The following articles (labelled with PubMed ID or TBD) are for your review
PMID | Data | Article Title | Organization |
28621538 |
63 |
Discovery of Highly Potent and Selective Small-Molecule Reversible Factor D Inhibitors Demonstrating Alternative Complement Pathway Inhibition in Vivo. |
Novartis Pharma |
28085275 |
53 |
Structure-Based Design of Macrocyclic Factor XIa Inhibitors: Discovery of the Macrocyclic Amide Linker. |
Bristol-Myers Squibb |
28045547 |
73 |
Peptide Macrocycle Inhibitor of Coagulation Factor XII with Subnanomolar Affinity and High Target Selectivity. |
Ecole Polytechnique F�D�Rale De Lausanne (Epfl) |
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 |
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 |
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 |
26151189 |
56 |
Structure-Based Design of Macrocyclic Coagulation Factor VIIa Inhibitors. |
TBA |
26005539 |
23 |
Discovery of a Potent Parenterally Administered Factor XIa Inhibitor with Hydroxyquinolin-2(1H)-one as the P2' Moiety. |
Bristol-Myers Squibb |
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 |
25405503 |
109 |
Phenylimidazoles as potent and selective inhibitors of coagulation factor XIa with in vivo antithrombotic activity. |
Bristol-Myers Squibb |
24900827 |
8 |
Inhibitors of Factor XIa and Plasma Kallikrein May Treat Thromboembolic Disorders and Many Diabetes Complications. |
Therachem Research Medilab (India) |
660589 |
3 |
Inactivation of trypsin-like proteases by sulfonylation. Variation of positively charged group and inhibitor length. |
TBA |
24613052 |
69 |
Pyrrolopyrimidine-inhibitors with hydantoin moiety as spacer can explore P4/S4 interaction on plasmin. |
Hiroshima International University |
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 |
16644215 |
52 |
Design and synthesis of selective keto-1,2,4-oxadiazole-based tryptase inhibitors. |
Celera Genomics |
22276953 |
63 |
A new strategy for the development of highly potent and selective plasmin inhibitors. |
Philipps University Marburg |
22386244 |
4 |
Human kallikrein 6 inhibitors with a para-amidobenzylanmine P1 group identified through virtual screening. |
Sanofi Pharmaceuticals |
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 |
16250649 |
10 |
Selective inhibitors of the serine protease plasmin: probing the S3 and S3' subsites using a combinatorial library. |
Brown University |
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 |
10669559 |
180 |
Protease inhibitors: current status and future prospects. |
University of Queensland |
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. |
Merck Research Laboratories |
9301673 |
234 |
Synthesis and structure-activity relationships of potent thrombin inhibitors: piperazides of 3-amidinophenylalanine. |
Klinikum Der Friedrich-Schiller-Universit£T Jena |
8478905 |
53 |
Inhibition studies of some serine and thiol proteinases by new leupeptin analogues. |
University of Arkansas |
10091673 |
21 |
Synthesis of potent and selective inhibitors of human plasma kallikrein. |
The Procter & Gamble |
| 24 |
L-373,890, An achiral, noncovalent, subnanomolar thrombin inhibitor |
TBA |
22047802 |
8 |
The arginine mimickingß-amino acidß³hPhe(3-H2N-CH2) as S1 ligand in cyclotheonamide-basedß-tryptase inhibitors. |
Universit£T Bielefeld |
21995444 |
32 |
Discovery of N-[2-hydroxy-6-(4-methoxybenzamido)phenyl]-4- (4-methyl-1,4-diazepan-1-yl)benzamide (darexaban, YM150) as a potent and orally available factor Xa inhibitor. |
Astellas Pharma |
21944858 |
12 |
Identification of novel plasmin inhibitors possessing nitrile moiety as warhead. |
Hiroshima International University |
21741839 |
83 |
Development of substrate analogue inhibitors for the human airway trypsin-like protease HAT. |
Philipps University Marburg |
19483697 |
23 |
Phage-encoded combinatorial chemical libraries based on bicyclic peptides. |
Laboratory of Molecular Biology, Medical Research Council |
| 13 |
Characterization of LY806303 as a potent and selective inhibitor of thrombin |
TBA |
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 |
17420122 |
18 |
Selective and dual action orally active inhibitors of thrombin and factor Xa. |
Glaxosmithkline |
16725321 |
13 |
Novel, potent, selective, and orally bioavailable human betaII-tryptase inhibitors. |
Celera Genomics |
16413183 |
16 |
