Target Information

Target General Infomation
Target ID
T94033
Former ID
TTDS00202
Target Name
Coagulation factor IIa
Gene Name
F2
Synonyms
Coagulation factor II; Prothrombin; F2
Target Type
Successful
Disease Atopic dermatitis [ICD9: 691.8, 692.9; ICD10: L00-L99]
Angina pectoris [ICD9: 413; ICD10: I20]
Blood forming organ disorders [ICD10: D75.9]
Bleeding [ICD9: 444, 453; ICD10: I74, I80-I82]
Blood coagulation disorders [ICD10: D65-D68]
Coagulation [ICD10: I80-I82]
Cardiovascular disorder [ICD10: I00-I99]
Cancer [ICD9: 140-229; ICD10: C00-C96]
Heart arrhythmia [ICD10: I47-I49]
Myocardial infarction [ICD9: 410; ICD10: I21, I22]
Neurological disease [ICD9: 338, 338.2, 410, 782.3,780; ICD10: I21, I22, R52, R52.1-R52.2, R60.9, G89]
Nonvalvular atrial fibrillation; Thrombosis [ICD9: 427.31, 437.6, 453, 671.5, 671.9; ICD10: I48, I80-I82]
Solid tumours [ICD9: 140-199, 210-229; ICD10: C00-D48]
Stroke in atrial fibrillation [ICD9: 427.31, 434.91; ICD10: I48, I61-I63]
Thrombocytopenia [ICD9: 287.3, 287.4, 287.5; ICD10: D69.6, P61.0]
Thrombosis [ICD9: 437.6, 453, 671.5, 671.9; ICD10: I80-I82]
Thromboembolism [ICD9: 437.6, 453, 671.5, 671.9; ICD10: I80-I82]
Venous thrombosis [ICD9: 437.6, 453, 671.5, 671.9; ICD10: I80-I82]
Unspecified [ICD code not available]
Function
Thrombin, which cleaves bonds after arg and lys, converts fibrinogen to fibrin and activates factors v, vii, viii, xiii, and, in complex with thrombomodulin, protein c.
BioChemical Class
Peptidase
Target Validation
T94033
UniProt ID
P00734
EC Number
EC 3.4.21.5
Sequence
MAHVRGLQLPGCLALAALCSLVHSQHVFLAPQQARSLLQRVRRANTFLEEVRKGNLEREC
VEETCSYEEAFEALESSTATDVFWAKYTACETARTPRDKLAACLEGNCAEGLGTNYRGHV
NITRSGIECQLWRSRYPHKPEINSTTHPGADLQENFCRNPDSSTTGPWCYTTDPTVRRQE
CSIPVCGQDQVTVAMTPRSEGSSVNLSPPLEQCVPDRGQQYQGRLAVTTHGLPCLAWASA
QAKALSKHQDFNSAVQLVENFCRNPDGDEEGVWCYVAGKPGDFGYCDLNYCEEAVEEETG
DGLDEDSDRAIEGRTATSEYQTFFNPRTFGSGEADCGLRPLFEKKSLEDKTERELLESYI
DGRIVEGSDAEIGMSPWQVMLFRKSPQELLCGASLISDRWVLTAAHCLLYPPWDKNFTEN
DLLVRIGKHSRTRYERNIEKISMLEKIYIHPRYNWRENLDRDIALMKLKKPVAFSDYIHP
VCLPDRETAASLLQAGYKGRVTGWGNLKETWTANVGKGQPSVLQVVNLPIVERPVCKDST
RIRITDNMFCAGYKPDEGKRGDACEGDSGGPFVMKSPFNNRWYQMGIVSWGEGCDRDGKY
GFYTHVFRLKKWIQKVIDQFGE
Drugs and Mode of Action
Drug(s) Anisindione Drug Info Approved Coagulation [538440], [541995]
Bivalirudin Drug Info Approved Thrombocytopenia [536361], [541605]
Dabigatran Drug Info Approved Stroke in atrial fibrillation [531351], [541518]
Lepirudin Drug Info Approved Thrombocytopenia [536361], [541604]
Hirudin Drug Info Phase 4 Discovery agent [524467]
MELAGATRAN Drug Info Phase 3 Discovery agent [521709], [541520]
SR-123781A Drug Info Phase 2/3 Venous thrombosis [521845]
EFEGATRAN SULFATE HYDRATE Drug Info Phase 2 Myocardial infarction [527625]
EP-217609 Drug Info Phase 2 Thrombosis [549210]
LB-30870 Drug Info Phase 2 Myocardial infarction [551846]
NU-172 Drug Info Phase 2 Thrombosis [522521]
Odiparcil Drug Info Phase 2 Cardiovascular disorder [521747]
Pegmusirudin Drug Info Phase 2 Angina pectoris [521580]
