Current Protein Identity:P00749 New Search
Main Difference Dimensions in This Set
Different construct Different mutation/modification Different assembly state Different ligand/ion Different experimental method Different experimental conditions Different structure-quality metrics

Difference tags compare only the current result set; every original PDB and assembly record remains separate.

Related-Structure Differences

Each row represents one biological assembly in one PDB entry; multiple monomers of the same protein are listed separately.

PDB Entry Assembly / Oligomeric State Construct Mutations and Modifications Ligands, Ions and Non-polymers Experimental Method Experimental Conditions Structure Quality
1C5W STRUCTURAL BASIS FOR SELECTIVITY OF A SMALL MOLECULE, S1-BINDING, SUB-MICROMOLAR INHIBITOR OF UROKINASE TYPE PLASMINOGEN ACTIVATOR Deposited 1999-12-22 Assembly 1 Protein homooligomer Homooligomer;Protein × 2 PDB declaration: dimeric(2) Consistent with protein count
Chain A 156–178(23 aa) Fragment:SHORT CHAIN
Chain B 179–431(253 aa) Fragment:CATALYTIC DOMAIN
Not recorded FLC CITRATE ANION × 3 ESI 4-IODOBENZO[B]THIOPHENE-2-CARBOXAMIDINE × 1 X-RAY DIFFRACTION
X-ray crystallization conditions pH 6.5;LMW human uPA/A145 was concentrated to 10 mg/ml and incubated in 50 mM HEPES, 5.0 mM NaCl. pH 7.0, 1.4 mM 4-iodobenzo[b]thiophene-2-carboxamidine for 15 min on ice. The complex was crystallized by vapor diffusion in hanging drops containing equal volumes of protein-inhibitor solution (0.28 mM uPA/A145, 1.4 mM inhibitor) and well solution (20 % 2-propanol, 20 % PEG 4K, 100 mM sodium citrate, pH 6.5) sealed over the well.
Resolution 1.94 Å R-free 0.211
1C5X STRUCTURAL BASIS FOR SELECTIVITY OF A SMALL MOLECULE, S1-BINDING, SUB-MICROMOLAR INHIBITOR OF UROKINASE TYPE PLASMINOGEN ACTIVATOR Deposited 1999-12-22 Assembly 1 Protein homooligomer Homooligomer;Protein × 2 PDB declaration: dimeric(2) Consistent with protein count
Chain A 156–178(23 aa) Fragment:SHORT CHAIN
Chain B 179–431(253 aa) Fragment:CATALYTIC DOMAIN
Not recorded FLC CITRATE ANION × 3 ESI 4-IODOBENZO[B]THIOPHENE-2-CARBOXAMIDINE × 1 X-RAY DIFFRACTION
X-ray crystallization conditions pH 6.5;LMW human uPA/A145 was concentrated to 10 mg/ml and incubated in 50 mM HEPES, 5.0 mM NaCl. pH 7.4, 1.4 mM 4-iodobenzo[b]thiophene-2-carboxamidine for 15 min on ice. The complex was crystallized by vapor diffusion in hanging drops containing equal volumes of protein-inhibitor solution (0.28 mM uPA/A145, 1.4 mM inhibitor) and well solution (20 % 2-propanol, 20 % PEG 4K, 100 mM sodium citrate, pH 6.5) sealed over the well.
Resolution 1.75 Å R-free 0.244
1C5Y STRUCTURAL BASIS FOR SELECTIVITY OF A SMALL MOLECULE, S1-BINDING, SUB-MICROMOLAR INHIBITOR OF UROKINASE TYPE PLASMINOGEN ACTIVATOR Deposited 1999-12-22 Assembly 1 Protein homooligomer Homooligomer;Protein × 2 PDB declaration: dimeric(2) Consistent with protein count
Chain A 156–178(23 aa) Fragment:SHORT CHAIN
Chain B 179–431(253 aa) Fragment:CATALYTIC DOMAIN
Not recorded FLC CITRATE ANION × 3 ESP THIENO[2,3-B]PYRIDINE-2-CARBOXAMIDINE × 1 X-RAY DIFFRACTION
X-ray crystallization conditions pH 6.5;LMW human uPA/A145 was concentrated to 10 mg/ml and incubated in 50 mM HEPES, 5.0 mM NaCl. pH 7.0, 5.0 mM thieno[2,3-b]pyridine-2-carboxamidine for 15 min on ice. The complex was crystallized by vapor diffusion in hanging drops containing equal volumes of protein-inhibitor solution (0.28 mM uPA/A145, 1.4 mM inhibitor and well solution (20 % 2-propanol, 20 % PEG 4K, 100 mM sodium citrate, pH 6.5) sealed over the well.
