The following articles (labelled with PubMed ID or TBD) are for your review
PMID | Data | Article Title | Organization |
10782685 |
9 |
Synthesis of a cyanopeptide-analogue with trypsin activating properties.![EBI](/images/logo_chembl.png) |
Ernst-Moritz-Arndt-University |
27287367 |
36 |
Evaluation of bisbenzamidines as inhibitors for matriptase-2.![EBI](/images/logo_chembl.png) |
University of Bonn |
27015008 |
51 |
Atropisomer Control in Macrocyclic Factor VIIa Inhibitors.![EBI](/images/logo_chembl.png) |
Bristol-Myers Squibb Research & Development |
26985294 |
114 |
Design and Synthesis of Nonpeptide Inhibitors of Hepatocyte Growth Factor Activation.![EBI](/images/logo_chembl.png) |
Southern Research |
27073051 |
71 |
Orally bioavailable pyridine and pyrimidine-based Factor XIa inhibitors: Discovery of the methyl N-phenyl carbamate P2 prime group.![EBI](/images/logo_chembl.png) |
Bristol-Myers Squibb |
26732532 |
69 |
Active site-directed plasmin inhibitors: Extension on the P2 residue.![EBI](/images/logo_chembl.png) |
Kobe Gakuin University |
26704266 |
80 |
Novel phenylalanine derived diamides as Factor XIa inhibitors.![EBI](/images/logo_chembl.png) |
Bristol-Myers Squibb |
26421993 |
44 |
Structure-guided discovery of 2-aryl/pyridin-2-yl-1H-indole derivatives as potent and selective hepsin inhibitors.![EBI](/images/logo_chembl.png) |
Aurigene Discovery Technologies |
26367391 |
6 |
Phenylalanine and Phenylglycine Analogues as Arginine Mimetics in Dengue Protease Inhibitors.![EBI](/images/logo_chembl.png) |
Heidelberg University |
26393374 |
34 |
Improving the Selectivity of Engineered Protease Inhibitors: Optimizing the P2 Prime Residue Using a Versatile Cyclic Peptide Library.![EBI](/images/logo_chembl.png) |
Queensland University of Technology |
26114810 |
8 |
Synthesis of 3,4-diaminobenzoyl derivatives as factor Xa inhibitors.![EBI](/images/logo_chembl.png) |
Southeast University |
26122211 |
3 |
Discovery of non-competitive thrombin inhibitor derived from competitive tryptase inhibitor skeleton: Shift in molecular recognition resulted from skeletal conversion of carboxylate into phosphonate.![EBI](/images/logo_chembl.png) |
Tokyo University of Pharmacy and Life Sciences |
25592713 |
37 |
Pyridine and pyridinone-based factor XIa inhibitors.![EBI](/images/logo_chembl.png) |
Bristol-Myers Squibb |
26151189 |
56 |
Structure-Based Design of Macrocyclic Coagulation Factor VIIa Inhibitors.![EBI](/images/logo_chembl.png) |
TBA |
26005539 |
23 |
Discovery of a Potent Parenterally Administered Factor XIa Inhibitor with Hydroxyquinolin-2(1H)-one as the P2' Moiety.![EBI](/images/logo_chembl.png) |
Bristol-Myers Squibb |
25782055 |
9 |
Discovery of a Cyclic Boronic Acidß-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases.![EBI](/images/logo_chembl.png) |
Rempex Pharmaceuticals |
25881820 |
62 |
Design and synthesis of potent, selective phenylimidazole-based FVIIa inhibitors.![EBI](/images/logo_chembl.png) |
Bristol-Myers Squibb R & D |
25728130 |
79 |
Structure-based design of inhibitors of coagulation factor XIa with novel P1 moieties.![EBI](/images/logo_chembl.png) |
Bristol-Myers Squibb |
24951330 |
25 |
Orally bioavailable factor Xa inhibitors containing alpha-substituted gem-dimethyl P4 moieties.![EBI](/images/logo_chembl.png) |
Bristol-Myers Squibb |
25523211 |
18 |
Identification of potent orally active factor Xa inhibitors based on conjugation strategy and application of predictable fragment recommender system.![EBI](/images/logo_chembl.png) |
Astellas Pharma |
25438755 |
9 |
Novel strategy to boost oral anticoagulant activity of blood coagulation enzyme inhibitors based on biotransformation into hydrophilic conjugates.![EBI](/images/logo_chembl.png) |
Astellas Pharma |
25405503 |
109 |
Phenylimidazoles as potent and selective inhibitors of coagulation factor XIa with in vivo antithrombotic activity.![EBI](/images/logo_chembl.png) |
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](/images/logo_chembl.png) |
Chinese Academy of Sciences |
23586812 |
38 |
Development of a selective peptide macrocycle inhibitor of coagulation factor XII toward the generation of a safe antithrombotic therapy.![EBI](/images/logo_chembl.png) |
Ecole Polytechnique F�D�Rale De Lausanne Epfl |
23294255 |
114 |
Development of new cyclic plasmin inhibitors with excellent potency and selectivity.![EBI](/images/logo_chembl.png) |
Philipps University Marburg |
10602702 |
22 |
Simple linear QSAR models based on quantum similarity measures.![EBI](/images/logo_chembl.png) |
Czech Academy of Sciences |
12565961 |
177 |
Structure-activity relationships of substituted benzothiophene-anthranilamide factor Xa inhibitors.![EBI](/images/logo_chembl.png) |
Berlex Biosciences |
22726924 |
14 |
Discovery of benzothiazole guanidines as novel inhibitors of thrombin and trypsin IV.![EBI](/images/logo_chembl.png) |
Astrazeneca |
16250649 |
10 |
Selective inhibitors of the serine protease plasmin: probing the S3 and S3' subsites using a combinatorial library.![EBI](/images/logo_chembl.png) |
