107 articles for thisTarget

---

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

PMID	Data	Article Title	Organization
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
27073051	71	Orally bioavailable pyridine and pyrimidine-based Factor XIa inhibitors: Discovery of the methyl N-phenyl carbamate P2 prime group.	Bristol-Myers Squibb
26732532	69	Active site-directed plasmin inhibitors: Extension on the P2 residue.	Kobe Gakuin University
26704266	80	Novel phenylalanine derived diamides as Factor XIa inhibitors.	Bristol-Myers Squibb
26421993	44	Structure-guided discovery of 2-aryl/pyridin-2-yl-1H-indole derivatives as potent and selective hepsin inhibitors.	Aurigene Discovery Technologies
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
25921265	21	Novel type of plasmin inhibitors: providing insight into P4 moiety and alternative scaffold to pyrrolopyrimidine.	Hiroshima International University
25782055	9	Discovery of a Cyclic Boronic Acidß-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases.	Rempex Pharmaceuticals
24951330	25	Orally bioavailable factor Xa inhibitors containing alpha-substituted gem-dimethyl P4 moieties.	Bristol-Myers Squibb
24794746	168	Structure-guided discovery of 1,3,5 tri-substituted benzenes as potent and selective matriptase inhibitors exhibiting in vivo antitumor efficacy.	Aurigene Discovery Technologies
24613052	69	Pyrrolopyrimidine-inhibitors with hydantoin moiety as spacer can explore P4/S4 interaction on plasmin.	Hiroshima International University
24610996	16	Thrombin inhibitory activity of some polyphenolic compounds.	University of Lodz
24900621	48	Discovery of Pyridyl Bis(oxy)dibenzimidamide Derivatives as Selective Matriptase Inhibitors.	Aurigene Discovery Technologies
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
23294255	114	Development of new cyclic plasmin inhibitors with excellent potency and selectivity.	Philipps University Marburg
19385614	303	Large-scale application of high-throughput molecular mechanics with Poisson-Boltzmann surface area for routine physics-based scoring of protein-ligand complexes.	Abbott Laboratories
16644215	52	Design and synthesis of selective keto-1,2,4-oxadiazole-based tryptase inhibitors.	Celera Genomics
23123017	23	Synthesis and docking studies of novel antitumor benzimidazoles.	National Research Center
22771232	18	Design, synthesis, biochemical studies, cellular characterization, and structure-based computational studies of small molecules targeting the urokinase receptor.	Indiana University
23088498	8	Bicyclization and tethering to albumin yields long-acting peptide antagonists.	Ecole Polytechnique F�D�Rale De Lausanne
22366654	33	2-Amidino analogs of glycine-amiloride conjugates: inhibitors of urokinase-type plasminogen activator.	University of Louisville
20121198	63	Studies of benzothiophene template as potent factor IXa (FIXa) inhibitors in thrombosis.	Trigen
19715320	87	Grassystatins A-C from marine cyanobacteria, potent cathepsin E inhibitors that reduce antigen presentation.	University of Florida
18052026	97	Small, potent, and selective diaryl phosphonate inhibitors for urokinase-type plasminogen activator with in vivo antimetastatic properties.	University of Antwerp
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
15214773	76	Fragment-based drug discovery.	Sunesis Pharmaceuticals
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).	Pharmaceutical Research Institute
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.	Dupont Pharmaceuticals
9301673	234	Synthesis and structure-activity relationships of potent thrombin inhibitors: piperazides of 3-amidinophenylalanine.	Klinikum Der Friedrich-Schiller-Universit£T Jena
8496923	9	New mechanism-based inactivators of trypsin-like proteinases. Selective inactivation of urokinase by functionalized cyclopeptides incorporating a sulfoniomethyl-substituted m-aminobenzoic acid residue.	Cnrs-Cercoa
1527787	11	Synthesis and biological activity of ketomethylene pseudopeptide analogues as thrombin inhibitors.	Thrombosis Research Institute