Resolution 1.65 Å R-free 0.246
1C5Z STRUCTURAL BASIS FOR SELECTIVITY OF A SMALL MOLECULE, S1-BINDING, SUB-MICROMOLAR INHIBITOR OF UROKINASE TYPE PLASMINOGEN ACTIVATOR Deposited 1999-12-22 Assembly 1 Protein homooligomer Homooligomer;Protein × 2 PDB declaration: dimeric(2) Consistent with protein count
Chain A 156–178(23 aa) Fragment:SHORT CHAIN
Chain B 179–431(253 aa) Fragment:CATALYTIC DOMAIN
Not recorded FLC CITRATE ANION × 3 BEN BENZAMIDINE × 1 X-RAY DIFFRACTION
X-ray crystallization conditions pH 6.5;LMW human uPA/A145 was concentrated to 10 mg/ml and incubated in 50 mM HEPES, 5.0 mM NaCl. pH 7.0, 5.0 mM benzamidne for 15 min on ice. The complex was crystallized by vapor diffusion in hanging drops containing equal volumes of protein-inhibitor solution (0.28 mM uPA/A145, 1.4 mM inhibitor) and well solution (20 % 2-propanol, 20 % PEG 4K, 100 mM sodium citrate, pH 6.5) sealed over the well.
Resolution 1.85 Å R-free 0.237
1EJN UROKINASE PLASMINOGEN ACTIVATOR B-CHAIN INHIBITOR COMPLEX Deposited 2000-04-22 Assembly 1 Protein monomer Monomer;Protein × 1 PDB declaration: monomeric(1) Consistent with protein count
Chain A 159–411(253 aa) Fragment:B CHAIN
Mutation:C279S SO4 SULFATE ION × 1 AGB N-(1-ADAMANTYL)-N'-(4-GUANIDINOBENZYL)UREA × 1 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, SITTING DROP;pH 5.2;298 K;pH 5.2, VAPOR DIFFUSION, SITTING DROP, temperature 298K
Resolution 1.80 Å R-free 0.240
1F5L UROKINASE PLASMINOGEN ACTIVATOR B-CHAIN-AMILORIDE COMPLEX Deposited 2000-06-15 Assembly 1 Protein monomer Monomer;Protein × 1 PDB declaration: monomeric(1) Consistent with protein count
Chain A 159–411(253 aa) Fragment:B CHAIN
Mutation:C279S SO4 SULFATE ION × 2 AMR 3,5-DIAMINO-N-(AMINOIMINOMETHYL)-6-CHLOROPYRAZINECARBOXAMIDE × 1 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, SITTING DROP;pH 5.2;298 K;pH 5.2, VAPOR DIFFUSION, SITTING DROP, temperature 298K
Resolution 2.10 Å R-free 0.250
1F92 UROKINASE PLASMINOGEN ACTIVATOR B CHAIN-UKI-1D COMPLEX Deposited 2000-07-06 Assembly 1 Protein monomer Monomer;Protein × 1 PDB declaration: monomeric(1) Consistent with protein count
Chain A 159–411(253 aa) Fragment:B CHAIN
Mutation:C279S SO4 SULFATE ION × 2 UKP [2,4,6-TRIISOPROPYL-PHENYLSULFONYL-L-[3-AMIDINO-PHENYLALANINYL]]-N'-BETA-ALANINYL-PIPERAZINE × 1 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, SITTING DROP;pH 5.2;298 K;pH 5.2, VAPOR DIFFUSION, SITTING DROP, temperature 298K
Resolution 2.60 Å R-free 0.248
1FV9 Crystal structure of human microurokinase in complex with 2-amino-5-hydroxy-benzimidazole Deposited 2000-09-19 Assembly 1 Protein monomer Monomer;Protein × 1 PDB declaration: monomeric(1) Consistent with protein count
Chain A 179–423(245 aa) Fragment:B CHAIN (16-243)
Mutation:C122A, N145Q SO4 SULFATE ION × 1 172 2-AMINO-5-HYDROXY-BENZIMIDAZOLE × 1 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, HANGING DROP;291 K;0.15M LiSo4, 20% PEG 4000, succinate buffer, VAPOR DIFFUSION, HANGING DROP, temperature 18K
Resolution 3.00 Å