Brown University |
15887966 |
58 |
Synthesis and structure-activity relationships of novel selective factor Xa inhibitors with a tetrahydroisoquinoline ring.![EBI](/images/logo_chembl.png) |
Central Pharmaceutical Research Institute |
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](/images/logo_chembl.png) |
Pharmaceutical Research Institute |
12930148 |
41 |
Potent, small-molecule inhibitors of human mast cell tryptase. Antiasthmatic action of a dipeptide-based transition-state analogue containing a benzothiazole ketone.![EBI](/images/logo_chembl.png) |
Johnson & Johnson Pharmaceutical Research & Development |
12904065 |
30 |
Efficacious and orally bioavailable thrombin inhibitors based on a 2,5-thienylamidine at the P1 position: discovery of N-carboxymethyl-d-diphenylalanyl-l-prolyl[(5-amidino-2-thienyl)methyl]amide.![EBI](/images/logo_chembl.png) |
Lg Life Sciences |
12190311 |
37 |
Discovery of further pyrrolidine trans-lactams as inhibitors of human neutrophil elastase (HNE) with potential as development candidates and the crystal structure of HNE complexed with an inhibitor (GW475151).![EBI](/images/logo_chembl.png) |
Gsk |
12036356 |
234 |
Design, synthesis, and activity of a novel series of factor Xa inhibitors: optimization of arylamidine groups.![EBI](/images/logo_chembl.png) |
Berlex Biosciences |
12036355 |
36 |
Simple, intuitive calculations of free energy of binding for protein-ligand complexes. 1. Models without explicit constrained water.![EBI](/images/logo_chembl.png) |
University of Parma |
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](/images/logo_chembl.png) |
Dupont Pharmaceuticals |
10794696 |
233 |
Protease inhibitors: synthesis and QSAR study of novel classes of nonbasic thrombin inhibitors incorporating sulfonylguanidine and O-methylsulfonylisourea moieties at P1.![EBI](/images/logo_chembl.png) |
Universit£ |
10669559 |
180 |
Protease inhibitors: current status and future prospects.![EBI](/images/logo_chembl.png) |
University of Queensland |
10956211 |
14 |
GRID/CPCA: a new computational tool to design selective ligands.![EBI](/images/logo_chembl.png) |
Boehringer Ingelheim Pharma |
10425086 |
83 |
Design and synthesis of isoxazoline derivatives as factor Xa inhibitors. 1.![EBI](/images/logo_chembl.png) |
Dupont Pharmaceuticals |
9464370 |
28 |
Discovery and development of the novel potent orally active thrombin inhibitor N-(9-hydroxy-9-fluorenecarboxy)prolyl trans-4-aminocyclohexylmethyl amide (L-372,460): coapplication of structure-based design and rapid multiple analogue synthesis on solid support.![EBI](/images/logo_chembl.png) |
Merck Research Laboratories |
9836616 |
92 |
Tetrahydro-isoquinoline-based factor Xa inhibitors.![EBI](/images/logo_chembl.png) |
Boehringer Mannheim |
9083470 |
9 |
Design of highly potent noncovalent thrombin inhibitors that utilize a novel lipophilic binding pocket in the thrombin active site.![EBI](/images/logo_chembl.png) |
Merck Research Laboratories |
9357536 |
47 |
Synthesis of a series of potent and orally bioavailable thrombin inhibitors that utilize 3,3-disubstituted propionic acid derivatives in the P3 position.![EBI](/images/logo_chembl.png) |
Merck Research Laboratories |
2319567 |
29 |
Analogues of 1,5-bis(4-amidinophenoxy)pentane (pentamidine) in the treatment of experimental Pneumocystis carinii pneumonia.![EBI](/images/logo_chembl.png) |
University of North Carolina |
15081015 |
91 |
Solid-phase synthesis and SAR of 4-carboxy-2-azetidinone mechanism-based tryptase inhibitors.![EBI](/images/logo_chembl.png) |
The Bristol-Myers Squibb Pharmaceutical Research Institute |
12873514 |
56 |
Design and synthesis of potent and selective macrocyclic thrombin inhibitors.![EBI](/images/logo_chembl.png) |
Merck Research Laboratories |
11858993 |
60 |
Novel, potent non-covalent thrombin inhibitors incorporating p(3)-lactam scaffolds.![EBI](/images/logo_chembl.png) |
Corvas International |
10698459 |
41 |
The de novo design and synthesis of cyclic urea inhibitors of factor Xa: optimization of the S4 ligand.![EBI](/images/logo_chembl.png) |
Dupont Pharmaceuticals |
10915051 |
43 |
The design and synthesis of thrombin inhibitors: analogues of MD805 containing non-polar surrogates for arginine at the P1 position.![EBI](/images/logo_chembl.png) |
Novartis Horsham Research Centre |
10201829 |
9 |
1-Aminoisoquinoline as benzamidine isoster in the design and synthesis of orally active thrombin inhibitors.![EBI](/images/logo_chembl.png) |
Nv Organon |
10522702 |
26 |
Design, synthesis and testing of amino-bicycloaryl based orally bioavailable thrombin inhibitors.![EBI](/images/logo_chembl.png) |
Nv Organon |
10498204 |
25 |
Aminoisoquinolines: design and synthesis of an orally active benzamidine isostere for the inhibition of factor XA.![EBI](/images/logo_chembl.png) |
Rh£Ne-Poulenc Rorer |
9873373 |
20 |
