133 articles for thisTarget

---

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

PMID	Data	Article Title	Organization
28085275	53	Structure-Based Design of Macrocyclic Factor XIa Inhibitors: Discovery of the Macrocyclic Amide Linker.	Bristol-Myers Squibb
28197309	40	Structure-Guided Design of Novel, Potent, and Selective Macrocyclic Plasma Kallikrein Inhibitors.	Global Blood Therapeutics
27994741	48	Discovery of Phenylglycine Lactams as Potent Neutral Factor VIIa Inhibitors.	Bristol-Myers Squibb R & D
27739691	7	Fragment-to-Lead Medicinal Chemistry Publications in 2015.	Astex Pharmaceuticals
27455395	66	Discovery of a Highly Potent, Selective, and Orally Bioavailable Macrocyclic Inhibitor of Blood Coagulation Factor VIIa-Tissue Factor Complex.	Bristol-Myers Squibb R & D
27015008	51	Atropisomer Control in Macrocyclic Factor VIIa Inhibitors.	Bristol-Myers Squibb Research & Development
27073051	71	Orally bioavailable pyridine and pyrimidine-based Factor XIa inhibitors: Discovery of the methyl N-phenyl carbamate P2 prime group.	Bristol-Myers Squibb
26704266	80	Novel phenylalanine derived diamides as Factor XIa inhibitors.	Bristol-Myers Squibb
25592713	37	Pyridine and pyridinone-based factor XIa inhibitors.	Bristol-Myers Squibb
26005539	23	Discovery of a Potent Parenterally Administered Factor XIa Inhibitor with Hydroxyquinolin-2(1H)-one as the P2' Moiety.	Bristol-Myers Squibb
25990761	66	Novel Small Molecule Inhibitors of Activated Thrombin Activatable Fibrinolysis Inhibitor (TAFIa) from Natural Product Anabaenopeptin.	Institute For Infection Research
25728130	79	Structure-based design of inhibitors of coagulation factor XIa with novel P1 moieties.	Bristol-Myers Squibb
24951330	25	Orally bioavailable factor Xa inhibitors containing alpha-substituted gem-dimethyl P4 moieties.	Bristol-Myers Squibb
25517413	1	Total synthesis of clavatadine A.	Central Washington University
25453807	13	A simple, general approach of allosteric coagulation enzyme inhibition through monosulfated hydrophobic scaffolds.	Virginia Commonwealth University
25405503	109	Phenylimidazoles as potent and selective inhibitors of coagulation factor XIa with in vivo antithrombotic activity.	Bristol-Myers Squibb
25179681	81	Design, synthesis, and structure-activity and structure-pharmacokinetic relationship studies of novel [6,6,5] tricyclic fused oxazolidinones leading to the discovery of a potent, selective, and orally bioavailable FXa inhibitor.	Chinese Academy of Sciences
24666186	15	Allosteric inhibition of human factor XIa: discovery of monosulfated benzofurans as a class of promising inhibitors.	Virginia Commonwealth University
24900827	8	Inhibitors of Factor XIa and Plasma Kallikrein May Treat Thromboembolic Disorders and Many Diabetes Complications.	Therachem Research Medilab (India)
24405333	69	Tetrahydroquinoline derivatives as potent and selective factor XIa inhibitors.	Bristol-Myers Squibb
24418773	61	Design, synthesis, and SAR of a series of activated protein C (APC) inhibitors with selectivity against thrombin for the treatment of haemophilia.	Astrazeneca
24900796	42	Design and Synthesis of Phenylpyrrolidine Phenylglycinamides As Highly Potent and Selective TF-FVIIa Inhibitors.	Bristol-Myers Squibb R & D
23927973	41	Discovery of nonbenzamidine factor VIIa inhibitors using a biaryl acid scaffold.	Bristol-Myers Squibb Research & Development
23602442	28	Discovery of diarylurea P2Y(1) antagonists with improved aqueous solubility.	Bristol-Myers Squibb
23586812	38	Development of a selective peptide macrocycle inhibitor of coagulation factor XII toward the generation of a safe antithrombotic therapy.	Ecole Polytechnique F�D�Rale De Lausanne Epfl
23451707	23	Discovery of allosteric modulators of factor XIa by targeting hydrophobic domains adjacent to its heparin-binding site.	Virginia Commonwealth University
23316863	1	Sulfated pentagalloylglucoside is a potent, allosteric, and selective inhibitor of factor XIa.	Virginia Commonwealth University
23294255	114	Development of new cyclic plasmin inhibitors with excellent potency and selectivity.	Philipps University Marburg
16644215	52	Design and synthesis of selective keto-1,2,4-oxadiazole-based tryptase inhibitors.	Celera Genomics
22770607	54	Potent direct inhibitors of factor Xa based on the tetrahydroisoquinoline scaffold.	Virginia Commonwealth University
19715320	87	Grassystatins A-C from marine cyanobacteria, potent cathepsin E inhibitors that reduce antigen presentation.	University of Florida
