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84 articles for thisTarget


The following articles (labelled with PubMed ID or TBD) are for your review
PMIDDataArticle TitleOrganization
28085275 53 Structure-Based Design of Macrocyclic Factor XIa Inhibitors: Discovery of the Macrocyclic Amide Linker.EBI Bristol-Myers Squibb
27073051 71 Orally bioavailable pyridine and pyrimidine-based Factor XIa inhibitors: Discovery of the methyl N-phenyl carbamate P2 prime group.EBI Bristol-Myers Squibb
26704266 80 Novel phenylalanine derived diamides as Factor XIa inhibitors.EBI Bristol-Myers Squibb
25592713 37 Pyridine and pyridinone-based factor XIa inhibitors.EBI Bristol-Myers Squibb
26005539 23 Discovery of a Potent Parenterally Administered Factor XIa Inhibitor with Hydroxyquinolin-2(1H)-one as the P2' Moiety.EBI Bristol-Myers Squibb
25990761 66 Novel Small Molecule Inhibitors of Activated Thrombin Activatable Fibrinolysis Inhibitor (TAFIa) from Natural Product Anabaenopeptin.EBI Institute For Infection Research
25881820 62 Design and synthesis of potent, selective phenylimidazole-based FVIIa inhibitors.EBI Bristol-Myers Squibb R & D
25728130 79 Structure-based design of inhibitors of coagulation factor XIa with novel P1 moieties.EBI Bristol-Myers Squibb
25405503 109 Phenylimidazoles as potent and selective inhibitors of coagulation factor XIa with in vivo antithrombotic activity.EBI 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.EBI Chinese Academy of Sciences
24102612 105 Synthesis and biological evaluation of direct thrombin inhibitors bearing 4-(piperidin-1-yl)pyridine at the P1 position with potent anticoagulant activity.EBI University of Bari &Quot;Aldo Moro&Quot
23927973 41 Discovery of nonbenzamidine factor VIIa inhibitors using a biaryl acid scaffold.EBI Bristol-Myers Squibb Research & Development
23478148 10 Discovery and gram-scale synthesis of BMS-593214, a potent, selective FVIIa inhibitor.EBI Bristol-Myers Squibb Pharmaceutical Research Institute
23602442 28 Discovery of diarylurea P2Y(1) antagonists with improved aqueous solubility.EBI Bristol-Myers Squibb
16644215 52 Design and synthesis of selective keto-1,2,4-oxadiazole-based tryptase inhibitors.EBI Celera Genomics
22770607 54 Potent direct inhibitors of factor Xa based on the tetrahydroisoquinoline scaffold.EBI Virginia Commonwealth University
18053726 364 Inhibitors of proteases and amide hydrolases that employ an alpha-ketoheterocycle as a key enabling functionality.EBI Johnson & Johnson Pharmaceutical Research & 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.EBI Bristol-Myers Squibb
15837303 52 Solid-phase synthesis of naphthylamidines as factor VIIa/tissue factor inhibitors.EBI Berlex Biosciences
14640539 112 Discovery of 1-(2-aminomethylphenyl)-3-trifluoromethyl-N- [3-fluoro-2'-(aminosulfonyl)[1,1'-biphenyl)]-4-yl]-1H-pyrazole-5-carboxyamide (DPC602), a potent, selective, and orally bioavailable factor Xa inhibitor(1).EBI Pharmaceutical Research Institute
12954057 113 Polymer-assisted solution-phase library synthesis and crystal structure of alpha-ketothiazoles as tissue factor VIIa inhibitors.EBI Pharmacia
11170646 106 Discovery of 1-[3-(aminomethyl)phenyl]-N-3-fluoro-2'-(methylsulfonyl)-[1,1'-biphenyl]-4-yl]-3-(trifluoromethyl)-1H-pyrazole-5-carboxamide (DPC423), a highly potent, selective, and orally bioavailable inhibitor of blood coagulation factor Xa.EBI Dupont Pharmaceuticals
12824035 39 Polymer-assisted solution-phase (PASP) parallel synthesis of an alpha-ketothiazole library as tissue factor VIIa inhibitors.EBI Pharmacia
