeneca
Addition of Fluorine and a Late-Stage Functionalization (LSF) of the Oral SERD AZD9833.
Astrazeneca
Discovery of Proteolysis-Targeting Chimera Molecules that Selectively Degrade the IRAK3 Pseudokinase.
Astrazeneca
The discovery and evaluation of 3-amino-2(1H)-pyrazinones as a novel series of selective p38α MAP kinase inhibitors.
Astrazeneca
Discovery and optimization of a series of carbazole ureas as NPY5 antagonists for the treatment of obesity.
Astrazeneca
Design, Synthesis, and Biological Activity of Substrate Competitive SMYD2 Inhibitors.
Astrazeneca
Discovery of AZD4573, a Potent and Selective Inhibitor of CDK9 That Enables Short Duration of Target Engagement for the Treatment of Hematological Malignancies.
Astrazeneca
Discovery of AZD9833, a Potent and Orally Bioavailable Selective Estrogen Receptor Degrader and Antagonist.
Astrazeneca
Optimization of a series of potent, selective and orally bioavailable SYK inhibitors.
Astrazeneca
Potent and Selective Inhibitors of MTH1 Probe Its Role in Cancer Cell Survival.
Astrazeneca
Identification of a novel series of azabenzimidazole-derived inhibitors of spleen tyrosine kinase.
Astrazeneca
Novel 4-piperidinopyridine inhibitors of oxidosqualene cyclase-lanosterol synthase derived by consideration of inhibitor pK(a).
Astrazeneca
Emerging small-molecule therapeutic approaches for amyotrophic lateral sclerosis and frontotemporal dementia.
Astrazeneca
Identification and Optimization of Pyrrolidine Derivatives as Highly Potent Ghrelin Receptor Full Agonists.
Astrazeneca
Promiscuity of in Vitro Secondary Pharmacology Assays and Implications for Lead Optimization Strategies.
Astrazeneca
A novel series of 4-piperidinopyridine and 4-piperidinopyrimidine inhibitors of 2,3-oxidosqualene cyclase-lanosterol synthase.
Astrazeneca
Identification of novel GPR81 agonist lead series for target biology evaluation.
Astrazeneca
Heteroarylamide smoothened inhibitors: Discovery of N-[2,4-dimethyl-5-(1-methylimidazol-4-yl)phenyl]-4-(2-pyridylmethoxy)benzamide (AZD8542) and N-[5-(1H-imidazol-2-yl)-2,4-dimethyl-phenyl]-4-(2- pyridylmethoxy)benzamide (AZD7254).
Astrazeneca
Discovery of Novel 3-Quinoline Carboxamides as Potent, Selective, and Orally Bioavailable Inhibitors of Ataxia Telangiectasia Mutated (ATM) Kinase.
Astrazeneca
Tool inhibitors and assays to interrogate the biology of the TRAF2 and NCK interacting kinase.
Astrazeneca
Optimization of a Series of Bivalent Triazolopyridazine Based Bromodomain and Extraterminal Inhibitors: The Discovery of (3R)-4-[2-[4-[1-(3-Methoxy-[1,2,4]triazolo[4,3-b]pyridazin-6-yl)-4-piperidyl]phenoxy]ethyl]-1,3-dimethyl-piperazin-2-one (AZD5153).
Astrazeneca
Macrocyclic Prodrugs of a Selective Nonpeptidic Direct Thrombin Inhibitor Display High Permeability, Efficient Bioconversion but Low Bioavailability.
Astrazeneca
New alpha-substituted succinate-based hydroxamic acids as TNFalpha convertase inhibitors.
Astrazeneca
Structure-Based Design and Pharmacokinetic Optimization of Covalent Allosteric Inhibitors of the Mutant GTPase KRAS
Astrazeneca
Design and synthesis of potent non-polyglutamatable quinazoline antifolate thymidylate synthase inhibitors.
Astrazeneca
Potassium channel blocking 1,2-bis(aryl)ethane-1,2-diamines active as antiarrhythmic agents.
Astrazeneca
New Modalities, Technologies, and Partnerships in Probe and Lead Generation: Enabling a Mode-of-Action Centric Paradigm.
Astrazeneca
Tricyclic Indazoles-A Novel Class of Selective Estrogen Receptor Degrader Antagonists.
Astrazeneca
Structural and Molecular Insight into Resistance Mechanisms of First Generation cMET Inhibitors.
Astrazeneca
Scaffold Morphing To Identify Novel DprE1 Inhibitors with Antimycobacterial Activity.