2231595	96	Selective inhibition of urokinase by substituted phenylguanidines: quantitative structure-activity relationship analyses.	Abbott Laboratories
15081015	91	Solid-phase synthesis and SAR of 4-carboxy-2-azetidinone mechanism-based tryptase inhibitors.	The Bristol-Myers Squibb Pharmaceutical Research Institute
22285569	107	Synthesis and evaluation of non-basic inhibitors of urokinase-type plasminogen activator (uPA).	University of Antwerp
22041058	44	Arylsulfonamidopiperidone derivatives as a novel class of factor Xa inhibitors.	Bristol-Myers Squibb
21978672	49	Synthesis and preliminary evaluation of amiloride analogs as inhibitors of the urokinase-type plasminogen activator (uPA).	University of Wollongong
21741848	66	Design, synthesis and evaluation of N-benzoylindazole derivatives and analogues as inhibitors of human neutrophil elastase.	Universit£
19483697	23	Phage-encoded combinatorial chemical libraries based on bicyclic peptides.	Laboratory of Molecular Biology, Medical Research Council
20405925	5	Multiple toxin production in the cyanobacterium microcystis: isolation of the toxic protease inhibitor cyanopeptolin 1020.	University of Basel
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.	Johnson & Johnson Pharmaceutical Research and Development
20121197	148	Structure based drug design: development of potent and selective factor IXa (FIXa) inhibitors.	Trigen
19703768	63	Identification of orally bioavailable, non-amidine inhibitors of Urokinase Plasminogen Activator (uPA).	Berlex Biosciences
19541481	57	Cyanoguanidine-based lactam derivatives as a novel class of orally bioavailable factor Xa inhibitors.	Bristol-Myers Squibb
19250826	100	Incorporation of neutral C-terminal residues in 3-amidinophenylalanine-derived matriptase inhibitors.	The Medicines Company (Leipzig)
19036586	128	Modification of the N-terminal sulfonyl residue in 3-amidinophenylalanine-based matriptase inhibitors.	Curacyte Discovery
18457385	41	Recent developments in fragment-based drug discovery.	Astex Therapeutics
18163548	15	Fragment-based discovery of mexiletine derivatives as orally bioavailable inhibitors of urokinase-type plasminogen activator.	Astex Therapeutics
17905583	2	Geometry of GPPE binding to picrate and to the urokinase type plasminogen activator.	Pedagogical 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
17583500	31	Aminopyrrolidineamide inhibitors of site-1 protease.	Pfizer
17462889	110	From selective substrate analogue factor Xa inhibitors to dual inhibitors of thrombin and factor Xa. Part 3.	Curacyte Discovery
16970403	74	Diphenyl phosphonate inhibitors for the urokinase-type plasminogen activator: optimization of the P4 position.	University of Antwerp
16725321	13	Novel, potent, selective, and orally bioavailable human betaII-tryptase inhibitors.	Celera Genomics
16546384	10	Inhibition of trypsin and urokinase by Cbz-amino(4-guanidinophenyl)methanephosphonate aromatic ester derivatives: the influence of the ester group on their biological activity.	Wroclaw University of Technology
16460935	39	A novel series of arylsulfonylthiophene-2-carboxamidine inhibitors of the complement component C1s.	Johnson & Johnson Pharmaceutical Research and Development
16213711	37	Ketene aminal-based lactam derivatives as a novel class of orally active FXa inhibitors.	Bristol-Myers Squibb Pharmaceutical Research Institute
15801822	28	9-hydroxyazafluorenes and their use in thrombin inhibitors.	Merck Research Laboratories
15582418	103	Naphthamidine urokinase plasminogen activator inhibitors with improved pharmacokinetic properties.	Abbott Laboratories
15149680	58	Selective urokinase-type plasminogen activator (uPA) inhibitors. Part 3: 1-isoquinolinylguanidines.	Pfizer
15149645	92	Interaction with the S1 beta-pocket of urokinase: 8-heterocycle substituted and 6,8-disubstituted 2-naphthamidine urokinase inhibitors.	Abbott Laboratories
15115382	16	Development of irreversible diphenyl phosphonate inhibitors for urokinase plasminogen activator.	University of Antwerp
