Target Information
Target General Infomation | |||||
---|---|---|---|---|---|
Target ID |
T94033
|
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Former ID |
TTDS00202
|
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Target Name |
Coagulation factor IIa
|
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Gene Name |
F2
|
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Synonyms |
Coagulation factor II; Prothrombin; F2
|
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Target Type |
Successful
|
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Disease | Atopic dermatitis [ICD9: 691.8, 692.9; ICD10: L00-L99] | ||||
Angina pectoris [ICD9: 413; ICD10: I20] | |||||
Bleeding [ICD9: 444, 453; ICD10: I74, I80-I82] | |||||
Blood coagulation disorders [ICD10: D65-D68] | |||||
Blood forming organ disorders [ICD10: D75.9] | |||||
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] | |||||
Nonvalvular atrial fibrillation; Thrombosis [ICD9: 427.31, 437.6, 453, 671.5, 671.9; ICD10: I48, I80-I82] | |||||
Neurological disease [ICD9: 338, 338.2, 410, 782.3,780; ICD10: I21, I22, R52, R52.1-R52.2, R60.9, G89] | |||||
Stroke in atrial fibrillation [ICD9: 427.31, 434.91; ICD10: I48, I61-I63] | |||||
Solid tumours [ICD9: 140-199, 210-229; ICD10: C00-D48] | |||||
Thrombosis [ICD9: 437.6, 453, 671.5, 671.9; ICD10: I80-I82] | |||||
Thromboembolism [ICD9: 437.6, 453, 671.5, 671.9; ICD10: I80-I82] | |||||
Thrombocytopenia [ICD9: 287.3, 287.4, 287.5; ICD10: D69.6, P61.0] | |||||
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.
|
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BioChemical Class |
Peptidase
|
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Target Validation |
T94033
|
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UniProt ID | |||||
EC Number |
EC 3.4.21.5
|
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Sequence |
MAHVRGLQLPGCLALAALCSLVHSQHVFLAPQQARSLLQRVRRANTFLEEVRKGNLEREC
VEETCSYEEAFEALESSTATDVFWAKYTACETARTPRDKLAACLEGNCAEGLGTNYRGHV NITRSGIECQLWRSRYPHKPEINSTTHPGADLQENFCRNPDSSTTGPWCYTTDPTVRRQE CSIPVCGQDQVTVAMTPRSEGSSVNLSPPLEQCVPDRGQQYQGRLAVTTHGLPCLAWASA QAKALSKHQDFNSAVQLVENFCRNPDGDEEGVWCYVAGKPGDFGYCDLNYCEEAVEEETG DGLDEDSDRAIEGRTATSEYQTFFNPRTFGSGEADCGLRPLFEKKSLEDKTERELLESYI DGRIVEGSDAEIGMSPWQVMLFRKSPQELLCGASLISDRWVLTAAHCLLYPPWDKNFTEN DLLVRIGKHSRTRYERNIEKISMLEKIYIHPRYNWRENLDRDIALMKLKKPVAFSDYIHP VCLPDRETAASLLQAGYKGRVTGWGNLKETWTANVGKGQPSVLQVVNLPIVERPVCKDST RIRITDNMFCAGYKPDEGKRGDACEGDSGGPFVMKSPFNNRWYQMGIVSWGEGCDRDGKY GFYTHVFRLKKWIQKVIDQFGE |
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Drugs and Mode of Action | |||||
Drug(s) | Anisindione | Drug Info | Approved | Coagulation | [1], [2] |
Bivalirudin | Drug Info | Approved | Thrombocytopenia | [3], [4] | |
Dabigatran | Drug Info | Approved | Stroke in atrial fibrillation | [5], [6] | |
Lepirudin | Drug Info | Approved | Thrombocytopenia | [3], [7] | |
Hirudin | Drug Info | Phase 4 | Discovery agent | [8] | |
MELAGATRAN | Drug Info | Phase 3 | Discovery agent | [9], [10] | |
SR-123781A | Drug Info | Phase 2/3 | Venous thrombosis | [11] | |
EFEGATRAN SULFATE HYDRATE | Drug Info | Phase 2 | Myocardial infarction | [12] | |
EP-217609 | Drug Info | Phase 2 | Thrombosis | [13] | |
LB-30870 | Drug Info | Phase 2 | Myocardial infarction | [14] | |
NU-172 | Drug Info | Phase 2 | Thrombosis | [15] | |
Odiparcil | Drug Info | Phase 2 | Cardiovascular disorder | [16] | |
