Target Validation Information
Target ID T27602
Target Name Trypsin
Target Type
Clinical Trial
Drug Potency against Target 4-(4-Benzyloxy-3-methoxy-benzylamino)-benzamidine Drug Info Ki = 580 nM [527397]
CVS-2139 Drug Info Ki = 20.8 nM [526306]
2-(2-Iodo-phenyl)-benzo[d][1,3]oxazin-4-one Drug Info IC50 = 15300 nM [534598]
Piperidine-1-carboxamidine Drug Info Ki = 360 nM [525858]
L-375378 Drug Info Ki = 1800 nM [526487]
RWJ-56423 Drug Info Ki = 8.1 nM [526956]
4-Indol-1-ylmethyl-benzamidine Drug Info Ki = 4590 nM [533527]
Macrocyclic tripeptide motif Drug Info Ki = 1 nM
GRASSYSTATIN A Drug Info IC50 = 10000 nM [530345]
6-Styryl-naphthalene-2-carboxamidine Drug Info Ki = 346 nM [527320]
1,3-Dibenzyl-[1,3]diazetidine-2,4-dione Drug Info IC50 = 39 nM [526092]
2-Propionyl-1H-indole-6-carboxamidine Drug Info Ki = 15300 nM [533527]
1,3-Di-p-tolyl-[1,3]diazetidine-2,4-dione Drug Info IC50 = 200 nM [526092]
8-Bromo-6-styryl-naphthalene-2-carboxamidine Drug Info Ki = 480 nM [527320]
8-Furan-3-yl-6-styryl-naphthalene-2-carboxamidine Drug Info Ki = 96 nM [527320]
BMY-44621 Drug Info IC50 = 7200 nM
L-370,518 Drug Info Ki = 11000 nM
CI-1031 Drug Info Ki = 280 nM [534797]
1-Benzyl-1H-indole-5-carboxamidine Drug Info Ki = 15400 nM [533527]
4-(5-Nitro-indol-1-ylmethyl)-benzamidine Drug Info Ki = 3440 nM [533527]
1-(3-Amino-benzyl)-1H-indole-5-carboxamidine Drug Info Ki = 16800 nM [533527]
4-(3,4-Diethoxy-benzylamino)-benzamidine Drug Info Ki = 2000 nM [527397]
CVS-2359 Drug Info Ki = 12.4 nM [526306]
2-(2-Hydroxy-phenyl)-1H-indole-5-carboxamidine Drug Info Ki = 8000 nM [526118]
INOGATRAN Drug Info Ki = 675 nM [534831]
1-(3-Nitro-benzyl)-1H-indole-5-carboxamidine Drug Info Ki = 7770 nM [533527]
RWJ-50353 Drug Info Ki = 3.1 nM [527480]
MELAGATRAN Drug Info IC50 = 11.9 nM [528066]
Tert-butyloxy carbonyl-D-Phe-pro-Arg-H Drug Info IC50 = 14 nM [533588]
GR-133686 Drug Info IC50 = 70 nM [534803]
References
Ref 527397Bioorg Med Chem Lett. 2005 Feb 1;15(3):817-22.Design of selective phenylglycine amide tissue factor/factor VIIa inhibitors.
Ref 526306Bioorg Med Chem Lett. 2002 Apr 22;12(8):1203-8.Non-covalent thrombin inhibitors featuring P(3)-heterocycles with P(1)-monocyclic arginine surrogates.
Ref 534598J Med Chem. 1998 Mar 26;41(7):1060-7.2-amino-4H-3,1-benzoxazin-4-ones as inhibitors of C1r serine protease.
Ref 525858J Med Chem. 2000 Aug 10;43(16):3033-44.GRID/CPCA: a new computational tool to design selective ligands.
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 526956J Med Chem. 2004 Feb 12;47(4):769-87.Inhibitors of serine proteases as potential therapeutic agents: the road from thrombin to tryptase to cathepsin G.
