2B7D
 
 | | Factor VIIa Inhibitors: Chemical Optimization, Preclinical Pharmacokinetics, Pharmacodynamics, and Efficacy in a Baboon Thrombosis Model | | Descriptor: | (2R)-2-[5-(5-CARBAMIMIDOYL-1H-BENZOIMIDAZOL-2-YL)-6,2'-DIHYDROXY-5'-UREIDOMETHYL-BIPHENYL-3-YL]-SUCCINIC ACID, Coagulation factor VII, Tissue factor | | Authors: | Young, W.B, Mordenti, J, Torkelson, S, Shrader, W.D, Kolesnikov, A, Rai, R, Liu, L, Hu, H, Leahy, E.M, Green, M.J, Sprengeler, P.A, Katz, B.A, Yu, C, Janc, J.W, Elrod, K.C, Marzec, U.M, Hanson, S.R. | | Deposit date: | 2005-10-04 | | Release date: | 2006-02-14 | | Last modified: | 2023-08-23 | | Method: | X-RAY DIFFRACTION (2.24 Å) | | Cite: | Factor VIIa inhibitors: Chemical optimization, preclinical pharmacokinetics, pharmacodynamics, and efficacy in an arterial baboon thrombosis model.
Bioorg.Med.Chem.Lett., 16, 2006
|
|
2F9B
 | | Discovery of Novel Heterocyclic Factor VIIa Inhibitors | | Descriptor: | Coagulation factor VII, Tissue factor, {5-(5-AMINO-1H-PYRROLO[3,2-B]PYRIDIN-2-YL)-6-HYDROXY-3'-NITRO-BIPHENYL-3-YL]-ACETIC ACID | | Authors: | Rai, R, Kolesnikov, A, Sprengeler, P.A, Torkelson, S, Ton, T, Katz, B.A, Yu, C, Hendrix, J, Shrader, W.D, Stephens, R, Cabuslay, R, Sanford, E, Young, W.B. | | Deposit date: | 2005-12-05 | | Release date: | 2006-02-28 | | Last modified: | 2023-08-30 | | Method: | X-RAY DIFFRACTION (2.54 Å) | | Cite: | Discovery of novel heterocyclic factor VIIa inhibitors.
Bioorg.Med.Chem.Lett., 16, 2006
|
|
2FLR
 | | Novel 5-Azaindole Factor VIIa Inhibitors | | Descriptor: | Coagulation factor VII, Tissue factor, [2'-HYDROXY-3'-(1H-PYRROLO[3,2-C]PYRIDIN-2-YL)-BIPHENYL-3-YLMETHYL]-UREA | | Authors: | Riggs, J.R, Hu, H, Kolesnikov, A, Tong, Z, Leahy, E.M, Wesson, K.E, Shrader, W.D, Vijaykumar, D, Wahl, T.A, Sprengeler, P.A, Green, M.J, Yu, C, Katz, B.A, Young, W.B. | | Deposit date: | 2006-01-06 | | Release date: | 2007-01-23 | | Last modified: | 2017-10-18 | | Method: | X-RAY DIFFRACTION (2.35 Å) | | Cite: | Novel 5-azaindole factor VIIa inhibitors.
Bioorg.Med.Chem.Lett., 16, 2006
|
|
2ANW
 | | Expression, crystallization and three-dimensional structure of the catalytic domain of human plasma kallikrein: Implications for structure-based design of protease inhibitors | | Descriptor: | BENZAMIDINE, plasma kallikrein, light chain | | Authors: | Tang, J, Yu, C.L, Williams, S.R, Springman, E, Jeffery, D, Sprengeler, P.A, Estevez, A, Sampang, J, Shrader, W, Spencer, J.R, Young, W.B, McGrath, M.E, Katz, B.A. | | Deposit date: | 2005-08-11 | | Release date: | 2005-10-11 | | Last modified: | 2023-08-23 | | Method: | X-RAY DIFFRACTION (1.85 Å) | | Cite: | Expression, crystallization, and three-dimensional structure of the catalytic domain of human plasma kallikrein.