Peptidyl beta-homo-aspartals: specific inhibitors of interleukin-1 beta converting enzyme and its homologues (caspases).![EBI](/images/logo_chembl.png) |
Institute For Drug Research |
| 24 |
L-373,890, An achiral, noncovalent, subnanomolar thrombin inhibitor![EBI](/images/logo_chembl.png) |
TBA |
| 43 |
S1 heterocyclic thrombin inhibitors![EBI](/images/logo_chembl.png) |
TBA |
19841155 |
29 |
MK-7009, a potent and selective inhibitor of hepatitis C virus NS3/4A protease.![EBI](/images/logo_chembl.png) |
Merck Research Laboratories |
| 15 |
Rational design, synthesis, and serine protease inhibitory activity of a novel P1-argininal derivative featuring a conformationally constrained P2–P3 bicyclic lactam moiety![EBI](/images/logo_chembl.png) |
TBA |
| 37 |
Synthesis and biological activity of P2–P4 azapeptidomimetic P1-argininal and P1-ketoargininamide derivatives: a novel class of serine protease inhibitors![EBI](/images/logo_chembl.png) |
TBA |
| 32 |
Bisbenzamidine isoxazoline derivatives as factor Xa inhibitors![EBI](/images/logo_chembl.png) |
TBA |
| 27 |
Rational design and synthesis of a novel, selective class of thrombin inhibitors: P1-argininal derivatives incorporating P3---P4 quaternary lactam dipeptide surrogates![EBI](/images/logo_chembl.png) |
TBA |
| 44 |
Biaryl substituted alkylboronate esters as thrombin inhibitors![EBI](/images/logo_chembl.png) |
TBA |
| 3 |
An efficient preparation of the potent and selective pseudopeptide thrombin inhibitor, inogatran![EBI](/images/logo_chembl.png) |
TBA |
| 25 |
Design and synthesis of a novel class of thrombin inhibitors incorporating heterocyclic dipeptide surrogates![EBI](/images/logo_chembl.png) |
TBA |
| 15 |
RATIONAL DESIGN, SYNTHESIS, AND SERINE PROTEASE INHIBITORY ACTIVITY OF NOVEL P1-ARGININOYL HETEROCYCLES![EBI](/images/logo_chembl.png) |
TBA |
| 78 |
Synthesis and evaluation of 2-aryl-4H-3,1-benzoxazin-4-ones as C1r serine protease inhibitors![EBI](/images/logo_chembl.png) |
TBA |
| 61 |
(N-acyl-N-alkyl)glycyl borolysine analogs: A new class of potent thrombin inhibitors![EBI](/images/logo_chembl.png) |
TBA |
16759084 |
12 |
Isatin compounds as noncovalent SARS coronavirus 3C-like protease inhibitors.![EBI](/images/logo_chembl.png) |
Peking University |
16137886 |
88 |
Development of an oxazolopyridine series of dual thrombin/factor Xa inhibitors via structure-guided lead optimization.![EBI](/images/logo_chembl.png) |
Merck Research Laboratories |
15801822 |
28 |
9-hydroxyazafluorenes and their use in thrombin inhibitors.![EBI](/images/logo_chembl.png) |
Merck Research Laboratories |
15501047 |
75 |
Chlorothiophenecarboxamides as P1 surrogates of inhibitors of blood coagulation factor Xa.![EBI](/images/logo_chembl.png) |
Merck |
15341970 |
59 |
P4 and P1' optimization of bicycloproline P2 bearing tetrapeptidyl alpha-ketoamides as HCV protease inhibitors.![EBI](/images/logo_chembl.png) |
Eli Lilly |
15203158 |
84 |
Halothiophene benzimidazoles as P1 surrogates of inhibitors of blood coagulation factor Xa.![EBI](/images/logo_chembl.png) |
Merck |
15149645 |
92 |
Interaction with the S1 beta-pocket of urokinase: 8-heterocycle substituted and 6,8-disubstituted 2-naphthamidine urokinase inhibitors.![EBI](/images/logo_chembl.png) |
Abbott Laboratories |
15149641 |
44 |
A novel series of potent and selective small molecule inhibitors of the complement component C1s.![EBI](/images/logo_chembl.png) |
3-Dimensional Pharmaceuticals |
15081014 |
35 |
Synthesis of potent and highly selective nonguanidine azetidinone inhibitors of human tryptase.![EBI](/images/logo_chembl.png) |
The Bristol-Myers Squibb Pharmaceutical Research Institute |
15080981 |
72 |
N,N-Dialkylated 4-(4-arylsulfonylpiperazine-1-carbonyl)-benzamidines and 4-((4-arylsulfonyl)-2-oxo-piperazin-1-ylmethyl)-benzamidines as potent factor Xa inhibitors.![EBI](/images/logo_chembl.png) |
Millennium Pharmaceuticals |
15013007 |
319 |
Design, synthesis, and SAR of anthranilamide-based factor Xa inhibitors with improved functional activity.![EBI](/images/logo_chembl.png) |
Millennium Pharmaceuticals |
15013006 |
69 |
Design, synthesis, and SAR of anthranilamide-based factor Xa inhibitors incorporating substituted biphenyl P4 motifs.![EBI](/images/logo_chembl.png) |
Millennium Pharmaceuticals |
15006404 |
56 |
Thrombin inhibitors built on an azaphenylalanine scaffold.![EBI](/images/logo_chembl.png) |
University of Ljubljana |
14980671 |
78 |
1-(2-Naphthyl)-1H-pyrazole-5-carboxylamides as potent factor Xa inhibitors. Part 3: Design, synthesis and SAR of orally bioavailable benzamidine-P4 inhibitors.![EBI](/images/logo_chembl.png) |
Millennium Pharmaceuticals |
14980670 |
107 |
1-(2-Naphthyl)-1H-pyrazole-5-carboxylamides as potent factor Xa inhibitors. Part 2: A survey of P4 motifs.![EBI](/images/logo_chembl.png) |
Millennium Pharmaceuticals |
14761180 |
31 |
Inhibitors of serine proteases as potential therapeutic agents: the road from thrombin to tryptase to cathepsin G.![EBI](/images/logo_chembl.png) |
Johnson & Johnson Pharmaceutical Research & Development |