18053726	364	Inhibitors of proteases and amide hydrolases that employ an alpha-ketoheterocycle as a key enabling functionality.	Johnson & Johnson Pharmaceutical Research & Development
18054227	45	Structure-activity relationship and pharmacokinetic profile of 5-ketopyrazole factor Xa inhibitors.	Bristol-Myers Squibb Research and Development
17588746	103	SAR and X-ray structures of enantiopure 1,2-cis-(1R,2S)-cyclopentyldiamine and cyclohexyldiamine derivatives as inhibitors of coagulation Factor Xa.	Bristol-Myers Squibb
16876411	17	Synthesis and in vitro biological evaluation of aryl boronic acids as potential inhibitors of factor XIa.	Daiichi Asubio Medical Research Laboratories
12270173	23	Targeting thrombin and factor VIIa: design, synthesis, and inhibitory activity of functionally relevant indolizidinones.	Universit£
22041058	44	Arylsulfonamidopiperidone derivatives as a novel class of factor Xa inhibitors.	Bristol-Myers Squibb
21035339	16	Design and synthesis of macrocyclic indoles targeting blood coagulation cascade Factor XIa.	Université
20650636	118	Discovery of a factor Xa inhibitor (3R,4R)-1-(2,2-difluoro-ethyl)-pyrrolidine-3,4-dicarboxylic acid 3-[(5-chloro-pyridin-2-yl)-amide] 4-[[2-fluoro-4-(2-oxo-2H-pyridin-1-yl)-phenyl]-amide] as a clinical candidate.	F. Hoffmann-La Roche
20405925	5	Multiple toxin production in the cyanobacterium microcystis: isolation of the toxic protease inhibitor cyanopeptolin 1020.	University of Basel
18674905	58	Factor VIIa inhibitors: target hopping in the serine protease family using X-ray structure determination.	Chugai Pharmaceutical
18510371	2	Clavatadine A, a natural product with selective recognition and irreversible inhibition of factor XIa.	Griffith University
17643988	92	Enantiopure five-membered cyclicdiamine derivatives as potent and selective inhibitors of factor Xa. Improving in vitro metabolic stability via core modifications.	Bristol-Myers Squibb
16524727	25	Synthesis, SAR exploration, and X-ray crystal structures of factor XIa inhibitors containing an alpha-ketothiazole arginine.	Daiichi Asubio Medical Research Laboratories
32527459	67	Discovery of hydroxy pyrimidine Factor IXa inhibitors.	Merck
32340773	110	Design and synthesis of novel proline based factor XIa selective inhibitors as leads for potential new anticoagulants.	Merck
32551603	185	Structure-Based Design and Preclinical Characterization of Selective and Orally Bioavailable Factor XIa Inhibitors: Demonstrating the Power of an Integrated S1 Protease Family Approach.	Novartis Institutes For Biomedical Research
32456431	24	Discovery of a High Affinity, Orally Bioavailable Macrocyclic FXIa Inhibitor with Antithrombotic Activity in Preclinical Species.	Bristol Myers Squibb
31932224	25	Orally bioavailable amine-linked macrocyclic inhibitors of factor XIa.	Bristol-Myers Squibb
27434175	54	Substrate-Guided Design of Selective FXIIa Inhibitors Based on the Plant-Derived Momordica cochinchinensis Trypsin Inhibitor-II (MCoTI-II) Scaffold.	The University of Queensland
27347787	32	Macrocyclic Prodrugs of a Selective Nonpeptidic Direct Thrombin Inhibitor Display High Permeability, Efficient Bioconversion but Low Bioavailability.	Astrazeneca
27280436	304	Optimization of Cyclic Plasmin Inhibitors: From Benzamidines to Benzylamines.	Philipps University Marburg
30707839	63	Suppression of Tumor Growth and Metastases by Targeted Intervention in Urokinase Activity with Cyclic Peptides.	Chinese Academy of Sciences
31679971	44	6-Substituted amiloride derivatives as inhibitors of the urokinase-type plasminogen activator for use in metastatic disease.	University of Wollongong
31445854	43	Structure based design of macrocyclic factor XIa inhibitors: Discovery of cyclic P1 linker moieties with improved oral bioavailability.	Bristol-Myers Squibb
30995036	52	Design, Synthesis, and Preclinical Characterization of Selective Factor D Inhibitors Targeting the Alternative Complement Pathway.	Novartis Institutes For Biomedical Research
30520638	54	Highly Potent and Selective Plasmin Inhibitors Based on the Sunflower Trypsin Inhibitor-1 Scaffold Attenuate Fibrinolysis in Plasma.	The University of Queensland
31833761	32	Potent, Orally Bioavailable, and Efficacious Macrocyclic Inhibitors of Factor XIa. Discovery of Pyridine-Based Macrocycles Possessing Phenylazole Carboxamide P1 Groups.	Bristol-Myers Squibb
31658420	98	Fibrinolysis Inhibitors: Potential Drugs for the Treatment and Prevention of Bleeding.	Philipps University Marburg