Pegmusirudin | Drug Info | Phase 2 | Angina pectoris | [17] | |
Recombinant RGD-hirudin | Drug Info | Phase 2 | Thrombosis | [18] | |
AZD-8165 | Drug Info | Phase 1 | Thrombosis | [19], [20] | |
DP-4088 | Drug Info | Phase 1 | Blood coagulation disorders | [21] | |
EP-42675 | Drug Info | Phase 1 | Thrombosis | [22] | |
RWJ-671818 | Drug Info | Phase 1 | Thrombosis | [23] | |
Solulin | Drug Info | Phase 1 | Thrombosis | [24] | |
SSR-128428 | Drug Info | Phase 1 | Thromboembolism | [25] | |
H376/95 | Drug Info | Withdrawn from market | Discovery agent | [26] | |
Ximelagatran | Drug Info | Withdrawn from market | Coagulation | [3], [27] | |
AZD0837 | Drug Info | Discontinued in Phase 2 | Nonvalvular atrial fibrillation; Thrombosis | [28], [29] | |
Dermolastin | Drug Info | Discontinued in Phase 2 | Atopic dermatitis | [30] | |
INOGATRAN | Drug Info | Discontinued in Phase 2 | Myocardial infarction | [31] | |
Napsagatran | Drug Info | Discontinued in Phase 2 | Myocardial infarction | [32] | |
SSR-182289 | Drug Info | Discontinued in Phase 2 | Myocardial infarction | [33] | |
Vasoflux | Drug Info | Discontinued in Phase 2 | Myocardial infarction | [34] | |
ARC-183 | Drug Info | Discontinued in Phase 1 | Blood forming organ disorders | [35] | |
BCX-1470 | Drug Info | Discontinued in Phase 1 | Bleeding | [36] | |
CJC-1004 | Drug Info | Discontinued in Phase 1 | Thrombosis | [37] | |
CVS-1123 | Drug Info | Discontinued in Phase 1 | Myocardial infarction | [38] | |
GW-473178 | Drug Info | Discontinued in Phase 1 | Heart arrhythmia | [39] | |
Licostinel | Drug Info | Discontinued in Phase 1 | Neurological disease | [40] | |
MPC-0920 | Drug Info | Discontinued in Phase 1 | Thrombosis | [41] | |
S-18326 | Drug Info | Discontinued in Phase 1 | Myocardial infarction | [42] | |
UK-156406 | Drug Info | Discontinued in Phase 1 | Myocardial infarction | [43] | |
BCH-2763 | Drug Info | Terminated | Thrombosis | [44] | |
BMS-189664 | Drug Info | Terminated | Myocardial infarction | [45] | |
CVS-995 | Drug Info | Terminated | Myocardial infarction | [46] | |
DuP 714 | Drug Info | Terminated | Thromboembolism | [47] | |
Efegatran | Drug Info | Terminated | Discovery agent | [48] | |
GS-522 | Drug Info | Terminated | Thromboembolism | [49] | |
Hementin | Drug Info | Terminated | Thromboembolism | [50] | |
L-373890 | Drug Info | Terminated | Thrombosis | [51] | |
L-374,087 | Drug Info | Terminated | Thrombosis | [52] | |
LB30057 | Drug Info | Terminated | Discovery agent | [53] | |
Org-34092 | Drug Info | Terminated | Thromboembolism | [54] | |
PPACK | Drug Info | Terminated | Discovery agent | [55] | |
SR-80027A | Drug Info | Terminated | Thromboembolism | [56] | |
Inhibitor | (3,4-dichlorophenyl)(1H-pyrazol-1-yl)methanone | Drug Info | [57] | ||
(3-nitro-1H-pyrazol-1-yl)(p-tolyl)methanone | Drug Info | [57] | |||
(3-nitro-1H-pyrazol-1-yl)(phenyl)methanone | Drug Info | [57] | |||
(4-bromo-1H-pyrazol-1-yl)(p-tolyl)methanone | Drug Info | [57] | |||
(4-nitro-1H-pyrazol-1-yl)(o-tolyl)methanone | Drug Info | [57] | |||
(4-nitro-1H-pyrazol-1-yl)(phenyl)methanone | Drug Info | [57] | |||
1,2,3,4,6-penta-O-galloyl-beta-D-glucose | Drug Info | [58] | |||
1-(HYDROXYMETHYLENEAMINO)-8-HYDROXY-OCTANE | Drug Info | [59] | |||
1-benzoyl-N-phenyl-1H-pyrazole-3-carboxamide | Drug Info | [57] | |||
2-(2-Hydroxy-phenyl)-1H-indole-5-carboxamidine | Drug Info | [60] | |||
2-NAPHTHALENESULFONIC ACID | Drug Info | [59] | |||