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.![EBI](/images/logo_chembl.png) |
Abbott Laboratories |
14698147 |
60 |
Synthesis of potent and selective 2-azepanone inhibitors of human tryptase.![EBI](/images/logo_chembl.png) |
The Bristol-Myers Squibb Pharmaceutical Research Institute |
14505652 |
45 |
Unexpected enhancement of thrombin inhibitor potency with o-aminoalkylbenzylamides in the P1 position.![EBI](/images/logo_chembl.png) |
Merck Research Laboratories |
12824026 |
14 |
Structure-based drug design of pyrazinone antithrombotics as selective inhibitors of the tissue factor VIIa complex.![EBI](/images/logo_chembl.png) |
Pharmacia |
12824020 |
31 |
Heterocyclic thrombin inhibitors. Part 1: design and synthesis of amidino-phenoxy quinoline derivatives.![EBI](/images/logo_chembl.png) |
Boehringer Ingelheim Pharma |
12668020 |
29 |
Oxyguanidines: application to non-peptidic phenyl-based thrombin inhibitors.![EBI](/images/logo_chembl.png) |
3-Dimensional Pharmaceuticals |
12668008 |
34 |
3-amino-4-sulfonylpyridinone acetamide and related pyridothiadiazine thrombin inhibitors.![EBI](/images/logo_chembl.png) |
Merck Research Laboratories |
12643903 |
81 |
Nonbenzamidine isoxazoline derivatives as factor Xa inhibitors.![EBI](/images/logo_chembl.png) |
Bristol-Myers Squibb |
12639567 |
135 |
Design, synthesis, and structure-activity relationships of unsubstituted piperazinone-based transition state factor Xa inhibitors.![EBI](/images/logo_chembl.png) |
Millennium Pharmaceuticals |
12617893 |
28 |
Azaindoles: moderately basic P1 groups for enhancing the selectivity of thrombin inhibitors.![EBI](/images/logo_chembl.png) |
Merck Research Laboratories |
12617892 |
43 |
Novel thrombin inhibitors incorporating non-basic partially saturated heterobicyclic P1-arginine mimetics.![EBI](/images/logo_chembl.png) |
University of Ljubljana |
12593666 |
30 |
Structure-activity relationship study and drug profile of N-(4-fluorophenylsulfonyl)-L-valyl-L-leucinal (SJA6017) as a potent calpain inhibitor.![EBI](/images/logo_chembl.png) |
Senju Pharmaceutical |
12593648 |
53 |
Discovery of an orally efficacious inhibitor of coagulation factor Xa which incorporates a neutral P1 ligand.![EBI](/images/logo_chembl.png) |
Aventis Pharmaceuticals |
12570369 |
60 |
Metabolism-directed optimization of 3-aminopyrazinone acetamide thrombin inhibitors. Development of an orally bioavailable series containing P1 and P3 pyridines.![EBI](/images/logo_chembl.png) |
Merck Research Laboratories |
12565931 |
37 |
Nonbenzamidine tetrazole derivatives as factor Xa inhibitors.![EBI](/images/logo_chembl.png) |
Bristol-Myers Squibb |
12482444 |
38 |
Design and synthesis of factor Xa inhibitors and their prodrugs.![EBI](/images/logo_chembl.png) |
Millennium Pharmaceuticals |
12482415 |
30 |
Small, low nanomolar, noncovalent thrombin inhibitors lacking a group to fill the 'distal binding pocket'.![EBI](/images/logo_chembl.png) |
Merck Research Laboratories |
12113838 |
36 |
Substituted acrylamides as factor Xa inhibitors: improving bioavailability by P1 modification.![EBI](/images/logo_chembl.png) |
Millennium Pharmaceuticals |
12039587 |
39 |
Optimization of the beta-aminoester class of factor Xa inhibitors. Part 2: Identification of FXV673 as a potent and selective inhibitor with excellent In vivo anticoagulant activity.![EBI](/images/logo_chembl.png) |
Aventis Pharmaceuticals |
12039586 |
42 |
Optimization of the beta-aminoester class of factor Xa inhibitors. Part 1: P(4) and side-chain modifications for improved in vitro potency.![EBI](/images/logo_chembl.png) |
Aventis Pharmaceuticals |
12039584 |
59 |
Design, synthesis, and SAR of monobenzamidines and aminoisoquinolines as factor Xa inhibitors.![EBI](/images/logo_chembl.png) |
Millennium Pharmaceuticals |
12039583 |
140 |
Design, synthesis and biological activity of novel non-amidine factor Xa inhibitors. Part 1: P(1) structure-activity relationships of the substituted 1-(2-Naphthyl)-1H-pyrazole-5-carboxylamides.![EBI](/images/logo_chembl.png) |
Millennium Pharmaceuticals |
12036353 |
38 |
Design of selective thrombin inhibitors based on the (R)-Phe-Pro-Arg sequence.![EBI](/images/logo_chembl.png) |
Pfizer |
12031331 |
48 |
Design, synthesis, and SAR of substituted acrylamides as factor Xa inhibitors.![EBI](/images/logo_chembl.png) |
Millennium Pharmaceuticals |
11965378 |
78 |
Benzimidazole-based fXa inhibitors with improved thrombin and trypsin selectivity.![EBI](/images/logo_chembl.png) |
Berlex Biosciences |
11960487 |
30 |
Structure-based design of novel potent nonpeptide thrombin inhibitors.![EBI](/images/logo_chembl.png) |
Boehringer Ingelheim Pharma |
11958994 |
31 |
Benzimidazoles and isosteric compounds as potent and selective factor Xa inhibitors.![EBI](/images/logo_chembl.png) |
Aventis Pharmaceuticals |
11934589 |
57 |
Non-covalent thrombin inhibitors featuring P(3)-heterocycles with P(1)-monocyclic arginine surrogates.![EBI](/images/logo_chembl.png) |