31563807	63	Discovery of novel, potent, isosteviol-based antithrombotic agents.	Peking University
26536069	89	Design of Specific Serine Protease Inhibitors Based on a Versatile Peptide Scaffold: Conversion of a Urokinase Inhibitor to a Plasma Kallikrein Inhibitor.	Aarhus University
29072911	16	Design of Small-Molecule Active-Site Inhibitors of the S1A Family Proteases as Procoagulant and Anticoagulant Drugs.	University of Nottingham
29501396	59	Pyridazine and pyridazinone derivatives as potent and selective factor XIa inhibitors.	Bristol-Myers Squibb
30130401	71	6-Substituted Hexamethylene Amiloride (HMA) Derivatives as Potent and Selective Inhibitors of the Human Urokinase Plasminogen Activator for Use in Cancer.	University of Wollongong
29775297	7	Factor XIa Inhibitors as New Anticoagulants.	Bristol-Myers Squibb
28687203	29	Macrocyclic inhibitors of Factor XIa: Discovery of alkyl-substituted macrocyclic amide linkers with improved potency.	Bristol-Myers Squibb
28780160	14	Macrocyclic factor XIa inhibitors.	Bristol-Myers Squibb
27976897	39	Potent, Selective, Allosteric Inhibition of Human Plasmin by Sulfated Non-Saccharide Glycosaminoglycan Mimetics.	Virginia Commonwealth University
29517911	87	Stable and Long-Lasting, Novel Bicyclic Peptide Plasma Kallikrein Inhibitors for the Treatment of Diabetic Macular Edema.	Bicycle Therapeutics
29077405	63	Discovery of a Parenteral Small Molecule Coagulation Factor XIa Inhibitor Clinical Candidate (BMS-962212).	Bristol-Myers Squibb
32321856	4	Structure-based design of antiviral drug candidates targeting the SARS-CoV-2 main protease.	Shanghai Institute of Materia Medica
24090423	13	Identification and structure-activity relationship study of carvacrol derivatives as Mycobacterium tuberculosis chorismate mutase inhibitors.	Birla Institute of Technology
	18	Novel multi-targeted agents for Alzheimer's disease: Synthesis, biological evaluation, and molecular modeling of novel 2-[4-(4-substitutedpiperazin-1-yl)phenyl]benzimidazoles	Hacettepe University
15449728	11	Design and synthesis of indole and tetrahydroisoquinoline hydantoin derivatives as human chymase inhibitors.	UniversitÉ
15499999	35	Benzolamide is not a membrane-impermeant carbonic anhydrase inhibitor.	UniversitÀ Degli Studi Di Firenze
8910390	13	Molecular and pharmacological characterization of native cortical gamma-aminobutyric acidA receptors containing both alpha1 and alpha3 subunits.	Universidad De Sevilla
8097479	3	A human somatostatin receptor (SSTR3), located on chromosome 22, displays preferential affinity for somatostatin-14 like peptides.	University of Toronto
7791120	11	Characterization and distribution of binding sites for a new neurotensin receptor antagonist ligand, [3H]SR 48692, in the guinea pig brain.	Hospital Saint-Antoine
16407991	13	Activity-based probes that target diverse cysteine protease families.	Stanford University
19848404	44	Discovery of potent and selective inhibitors of the mammalian target of rapamycin (mTOR) kinase.	Wyeth Research
19678708	28	Design, synthesis, and structure-activity relationships of aminopyridine N-oxides, a novel scaffold for the potent and selective inhibition of p38 mitogen activated protein kinase.	Almirall
18178084	24	Carbamate-appended N-alkylsulfonamides as inhibitors of gamma-secretase.	Bristol-Myers Squibb
19243938	3	Design, synthesis, and evaluation of peptidomimetics containing Freidinger lactams as STAT3 inhibitors.	University of Michigan At Ann Arbor
18783202	16	Identification of BRAF inhibitors through in silico screening.	University of Pennsylvania
18260617	131	3-Amino-benzo[d]isoxazoles as Novel Multitargeted Inhibitors of Receptor Tyrosine Kinases.	Abbott Laboratories
18020435	55	4,5-diarylisoxazole Hsp90 chaperone inhibitors: potential therapeutic agents for the treatment of cancer.	Vernalis (R&D)
16386422	40	Discovery and SAR study of novel dihydroquinoline containing glucocorticoid receptor ligands.	Boehringer Ingelheim Pharmaceuticals
17350258	27	Lead optimization of methionine aminopeptidase-2 (MetAP2) inhibitors containing sulfonamides of 5,6-disubstituted anthranilic acids.	Abbott Laboratories
12954329	8	The structure of JNK3 in complex with small molecule inhibitors: structural basis for potency and selectivity.	Merck Research Laboratories
15482920	11	Isoxazole carboxylic acids as protein tyrosine phosphatase 1B (PTP1B) inhibitors.	Abbott Laboratories
12747781	29	Discovery and structure-activity relationship of oxalylarylaminobenzoic acids as inhibitors of protein tyrosine phosphatase 1B.	Abbott Laboratories