2-nas-phe(3-am)-4-(2-guanidinoethyl)piperidine | Drug Info | [61] | |||
3-(4-HYDROXY-PHENYL)PYRUVIC ACID | Drug Info | [59] | |||
3-chlorophenyl 2-oxo-2H-chromene-3-carboxylate | Drug Info | [62] | |||
4-(2,5-DIAMINO-5-HYDROXY-PENTYL)-PHENOL | Drug Info | [59] | |||
4-(3,4-Diethoxy-benzylamino)-benzamidine | Drug Info | [63] | |||
4-(4-Benzyloxy-3-methoxy-benzylamino)-benzamidine | Drug Info | [63] | |||
4-Iodobenzo[B]Thiophene-2-Carboxamidine | Drug Info | [59] | |||
4-TERT-BUTYLBENZENESULFONIC ACID | Drug Info | [59] | |||
4-[3-(4-CHLOROPHENYL)-1H-PYRAZOL-5-YL]PIPERIDINE | Drug Info | [59] | |||
5-desgalloylstachyurin | Drug Info | [58] | |||
6-(2-HYDROXY-CYCLOPENTYL)-7-OXO-HEPTANAMIDINE | Drug Info | [59] | |||
AC-(D)PHE-PRO-BOROHOMOLYS-OH | Drug Info | [59] | |||
AC-(D)PHE-PRO-BOROHOMOORNITHINE-OH | Drug Info | [59] | |||
AC-(D)PHE-PRO-BOROLYS-OH | Drug Info | [59] | |||
AZD-8165 | Drug Info | [64] | |||
AZD0837 | Drug Info | [65] | |||
Bbs-Arg-(D-Pip)-Gly-(EQKLISEEDL)-Gly-Hir | Drug Info | [66] | |||
Bbs-Arg-(D-Pip)-Gly-(SPH(pY)EKVS)-Gly-Hir | Drug Info | [66] | |||
Bbs-Arg-(D-Pip)-Gly-(SPHYEKVS)-Gly-Hir | Drug Info | [66] | |||
Bbs-Arg-(D-Pip)-Gly-S-(GS)1-Gly-Hir | Drug Info | [66] | |||
Bbs-Arg-(D-Pip)-Gly-S-(GS)11-Gly-Hir | Drug Info | [66] | |||
Bbs-Arg-(D-Pip)-Gly-S-(GS)13-Gly-Hir | Drug Info | [66] | |||
Bbs-Arg-(D-Pip)-Gly-S-(GS)3-Gly-Hir | Drug Info | [66] | |||
Bbs-Arg-(D-Pip)-Gly-S-(GS)5-Gly-Hir | Drug Info | [66] | |||
Bbs-Arg-(D-Pip)-Gly-S-(GS)7-Gly-Hir | Drug Info | [66] | |||
Bbs-Arg-(D-Pip)-Gly-S-(GS)9-Gly-Hir | Drug Info | [66] | |||
BCH-2763 | Drug Info | [67] | |||
BCX-1470 | Drug Info | [68] | |||
BENZOTHIAZOLE | Drug Info | [59] | |||
Beta-(2-Naphthyl)-Alanine | Drug Info | [59] | |||
Beta-phenyl-D-phenylalanyl-N-propyl-L-prolinamide | Drug Info | [59] | |||
Bivalirudin | Drug Info | [69] | |||
Bivalirudine | Drug Info | [70] | |||
BMS-189664 | Drug Info | [71] | |||
BMS-344577 | Drug Info | [72] | |||
BMS-740808 | Drug Info | [73] | |||
CASUARIIN | Drug Info | [58] | |||
CHLORODYSINOSIN A | Drug Info | [74] | |||
CJC-1004 | Drug Info | [75] | |||
COCHINCHINENENE B | Drug Info | [76] | |||
COCHINCHINENIN B | Drug Info | [76] | |||
CRA_8696 | Drug Info | [59] | |||
CVS-1123 | Drug Info | [77] | |||
CVS-995 | Drug Info | [78] | |||
Cyclotheonamide E | Drug Info | [79] | |||
Cyclotheonamide E4 | Drug Info | [79] | |||
Cyclotheonamide E5 | Drug Info | [79] | |||
D-leucyl-N-(3-chlorobenzyl)-L-prolinamide | Drug Info | [59] | |||
D-leucyl-N-(4-carbamimidoylbenzyl)-L-prolinamide | Drug Info | [59] | |||
D-phenylalanyl-N-(3-chlorobenzyl)-L-prolinamide | Drug Info | [59] | |||
D-phenylalanyl-N-(3-fluorobenzyl)-L-prolinamide | Drug Info | [59] | |||
D-phenylalanyl-N-(3-methylbenzyl)-L-prolinamide | Drug Info | [59] | |||
D-phenylalanyl-N-benzyl-L-prolinamide | Drug Info | [59] | |||
D-Pro-Phe-Arg chloromethyl ketone | Drug Info | [80] | |||
Dabigatran | Drug Info | [5] | |||
Dermolastin | Drug Info | [81], [82], [83], [84] | |||
Desirudine | Drug Info | [70] | |||
DP-4088 | Drug Info | [64] | |||
DuP 714 | Drug Info | [85] | |||
DYSINOSIN A | Drug Info | [74] | |||
Efegatran | Drug Info | [85] | |||
EFEGATRAN SULFATE HYDRATE | Drug Info | [71] | |||
Enoxaprin | Drug Info | [86] | |||
Gamma-Carboxy-Glutamic Acid | Drug Info | [87] | |||
GR-133686 | Drug Info | [88] | |||
GS-522 | Drug Info | [89] | |||
GW-473178 | Drug Info | [90] | |||