Small molecule inhibitors of plasma kallikrein. |
Celera Genomics |
16213711 |
37 |
Ketene aminal-based lactam derivatives as a novel class of orally active FXa inhibitors. |
Bristol-Myers Squibb Pharmaceutical Research Institute |
15013007 |
319 |
Design, synthesis, and SAR of anthranilamide-based factor Xa inhibitors with improved functional activity. |
Millennium Pharmaceuticals |
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 |
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 |
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 |
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 |
10560742 |
85 |
3-Amidinophenylalanine-based inhibitors of urokinase. |
UniversitäT Jena |
31521475 |
205 |
Design and development of a series of borocycles as selective, covalent kallikrein 5 inhibitors. |
Glaxosmithkline |
31005442 |
64 |
Structure guided drug design to develop kallikrein 5 inhibitors to treat Netherton syndrome. |
Glaxosmithkline R&D |
29851477 |
6 |
New Modalities, Technologies, and Partnerships in Probe and Lead Generation: Enabling a Mode-of-Action Centric Paradigm. |
Astrazeneca |
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 |
9784099 |
84 |
Design of benzamidine-type inhibitors of factor Xa. |
Institut FüR Biochemie |
9703466 |
35 |
Design and synthesis of a series of potent and orally bioavailable noncovalent thrombin inhibitors that utilize nonbasic groups in the P1 position. |
Merck Research Laboratories |
30613336 |
32 |
Potent, Selective, and Cell-Penetrating Inhibitors of Kallikrein-Related Peptidase 4 Based on the Cyclic Peptide MCoTI-II. |
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. |
Merck Research Laboratories |
31563807 |
63 |
Discovery of novel, potent, isosteviol-based antithrombotic agents. |
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. |
University of Antwerp (Ua) |
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 |
28835783 |
6 |
Plasma Kallikrein Inhibitors for the Treatment of Retinal Vascular Permeability Associated with Diabetic Retinopathy and Diabetic Macular Edema. |
Therachem Research Medilab (India) |
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 |
28460818 |
29 |
Neutral macrocyclic factor VIIa inhibitors. |
Bristol-Myers Squibb Research and Development |
| 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 |
8910390 |
13 |
Molecular and pharmacological characterization of native cortical gamma-aminobutyric acidA receptors containing both alpha1 and alpha3 subunits. |
Universidad De Sevilla |
19199284 |
24 |
Development and biological evaluation of a novel aurora A kinase inhibitor. |
Parc De Recerca Biomedica De Barcelona |
8097479 |
3 |
A human somatostatin receptor (SSTR3), located on chromosome 22, displays preferential affinity for somatostatin-14 like peptides. |
University of Toronto |
16407991 |
13 |
Activity-based probes that target diverse cysteine protease families. |
Stanford University |
20550146 |
32 |
Correlating solution binding and ESI-MS stabilities by incorporating solvation effects in a confined cucurbit[8]uril system. |
University of Cambridge |
19699645 |
12 |
Design, synthesis, and biological evaluation of hydroquinone derivatives as novel inhibitors of the sarco/endoplasmic reticulum calcium ATPase. |
Northern Kentucky University |
15911271 |
22 |
Inhibition of IKK-2 by 2-[(aminocarbonyl)amino]-5-acetylenyl-3-thiophenecarboxamides. |
Pfizer |
17292610 |
17 |
Design, synthesis, and evaluation of non-steroidal farnesoid X receptor (FXR) antagonist. |
University of Tokyo |
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) |
16539374 |
16 |
Synthesis, pharmacological evaluation, and molecular modeling studies of novel peptidic CAAX analogues as farnesyl-protein-transferase inhibitors. |
Universita Di Napoli Federico Ii |
15863311 |
244 |
Discovery of potent and selective phenylalanine based dipeptidyl peptidase IV inhibitors. |
Merck Research Laboratories |
11101352 |
88 |
Pyrido[2,3-d]pyrimidin-7-one inhibitors of cyclin-dependent kinases. |
Parke-Davis Pharmaceutical Research |
24058293 |
12 |
Modulation of global low-frequency motions underlies allosteric regulation: demonstration in CRP/FNR family transcription factors. |
Durham University |
11784141 |
11 |
Beta-strand mimicking macrocyclic amino acids: templates for protease inhibitors with antiviral activity. |
University of Queensland |