1GI7 A NOVEL SERINE PROTEASE INHIBITION MOTIF INVOLVING A MULTI-CENTERED SHORT HYDROGEN BONDING NETWORK AT THE ACTIVE SITE Deposited 2001-01-22 Assembly 1 Protein homooligomer Homooligomer;Protein × 2 PDB declaration: dimeric(2) Consistent with protein count
Chain A 156–178(23 aa) Fragment:SHORT CHAIN
Chain B 179–423(245 aa) Fragment:CATALYTIC DOMAIN
Mutation:N145A 120 2-(2-OXO-1,2-DIHYDRO-PYRIDIN-3-YL)-1H-BENZOIMIDAZOLE-5-CARBOXAMIDINE × 1 CIT CITRIC ACID × 2 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION;pH 6.5;298 K;2-propanol PEG 4000, pH 6.5, vapor diffusion at 298 K, pH 6.50
Resolution 1.79 Å R-free 0.220
1GI8 A NOVEL SERINE PROTEASE INHIBITION MOTIF INVOLVING A MULTI-CENTERED SHORT HYDROGEN BONDING NETWORK AT THE ACTIVE SITE Deposited 2001-01-22 Assembly 1 Protein homooligomer Homooligomer;Protein × 2 PDB declaration: dimeric(2) Consistent with protein count
Chain A 156–178(23 aa) Fragment:SHORT CHAIN
Chain B 179–423(245 aa) Fragment:CATALYTIC DOMAIN
Mutation:N145A CIT CITRIC ACID × 2 BMZ 2-(2-HYDROXY-PHENYL)-1H-BENZOIMIDAZOLE-5-CARBOXAMIDINE × 1 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION;pH 6.5;298 K;2-propanol PEG 4000, pH 6.5, vapor diffusion at 298 K, pH 6.50
Resolution 1.75 Å R-free 0.254
1GI9 A NOVEL SERINE PROTEASE INHIBITION MOTIF INVOLVING A MULTI-CENTERED SHORT HYDROGEN BONDING NETWORK AT THE ACTIVE SITE Deposited 2001-01-22 Assembly 1 Protein homooligomer Homooligomer;Protein × 2 PDB declaration: dimeric(2) Consistent with protein count
Chain A 156–178(23 aa) Fragment:SHORT CHAIN
Chain B 179–423(245 aa) Fragment:CATALYTIC DOMAIN
Mutation:N145A 123 2-(2-HYDROXY-5-METHOXY-PHENYL)-1H-BENZOIMIDAZOLE-5-CARBOXAMIDINE × 1 CIT CITRIC ACID × 2 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION;pH 6.5;298 K;2-propanol PEG 4000, pH 6.5, vapor diffusion at 298 K, pH 6.50
Resolution 1.80 Å R-free 0.238
1GJ7 ENGINEERING INHIBITORS HIGHLY SELECTIVE FOR THE S1 SITES OF SER190 TRYPSIN-LIKE SERINE PROTEASE DRUG TARGETS Deposited 2001-04-27 Assembly 1 Protein homooligomer Homooligomer;Protein × 2 PDB declaration: dimeric(2) Consistent with protein count
Chain A 156–178(23 aa) Fragment:SHORT CHAIN
Chain B 179–431(253 aa) Fragment:CATALYTIC DOMAIN
Mutation:N145A CIT CITRIC ACID × 2 132 6-CHLORO-2-(2-HYDROXY-BIPHENYL-3-YL)-1H-INDOLE-5-CARBOXAMIDINE × 1 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION;pH 6.5;298 K;2-propanol PEG 4000, pH 6.5, vapor diffusion at 298 K, pH 6.50
Resolution 1.50 Å R-free 0.230
1GJ8 ENGINEERING INHIBITORS HIGHLY SELECTIVE FOR THE S1 SITES OF SER190 TRYPSIN-LIKE SERINE PROTEASE DRUG TARGETS Deposited 2001-04-27 Assembly 1 Protein homooligomer Homooligomer;Protein × 2 PDB declaration: dimeric(2) Consistent with protein count
Chain A 156–178(23 aa) Fragment:SHORT CHAIN
Chain B 179–431(253 aa) Fragment:CATALYTIC DOMAIN
Mutation:N145A CIT CITRIC ACID × 2 133 6-FLUORO-2-(2-HYDROXY-3-ISOBUTOXY-PHENYL)-1H-BENZOIMIDAZOLE-5-CARBOXAMIDINE × 1 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION;pH 6.5;298 K;2-propanol, PEG 4000, pH 6.5, vapor diffusion at 298 K, pH 6.50