Corvas International |
11844691 |
107 |
4-amidinobenzylamine-based inhibitors of urokinase.![EBI](/images/logo_chembl.png) |
Universitat Jena |
11689072 |
49 |
Exploiting subsite S1 of trypsin-like serine proteases for selectivity: potent and selective inhibitors of urokinase-type plasminogen activator.![EBI](/images/logo_chembl.png) |
Axys Pharmaceuticals |
11677132 |
65 |
Design, synthesis, and SAR of amino acid derivatives as factor Xa inhibitors.![EBI](/images/logo_chembl.png) |
Cor Therapeutics |
11549459 |
5 |
Synthesis and evaluation of the sunflower derived trypsin inhibitor as a potent inhibitor of the type II transmembrane serine protease, matriptase.![EBI](/images/logo_chembl.png) |
National Cancer Institute-Frederick |
11527714 |
66 |
Design and synthesis of glycolic and mandelic acid derivatives as factor Xa inhibitors.![EBI](/images/logo_chembl.png) |
Cor Therapeutics |
11527709 |
19 |
Optimization of a screening lead for factor VIIa/TF.![EBI](/images/logo_chembl.png) |
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.![EBI](/images/logo_chembl.png) |
Axys Pharmaceuticals |
11459634 |
94 |
Development of potent and selective factor Xa inhibitors.![EBI](/images/logo_chembl.png) |
Axys Pharmaceuticals |
11425524 |
62 |
Dibasic inhibitors of human mast cell tryptase. Part 3: identification of a series of potent and selective inhibitors containing the benzamidine functionality.![EBI](/images/logo_chembl.png) |
Axys Pharmaceuticals |
32340773 |
110 |
Design and synthesis of novel proline based factor XIa selective inhibitors as leads for potential new anticoagulants.![EBI](/images/logo_chembl.png) |
Merck |
11378359 |
57 |
Structure-based design, synthesis and SAR of a novel series of thiopheneamidine urokinase plasminogen activator inhibitors.![EBI](/images/logo_chembl.png) |
3-Dimensional Pharmaceuticals |
32605372 |
92 |
A New Class of Dengue and West Nile Virus Protease Inhibitors with Submicromolar Activity in Reporter Gene DENV-2 Protease and Viral Replication Assays.![EBI](/images/logo_chembl.png) |
Heidelberg University |
32150407 |
27 |
Discovery of Cyclic Boronic Acid QPX7728, an Ultrabroad-Spectrum Inhibitor of Serine and Metallo-?-lactamases.![EBI](/images/logo_chembl.png) |
Qpex Biopharma |
11266180 |
74 |
The design of phenylglycine containing benzamidine carboxamides as potent and selective inhibitors of factor Xa.![EBI](/images/logo_chembl.png) |
Prosthetics Molecular Design |
11266160 |
57 |
Synthesis and SAR of benzamidine factor Xa inhibitors containing a vicinally-substituted heterocyclic core.![EBI](/images/logo_chembl.png) |
Dupont Pharmaceuticals |
11212109 |
14 |
The identification of alpha-ketoamides as potent inhibitors of hepatitis C virus NS3-4A proteinase.![EBI](/images/logo_chembl.png) |
Roche Discover Welwyn |
11212093 |
21 |
Potent and selective bicyclic lactam inhibitors of thrombin. Part 4: transition state inhibitors.![EBI](/images/logo_chembl.png) |
Biochem Pharma |
11087565 |
86 |
Design, synthesis, and biological evaluation of potent and selective amidino bicyclic factor Xa inhibitors.![EBI](/images/logo_chembl.png) |
Dupont Pharmaceuticals |
11078188 |
20 |
1-Oxacephem-based human chymase inhibitors: discovery of stable inhibitors in human plasma.![EBI](/images/logo_chembl.png) |
Shionogi |
11063603 |
53 |
Rational design, synthesis, and biological activity of benzoxazinones as novel factor Xa inhibitors.![EBI](/images/logo_chembl.png) |
Pfizer |
11055356 |
236 |
Dibasic inhibitors of human mast cell tryptase. Part 2: structure-activity relationships and requirements for potent activity.![EBI](/images/logo_chembl.png) |
Axys Pharmaceuticals |
11055355 |
72 |
Dibasic inhibitors of human mast cell tryptase. Part 1: synthesis and optimization of a novel class of inhibitors.![EBI](/images/logo_chembl.png) |
Axys Pharmaceuticals |
11055344 |
37 |
Novel, potent and selective chimeric FXa inhibitors featuring hydrophobic P1-ketoamide moieties.![EBI](/images/logo_chembl.png) |
Corvas International |
10937736 |
35 |
Nonbenzamidine compounds as selective factor Xa inhibitors.![EBI](/images/logo_chembl.png) |
Aventis Pharmaceuticals |
10915052 |
20 |
The design and synthesis of thrombin inhibitors: the introduction of in vivo efficacy and oral bioavailability into benzthiazolylalanine inhibitors.![EBI](/images/logo_chembl.png) |
Novartis Horsham Research Centre |
27434175 |
54 |
Substrate-Guided Design of Selective FXIIa Inhibitors Based on the Plant-Derived Momordica cochinchinensis Trypsin Inhibitor-II (MCoTI-II) Scaffold.![EBI](/images/logo_chembl.png) |
The University of Queensland |
10866385 |
13 |
Mass spectrometry reveals elastase inhibitors from the reactive centre loop of alpha1-antitrypsin.![EBI](/images/logo_chembl.png) |
The Oxford Centre For Molecular Sciences |
10853668 |
52 |
Design, synthesis, and in vitro biological activity of indole-based factor Xa inhibitors.![EBI](/images/logo_chembl.png) |
Berlex Biosciences |