Recombinant RGD-hirudin Drug Info Phase 2 Thrombosis [530928]
AZD-8165 Drug Info Phase 1 Thrombosis [523086], [542697]
DP-4088 Drug Info Phase 1 Blood coagulation disorders [548782]
EP-42675 Drug Info Phase 1 Thrombosis [548235]
RWJ-671818 Drug Info Phase 1 Thrombosis [530660]
Solulin Drug Info Phase 1 Thrombosis [531504]
SSR-128428 Drug Info Phase 1 Thromboembolism [547951]
H376/95 Drug Info Withdrawn from market Discovery agent [521708]
Ximelagatran Drug Info Withdrawn from market Coagulation [536361], [541519]
AZD0837 Drug Info Discontinued in Phase 2 Nonvalvular atrial fibrillation; Thrombosis [542662], [547675]
Dermolastin Drug Info Discontinued in Phase 2 Atopic dermatitis [547642]
INOGATRAN Drug Info Discontinued in Phase 2 Myocardial infarction [545842]
Napsagatran Drug Info Discontinued in Phase 2 Myocardial infarction [545647]
SSR-182289 Drug Info Discontinued in Phase 2 Myocardial infarction [547360]
Vasoflux Drug Info Discontinued in Phase 2 Myocardial infarction [546404]
ARC-183 Drug Info Discontinued in Phase 1 Blood forming organ disorders [547835]
BCX-1470 Drug Info Discontinued in Phase 1 Bleeding [546724]
CJC-1004 Drug Info Discontinued in Phase 1 Thrombosis [547263]
CVS-1123 Drug Info Discontinued in Phase 1 Myocardial infarction [545765]
GW-473178 Drug Info Discontinued in Phase 1 Heart arrhythmia [547305]
Licostinel Drug Info Discontinued in Phase 1 Neurological disease [545531]
MPC-0920 Drug Info Discontinued in Phase 1 Thrombosis [548226]
S-18326 Drug Info Discontinued in Phase 1 Myocardial infarction [545791]
UK-156406 Drug Info Discontinued in Phase 1 Myocardial infarction [546743]
BCH-2763 Drug Info Terminated Thrombosis [546230]
BMS-189664 Drug Info Terminated Myocardial infarction [546805]
CVS-995 Drug Info Terminated Myocardial infarction [545766]
DuP 714 Drug Info Terminated Thromboembolism [545010]
Efegatran Drug Info Terminated Discovery agent [545040]
GS-522 Drug Info Terminated Thromboembolism [545438]
Hementin Drug Info Terminated Thromboembolism [545852]
L-373890 Drug Info Terminated Thrombosis [546669]
L-374,087 Drug Info Terminated Thrombosis [546605]
LB30057 Drug Info Terminated Discovery agent [546602]
Org-34092 Drug Info Terminated Thromboembolism [546864]
PPACK Drug Info Terminated Discovery agent [545056]
SR-80027A Drug Info Terminated Thromboembolism [545878]
Inhibitor (3,4-dichlorophenyl)(1H-pyrazol-1-yl)methanone Drug Info [529037]
(3-nitro-1H-pyrazol-1-yl)(p-tolyl)methanone Drug Info [529037]
(3-nitro-1H-pyrazol-1-yl)(phenyl)methanone Drug Info [529037]
(4-bromo-1H-pyrazol-1-yl)(p-tolyl)methanone Drug Info [529037]
(4-nitro-1H-pyrazol-1-yl)(o-tolyl)methanone Drug Info [529037]
(4-nitro-1H-pyrazol-1-yl)(phenyl)methanone Drug Info [529037]
1,2,3,4,6-penta-O-galloyl-beta-D-glucose Drug Info [534762]
1-(HYDROXYMETHYLENEAMINO)-8-HYDROXY-OCTANE Drug Info [551374]
1-benzoyl-N-phenyl-1H-pyrazole-3-carboxamide Drug Info [529037]
2-(2-Hydroxy-phenyl)-1H-indole-5-carboxamidine Drug Info [526118]
2-NAPHTHALENESULFONIC ACID Drug Info [551374]