Resolution 1.64 Å R-free 0.221
1GJ9 ENGINEERING INHIBITORS HIGHLY SELECTIVE FOR THE S1 SITES OF SER190 TRYPSIN-LIKE SERINE PROTEASE DRUG TARGETS Deposited 2001-04-30 Assembly 1 Protein homooligomer Homooligomer;Protein × 2 PDB declaration: dimeric(2) Consistent with protein count
Chain A 156–178(23 aa) Fragment:SHORT CHAIN
Chain B 179–431(253 aa) Fragment:CATALYTIC DOMAIN
Mutation:N145A CIT CITRIC ACID × 2 134 6-FLUORO-2-[2-HYDROXY-3-(2-METHYL-CYCLOHEXYLOXY)-PHENYL]-1H-INDOLE-5-CARBOXAMIDINE × 1 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION;pH 6.5;298 K;2-propanol PEG 4000, pH 6.5, vapor diffusion at 298 K, pH 6.50
Resolution 1.80 Å R-free 0.222
1GJA ENGINEERING INHIBITORS HIGHLY SELECTIVE FOR THE S1 SITES OF SER190 TRYPSIN-LIKE SERINE PROTEASE DRUG TARGETS Deposited 2001-04-27 Assembly 1 Protein homooligomer Homooligomer;Protein × 2 PDB declaration: dimeric(2) Consistent with protein count
Chain A 156–178(23 aa) Fragment:SHORT CHAIN
Chain B 179–431(253 aa) Fragment:CATALYTIC DOMAIN
Mutation:N145A CIT CITRIC ACID × 2 135 N-(4-CARBAMIMIDOYL-PHENYL)-2-HYDROXY-BENZAMIDE × 1 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION;pH 6.5;298 K;2-propanol PEG 4000, pH 6.5, vapor diffusion at 298 K, pH 6.50
Resolution 1.56 Å R-free 0.209
1GJB ENGINEERING INHIBITORS HIGHLY SELECTIVE FOR THE S1 SITES OF SER190 TRYPSIN-LIKE SERINE PROTEASE DRUG TARGETS Deposited 2001-04-27 Assembly 1 Protein homooligomer Homooligomer;Protein × 2 PDB declaration: dimeric(2) Consistent with protein count
Chain A 156–178(23 aa) Fragment:SHORT CHAIN
Chain B 179–431(253 aa) Fragment:CATALYTIC DOMAIN
Mutation:N145A CIT CITRIC ACID × 2 130 2-(2-HYDROXY-BIPHENYL)-1H-BENZOIMIDAZOLE-5-CARBOXAMIDINE × 1 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION;pH 6.5;298 K;2-propanol, PEG 4000, pH 6.5, vapor diffusion at 298 K, pH 6.50
Resolution 1.90 Å R-free 0.259
1GJC ENGINEERING INHIBITORS HIGHLY SELECTIVE FOR THE S1 SITES OF SER190 TRYPSIN-LIKE SERINE PROTEASE DRUG TARGETS Deposited 2001-04-27 Assembly 1 Protein homooligomer Homooligomer;Protein × 2 PDB declaration: dimeric(2) Consistent with protein count
Chain A 156–178(23 aa) Fragment:SHORT CHAIN
Chain B 179–431(253 aa) Fragment:CATALYTIC DOMAIN
Mutation:N145A CIT CITRIC ACID × 2 130 2-(2-HYDROXY-BIPHENYL)-1H-BENZOIMIDAZOLE-5-CARBOXAMIDINE × 1 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION;pH 6.5;298 K;2-propanol, PEG 4000, pH 6.5, vapor diffusion at 298 K, pH 6.50
Resolution 1.73 Å R-free 0.242
1GJD ENGINEERING INHIBITORS HIGHLY SELECTIVE FOR THE S1 SITES OF SER190 TRYPSIN-LIKE SERINE PROTEASE DRUG TARGETS Deposited 2001-05-03 Assembly 1 Protein homooligomer Homooligomer;Protein × 2 PDB declaration: dimeric(2) Consistent with protein count
Chain A 156–178(23 aa) Fragment:SHORT CHAIN
Chain B 179–431(253 aa) Fragment:CATALYTIC DOMAIN