H376/95 | Drug Info | [69] | |||
Haempatch | Drug Info | [64] | |||
Hementin | Drug Info | [91] | |||
Hemi-Babim | Drug Info | [59] | |||
Heparin-Cantithrombin III | Drug Info | [92] | |||
Hirudin | Drug Info | [69], [93], [94] | |||
Hirulog | Drug Info | [94] | |||
L-370,518 | Drug Info | [94] | |||
L-373890 | Drug Info | [95] | |||
L-374,087 | Drug Info | [96] | |||
L-375378 | Drug Info | [97] | |||
LB-30870 | Drug Info | [71] | |||
LB30057 | Drug Info | [98] | |||
LB30812 | Drug Info | [99] | |||
Lepirudin | Drug Info | [100] | |||
Lepirudine | Drug Info | [70] | |||
Licostinel | Drug Info | [101] | |||
Lysophosphotidylserine | Drug Info | [87] | |||
Macrocyclic tripeptide motif | Drug Info | [102] | |||
MELAGATRAN | Drug Info | [103] | |||
Melogatran | Drug Info | [92] | |||
Methyl L-phenylalaninate | Drug Info | [59] | |||
METHYL-PHE-PRO-AMINO-CYCLOHEXYLGLYCINE | Drug Info | [59] | |||
MPC-0920 | Drug Info | [104] | |||
N4-(N,N-DIPHENYLCARBAMOYL)-AMINOGUANIDINE | Drug Info | [59] | |||
Napsagatran | Drug Info | [105] | |||
NU-172 | Drug Info | [106], [107] | |||
Odiparcil | Drug Info | [108] | |||
Org-34092 | Drug Info | [64] | |||
OSCILLARIN | Drug Info | [74] | |||
PEDUNCULAGIN | Drug Info | [58] | |||
PPACK | Drug Info | [85] | |||
RAZAXABAN | Drug Info | [109] | |||
RWJ-50353 | Drug Info | [110] | |||
S-18326 | Drug Info | [71] | |||
S-2238 | Drug Info | [111] | |||
SC-79407 | Drug Info | [96] | |||
SR-80027A | Drug Info | [112] | |||
SSR-182289 | Drug Info | [71] | |||
Tellimagrandin II | Drug Info | [58] | |||
UK-156406 | Drug Info | [71] | |||
Vasoflux | Drug Info | [113] | |||
VE-04051645 | Drug Info | [64] | |||
Ximelagatran | Drug Info | [114] | |||
Modulator | Anisindione | Drug Info | [115] | ||
bufrudin, Biopharm | Drug Info | ||||
CVS-1578 | Drug Info | ||||
EP-217609 | Drug Info | ||||
EP-42675 | Drug Info | [116] | |||
INOGATRAN | Drug Info | ||||
Pegmusirudin | Drug Info | [64] | |||
Recombinant RGD-hirudin | Drug Info | [117] | |||
RWJ-671818 | Drug Info | [23] | |||
Solulin | Drug Info | [24] | |||
SR-123781A | Drug Info | [118] | |||
SSR-128428 | Drug Info | ||||
TB-101 | Drug Info | [64] | |||
TB-102 | Drug Info | [64] | |||
Tumor vascular thrombogen | Drug Info | [64] | |||
Cofactor | Vitamin K | Drug Info | [119] | ||
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 1 | FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (NDA) 010909. | ||||
REF 2 | (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 3 | Natural 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 4 | (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 5 | Mullard A: 2010 FDA drug approvals. Nat Rev Drug Discov. 2011 Feb;10(2):82-5. | ||||
REF 6 | (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 7 | (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 8 | ClinicalTrials.gov (NCT01960569) Topical r-Hirudin ( Thrombexx ) Efficacy in Treatment of Haematomas. U.S. National Institutes of Health. | ||||
REF 9 | ClinicalTrials.gov (NCT00206089) Melagatran/Ximelagatran Versus Enoxaparin for the Prevention of Venous Thromboembolic Events. U.S. National Institutes of Health. | ||||
REF 10 | (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 11 | ClinicalTrials.gov (NCT00338897) Dose Ranging Study in Elective Total Hip Replacement Surgery. U.S. National Institutes of Health. | ||||
REF 12 | Efegatran. Institute for drug research/IVAX. IDrugs. 2001 Jun;4(6):691-4. | ||||