J.Biol.Chem., 280, 2005
|
|
2ANY
 | | Expression, Crystallization and the Three-dimensional Structure of the Catalytic Domain of Human Plasma Kallikrein: Implications for Structure-Based Design of Protease Inhibitors | | Descriptor: | BENZAMIDINE, PHOSPHATE ION, plasma kallikrein, ... | | Authors: | Tang, J, Yu, C.L, Williams, S.R, Springman, E, Jeffery, D, Sprengeler, P.A, Estevez, A, Sampang, J, Shrader, W, Spencer, J.R, Young, W.B, McGrath, M.E, Katz, B.A. | | Deposit date: | 2005-08-11 | | Release date: | 2005-10-11 | | Last modified: | 2023-08-23 | | Method: | X-RAY DIFFRACTION (1.4 Å) | | Cite: | Expression, crystallization, and three-dimensional structure of the catalytic domain of human plasma kallikrein.
J.Biol.Chem., 280, 2005
|
|
1O5E
 | | Dissecting and Designing Inhibitor Selectivity Determinants at the S1 site Using an Artificial Ala190 Protease (Ala190 uPA) | | Descriptor: | 6-CHLORO-2-(2-HYDROXY-BIPHENYL-3-YL)-1H-INDOLE-5-CARBOXAMIDINE, Serine protease hepsin | | Authors: | Katz, B.A, Luong, C, Ho, J.D, Somoza, J.R, Gjerstad, E, Tang, J, Williams, S.R, Verner, E, Mackman, R.L, Young, W.B, Sprengeler, P.A, Chan, H, Mortara, K, Janc, J.W, McGrath, M.E. | | Deposit date: | 2003-09-09 | | Release date: | 2004-09-21 | | Last modified: | 2023-12-27 | | Method: | X-RAY DIFFRACTION (1.75 Å) | | Cite: | Dissecting and designing inhibitor selectivity determinants at the S1 site using an artificial Ala190 protease (Ala190 uPA).
J.Mol.Biol., 344, 2004
|
|
1O5D
 | | Dissecting and Designing Inhibitor Selectivity Determinants at the S1 site Using an Artificial Ala190 Protease (Ala190 uPA) | | Descriptor: | 2-{5-[AMINO(IMINIO)METHYL]-6-FLUORO-1H-BENZIMIDAZOL-2-YL}-6-[(2-METHYLCYCLOHEXYL)OXY]BENZENOLATE, Coagulation factor VII, Tissue factor | | Authors: | Katz, B.A, Luong, C, Ho, J.D, Somoza, J.R, Gjerstad, E, Tang, J, Williams, S.R, Verner, E, Mackman, R.L, Young, W.B, Sprengeler, P.A, Chan, H, Mortara, K, Janc, J.W, McGrath, M.E. | | Deposit date: | 2003-09-09 | | Release date: | 2004-09-21 | | Last modified: | 2023-12-27 | | Method: | X-RAY DIFFRACTION (2.05 Å) | | Cite: | Dissecting and designing inhibitor selectivity determinants at the S1 site using an artificial Ala190 protease (Ala190 uPA).
J.Mol.Biol., 344, 2004
|
|
1O5A
 | | Dissecting and Designing Inhibitor Selectivity Determinants at the S1 site Using an Artificial Ala190 Protease (Ala190 uPA) | | Descriptor: | 3-{5-[AMINO(IMINIO)METHYL]-1H-INDOL-2-YL}-1,1'-BIPHENYL-2-OLATE, CITRIC ACID, Urokinase-type plasminogen activator | | Authors: | Katz, B.A, Luong, C, Ho, J.D, Somoza, J.R, Gjerstad, E, Tang, J, Williams, S.R, Verner, E, Mackman, R.L, Young, W.B, Sprengeler, P.A, Chan, H, Mortara, K, Janc, J.W, McGrath, M.E. | | Deposit date: | 2003-09-09 | | Release date: | 2004-09-21 | | Last modified: | 2023-12-27 | | Method: | X-RAY DIFFRACTION (1.68 Å) | | Cite: | Dissecting and designing inhibitor selectivity determinants at the S1 site using an artificial Ala190 protease (Ala190 uPA)
J.Mol.Biol., 344, 2004
|
|
1O5F
 | | Dissecting and Designing Inhibitor Selectivity Determinants at the S1 site Using an Artificial Ala190 Protease (Ala190 uPA) | | Descriptor: | 2-{5-[AMINO(IMINIO)METHYL]-6-FLUORO-1H-BENZIMIDAZOL-2-YL}-6-[(2-METHYLCYCLOHEXYL)OXY]BENZENOLATE, Serine protease hepsin | | Authors: | Katz, B.A, Luong, C, Ho, J.D, Somoza, J.R, Gjerstad, E, Tang, J, Williams, S.R, Verner, E, Mackman, R.L, Young, W.B, Sprengeler, P.A, Chan, H, Mortara, K, Janc, J.W, McGrath, M.E. | | Deposit date: | 2003-09-09 | | Release date: | 2004-09-21 | | Last modified: | 2023-12-27 | | Method: | X-RAY DIFFRACTION (1.78 Å) | | Cite: | Dissecting and designing inhibitor selectivity determinants at the S1 site using an artificial Ala190 protease (Ala190 uPA).