27476144 |
94 |
Trypsin inhibitors for the treatment of pancreatitis.![EBI](/images/logo_chembl.png) |
Novartis Pharma |
10843219 |
20 |
Bicyclic pyridones as potent, efficacious and orally bioavailable thrombin inhibitors.![EBI](/images/logo_chembl.png) |
Merck Research Laboratories |
27347787 |
32 |
Macrocyclic Prodrugs of a Selective Nonpeptidic Direct Thrombin Inhibitor Display High Permeability, Efficient Bioconversion but Low Bioavailability.![EBI](/images/logo_chembl.png) |
Astrazeneca |
27280436 |
304 |
Optimization of Cyclic Plasmin Inhibitors: From Benzamidines to Benzylamines.![EBI](/images/logo_chembl.png) |
Philipps University Marburg |
10782677 |
73 |
Guanylpiperidine peptidomimetics: potent and selective bis-cation inhibitors of factor Xa.![EBI](/images/logo_chembl.png) |
Corvas International |
10698439 |
68 |
Amido-(propyl and allyl)-hydroxybenzamidines: development of achiral inhibitors of factor Xa.![EBI](/images/logo_chembl.png) |
Rhone-Poulenc Rorer |
10669563 |
7 |
Structural basis of the thrombin selectivity of a ligand that contains the constrained arginine mimic (2S)-2-amino-(3S)-3-(1-carbamimidoyl- piperidin-3-yl)-propanoic acid at P1.![EBI](/images/logo_chembl.png) |
Warner-Lambert |
31679971 |
44 |
6-Substituted amiloride derivatives as inhibitors of the urokinase-type plasminogen activator for use in metastatic disease.![EBI](/images/logo_chembl.png) |
University of Wollongong |
10617091 |
73 |
Exploratory solid-phase synthesis of factor Xa inhibitors: discovery and application of p3-heterocyclic amides as novel types of non-basic arginine surrogates.![EBI](/images/logo_chembl.png) |
Corvas International |
10509929 |
116 |
Synthesis, SAR and in vivo activity of novel thienopyridine sulfonamide pyrrolidinones as factor Xa inhibitors.![EBI](/images/logo_chembl.png) |
RhôNe-Poulenc Rorer |
10498211 |
42 |
Novel benzo-fused lactam scaffolds as factor Xa inhibitors.![EBI](/images/logo_chembl.png) |
Corvas International |
10498197 |
58 |
The design of potent and selective inhibitors of thrombin utilizing a piperazinedione template: part 2.![EBI](/images/logo_chembl.png) |
Warner-Lambert |
10498196 |
42 |
The design of potent and selective inhibitors of thrombin utilizing a piperazinedione template: part 1.![EBI](/images/logo_chembl.png) |
Warner-Lambert |
31445854 |
43 |
Structure based design of macrocyclic factor XIa inhibitors: Discovery of cyclic P1 linker moieties with improved oral bioavailability.![EBI](/images/logo_chembl.png) |
Bristol-Myers Squibb |
31395511 |
29 |
Structure-activity analysis of peptidic Chlamydia HtrA inhibitors.![EBI](/images/logo_chembl.png) |
University of Otago |
10425106 |
12 |
4-Heterocyclohexanone-based inhibitors of the serine protease plasmin.![EBI](/images/logo_chembl.png) |
Brown University |
10425087 |
110 |
Design and synthesis of isoxazoline derivatives as factor Xa inhibitors. 2.![EBI](/images/logo_chembl.png) |
Dupont Pharmaceuticals |
10397495 |
49 |
Thrombin inhibitors based on [5,5] trans-fused indane lactams.![EBI](/images/logo_chembl.png) |
Glaxo Wellcome Research and Development |
10328312 |
27 |
Preparation of pyrrolidine and isoxazolidine benzamidines as potent inhibitors of coagulation factor Xa.![EBI](/images/logo_chembl.png) |
Dupont Pharmaceuticals |
10328293 |
23 |
The discovery of orally available thrombin inhibitors: optimisation of the P1 pharmacophore.![EBI](/images/logo_chembl.png) |
Novartis Horsham Research Centre |
10230612 |
22 |
Design and synthesis of potent and selective 5,6-fused heterocyclic thrombin inhibitors.![EBI](/images/logo_chembl.png) |
Dupont Pharmaceuticals |
10206557 |
36 |
Investigation of the S3 site of thrombin: design, synthesis and biological activity of 4-substituted 3-amino-2-pyridones incorporating P1-argininals.![EBI](/images/logo_chembl.png) |
Corvas International |
10206546 |
27 |
Potent and selective bicyclic lactam inhibitors of thrombin: Part 3: P1' modifications.![EBI](/images/logo_chembl.png) |
Warner-Lambert |
10206542 |
50 |
Benzenesulfonamide derivatives of 2-substituted 4H-3,1-benzoxazin-4-ones and benzthiazin-4-ones as inhibitors of complement C1r protease.![EBI](/images/logo_chembl.png) |
Warner-Lambert |
30446438 |
36 |
Design, synthesis and biological evaluation of anthranilamide derivatives as potential factor Xa (fXa) inhibitors.![EBI](/images/logo_chembl.png) |
China Pharmaceutical University |
10091694 |
90 |
Symmetrical anhydride-type serine protease inhibitors: structure-activity relationship studies of human chymase inhibitors.![EBI](/images/logo_chembl.png) |
Nippon Steel |
9934495 |
26 |
Alkoxide-catalyzed ring-opening of a novel homosaccharin derivative: synthesis of potent, selective P3-lactam thrombin inhibitors containing P4-o-alkoxycarbonylbenzylsulfonamide residues.![EBI](/images/logo_chembl.png) |
Corvas International |
9873743 |
13 |
Potent and selective bicyclic lactam inhibitors of thrombin: Part 2: P1 modifications.![EBI](/images/logo_chembl.png) |