REF 13 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800033781) | ||||
REF 14 | Frontiers in Anti-Infective Drug Discovery, Atta-ur-Rahman, ??. Iqbal Choudhary. Page(57). | ||||
REF 15 | ClinicalTrials.gov (NCT00808964) Study of NU172 as Anticoagulation in Patients Undergoing Off-pump CABG Surgery. U.S. National Institutes of Health. | ||||
REF 16 | ClinicalTrials.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 17 | ClinicalTrials.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 18 | The antithrombotic effect of a novel hirudin derivative after reconstruction of carotid artery in rabbits. Thromb Res. 2010 Oct;126(4):e339-43. | ||||
REF 19 | ClinicalTrials.gov (NCT01150812) Oral AZD8165 After Single Oral Ascending Doses in Healthy Male Subjects. U.S. National Institutes of Health. | ||||
REF 20 | (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 21 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800028740) | ||||
REF 22 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800023539) | ||||
REF 23 | J 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 24 | The thrombomodulin analog Solulin promotes reperfusion and reduces infarct volume in a thrombotic stroke model. J Thromb Haemost. 2011 Jun;9(6):1174-82. | ||||
REF 25 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800020651) | ||||
REF 26 | ClinicalTrials.gov (NCT00206063) Long Term Open Follow-up With H376/95 vs. Warfarin. U.S. National Institutes of Health. | ||||
REF 27 | (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 28 | (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 29 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800018351) | ||||
REF 30 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800018071) | ||||
REF 31 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800005012) | ||||
REF 32 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800004026) | ||||
REF 33 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800015478) | ||||
REF 34 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800007938) | ||||
REF 35 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800019755) | ||||
REF 36 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800009938) | ||||
REF 37 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800014574) | ||||
REF 38 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800004614) | ||||
REF 39 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800015039) | ||||
REF 40 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003616) | ||||
REF 41 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800023381) | ||||
REF 42 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800004736) | ||||
REF 43 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800010067) | ||||
REF 44 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800007017) | ||||
REF 45 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800010403) | ||||
REF 46 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800004615) | ||||
REF 47 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001867) | ||||
REF 48 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001951) | ||||
REF 49 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003259) | ||||
REF 50 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800005051) | ||||
REF 51 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800009558) | ||||
REF 52 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800009151) | ||||