2-nas-phe(3-am)-4-(2-guanidinoethyl)piperidine Drug Info [528292]
3-(4-HYDROXY-PHENYL)PYRUVIC ACID Drug Info [551374]
3-chlorophenyl 2-oxo-2H-chromene-3-carboxylate Drug Info [527883]
4-(2,5-DIAMINO-5-HYDROXY-PENTYL)-PHENOL Drug Info [551374]
4-(3,4-Diethoxy-benzylamino)-benzamidine Drug Info [527397]
4-(4-Benzyloxy-3-methoxy-benzylamino)-benzamidine Drug Info [527397]
4-Iodobenzo[B]Thiophene-2-Carboxamidine Drug Info [551374]
4-TERT-BUTYLBENZENESULFONIC ACID Drug Info [551374]
4-[3-(4-CHLOROPHENYL)-1H-PYRAZOL-5-YL]PIPERIDINE Drug Info [551374]
5-desgalloylstachyurin Drug Info [534762]
6-(2-HYDROXY-CYCLOPENTYL)-7-OXO-HEPTANAMIDINE Drug Info [551374]
AC-(D)PHE-PRO-BOROHOMOLYS-OH Drug Info [551374]
AC-(D)PHE-PRO-BOROHOMOORNITHINE-OH Drug Info [551374]
AC-(D)PHE-PRO-BOROLYS-OH Drug Info [551374]
AZD-8165 Drug Info [543606]
AZD0837 Drug Info [550288]
Bbs-Arg-(D-Pip)-Gly-(EQKLISEEDL)-Gly-Hir Drug Info [527780]
Bbs-Arg-(D-Pip)-Gly-(SPH(pY)EKVS)-Gly-Hir Drug Info [527780]
Bbs-Arg-(D-Pip)-Gly-(SPHYEKVS)-Gly-Hir Drug Info [527780]
Bbs-Arg-(D-Pip)-Gly-S-(GS)1-Gly-Hir Drug Info [527780]
Bbs-Arg-(D-Pip)-Gly-S-(GS)11-Gly-Hir Drug Info [527780]
Bbs-Arg-(D-Pip)-Gly-S-(GS)13-Gly-Hir Drug Info [527780]
Bbs-Arg-(D-Pip)-Gly-S-(GS)3-Gly-Hir Drug Info [527780]
Bbs-Arg-(D-Pip)-Gly-S-(GS)5-Gly-Hir Drug Info [527780]
Bbs-Arg-(D-Pip)-Gly-S-(GS)7-Gly-Hir Drug Info [527780]
Bbs-Arg-(D-Pip)-Gly-S-(GS)9-Gly-Hir Drug Info [527780]
BCH-2763 Drug Info [538083]
BCX-1470 Drug Info [544115]
BENZOTHIAZOLE Drug Info [551374]
Beta-(2-Naphthyl)-Alanine Drug Info [551374]
Beta-phenyl-D-phenylalanyl-N-propyl-L-prolinamide Drug Info [551374]
Bivalirudin Drug Info [535224]
Bivalirudine Drug Info [535345]
BMS-189664 Drug Info [551871]
BMS-344577 Drug Info [530503]
BMS-740808 Drug Info [529194]
CASUARIIN Drug Info [534762]
CHLORODYSINOSIN A Drug Info [530312]
CJC-1004 Drug Info [526666]
COCHINCHINENENE B Drug Info [529057]
COCHINCHINENIN B Drug Info [529057]
CRA_8696 Drug Info [551374]
CVS-1123 Drug Info [534333]
CVS-995 Drug Info [534248]
Cyclotheonamide E Drug Info [526298]
Cyclotheonamide E4 Drug Info [526298]
Cyclotheonamide E5 Drug Info [526298]
D-leucyl-N-(3-chlorobenzyl)-L-prolinamide Drug Info [551374]
D-leucyl-N-(4-carbamimidoylbenzyl)-L-prolinamide Drug Info [551374]
D-phenylalanyl-N-(3-chlorobenzyl)-L-prolinamide Drug Info [551374]
D-phenylalanyl-N-(3-fluorobenzyl)-L-prolinamide Drug Info [551374]
D-phenylalanyl-N-(3-methylbenzyl)-L-prolinamide Drug Info [551374]
D-phenylalanyl-N-benzyl-L-prolinamide Drug Info [551374]
D-Pro-Phe-Arg chloromethyl ketone Drug Info [529454]
Dabigatran Drug Info [531351]
Dermolastin Drug Info [536190], [536840], [537435], [551533]
Desirudine Drug Info [535345]
DP-4088 Drug Info [543606]
DuP 714 Drug Info [535205]
DYSINOSIN A Drug Info [530312]
Efegatran Drug Info [535205]
EFEGATRAN SULFATE HYDRATE Drug Info [551871]
Enoxaprin Drug Info [537910]
Gamma-Carboxy-Glutamic Acid Drug Info [551393]
GR-133686 Drug Info [534803]
GS-522 Drug Info [534196]
GW-473178 Drug Info [547306]
H376/95 Drug Info [535224]