Astrazeneca
Discovery of a Thiadiazole-Pyridazine-Based Allosteric Glutaminase 1 Inhibitor Series That Demonstrates Oral Bioavailability and Activity in Tumor Xenograft Models.
Astrazeneca
Evolution of PI3Kγ and δ Inhibitors for Inflammatory and Autoimmune Diseases.
Astrazeneca
Free Ligand 1D NMR Conformational Signatures To Enhance Structure Based Drug Design of a Mcl-1 Inhibitor (AZD5991) and Other Synthetic Macrocycles.
Astrazeneca
Discovery of a Potent and Selective Oral Inhibitor of ERK1/2 (AZD0364) That Is Efficacious in Both Monotherapy and Combination Therapy in Models of Nonsmall Cell Lung Cancer (NSCLC).
Astrazeneca
Discovery of a Series of 5-Azaquinazolines as Orally Efficacious IRAK4 Inhibitors Targeting MyD88
Astrazeneca
Building Bridges in a Series of Estrogen Receptor Degraders: An Application of Metathesis in Medicinal Chemistry.
Astrazeneca
DPP1 Inhibitors: Exploring the Role of Water in the S2 Pocket of DPP1 with Substituted Pyrrolidines.
Astrazeneca
Discovery of Potent and Orally Bioavailable Inverse Agonists of the Retinoic Acid Receptor-Related Orphan Receptor C2.
Astrazeneca
Discovery of a series of 8-(2,3-dihydro-1,4-benzoxazin-4-ylmethyl)-2-morpholino-4-oxo-chromene-6-carboxamides as PI3Kβ/δ inhibitors for the treatment of PTEN-deficient tumours.
Astrazeneca
Fragment-assisted hit investigation involving integrated HTS and fragment screening: Application to the identification of phosphodiesterase 10A (PDE10A) inhibitors.
Astrazeneca
Discovery of benzothiazoles as antimycobacterial agents: Synthesis, structure-activity relationships and binding studies with Mycobacterium tuberculosis decaprenylphosphoryl-β-D-ribose 2'-oxidase.
Astrazeneca
Discovery of AZ0108, an orally bioavailable phthalazinone PARP inhibitor that blocks centrosome clustering.
Astrazeneca
Structure guided lead generation for M. tuberculosis thymidylate kinase (Mtb TMK): discovery of 3-cyanopyridone and 1,6-naphthyridin-2-one as potent inhibitors.
Astrazeneca
Lactam sulfonamides as potent inhibitors of the Kv1.5 potassium ion channel.
Astrazeneca
Discovery of spirofused piperazine and diazepane amides as selective histamine-3 antagonists with in vivo efficacy in a mouse model of cognition.
Astrazeneca
Conformational analysis of 5-lipoxygenase inhibitors: role of the substituents in chiral recognition and on the active conformations of the (methoxyalkyl)thiazole and methoxytetrahydropyran series.
Astrazeneca
Discovery of a novel class of dimeric Smac mimetics as potent IAP antagonists resulting in a clinical candidate for the treatment of cancer (AZD5582).
Astrazeneca
FGFR1 Kinase Inhibitors: Close Regioisomers Adopt Divergent Binding Modes and Display Distinct Biophysical Signatures.
Astrazeneca
Structure- and reactivity-based development of covalent inhibitors of the activating and gatekeeper mutant forms of the epidermal growth factor receptor (EGFR).
Astrazeneca
Mitigation of cardiovascular toxicity in a series of CSF-1R inhibitors, and the identification of AZD7507.
Astrazeneca
Core refinement toward permeable β-secretase (BACE-1) inhibitors with low hERG activity.
Astrazeneca
QSAR investigation of NaV1.7 active compounds using the SVM/Signature approach and the Bioclipse Modeling platform.
Astrazeneca
Synthesis and evaluation of pyridylbenzofuran, pyridylbenzothiazole and pyridylbenzoxazole derivatives as ¹⁸F-PET imaging agents for β-amyloid plaques.
Astrazeneca
Experimental solubility profiling of marketed CNS drugs, exploring solubility limit of CNS discovery candidate.
Astrazeneca
Synthesis and evaluation of 2-pyridylbenzothiazole, 2-pyridylbenzoxazole and 2-pyridylbenzofuran derivatives as 11C-PET imaging agents for beta-amyloid plaques.
Astrazeneca
Discovery and Characterization of AZD6738, a Potent Inhibitor of Ataxia Telangiectasia Mutated and Rad3 Related (ATR) Kinase with Application as an Anticancer Agent.