Mutation:N145A CIT CITRIC ACID × 2 136 N-(4-CARBAMIMIDOYL-3-CHORO-PHENYL)-2-HYDROXY-3-IODO-5-METHYL-BENZAMIDE × 1 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION;pH 6.5;298 K;2-propanol, PEG 4000, pH 6.5, vapor diffusion at 298 K, pH 6.50
Resolution 1.75 Å R-free 0.189
1KDU SEQUENTIAL 1H NMR ASSIGNMENTS AND SECONDARY STRUCTURE OF THE KRINGLE DOMAIN FROM UROKINASE Deposited 1993-07-15 Assembly 1 Protein monomer Monomer;Protein × 1 PDB declaration: monomeric(1) Consistent with protein count
Chain A 69–153(85 aa)
Not recorded No recorded non-water small molecule SOLUTION NMR mmCIF provides none of the parsed conditions Resolution not provided
1LMW LMW U-PA Structure complexed with EGRCMK (GLU-GLY-ARG Chloromethyl Ketone) Deposited 1995-07-26 Assembly 1 Protein homooligomer Homooligomer;Protein × 2 PDB declaration: dimeric(2) Consistent with protein count
Chain A 156–178(23 aa)
Chain B 179–431(253 aa)
Not recorded 0GJ L-alpha-glutamyl-N-{(1S)-4-{[amino(iminio)methyl]amino}-1-[(1S)-2-chloro-1-hydroxyethyl]butyl}glycinamide × 1 X-RAY DIFFRACTION mmCIF provides none of the parsed conditions Resolution 2.50 Å
1LMW LMW U-PA Structure complexed with EGRCMK (GLU-GLY-ARG Chloromethyl Ketone) Deposited 1995-07-26 Assembly 2 Protein homooligomer Homooligomer;Protein × 2 PDB declaration: dimeric(2) Consistent with protein count
Chain C 156–178(23 aa)
Chain D 179–431(253 aa)
Not recorded 0GJ L-alpha-glutamyl-N-{(1S)-4-{[amino(iminio)methyl]amino}-1-[(1S)-2-chloro-1-hydroxyethyl]butyl}glycinamide × 1 X-RAY DIFFRACTION mmCIF provides none of the parsed conditions Resolution 2.50 Å
1O3P Elaborate Manifold of Short Hydrogen Bond Arrays Mediating Binding of Active Site-Directed Serine Protease Inhibitors Deposited 2003-03-06 Assembly 1 Protein homooligomer Homooligomer;Protein × 2 PDB declaration: dimeric(2) Consistent with protein count
Chain A 156–178(23 aa) Fragment:SHORT CHAIN
Chain B 179–431(253 aa) Fragment:CATALYTIC DOMAIN
Mutation:N145A CIT CITRIC ACID × 2 655 2-{5-[AMINO(IMINIO)METHYL]-1H-BENZIMIDAZOL-2-YL}-6-(CYCLOPENTYLOXY)BENZENOLATE × 1 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION;pH 6.5;298 K;2-propanol, PEG 4000, pH 6.5, vapor diffusion at 298 K, pH 6.50
Resolution 1.81 Å R-free 0.249
1O5A Dissecting and Designing Inhibitor Selectivity Determinants at the S1 site Using an Artificial Ala190 Protease (Ala190 uPA) Deposited 2003-09-09 Assembly 1 Protein homooligomer Homooligomer;Protein × 2 PDB declaration: dimeric(2) Consistent with protein count
Chain A 156–178(23 aa) Fragment:SHORT CHAIN
Chain B 179–431(253 aa) Fragment:CATALYTIC DOMAIN
Mutation:N145A/S190A 696 3-{5-[AMINO(IMINIO)METHYL]-1H-INDOL-2-YL}-1,1'-BIPHENYL-2-OLATE × 1 CIT CITRIC ACID × 1 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION;pH 6.5;298 K;2-propanol, PEG 4000, pH 6.5, vapor diffusion at 298 K, pH 6.5, pH 6.50
Resolution 1.68 Å R-free 0.245
1O5B Dissecting and Designing Inhibitor Selectivity Determinants at the S1 site Using an Artificial Ala190 Protease (Ala190 uPA) Deposited 2003-09-09 Assembly 1 Protein homooligomer Homooligomer;Protein × 2 PDB declaration: dimeric(2) Consistent with protein count