REF 53 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800009139) | ||||
REF 54 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800010730) | ||||
REF 55 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001987) | ||||
REF 56 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800005178) | ||||
REF 57 | J 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 58 | J 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 59 | The Protein Data Bank. Nucleic Acids Res. 2000 Jan 1;28(1):235-42. | ||||
REF 60 | J 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 61 | J Med Chem. 2006 Jul 13;49(14):4116-26.Secondary amides of sulfonylated 3-amidinophenylalanine. New potent and selective inhibitors of matriptase. | ||||
REF 62 | J Med Chem. 2005 Dec 1;48(24):7592-603.3,6-disubstituted coumarins as mechanism-based inhibitors of thrombin and factor Xa. | ||||
REF 63 | Bioorg Med Chem Lett. 2005 Feb 1;15(3):817-22.Design of selective phenylglycine amide tissue factor/factor VIIa inhibitors. | ||||
REF 64 | (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 65 | Clinical pipeline report, company report or official report of AstraZeneca (2009). | ||||
REF 66 | Bioorg 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 67 | BCH-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 68 | Recent Developments in Low Molecular Weight Complement Inhibitors. Mol Immunol. 2009 December; 47(2-3): 185-195. | ||||
REF 69 | New anticoagulants. Am Heart J. 2001 Aug;142(2 Suppl):S3-8. | ||||
REF 70 | New antithrombotic drugs (excluding plasminogen activators. Arch Mal Coeur Vaiss. 2001 Nov;94(11 Suppl):1225-32. | ||||
REF 71 | Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015 | ||||
REF 72 | Bioorg 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 73 | Bioorg 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 74 | Bioorg 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 75 | Gateways to clinical trials. Methods Find Exp Clin Pharmacol. 2003 Jun;25(5):387-408. | ||||
REF 76 | J 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 77 | CVS-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 78 | Synthesis, 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 79 | J Nat Prod. 2002 Mar;65(3):259-61.Cyclotheonamide E4 and E5, new potent tryptase inhibitors from an Ircinia species of sponge. | ||||
REF 80 | J Med Chem. 2008 Jun 12;51(11):3077-80. Epub 2008 May 7.Novel 3-carboxamide-coumarins as potent and selective FXIIa inhibitors. | ||||
REF 81 | rAAt (inhaled) Arriva/Hyland Immuno. Curr Opin Mol Ther. 2006 Feb;8(1):76-82. | ||||
REF 82 | Bioreactor 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 83 | Optimization 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 84 | Arriva-ProMetic recombinant alpha 1-antitrypsin (rAAT) moves into the clinic for dermatology applications. ProMetic Life Sciences. 2009. | ||||
REF 85 | Anticoagulation: the present and future. Clin Appl Thromb Hemost. 2001 Jul;7(3):195-204. | ||||
REF 86 | Low molecular weight heparins and their use in obstetrics and gynecology. Obstet Gynecol Surv. 1994 Jun;49(6):424-31. | ||||
REF 87 | How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. | ||||
REF 88 | Bioorg 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 89 | A novel oligodeoxynucleotide inhibitor of thrombin. I. In vitro metabolic stability in plasma and serum. Pharm Res. 1995 Dec;12(12):1937-42. | ||||