15081014	35	Synthesis of potent and highly selective nonguanidine azetidinone inhibitors of human tryptase.	The Bristol-Myers Squibb Pharmaceutical Research Institute
14711304	117	Identification of novel binding interactions in the development of potent, selective 2-naphthamidine inhibitors of urokinase. Synthesis, structural analysis, and SAR of N-phenyl amide 6-substitution.	Abbott Laboratories
14698147	60	Synthesis of potent and selective 2-azepanone inhibitors of human tryptase.	The Bristol-Myers Squibb Pharmaceutical Research Institute
12113833	183	4-Aminoarylguanidine and 4-aminobenzamidine derivatives as potent and selective urokinase-type plasminogen activator inhibitors.	Celera
12113832	120	2-(2-Hydroxy-3-alkoxyphenyl)-1H-benzimidazole-5-carboxamidine derivatives as potent and selective urokinase-type plasminogen activator inhibitors.	Celera
11844691	107	4-amidinobenzylamine-based inhibitors of urokinase.	Universitat Jena
11814826	14	Design and synthesis of 4,5-disubstituted-thiophene-2-amidines as potent urokinase inhibitors.	3-Dimensional Pharmaceuticals
11755350	31	Selective urokinase-type plasminogen activator (uPA) inhibitors. Part 2: (3-Substituted-5-halo-2-pyridinyl)guanidines.	Pfizer
11755349	24	Selective urokinase-type plasminogen activator (uPA) inhibitors. Part 1: 2-Pyridinylguanidines.	Pfizer
11689072	49	Exploiting subsite S1 of trypsin-like serine proteases for selectivity: potent and selective inhibitors of urokinase-type plasminogen activator.	Axys Pharmaceuticals
11527709	19	Optimization of a screening lead for factor VIIa/TF.	Axys Pharmaceuticals
11495587	198	Development of serine protease inhibitors displaying a multicentered short (<2.3 A) hydrogen bond binding mode: inhibitors of urokinase-type plasminogen activator and factor Xa.	Axys Pharmaceuticals
11459634	94	Development of potent and selective factor Xa inhibitors.	Axys Pharmaceuticals
11378359	57	Structure-based design, synthesis and SAR of a novel series of thiopheneamidine urokinase plasminogen activator inhibitors.	3-Dimensional Pharmaceuticals
11311057	15	Structure-based approach for the discovery of bis-benzamidines as novel inhibitors of matriptase.	Georgetown University Medical Center
11294390	43	Synthesis of thiophene-2-carboxamidines containing 2-aminothiazoles and their biological evaluation as urokinase inhibitors.	3-Dimensional Pharmaceuticals
11052791	6	Identification of novel inhibitors of urokinase via NMR-based screening.	Abbott Laboratories
10853674	32	Synthesis and biological activity of peptidyl aldehyde urokinase inhibitors.	Corvas International
10560742	85	3-Amidinophenylalanine-based inhibitors of urokinase.	UniversitäT Jena
10212122	35	Secondary structure peptide mimetics: design, synthesis, and evaluation of beta-strand mimetic thrombin inhibitors.	Molecumetics
9876114	111	Structural and functional analyses of benzamidine-based inhibitors in complex with trypsin: implications for the inhibition of factor Xa, tPA, and urokinase.	Institut FüR Biochemie
9873397	37	In vitro evaluation and crystallographic analysis of a new class of selective, non-amide-based thrombin inhibitors.	3-Dimensional Pharmaceuticals
9822554	14	1,2-Benzisothiazol-3-one 1,1-dioxide inhibitors of human mast cell tryptase.	Bristol-Myers Squibb Pharmaceutical Research Institute
9784099	84	Design of benzamidine-type inhibitors of factor Xa.	Institut FüR Biochemie
7739010	118	Characterization of a class of peptide boronates with neutral P1 side chains as highly selective inhibitors of thrombin.	Thrombosis Research Institute
6219223	94	Aromatic amidines: comparison of their ability to block respiratory syncytial virus induced cell fusion and to inhibit plasmin, urokinase, thrombin, and trypsin.	TBA
1447734	29	Effect of conformational mobility and hydrogen-bonding interactions on the selectivity of some guanidinoaryl-substituted mechanism-based inhibitors of trypsin-like serine proteases.	University of Illinois
27264434	13	3-aminopyrazolopyrazine derivatives as spleen tyrosine kinase inhibitors.	Jilin University