Haempatch Drug Info [543606]
Hementin Drug Info [533550]
Hemi-Babim Drug Info [551374]
Heparin-Cantithrombin III Drug Info [535514]
Hirudin Drug Info [535224], [535605], [538091]
Hirulog Drug Info [538091]
L-370,518 Drug Info [538091]
L-373890 Drug Info [534784]
L-374,087 Drug Info [535728]
L-375378 Drug Info [526487]
LB-30870 Drug Info [551871]
LB30057 Drug Info [535684]
LB30812 Drug Info [535774]
Lepirudin Drug Info [534921]
Lepirudine Drug Info [535345]
Licostinel Drug Info [535658]
Lysophosphotidylserine Drug Info [551393]
Macrocyclic tripeptide motif Drug Info [551309]
MELAGATRAN Drug Info [528017]
Melogatran Drug Info [535514]
Methyl L-phenylalaninate Drug Info [551374]
METHYL-PHE-PRO-AMINO-CYCLOHEXYLGLYCINE Drug Info [551374]
MPC-0920 Drug Info [549865]
N4-(N,N-DIPHENYLCARBAMOYL)-AMINOGUANIDINE Drug Info [551374]
Napsagatran Drug Info [534111]
NU-172 Drug Info [544213], [551844]
Odiparcil Drug Info [528425]
Org-34092 Drug Info [543606]
OSCILLARIN Drug Info [530312]
PEDUNCULAGIN Drug Info [534762]
PPACK Drug Info [535205]
RAZAXABAN Drug Info [530655]
RWJ-50353 Drug Info [529193]
S-18326 Drug Info [551871]
S-2238 Drug Info [535151]
SC-79407 Drug Info [535728]
SR-80027A Drug Info [533808]
SSR-182289 Drug Info [551871]
Tellimagrandin II Drug Info [534762]
UK-156406 Drug Info [551871]
Vasoflux Drug Info [534833]
VE-04051645 Drug Info [543606]
Ximelagatran Drug Info [537615]
Modulator Anisindione Drug Info [535724]
bufrudin, Biopharm Drug Info
CVS-1578 Drug Info
EP-217609 Drug Info
EP-42675 Drug Info [532552]
INOGATRAN Drug Info
Pegmusirudin Drug Info [543606]
Recombinant RGD-hirudin Drug Info [528917]
RWJ-671818 Drug Info [530660]
Solulin Drug Info [531504]
SR-123781A Drug Info [535183]
SSR-128428 Drug Info
TB-101 Drug Info [543606]
TB-102 Drug Info [543606]
Tumor vascular thrombogen Drug Info [543606]
Cofactor Vitamin K Drug Info [537752]
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM)
TEP EXP Info
Pathways
KEGG Pathway Neuroactive ligand-receptor interaction
Complement and coagulation cascades
Regulation of actin cytoskeleton
NetPath Pathway TCR Signaling Pathway
PANTHER Pathway Blood coagulation
Pathway Interaction Database Thrombin/protease-activated receptor (PAR) pathway
Angiopoietin receptor Tie2-mediated signaling
FOXA2 and FOXA3 transcription factor networks
PAR4-mediated thrombin signaling events
Syndecan-4-mediated signaling events
PAR1-mediated thrombin signaling events
PathWhiz Pathway Vitamin K Metabolism
Coagulation
Reactome Intrinsic Pathway of Fibrin Clot Formation
Common Pathway of Fibrin Clot Formation
Gamma-carboxylation of protein precursors
Transport of gamma-carboxylated protein precursors from the endoplasmic reticulum to the Golgi apparatus
Removal of aminoterminal propeptides from gamma-carboxylated proteins
Cell surface interactions at the vascular wall
Peptide ligand-binding receptors
Regulation of Insulin-like Growth Factor (IGF) transport and uptake by Insulin-like Growth Factor Binding Proteins (IGFBPs)
G alpha (q) signalling events