12270173 23 Targeting thrombin and factor VIIa: design, synthesis, and inhibitory activity of functionally relevant indolizidinones.EBI Universit£
22041058 44 Arylsulfonamidopiperidone derivatives as a novel class of factor Xa inhibitors.EBI Bristol-Myers Squibb
21641796 30 Design, synthesis and biological activity of novel peptidyl benzyl ketone FVIIa inhibitors.EBI Technical University of Denmark
20102150 35 Discovery and clinical evaluation of 1-{N-[2-(amidinoaminooxy)ethyl]amino}carbonylmethyl-6-methyl-3-[2,2-difluoro-2-phenylethylamino]pyrazinone (RWJ-671818), a thrombin inhibitor with an oxyguanidine P1 motif.EBI Johnson & Johnson Pharmaceutical Research and Development
19447619 3 Preparation of L-proline based aeruginosin 298-A analogs: optimization of the P1-moiety.EBI University of New Orleans
 37 Synthesis and biological activity of P2–P4 azapeptidomimetic P1-argininal and P1-ketoargininamide derivatives: a novel class of serine protease inhibitorsEBI TBA
19128974 28 Discovery of N-[(1R,2S,5S)-2-{[(5-chloroindol-2-yl)carbonyl]amino}-5-(dimethylcarbamoyl)cyclohexyl]-5-methyl-4,5,6,7-tetrahydrothiazolo[5,4-c]pyridine-2-carboxamide hydrochloride: a novel, potent and orally active direct inhibitor of factor Xa.EBI Daiichi Sankyo
18674905 58 Factor VIIa inhibitors: target hopping in the serine protease family using X-ray structure determination.EBI Chugai Pharmaceutical
15332844 8 Dysinosins B-D, inhibitors of factor VIIa and thrombin from the Australian sponge Lamellodysidea chlorea.EBI Griffith University
18159923 24 7-fluoroindazoles as potent and selective inhibitors of factor Xa.EBI Johnson & Johnson Pharmaceutical Research and Development
17643988 92 Enantiopure five-membered cyclicdiamine derivatives as potent and selective inhibitors of factor Xa. Improving in vitro metabolic stability via core modifications.EBI Bristol-Myers Squibb
17566736 60 Design, synthesis, and biological evaluation of pyrazinones containing novel P1 needles as inhibitors of TF/VIIa.EBI Pfizer
16714109 40 Design of novel, potent, and selective human beta-tryptase inhibitors based on alpha-keto-[1,2,4]-oxadiazoles.EBI Celera
16650987 10 Efforts toward oral bioavailability in factor VIIa inhibitors.EBI Celera
16458507 2 Factor VIIa inhibitors: a prodrug strategy to improve oral bioavailability.EBI Celera Genomics
16257204 37 Generation of potent coagulation protease inhibitors utilizing zinc-mediated chelation.EBI Celera
16213711 37 Ketene aminal-based lactam derivatives as a novel class of orally active FXa inhibitors.EBI Bristol-Myers Squibb Pharmaceutical Research Institute
15913999 8 Structure-based design and synthesis of pyrazinones containing novel P1 'side pocket' moieties as inhibitors of TF/VIIa.EBI Pfizer
15203149 72 Structure-based design of amidinophenylurea-derivatives for factor VIIa inhibition.EBI Aventis Pharma Deutschland
14552766 12 Synthesis and X-ray crystal structures of substituted fluorobenzene and benzoquinone inhibitors of the tissue factor VIIa complex.EBI Pharmacia
12699744 15 Phosphate ester serum albumin affinity tags greatly improve peptide half-life in vivo.EBI Genentech
12668013 42 Design, synthesis, and structure-activity relationship of a new class of amidinophenylurea-based factor VIIa inhibitors.EBI Aventis Pharma Deutschland
12593666 30 Structure-activity relationship study and drug profile of N-(4-fluorophenylsulfonyl)-L-valyl-L-leucinal (SJA6017) as a potent calpain inhibitor.EBI Senju Pharmaceutical
12270169 13 Albumin affinity tags increase peptide half-life in vivo.EBI Genentech