REF 90 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800015039) | ||||
REF 91 | Hementin: anticoagulant protease from the salivary gland of the leech Haementeria ghilianii. J Lab Clin Med. 1984 Jan;103(1):44-58. | ||||
REF 92 | Thrombin inhibitors in acute coronary artery disease. Eur Heart J. 2002 Aug;23(15):1142-4. | ||||
REF 93 | Probing the hirudin-thrombin interaction by incorporation of noncoded amino acids and molecular dynamics simulation. Biochemistry. 2002 Nov 19;41(46):13556-69. | ||||
REF 94 | Assessment of thrombin inhibitor efficacy in a novel rabbit model of simultaneous arterial and venous thrombosis. Thromb Haemost. 1998 Mar;79(3):656-62. | ||||
REF 95 | L-374,087, an efficacious, orally bioavailable, pyridinone acetamide thrombin inhibitor. Bioorg Med Chem Lett. 1998 Apr 7;8(7):817-22. | ||||
REF 96 | Pharmacological 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 97 | Bioorg 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 98 | Antithrombotic activity of LB30057, a newly synthesized direct thrombin inhibitor. Thromb Haemost. 2003 Jan;89(1):104-11. | ||||
REF 99 | 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. J Med Chem. 2003 Aug 14;46(17):3612-22. | ||||
REF 100 | Recombinant hirudin (lepirudin) as anticoagulant in intensive care patients treated with continuous hemodialysis. Kidney Int Suppl. 1999 Nov;(72):S46-50. | ||||
REF 101 | Neuroprotective agents for the treatment of acute ischemic stroke. Curr Neurol Neurosci Rep. 2003 Jan;3(1):9-20. | ||||
REF 102 | Novel thrombin inhibitors that are based on a macrocyclic tripeptide motif, Bioorg. Med. Chem. Lett. 6(24):2947-2952 (1996). | ||||
REF 103 | Bioorg 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 104 | Clinical pipeline report, company report or official report of MYRIAD GENETICS, INC. | ||||
REF 105 | Effects 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 106 | Nucleic acid aptamers: clinical applications and promising new horizons. Curr Med Chem. 2011; 18(27): 4206-4214. | ||||
REF 107 | Aptamers in Bioanalysis. M. Mascini. 2009. Wiley. Page(46). | ||||
REF 108 | A 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 109 | Bioorg Med Chem Lett. 2010 Feb 15;20(4):1373-7. Epub 2010 Jan 11.Phenyltriazolinones as potent factor Xa inhibitors. | ||||
REF 110 | Bioorg 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 111 | Screening for selective thrombin inhibitors in mushrooms. Blood Coagul Fibrinolysis. 2001 Mar;12(2):123-8. | ||||
REF 112 | Pharmacokinetic 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 113 | Vasoflux, a new anticoagulant with a novel mechanism of action. Circulation. 1999 Feb 9;99(5):682-9. | ||||
REF 114 | Ximelagatran increases membrane fluidity and changes membrane lipid composition in primary human hepatocytes. Toxicol In Vitro. 2009 Jul 16. | ||||
REF 115 | Anticoagulation with anisindione in a patient with a warfarin-induced skin eruption. Pharmacotherapy. 2003 Apr;23(4):533-6. | ||||
REF 116 | EP42675, 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 117 | The NMR solution structure of recombinant RGD-hirudin. Biochem Biophys Res Commun. 2007 Aug 17;360(1):103-8. Epub 2007 Jun 13. | ||||
REF 118 | SR123781A, a synthetic heparin mimetic. Thromb Haemost. 2001 May;85(5):852-60. | ||||
REF 119 | Plasma 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. |
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