Thrombin signalling through proteinase activated receptors (PARs)
WikiPathways Complement and Coagulation Cascades
Regulation of Actin Cytoskeleton
IL1 and megakaryotyces in obesity
Regulation of Insulin-like Growth Factor (IGF) Transport and Uptake by Insulin-like Growth Factor Binding Proteins (IGFBPs)
gamma carboxylation, hypusine formation and arylsulfatase activation
Blood Clotting Cascade
Gastrin-CREB signalling pathway via PKC and MAPK
Thrombin signalling through proteinase activated receptors (PARs)
Platelet Aggregation (Plug Formation)
GPCR ligand binding
GPCR downstream signaling
Formation of Fibrin Clot (Clotting Cascade)
Cell surface interactions at the vascular wall
Folate Metabolism
Vitamin B12 Metabolism
Selenium Micronutrient Network
References
Ref 521580ClinicalTrials.gov (NCT00074620) A Clinical Study to Assess the Safety of PEG-Hirudin (SPP200) Compared to Heparin in Patients Who Are on Haemodialysis. U.S. National Institutes of Health.
Ref 521708ClinicalTrials.gov (NCT00206063) Long Term Open Follow-up With H376/95 vs. Warfarin. U.S. National Institutes of Health.
Ref 521709ClinicalTrials.gov (NCT00206089) Melagatran/Ximelagatran Versus Enoxaparin for the Prevention of Venous Thromboembolic Events. U.S. National Institutes of Health.
Ref 521747ClinicalTrials.gov (NCT00240643) Use Of SB424323 With Aspirin In Non-Valvular Atrial Fibrillation In Patients At A Low Or Intermediate Risk For Stroke. U.S. National Institutes of Health.
Ref 521845ClinicalTrials.gov (NCT00338897) Dose Ranging Study in Elective Total Hip Replacement Surgery. U.S. National Institutes of Health.
Ref 522521ClinicalTrials.gov (NCT00808964) Study of NU172 as Anticoagulation in Patients Undergoing Off-pump CABG Surgery. U.S. National Institutes of Health.
Ref 523086ClinicalTrials.gov (NCT01150812) Oral AZD8165 After Single Oral Ascending Doses in Healthy Male Subjects. U.S. National Institutes of Health.
Ref 524467ClinicalTrials.gov (NCT01960569) Topical r-Hirudin ( Thrombexx ) Efficacy in Treatment of Haematomas. U.S. National Institutes of Health.
Ref 527625Efegatran. Institute for drug research/IVAX. IDrugs. 2001 Jun;4(6):691-4.
Ref 530660J Med Chem. 2010 Feb 25;53(4):1843-56.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.
Ref 530928The antithrombotic effect of a novel hirudin derivative after reconstruction of carotid artery in rabbits. Thromb Res. 2010 Oct;126(4):e339-43.
Ref 531351Mullard A: 2010 FDA drug approvals. Nat Rev Drug Discov. 2011 Feb;10(2):82-5.
Ref 531504The thrombomodulin analog Solulin promotes reperfusion and reduces infarct volume in a thrombotic stroke model. J Thromb Haemost. 2011 Jun;9(6):1174-82.
Ref 536361Natural products as sources of new drugs over the last 25 years. J Nat Prod. 2007 Mar;70(3):461-77. Epub 2007 Feb 20.
Ref 538440FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (NDA) 010909.
Ref 541518(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 6380).
Ref 541519(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 6381).