Astrazeneca
Novel inhibitors of As(III) S-adenosylmethionine methyltransferase (AS3MT) identified by virtual screening.
Astrazeneca
Optimization of permeability in a series of pyrrolotriazine inhibitors of IRAK4.
Astrazeneca
Discovery of 2,6-disubstituted pyrazine derivatives as inhibitors of CK2 and PIM kinases.
Astrazeneca
Discovery of N-(4-{[5-Fluoro-7-(2-methoxyethoxy)quinazolin-4-yl]amino}phenyl)-2-[4-(propan-2-yl)-1 H-1,2,3-triazol-1-yl]acetamide (AZD3229), a Potent Pan-KIT Mutant Inhibitor for the Treatment of Gastrointestinal Stromal Tumors.
Astrazeneca
Lowering Lipophilicity by Adding Carbon: One-Carbon Bridges of Morpholines and Piperazines.
Astrazeneca
Discovery of a Series of 3-Cinnoline Carboxamides as Orally Bioavailable, Highly Potent, and Selective ATM Inhibitors.
Astrazeneca
Discovery of a Novel Oral Glucocorticoid Receptor Modulator (AZD9567) with Improved Side Effect Profile.
Astrazeneca
The Identification of Potent, Selective, and Orally Available Inhibitors of Ataxia Telangiectasia Mutated (ATM) Kinase: The Discovery of AZD0156 (8-{6-[3-(Dimethylamino)propoxy]pyridin-3-yl}-3-methyl-1-(tetrahydro-2 H-pyran-4-yl)-1,3-dihydro-2 H-imidazo[4,5- c]quinolin-2-one).
Astrazeneca
Potent and Orally Bioavailable Inverse Agonists of RORγt Resulting from Structure-Based Design.
Astrazeneca
Discovery of a Series of Indole-2 Carboxamides as Selective Secreted Phospholipase A
Astrazeneca
Discovery and Optimization of a Novel Series of Highly Selective JAK1 Kinase Inhibitors.
Astrazeneca
Identification and Pharmacological Profile of an Indane Based Series of Ghrelin Receptor Full Agonists.
Astrazeneca
Discovery of AZD-2098 and AZD-1678, Two Potent and Bioavailable CCR4 Receptor Antagonists.
Astrazeneca
Structure-Guided Discovery of Potent and Selective Inhibitors of ERK1/2 from a Modestly Active and Promiscuous Chemical Start Point.
Astrazeneca
Indazole-6-phenylcyclopropylcarboxylic Acids as Selective GPR120 Agonists with in Vivo Efficacy.
Astrazeneca
Adventures in Scaffold Morphing: Discovery of Fused Ring Heterocyclic Checkpoint Kinase 1 (CHK1) Inhibitors.
Astrazeneca
Selective Nonsteroidal Glucocorticoid Receptor Modulators for the Inhaled Treatment of Pulmonary Diseases.
Astrazeneca
Discovery and Optimization of Pyrrolopyrimidine Inhibitors of Interleukin-1 Receptor Associated Kinase 4 (IRAK4) for the Treatment of Mutant MYD88
Astrazeneca
Identification of quinazoline based inhibitors of IRAK4 for the treatment of inflammation.
Astrazeneca
Mitigating the inhibition of human bile salt export pump by drugs: opportunities provided by physicochemical property modulation, in silico modeling, and structural modification.
Astrazeneca
Design and Synthesis of Soluble and Cell-Permeable PI3Kδ Inhibitors for Long-Acting Inhaled Administration.
Astrazeneca
Discovery of Pyrazolo[1,5-a]pyrimidine B-Cell Lymphoma 6 (BCL6) Binders and Optimization to High Affinity Macrocyclic Inhibitors.
Astrazeneca
Discovery of a series of 8-(1-phenylpyrrolidin-2-yl)-6-carboxamide-2-morpholino-4H-chromen-4-one as PI3Kβ/δ inhibitors for the treatment of PTEN-deficient tumours.
Astrazeneca
Inhibitors of guanosine monophosphate synthetase as therapeutic agents
University of Southern California
Tricyclic Fused Heterocyclic PDE3/4 Dual Inhibitor and Use Thereof
Xizang Haisco Pharmaceutical
Substituted pyrazolo[1,5-a]pyridine compounds as inhibitors of FGFR tyrosine kinases
Array Biopharma
Novel Dialkoxynaphtho[2,3-C]Furan-1(3H)-One Derivatives and Pharmaceutical Composition For Preventing or Treating Respiratory Disease or SARS-COV-2 Infection Disease, Comprising Same
Dong Wha Pharm.