11689072 49 Exploiting subsite S1 of trypsin-like serine proteases for selectivity: potent and selective inhibitors of urokinase-type plasminogen activator.EBI Axys Pharmaceuticals
11527709 19 Optimization of a screening lead for factor VIIa/TF.EBI Axys Pharmaceuticals
32527459 67 Discovery of hydroxy pyrimidine Factor IXa inhibitors.EBI Merck
32340773 110 Design and synthesis of novel proline based factor XIa selective inhibitors as leads for potential new anticoagulants.EBI 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.EBI Novartis Institutes For Biomedical Research
32456431 24 Discovery of a High Affinity, Orally Bioavailable Macrocyclic FXIa Inhibitor with Antithrombotic Activity in Preclinical Species.EBI Bristol Myers Squibb
31445854 43 Structure based design of macrocyclic factor XIa inhibitors: Discovery of cyclic P1 linker moieties with improved oral bioavailability.EBI Bristol-Myers Squibb
10212122 35 Secondary structure peptide mimetics: design, synthesis, and evaluation of beta-strand mimetic thrombin inhibitors.EBI Molecumetics
30446438 36 Design, synthesis and biological evaluation of anthranilamide derivatives as potential factor Xa (fXa) inhibitors.EBI China Pharmaceutical University
9873692 54 Preparation of meta-amidino-N,N-disubstituted anilines as potent inhibitors of coagulation factor Xa.EBI Dupont Pharmaceuticals
29400967 136 Fluorine and Fluorinated Motifs in the Design and Application of Bioisosteres for Drug Design.EBI Bristol-Myers Squibb
31833761 32 Potent, Orally Bioavailable, and Efficacious Macrocyclic Inhibitors of Factor XIa. Discovery of Pyridine-Based Macrocycles Possessing Phenylazole Carboxamide P1 Groups.EBI Bristol-Myers Squibb
9871540 100 Pyrazoles, 1,2,4-triazoles, and tetrazoles as surrogates for cis-amide bonds in boronate ester thrombin inhibitors.EBI Dupont Pharmaceuticals
31563807 63 Discovery of novel, potent, isosteviol-based antithrombotic agents.EBI Peking University
26575094 60 Discovery and SAR of Novel and Selective Inhibitors of Urokinase Plasminogen Activator (uPA) with an Imidazo[1,2-a]pyridine Scaffold.EBI University of Antwerp (Ua)
29501396 59 Pyridazine and pyridazinone derivatives as potent and selective factor XIa inhibitors.EBI Bristol-Myers Squibb
28780160 14 Macrocyclic factor XIa inhibitors.EBI Bristol-Myers Squibb
29517911 87 Stable and Long-Lasting, Novel Bicyclic Peptide Plasma Kallikrein Inhibitors for the Treatment of Diabetic Macular Edema.EBI Bicycle Therapeutics
29077405 63 Discovery of a Parenteral Small Molecule Coagulation Factor XIa Inhibitor Clinical Candidate (BMS-962212).EBI Bristol-Myers Squibb
28460818 29 Neutral macrocyclic factor VIIa inhibitors.EBI Bristol-Myers Squibb Research and Development
9802391 31 The cloned guinea pig pancreatic polypeptide receptor Y4 resembles more the human Y4 than does the rat Y4.BDB Uppsala University
9195867 15 Structure-based design and combinatorial chemistry yield low nanomolar inhibitors of cathepsin D.BDB University of California Berkeley
20383151 2 Small-molecule kinase inhibitors provide insight into Mps1 cell cycle function.BDB Dana-Farber Cancer Institute
19648931 16 Design, synthesis and selection of DNA-encoded small-molecule libraries.BDB Praecis Pharmaceuticals
19305397 22 Molecular docking and ligand specificity in fragment-based inhibitor discovery.BDB University of California San Francisco
19699645 12 Design, synthesis, and biological evaluation of hydroquinone derivatives as novel inhibitors of the sarco/endoplasmic reticulum calcium ATPase.BDB Northern Kentucky University