Warner-Lambert |
9873692 |
54 |
Preparation of meta-amidino-N,N-disubstituted anilines as potent inhibitors of coagulation factor Xa.![EBI](/images/logo_chembl.png) |
Dupont Pharmaceuticals |
9873654 |
37 |
5,5-trans lactone-containing inhibitors of serine proteases: identification of a novel, acylating thrombin inhibitor.![EBI](/images/logo_chembl.png) |
Glaxo Wellcome Research and Development |
9873607 |
21 |
The de novo design and synthesis of cyclic urea inhibitors of factor Xa: initial SAR studies.![EBI](/images/logo_chembl.png) |
Dupont Pharmaceuticals |
9873569 |
16 |
Design and construction of novel thrombin inhibitors featuring P3-P4 quaternary lactam dipeptide surrogates.![EBI](/images/logo_chembl.png) |
Corvas International |
9873535 |
13 |
Highly efficient and versatile synthesis of libraries of constrained beta-strand mimetics.![EBI](/images/logo_chembl.png) |
Molecumetics |
9873422 |
16 |
C6 modification of the pyridinone core of thrombin inhibitor L-374,087 as a means of enhancing its oral absorption.![EBI](/images/logo_chembl.png) |
Merck Research Laboratories |
9873418 |
16 |
Identification and SAR for a selective, nonpeptidyl thrombin inhibitor.![EBI](/images/logo_chembl.png) |
Merck Research Laboratories |
31833761 |
32 |
Potent, Orally Bioavailable, and Efficacious Macrocyclic Inhibitors of Factor XIa. Discovery of Pyridine-Based Macrocycles Possessing Phenylazole Carboxamide P1 Groups.![EBI](/images/logo_chembl.png) |
Bristol-Myers Squibb |
9871573 |
15 |
Discovery of LB30057, a benzamidrazone-based selective oral thrombin inhibitor.![EBI](/images/logo_chembl.png) |
Biotech Research Institute |
9871547 |
15 |
L-374,087, an efficacious, orally bioavailable, pyridinone acetamide thrombin inhibitor.![EBI](/images/logo_chembl.png) |
Merck Research Laboratories |
9871540 |
100 |
Pyrazoles, 1,2,4-triazoles, and tetrazoles as surrogates for cis-amide bonds in boronate ester thrombin inhibitors.![EBI](/images/logo_chembl.png) |
Dupont Pharmaceuticals |
30830783 |
13 |
Potential Anticancer Agents Characterized from Selected Tropical Plants.![EBI](/images/logo_chembl.png) |
The Ohio State University |
31103899 |
15 |
Synthesis and structure-activity relationships of small-molecular di-basic esters, amides and carbamates as flaviviral protease inhibitors.![EBI](/images/logo_chembl.png) |
Heidelberg University |
9822554 |
14 |
1,2-Benzisothiazol-3-one 1,1-dioxide inhibitors of human mast cell tryptase.![EBI](/images/logo_chembl.png) |
Bristol-Myers Squibb Pharmaceutical Research Institute |
9804686 |
16 |
Efficacious, orally bioavailable thrombin inhibitors based on 3-aminopyridinone or 3-aminopyrazinone acetamide peptidomimetic templates.![EBI](/images/logo_chembl.png) |
Merck Research Laboratories |
9703466 |
35 |
Design and synthesis of a series of potent and orally bioavailable noncovalent thrombin inhibitors that utilize nonbasic groups in the P1 position.![EBI](/images/logo_chembl.png) |
Merck Research Laboratories |
9484495 |
74 |
Identification and initial structure-activity relationships of a novel class of nonpeptide inhibitors of blood coagulation factor Xa.![EBI](/images/logo_chembl.png) |
Collegeville |
9438022 |
55 |
Rational design and synthesis of novel, potent bis-phenylamidine carboxylate factor Xa inhibitors.![EBI](/images/logo_chembl.png) |
Dupont Pharmaceuticals |
9379436 |
46 |
Orally active trifluoromethyl ketone inhibitors of human leukocyte elastase.![EBI](/images/logo_chembl.png) |
Zeneca Pharmaceuticals |
30613336 |
32 |
Potent, Selective, and Cell-Penetrating Inhibitors of Kallikrein-Related Peptidase 4 Based on the Cyclic Peptide MCoTI-II.![EBI](/images/logo_chembl.png) |
The University of Queensland |
9171866 |
12 |
Potent noncovalent thrombin inhibitors that utilize the unique amino acid D-dicyclohexylalanine in the P3 position. Implications on oral bioavailability and antithrombotic efficacy.![EBI](/images/logo_chembl.png) |
Merck Research Laboratories |
30833107 |
18 |
3-Acyltetramic acids as a novel class of inhibitors for human kallikreins 5 and 7.![EBI](/images/logo_chembl.png) |
Universidade Federal Fluminense |
31563807 |
63 |
Discovery of novel, potent, isosteviol-based antithrombotic agents.![EBI](/images/logo_chembl.png) |
Peking University |
8917639 |
50 |
Design, synthesis, and evolution of a novel, selective, and orally bioavailable class of thrombin inhibitors: P1-argininal derivatives incorporating P3-P4 lactam sulfonamide moieties.![EBI](/images/logo_chembl.png) |
Corvas International |
31413811 |
26 |
Iterative Optimization of the Cyclic Peptide SFTI-1 Yields Potent Inhibitors of Neutrophil Proteinase 3.![EBI](/images/logo_chembl.png) |
The University of Queensland |
8426361 |
111 |
Highly selective tripeptide thrombin inhibitors.![EBI](/images/logo_chembl.png) |
Eli Lilly |
24261937 |
6 |
Protease inhibitors from Microcystis aeruginosa bloom material collected from the Dalton Reservoir, Israel.![EBI](/images/logo_chembl.png) |