J.Mol.Biol., 344, 2004
|
|
1O5C
 | | Dissecting and Designing Inhibitor Selectivity Determinants at the S1 site Using an Artificial Ala190 Protease (Ala190 uPA) | | Descriptor: | 2-{5-[AMINO(IMINIO)METHYL]-6-FLUORO-1H-BENZIMIDAZOL-2-YL}-6-[(2-METHYLCYCLOHEXYL)OXY]BENZENOLATE, CITRIC ACID, Urokinase-type plasminogen activator | | Authors: | Katz, B.A, Luong, C, Ho, J.D, Somoza, J.R, Gjerstad, E, Tang, J, Williams, S.R, Verner, E, Mackman, R.L, Young, W.B, Sprengeler, P.A, Chan, H, Mortara, K, Janc, J.W, McGrath, M.E. | | Deposit date: | 2003-09-09 | | Release date: | 2004-09-21 | | Last modified: | 2023-12-27 | | Method: | X-RAY DIFFRACTION (1.63 Å) | | Cite: | Dissecting and designing inhibitor selectivity determinants at the S1 site using an artificial Ala190 protease (Ala190 uPA)
J.Mol.Biol., 344, 2004
|
|
1O5G
 | | Dissecting and Designing Inhibitor Selectivity Determinants at the S1 site Using an Artificial Ala190 Protease (Ala190 uPA) | | Descriptor: | 2-{5-[AMINO(IMINIO)METHYL]-6-FLUORO-1H-BENZIMIDAZOL-2-YL}-6-[(2-METHYLCYCLOHEXYL)OXY]BENZENOLATE, CALCIUM ION, Hirudin IIIB', ... | | Authors: | Katz, B.A, Luong, C, Ho, J.D, Somoza, J.R, Gjerstad, E, Tang, J, Williams, S.R, Verner, E, Mackman, R.L, Young, W.B, Sprengeler, P.A, Chan, H, Mortara, K, Janc, J.W, McGrath, M.E. | | Deposit date: | 2003-09-09 | | Release date: | 2004-09-21 | | Last modified: | 2023-11-15 | | Method: | X-RAY DIFFRACTION (1.75 Å) | | Cite: | Dissecting and designing inhibitor selectivity determinants at the S1 site using an artificial Ala190 protease (Ala190 uPA).
J.Mol.Biol., 344, 2004
|
|
1O5B
 | | Dissecting and Designing Inhibitor Selectivity Determinants at the S1 site Using an Artificial Ala190 Protease (Ala190 uPA) | | Descriptor: | 4-IODOBENZO[B]THIOPHENE-2-CARBOXAMIDINE, CITRIC ACID, Urokinase-type plasminogen activator | | Authors: | Katz, B.A, Luong, C, Ho, J.D, Somoza, J.R, Gjerstad, E, Tang, J, Williams, S.R, Verner, E, Mackman, R.L, Young, W.B, Sprengeler, P.A, Chan, H, Mortara, K, Janc, J.W, McGrath, M.E. | | Deposit date: | 2003-09-09 | | Release date: | 2004-09-21 | | Last modified: | 2023-12-27 | | Method: | X-RAY DIFFRACTION (1.85 Å) | | Cite: | Dissecting and designing inhibitor selectivity determinants at the S1 site using an artificial Ala190 protease (Ala190 uPA)
J.Mol.Biol., 344, 2004
|
|