Chain A 156–178(23 aa) Fragment:SHORT CHAIN
Chain B 179–431(253 aa) Fragment:CATALYTIC DOMAIN
Mutation:N145A/S190A ESI 4-IODOBENZO[B]THIOPHENE-2-CARBOXAMIDINE × 1 CIT CITRIC ACID × 3 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION;pH 6.5;298 K;2-propanol, PEG 4000, pH 6.5, vapor diffusion at 298 K, pH 6.5, pH 6.50
Resolution 1.85 Å R-free 0.240
1O5C Dissecting and Designing Inhibitor Selectivity Determinants at the S1 site Using an Artificial Ala190 Protease (Ala190 uPA) Deposited 2003-09-09 Assembly 1 Protein homooligomer Homooligomer;Protein × 2 PDB declaration: dimeric(2) Consistent with protein count
Chain A 156–178(23 aa) Fragment:SHORT CHAIN
Chain B 179–431(253 aa) Fragment:CATALYTIC DOMAIN
Mutation:N145A/S190A CR9 2-{5-[AMINO(IMINIO)METHYL]-6-FLUORO-1H-BENZIMIDAZOL-2-YL}-6-[(2-METHYLCYCLOHEXYL)OXY]BENZENOLATE × 1 CIT CITRIC ACID × 2 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION;pH 6.5;298 K;2-propanol, PEG 4000, pH 6.5, vapor diffusion at 298 K, pH 6.5, pH 6.50
Resolution 1.63 Å R-free 0.219
1OWD Substituted 2-Naphthamidine inhibitors of urokinase Deposited 2003-03-28 Assembly 1 Protein monomer Monomer;Protein × 1 PDB declaration: monomeric(1) Consistent with protein count
Chain A 179–423(245 aa) Fragment:residues 179-423
Not recorded 497 6-[AMINO(IMINO)METHYL]-N-[(4R)-4-ETHYL-1,2,3,4-TETRAHYDROISOQUINOLIN-6-YL]-2-NAPHTHAMIDE × 1 X-RAY DIFFRACTION mmCIF provides none of the parsed conditions Resolution 2.32 Å R-free 0.313
1OWE Substituted 2-Naphthamidine inhibitors of urokinase Deposited 2003-03-28 Assembly 1 Protein monomer Monomer;Protein × 1 PDB declaration: monomeric(1) Consistent with protein count
Chain A 179–423(245 aa) Fragment:residues 179-423
Not recorded SO4 SULFATE ION × 3 675 6-[(Z)-AMINO(IMINO)METHYL]-N-PHENYL-2-NAPHTHAMIDE × 1 X-RAY DIFFRACTION mmCIF provides none of the parsed conditions Resolution 1.60 Å R-free 0.236
1OWH Substituted 2-Naphthamidine Inhibitors of Urokinase Deposited 2003-03-28 Assembly 1 Protein monomer Monomer;Protein × 1 PDB declaration: monomeric(1) Consistent with protein count
Chain A 179–423(245 aa) Fragment:residues 179-423
Not recorded SO4 SULFATE ION × 3 239 6-[(Z)-AMINO(IMINO)METHYL]-N-[4-(AMINOMETHYL)PHENYL]-2-NAPHTHAMIDE × 1 X-RAY DIFFRACTION mmCIF provides none of the parsed conditions Resolution 1.61 Å R-free 0.265
1OWI Substituted 2-Naphthamidine Inhibitors of Urokinase Deposited 2003-03-28 Assembly 1 Protein monomer Monomer;Protein × 1 PDB declaration: monomeric(1) Consistent with protein count
Chain A 179–423(245 aa) Fragment:residues 179-423
Not recorded 426 6-[(Z)-AMINO(IMINO)METHYL]-N-[3-(CYCLOPENTYLOXY)PHENYL]-2-NAPHTHAMIDE × 1 X-RAY DIFFRACTION mmCIF provides none of the parsed conditions Resolution 2.93 Å R-free 0.349
1OWJ Substituted 2-Naphthamidine Inhibitors of Urokinase Deposited 2003-03-28 Assembly 1 Protein monomer Monomer;Protein × 1 PDB declaration: monomeric(1) Consistent with protein count