HETEROCYCLIC LACTAM COMPOUND, AND PREPARATION METHOD THEREFOR AND PHARMACEUTICAL USE THEREOF
Genfleet Therapeutics (Shanghai)
SALT OF COMPOUND FOR DEGRADING BTK, CRYSTAL FORM THEREOF, AND USE THEREOF IN MEDICINE
Haisco Pharmaceuticals
Pharmaceutical compositions comprising substituted nucleotides and nucleosides for treating viral infections
Emory University
Alkynyl(hetero)aromatic compound for inhibiting protein kinase activity
Shenzhen Targetrx
2-AMINOQUINAZOLINES AS LRRK2 INHIBITORS, PHARMACEUTICAL COMPOSITIONS, AND USES THEREOF
Merck Sharp & Dohme
Substituted 1,2,4-triazoles as intermediates in the synthesis of TYK2 inhibitors
Alumis
Certain (2S)-N-[(1S)-1-cyano-2-phenylethyl]-1,4-oxazepane-2-carboxamides as dipeptidyl peptidase 1 inhibitors
Astrazeneca
Isoquinoline amine compounds as mGluR4 allosteric potentiators, compositions, and methods of treating neurological dysfunction
Vanderbilt University
Indazolyl-spiro[2.2]pentane-carbonitrile derivatives as LRRK2 inhibitors, pharmaceutical compositions, and uses thereof
Merck Sharp & Dohme
Substituted n′-hydroxycarbamimidoyl-1,2,5-oxadiazole compounds as indoleamine 2,3-dioxygenase (IDO) inhibitors
Merck Sharp & Dohme
Thioether triazolopyridine and triazolopyrimidine inhibitors of myeloperoxidase
Bristol-Myers Squibb
Methods of treating intraocular pressure with activators of Tie-2
Aerpio Pharmaceuticals
Imidazooxazole derivative having antitumor effect, and pharmaceutical composition including same
Korea Institute of Science and Technology
Substituted pyrrolopyrimidine CDK inhibitor, pharmaceutical composition containing same and use thereof
Chia Tai Tianqing Pharmaceutical Group
Use of small molecule inhibitors targeting EYA tyrosine phosphatase
Cincinnati Childrens Hospital Medical Center
Substituted pyridyl-cycloalkyl-carboxylic acids, compositions containing them and medical uses thereof
Bayer Pharma Aktiengesellschaft
2-oxo-3,4-dihydroquinolin-6-yl sulphonamide CPDS and their use as plant growth regulators
University of California
Quinazolines as biogenic amine transport modulators
The United States of America As Represented By The Secretary, Department of Health and Human Services Office of Technology Transfer, National Institute of Health
Selective octahydro-cyclopenta[C] pyrrole negative modulators of NR2B
Cadent Therapeutics
Inhibition of fatty acid synthase by ginkgolic acids from the leaves of Ginkgo biloba and their cytotoxic activity.
Yeungnam University
Synthesis, stability, biochemical and pharmacokinetic properties of a new potent and selective 4-oxo-ß-lactam inhibitor of human leukocyte elastase.
University of Lisbon
Tetrahydroisoquinoline derivatives, pharmaceutical compositions and uses thereof
Boehringer Ingelheim International
Nicotinamide adenine dinucleotide-induced multimerization of the co-repressor CtBP1 relies on a switching tryptophan.
Oregon Health and Science University
Structure-Activity Relationships of Benzenesulfonamide-Based Inhibitors towards Carbonic Anhydrase Isoform Specificity.
University of Florida
MRSA Isolates from United States Hospitals Carry dfrG and dfrK Resistance Genes and Succumb to Propargyl-Linked Antifolates.
University of Connecticut
Design, synthesis, biological evaluation, NMR and DFT studies of structurally simplified trimethoxy benzamides as selective P-glycoprotein inhibitors: the role of molecular flatness.
Universit�� Di Bari Aldo Moro
Carbamate/urea derivatives containing piperidin and piperazin rings as H3 receptor inhibitors
Novartis
Substituted N-phenethyltriazoloneacetamides and use thereof
Bayer Intellectual Property
Reactivators of organophosphorous inhibited acetylcholinesterase
Southwest Research Institute
Thieno[3,2-D]pyrimidine derivatives having inhibitory activity for protein kinases
Hanmi Pharm.