Ref 541520(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 6382).
Ref 541604(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 6469).
Ref 541605(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 6470).
Ref 541995(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 6960).
Ref 542662(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7682).
Ref 542697(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7727).
Ref 545010Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001867)
Ref 545040Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001951)
Ref 545056Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001987)
Ref 545438Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003259)
Ref 545531Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003616)
Ref 545647Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800004026)
Ref 545765Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800004614)
Ref 545766Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800004615)
Ref 545791Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800004736)
Ref 545842Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800005012)
Ref 545852Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800005051)
Ref 545878Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800005178)
Ref 546230Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800007017)
Ref 546404Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800007938)
Ref 546602Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800009139)
Ref 546605Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800009151)
Ref 546669Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800009558)
Ref 546724Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800009938)
Ref 546743Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800010067)
Ref 546805Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800010403)
Ref 546864Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800010730)
Ref 547263Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800014574)
Ref 547305Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800015039)
Ref 547360Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800015478)
Ref 547642Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800018071)
Ref 547675Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800018351)
Ref 547835Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800019755)
Ref 547951Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800020651)
Ref 548226Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800023381)
Ref 548235Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800023539)
Ref 548782Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800028740)
Ref 549210Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800033781)
Ref 551846Frontiers in Anti-Infective Drug Discovery, Atta-ur-Rahman, ??. Iqbal Choudhary. Page(57).
Ref 526118J Med Chem. 2001 Aug 16;44(17):2753-71.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.
Ref 526298J Nat Prod. 2002 Mar;65(3):259-61.Cyclotheonamide E4 and E5, new potent tryptase inhibitors from an Ircinia species of sponge.
Ref 526487Bioorg Med Chem Lett. 2003 Jan 20;13(2):161-4.Small, low nanomolar, noncovalent thrombin inhibitors lacking a group to fill the 'distal binding pocket'.
Ref 526666Gateways to clinical trials. Methods Find Exp Clin Pharmacol. 2003 Jun;25(5):387-408.
Ref 527397Bioorg Med Chem Lett. 2005 Feb 1;15(3):817-22.Design of selective phenylglycine amide tissue factor/factor VIIa inhibitors.
Ref 527780Bioorg Med Chem Lett. 2005 Dec 1;15(23):5120-3. Epub 2005 Oct 3.Transforming bivalent ligands into retractable enzyme inhibitors through polypeptide-protein interactions.
Ref 527883J Med Chem. 2005 Dec 1;48(24):7592-603.3,6-disubstituted coumarins as mechanism-based inhibitors of thrombin and factor Xa.
Ref 528017Bioorg Med Chem Lett. 2006 May 15;16(10):2648-53. Epub 2006 Feb 3.Orally active thrombin inhibitors. Part 2: optimization of the P2-moiety.
Ref 528292J Med Chem. 2006 Jul 13;49(14):4116-26.Secondary amides of sulfonylated 3-amidinophenylalanine. New potent and selective inhibitors of matriptase.
Ref 528425A comparison of the beta-D-xyloside, odiparcil, to warfarin in a rat model of venous thrombosis. J Thromb Haemost. 2006 Sep;4(9):1989-96.
Ref 528917The NMR solution structure of recombinant RGD-hirudin. Biochem Biophys Res Commun. 2007 Aug 17;360(1):103-8. Epub 2007 Jun 13.
Ref 529037J Med Chem. 2007 Oct 4;50(20):4928-38. Epub 2007 Sep 12.N-benzoylpyrazoles are novel small-molecule inhibitors of human neutrophil elastase.
Ref 529057J Nat Prod. 2007 Oct;70(10):1570-7. Epub 2007 Sep 21.Anti-Helicobacter pylori and thrombin inhibitory components from Chinese dragon's blood, Dracaena cochinchinensis.
Ref 529193Bioorg Med Chem. 2008 Feb 15;16(4):1562-95. Epub 2007 Nov 6.Inhibitors of proteases and amide hydrolases that employ an alpha-ketoheterocycle as a key enabling functionality.
Ref 529194Bioorg Med Chem Lett. 2008 Jan 15;18(2):749-54. Epub 2007 Nov 17.Structure-activity relationship and pharmacokinetic profile of 5-ketopyrazole factor Xa inhibitors.