Ref 533527J Med Chem. 1983 Feb;26(2):294-8.Aromatic amidines: comparison of their ability to block respiratory syncytial virus induced cell fusion and to inhibit plasmin, urokinase, thrombin, and trypsin.
Ref 530345J Med Chem. 2009 Sep 24;52(18):5732-47.Grassystatins A-C from marine cyanobacteria, potent cathepsin E inhibitors that reduce antigen presentation.
Ref 527320Bioorg Med Chem Lett. 2005 Jan 3;15(1):93-8.Naphthamidine urokinase plasminogen activator inhibitors with improved pharmacokinetic properties.
Ref 526092Bioorg Med Chem Lett. 2001 Jul 9;11(13):1691-4.Inhibition of serine proteases: activity of 1,3-diazetidine-2,4-diones.
Ref 533527J Med Chem. 1983 Feb;26(2):294-8.Aromatic amidines: comparison of their ability to block respiratory syncytial virus induced cell fusion and to inhibit plasmin, urokinase, thrombin, and trypsin.
Ref 526092Bioorg Med Chem Lett. 2001 Jul 9;11(13):1691-4.Inhibition of serine proteases: activity of 1,3-diazetidine-2,4-diones.
Ref 527320Bioorg Med Chem Lett. 2005 Jan 3;15(1):93-8.Naphthamidine urokinase plasminogen activator inhibitors with improved pharmacokinetic properties.
Ref 527320Bioorg Med Chem Lett. 2005 Jan 3;15(1):93-8.Naphthamidine urokinase plasminogen activator inhibitors with improved pharmacokinetic properties.
Ref 534797Bioorg Med Chem Lett. 1998 Aug 18;8(16):2235-40.Design, synthesis, and biological activity of novel purine and bicyclic pyrimidine factor Xa inhibitors.
Ref 533527J Med Chem. 1983 Feb;26(2):294-8.Aromatic amidines: comparison of their ability to block respiratory syncytial virus induced cell fusion and to inhibit plasmin, urokinase, thrombin, and trypsin.
Ref 533527J Med Chem. 1983 Feb;26(2):294-8.Aromatic amidines: comparison of their ability to block respiratory syncytial virus induced cell fusion and to inhibit plasmin, urokinase, thrombin, and trypsin.
Ref 533527J Med Chem. 1983 Feb;26(2):294-8.Aromatic amidines: comparison of their ability to block respiratory syncytial virus induced cell fusion and to inhibit plasmin, urokinase, thrombin, and trypsin.
Ref 527397Bioorg Med Chem Lett. 2005 Feb 1;15(3):817-22.Design of selective phenylglycine amide tissue factor/factor VIIa inhibitors.
Ref 526306Bioorg Med Chem Lett. 2002 Apr 22;12(8):1203-8.Non-covalent thrombin inhibitors featuring P(3)-heterocycles with P(1)-monocyclic arginine surrogates.
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 534831Bioorg Med Chem Lett. 1998 Dec 15;8(24):3603-8.Novel acylguanidine containing thrombin inhibitors with reduced basicity at the P1 moiety.
Ref 533527J Med Chem. 1983 Feb;26(2):294-8.Aromatic amidines: comparison of their ability to block respiratory syncytial virus induced cell fusion and to inhibit plasmin, urokinase, thrombin, and trypsin.
Ref 527480J Med Chem. 2005 Mar 24;48(6):1984-2008.In-depth study of tripeptide-based alpha-ketoheterocycles as inhibitors of thrombin. Effective utilization of the S1' subsite and its implications to structure-based drug design.
Ref 528066Bioorg Med Chem Lett. 2006 May 15;16(10):2641-7. Epub 2006 Mar 6.Orally active thrombin inhibitors. Part 1: optimization of the P1-moiety.
Ref 533588J Med Chem. 1995 Oct 27;38(22):4446-53.Structure-activity study of tripeptide thrombin inhibitors using alpha-alkyl amino acids and other conformationally constrained amino acid substitutions.
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.

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