Dihydro-oxazolobenzodiazepinone compounds, a process for there preparation and pharmaceutical compositions containing them
Les Laboratoires Servier
Structural similarities between thiamin-binding protein and thiaminase-I suggest a common ancestor.
Cornell University
Multiple differences in agonist and antagonist pharmacology between human and guinea pig histamine H1-receptor.
University of Kansas
A comparison of the receptor binding and HERG channel affinities for a series of antipsychotic drugs.
Aventis Pharmaceuticals
Pharmacological characterization of the human ionotropic glutamate receptor subtype GluR3 stably expressed in mammalian cells.
Sibia Neurosciences
Atypical neuroleptics have low affinity for dopamine D2 receptors or are selective for D4 receptors.
University of Toronto
Cloning, expression and pharmacological characterization of rabbit adenosine A1 and A3 receptors.
Pfizer
[3H]5-hydroxytryptamine labels the agonist high affinity state of the cloned rat 5-HT4 receptor.
Synaptic Pharmaceutical
Cloning of cDNAs encoding the human gamma-aminobutyric acid type A receptor alpha 6 subunit and characterization of the pharmacology of alpha 6-containing receptors.
Merck Sharp & Dohme Research Laboratories
The design, synthesis and potential utility of fluorescence probes that target DFG-out conformation of p38alpha for high throughput screening binding assay.
Pfizer
1H-1,2,4-triazol-3-yl-anilines: novel potent inhibitors of vascular endothelial growth factor receptors 1 and 2.
Chemdiv
Characterization of recombinant human serotonin 5HT1A receptors expressed in Chinese hamster ovary cells. [3H]spiperone discriminates between the G-protein-coupled and -uncoupled forms.
University of Canterbury
Mouse 5-hydroxytryptamine5A and 5-hydroxytryptamine5B receptors define a new family of serotonin receptors: cloning, functional expression, and chromosomal localization.
Cnrs
[125]I-spectramide: a novel benzamide displaying potent and selective effects at the D2 dopamine receptor.
Nida Addiction Research Center
A comparison between dopamine-stimulated adenylate cyclase and 3H-SCH 23390 binding in rat striatum.
UniversitÉ
Pharmacologic comparison of selected agonists for the M1 muscarinic receptor in transfected murine fibroblast cells (B82).
University of Arizona
Binding properties of the C-terminal domain of VIAF.
The Burnham Institute For Medical Research
The importance of odorant conformation to the binding and activation of a representative olfactory receptor.
Columbia University
Novel behavior of O-methylated beta-cyclodextrins in inclusion of meso-tetraarylporphyrins.
Doshisha University
Design, synthesis, and characterization of new embelin derivatives as potent inhibitors of X-linked inhibitor of apoptosis protein.
University of Michigan
Discovery of potent, selective, and orally bioavailable pyridone-based dipeptidyl peptidase-4 inhibitors.
Merck Research Laboratories
Novel dual inhibitors of AChE and MAO derived from hydroxy aminoindan and phenethylamine as potential treatment for Alzheimer's disease.
Teva Pharmaceutical Industries
Hepatitis C virus NS3-4A serine protease inhibitors: use of a P2-P1 cyclopropyl alanine combination for improved potency.
Schering-Plough Research Institute
Hepatitis C virus NS3-4A serine protease inhibitors: SAR of P'2 moiety with improved potency.
Schering-Plough Research Institute
Discovery of aminopyridine-based inhibitors of bacterial enoyl-ACP reductase (FabI).
Glaxosmithkline
Tyrosine kinase inhibitors. 1. Structure-activity relationships for inhibition of epidermal growth factor receptor tyrosine kinase activity by 2,3-dihydro-2-thioxo-1H-indole-3-alkanoic acids and 2,2'-dithiobis(1H-indole-3-alkanoic acids).
University of Auckland
Aminodiol HIV protease inhibitors. 1. Design, synthesis, and preliminary SAR.
Bristol-Myers Squibb
Crystal-structure-based design and synthesis of novel C-terminal inhibitors of HIV protease.
Agouron Pharmaceuticals
Design and synthesis of peptidomimetic inhibitors of HIV-1 protease and renin. Evidence for improved transport.
University of Pennsylvania
Synthesis and antiviral activity of a series of HIV-1 protease inhibitors with functionality tethered to the P1 or P1' phenyl substituents: X-ray crystal structure assisted design.
Merck Research Laboratories