Tel-Aviv University |
8035417 |
23 |
Retro-binding tripeptide thrombin active-site inhibitors: discovery, synthesis, and molecular modeling.![EBI](/images/logo_chembl.png) |
Bristol-Myers Squibb Pharmaceutical Research Institute |
23777401 |
4 |
Aeruginosins from a Microcystis sp. bloom material collected in Varanasi, India.![EBI](/images/logo_chembl.png) |
Tel-Aviv University |
23718637 |
1 |
Metabolites from Microcystis aeruginosa bloom material collected at a water reservoir near Kibbutz Hafetz Haim, Israel.![EBI](/images/logo_chembl.png) |
Tel-Aviv University |
7629790 |
32 |
New orally active serine protease inhibitors.![EBI](/images/logo_chembl.png) |
Minase Research Institute |
7562936 |
10 |
Synthesis of tight binding inhibitors and their action on the proprotein-processing enzyme furin.![EBI](/images/logo_chembl.png) |
Friedrich Miescher-Institut |
7562931 |
41 |
Peptidyl alpha-ketoheterocyclic inhibitors of human neutrophil elastase. 3. In vitro and in vivo potency of a series of peptidyl alpha-ketobenzoxazoles.![EBI](/images/logo_chembl.png) |
Zeneca Pharmaceuticals |
21506603 |
4 |
HCV-NS3/4A protease inhibitory iridoid glucosides and dimeric foliamenthoic acid derivatives from Anarrhinum orientale.![EBI](/images/logo_chembl.png) |
Cairo University |
9214730 |
9 |
Effects of flavonoids isolated from scutellariae radix on fibrinolytic system induced by trypsin in human umbilical vein endothelial cells.![EBI](/images/logo_chembl.png) |
Ehime University |
17350836 |
5 |
Synthesis of fluorescent-labeled aeruginosin derivatives for high-throughput fluorescence correlation spectroscopy assays.![EBI](/images/logo_chembl.png) |
Graduate School of Science and Engineering |
12061879 |
44 |
SMall Molecule Growth 2001 (SMoG2001): an improved knowledge-based scoring function for protein-ligand interactions.![EBI](/images/logo_chembl.png) |
Harvard University |
29072911 |
16 |
Design of Small-Molecule Active-Site Inhibitors of the S1A Family Proteases as Procoagulant and Anticoagulant Drugs.![EBI](/images/logo_chembl.png) |
University of Nottingham |
29550094 |
28 |
Structure-based drug design of 1,3,6-trisubstituted 1,4-diazepan-7-ones as selective human kallikrein 7 inhibitors.![EBI](/images/logo_chembl.png) |
Asubio Pharma |
29501396 |
59 |
Pyridazine and pyridazinone derivatives as potent and selective factor XIa inhibitors.![EBI](/images/logo_chembl.png) |
Bristol-Myers Squibb |
30212625 |
107 |
Depsipeptides Featuring a Neutral P1 Are Potent Inhibitors of Kallikrein-Related Peptidase 6 with On-Target Cellular Activity.![EBI](/images/logo_chembl.png) |
German Cancer Research Center (Dkfz) |
30130401 |
71 |
6-Substituted Hexamethylene Amiloride (HMA) Derivatives as Potent and Selective Inhibitors of the Human Urokinase Plasminogen Activator for Use in Cancer.![EBI](/images/logo_chembl.png) |
University of Wollongong |
29775297 |
7 |
Factor XIa Inhibitors as New Anticoagulants.![EBI](/images/logo_chembl.png) |
Bristol-Myers Squibb |
29407959 |
82 |
The selectivity and bioavailability improvement of novel oral anticoagulants: An overview.![EBI](/images/logo_chembl.png) |
Hefei University of Technology |
29102227 |
19 |
Discovery and structure-activity relationship study of 1,3,6-trisubstituted 1,4-diazepane-7-ones as novel human kallikrein 7 inhibitors.![EBI](/images/logo_chembl.png) |
Asubio Pharma |
29936356 |
27 |
Engineering potent mesotrypsin inhibitors based on the plant-derived cyclic peptide, sunflower trypsin inhibitor-1.![EBI](/images/logo_chembl.png) |
The University of Queensland |
29808677 |
5 |
Jizanpeptins, Cyanobacterial Protease Inhibitors from a Symploca sp. Cyanobacterium Collected in the Red Sea.![EBI](/images/logo_chembl.png) |
Oregon State University |
2136920 |
39 |
New leupeptin analogues: synthesis and inhibition data.![EBI](/images/logo_chembl.png) |
University of Arkansas |
14744476 |
35 |
Milnacipran: a comparative analysis of human monoamine uptake and transporter binding affinity.![BDB](/images/logo_bindingdb.png) |
Emory University |
20626411 |
14 |
Fragment-based discovery of novel thymidylate synthase leads by NMR screening and group epitope mapping.![BDB](/images/logo_bindingdb.png) |
University of Washington |
15713402 |
51 |
Tryptamine and homotryptamine-based sulfonamides as potent and selective inhibitors of 15-lipoxygenase.![BDB](/images/logo_bindingdb.png) |
Bristol-Myers Squibb |
12657282 |
13 |
Aryl tetrahydropyridine inhibitors of farnesyltransferase: glycine, phenylalanine and histidine derivatives.![BDB](/images/logo_bindingdb.png) |
Abbott Laboratories |
24058293 |
12 |
Modulation of global low-frequency motions underlies allosteric regulation: demonstration in CRP/FNR family transcription factors.![BDB](/images/logo_bindingdb.png) |
Durham University |
10715152 |
151 |
5,6-Dihydropyran-2-ones possessing various sulfonyl functionalities: potent nonpeptidic inhibitors of HIV protease.![BDB](/images/logo_bindingdb.png) |
Parke-Davis Pharmaceutical Research |