Ref 529454J Med Chem. 2008 Jun 12;51(11):3077-80. Epub 2008 May 7.Novel 3-carboxamide-coumarins as potent and selective FXIIa inhibitors.
Ref 530312Bioorg Med Chem Lett. 2009 Sep 15;19(18):5429-32. Epub 2009 Jul 26.From natural products to achiral drug prototypes: potent thrombin inhibitors based on P2/P3 dihydropyrid-2-one core motifs.
Ref 530503Bioorg Med Chem Lett. 2009 Dec 15;19(24):6882-9. Epub 2009 Oct 23.Aroylguanidine-based factor Xa inhibitors: the discovery of BMS-344577.
Ref 530655Bioorg Med Chem Lett. 2010 Feb 15;20(4):1373-7. Epub 2010 Jan 11.Phenyltriazolinones as potent factor Xa inhibitors.
Ref 530660J Med Chem. 2010 Feb 25;53(4):1843-56.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.
Ref 531351Mullard A: 2010 FDA drug approvals. Nat Rev Drug Discov. 2011 Feb;10(2):82-5.
Ref 531504The thrombomodulin analog Solulin promotes reperfusion and reduces infarct volume in a thrombotic stroke model. J Thromb Haemost. 2011 Jun;9(6):1174-82.
Ref 531826A high affinity, antidote-controllable prothrombin and thrombin-binding RNA aptamer inhibits thrombin generation and thrombin activity. J Thromb Haemost. 2012 May;10(5):870-80.
Ref 532552EP42675, a synthetic parenteral dual-action anticoagulant: pharmacokinetics, pharmacodynamics, and absence of interactions with antiplatelet drugs. J Thromb Haemost. 2014 Jan;12(1):24-33.
Ref 533550Hementin: anticoagulant protease from the salivary gland of the leech Haementeria ghilianii. J Lab Clin Med. 1984 Jan;103(1):44-58.
Ref 533808Pharmacokinetic and antithrombotic properties of two pentasaccharides with high affinity to antithrombin III in the rabbit: comparison with CY216. Blood. 1994 Oct 15;84(8):2571-7.
Ref 534111Effects of napsagatran (Ro 46-6240), a new synthetic thrombin inhibitor and of heparin in a canine model of coronary artery thrombosis: comparison with an ex vivo annular perfusion chamber model. J Pharmacol Exp Ther. 1996 Apr;277(1):71-8.
Ref 534196A novel oligodeoxynucleotide inhibitor of thrombin. I. In vitro metabolic stability in plasma and serum. Pharm Res. 1995 Dec;12(12):1937-42.
Ref 534248Synthesis, structure, and structure-activity relationships of divalent thrombin inhibitors containing an alpha-keto-amide transition-state mimetic. Protein Sci. 1996 Mar;5(3):422-33.
Ref 534333CVS-1123, a direct thrombin inhibitor, prevents occlusive arterial and venous thrombosis in a canine model of vascular injury. J Cardiovasc Pharmacol. 1997 Feb;29(2):240-9.
Ref 534762J Nat Prod. 1998 Nov;61(11):1356-60.Effects of tannins from Geum japonicum on the catalytic activity of thrombin and factor Xa of blood coagulation cascade.
Ref 534784L-374,087, an efficacious, orally bioavailable, pyridinone acetamide thrombin inhibitor. Bioorg Med Chem Lett. 1998 Apr 7;8(7):817-22.
Ref 534803Bioorg Med Chem Lett. 1998 Nov 3;8(21):2955-60.5,5-trans lactone-containing inhibitors of serine proteases: identification of a novel, acylating thrombin inhibitor.
Ref 534833Vasoflux, a new anticoagulant with a novel mechanism of action. Circulation. 1999 Feb 9;99(5):682-9.
Ref 534921Recombinant hirudin (lepirudin) as anticoagulant in intensive care patients treated with continuous hemodialysis. Kidney Int Suppl. 1999 Nov;(72):S46-50.
Ref 535151Screening for selective thrombin inhibitors in mushrooms. Blood Coagul Fibrinolysis. 2001 Mar;12(2):123-8.
Ref 535183SR123781A, a synthetic heparin mimetic. Thromb Haemost. 2001 May;85(5):852-60.
Ref 535205Anticoagulation: the present and future. Clin Appl Thromb Hemost. 2001 Jul;7(3):195-204.
Ref 535224New anticoagulants. Am Heart J. 2001 Aug;142(2 Suppl):S3-8.
Ref 535345New antithrombotic drugs (excluding plasminogen activators. Arch Mal Coeur Vaiss. 2001 Nov;94(11 Suppl):1225-32.
Ref 535514Thrombin inhibitors in acute coronary artery disease. Eur Heart J. 2002 Aug;23(15):1142-4.
Ref 535605Probing the hirudin-thrombin interaction by incorporation of noncoded amino acids and molecular dynamics simulation. Biochemistry. 2002 Nov 19;41(46):13556-69.
Ref 535658Neuroprotective agents for the treatment of acute ischemic stroke. Curr Neurol Neurosci Rep. 2003 Jan;3(1):9-20.
Ref 535684Antithrombotic activity of LB30057, a newly synthesized direct thrombin inhibitor. Thromb Haemost. 2003 Jan;89(1):104-11.
Ref 535724Anticoagulation with anisindione in a patient with a warfarin-induced skin eruption. Pharmacotherapy. 2003 Apr;23(4):533-6.
Ref 535728Pharmacological intervention at disparate sites in the coagulation cascade: comparison of anti-thrombotic efficacy vs bleeding propensity in a rat model of acute arterial thrombosis. J Thromb Thrombolysis. 2002 Oct;14(2):113-21.
Ref 535774Efficacious 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. J Med Chem. 2003 Aug 14;46(17):3612-22.
Ref 536190rAAt (inhaled) Arriva/Hyland Immuno. Curr Opin Mol Ther. 2006 Feb;8(1):76-82.
Ref 536840Bioreactor strategies for improving production yield and functionality of a recombinant human protein in transgenic tobacco cell cultures. Biotechnol Bioeng. 2009 Feb 1;102(2):508-20.
Ref 537435Optimization of the bioprocessing conditions for scale-up of transient production of a heterologous protein in plants using a chemically inducible viral amplicon expression system. Biotechnol Prog. 2009 May-Jun;25(3):722-34.
Ref 537615Ximelagatran increases membrane fluidity and changes membrane lipid composition in primary human hepatocytes. Toxicol In Vitro. 2009 Jul 16.
Ref 537752Plasma levels of protein C and vitamin K-dependent coagulation factors in patients on long-term oral anticoagulant therapy. Tohoku J Exp Med. 1986 Aug;149(4):351-7.
Ref 537910Low molecular weight heparins and their use in obstetrics and gynecology. Obstet Gynecol Surv. 1994 Jun;49(6):424-31.
Ref 538083BCH-2763, a novel potent parenteral thrombin inhibitor, is an effective antithrombotic agent in rodent models of arterial and venous thrombosis--comparisons with heparin, r-hirudin, hirulog, inogatran and argatroban. Thromb Haemost. 1998 Feb;79(2):431-8.
Ref 538091Assessment of thrombin inhibitor efficacy in a novel rabbit model of simultaneous arterial and venous thrombosis. Thromb Haemost. 1998 Mar;79(3):656-62.
Ref 543606(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Target id: 2362).
Ref 544115Recent Developments in Low Molecular Weight Complement Inhibitors. Mol Immunol. 2009 December; 47(2-3): 185-195.
Ref 544213Nucleic acid aptamers: clinical applications and promising new horizons. Curr Med Chem. 2011; 18(27): 4206-4214.
Ref 547306Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800015039)
Ref 549865Clinical pipeline report, company report or official report of MYRIAD GENETICS, INC.
Ref 550288Clinical pipeline report, company report or official report of AstraZeneca (2009).
Ref 551309Novel thrombin inhibitors that are based on a macrocyclic tripeptide motif, Bioorg. Med. Chem. Lett. 6(24):2947-2952 (1996).
Ref 551374The Protein Data Bank. Nucleic Acids Res. 2000 Jan 1;28(1):235-42.
Ref 551393How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6.
Ref 551533Arriva-ProMetic recombinant alpha 1-antitrypsin (rAAT) moves into the clinic for dermatology applications. ProMetic Life Sciences. 2009.
Ref 551844Aptamers in Bioanalysis. M. Mascini. 2009. Wiley. Page(46).
Ref 551871Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015

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