Chain A 179–423(245 aa) Fragment:residues 179-423
Not recorded 155 6-[(Z)-AMINO(IMINO)METHYL]-N-(1-ISOPROPYL-3,4-DIHYDROISOQUINOLIN-7-YL)-2-NAPHTHAMIDE × 1 X-RAY DIFFRACTION mmCIF provides none of the parsed conditions Resolution 3.10 Å R-free 0.344
1OWK Substituted 2-Naphthamidine Inhibitors of Urokinase Deposited 2003-03-28 Assembly 1 Protein monomer Monomer;Protein × 1 PDB declaration: monomeric(1) Consistent with protein count
Chain A 179–423(245 aa) Fragment:residues 179-423
Not recorded 303 6-[(Z)-AMINO(IMINO)METHYL]-N-(1-ISOPROPYL-1,2,3,4-TETRAHYDROISOQUINOLIN-7-YL)-2-NAPHTHAMIDE × 1 X-RAY DIFFRACTION mmCIF provides none of the parsed conditions Resolution 2.80 Å R-free 0.236
1SC8 Urokinase Plasminogen Activator B-Chain-J435 Complex Deposited 2004-02-12 Assembly 1 Protein monomer Monomer;Protein × 1 PDB declaration: monomeric(1) Consistent with protein count
Chain U 164–425(262 aa) Fragment:B Chain
Mutation:C122S SO4 SULFATE ION × 2 2IN N-(BENZYLSULFONYL)SERYL-N~1~-{4-[AMINO(IMINO)METHYL]BENZYL}GLYCINAMIDE × 1 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, HANGING DROP;pH 5.2;277 K;sodium citrate, ammonium sulfate, litium sulfate, pH 5.2, VAPOR DIFFUSION, HANGING DROP, temperature 277K
Resolution 2.40 Å R-free 0.240
1SQA Substituted 2-Naphthamidine Inhibitors of Urokinase Deposited 2004-03-18 Assembly 1 Protein monomer Monomer;Protein × 1 PDB declaration: monomeric(1) Consistent with protein count
Chain A 179–423(245 aa)
Not recorded SO4 SULFATE ION × 3 UI1 6-[(Z)-AMINO(IMINO)METHYL]-N-[4-(AMINOMETHYL)PHENYL]-4-(PYRIMIDIN-2-YLAMINO)-2-NAPHTHAMIDE × 1 X-RAY DIFFRACTION mmCIF provides none of the parsed conditions Resolution 2.00 Å R-free 0.266
1SQO Substituted 2-Naphthamidine Inhibitors of Urokinase Deposited 2004-03-19 Assembly 1 Protein monomer Monomer;Protein × 1 PDB declaration: monomeric(1) Consistent with protein count
Chain A 179–423(245 aa)
Not recorded SO4 SULFATE ION × 3 UI2 8-(PYRIMIDIN-2-YLAMINO)NAPHTHALENE-2-CARBOXIMIDAMIDE × 1 X-RAY DIFFRACTION mmCIF provides none of the parsed conditions Resolution 1.84 Å R-free 0.284
1SQT Substituted 2-Naphthamidine Inhibitors of Urokinase Deposited 2004-03-19 Assembly 1 Protein monomer Monomer;Protein × 1 PDB declaration: monomeric(1) Consistent with protein count
Chain A 179–423(245 aa)
Not recorded UI3 7-METHOXY-8-[1-(METHYLSULFONYL)-1H-PYRAZOL-4-YL]NAPHTHALENE-2-CARBOXIMIDAMIDE × 1 X-RAY DIFFRACTION mmCIF provides none of the parsed conditions Resolution 1.90 Å R-free 0.236
1U6Q Substituted 2-Naphthamadine inhibitors of Urokinase Deposited 2004-07-30 Assembly 1 Protein monomer Monomer;Protein × 1 PDB declaration: monomeric(1) Consistent with protein count
Chain A 179–423(245 aa) Fragment:Residues 179-423
Not recorded 745 TRANS-6-(2-PHENYLCYCLOPROPYL)-NAPHTHALENE-2-CARBOXAMIDINE × 1 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, HANGING DROP;VAPOR DIFFUSION, HANGING DROP
Resolution 2.02 Å R-free 0.290
1URK SOLUTION STRUCTURE OF THE AMINO TERMINAL FRAGMENT OF UROKINASE-TYPE PLASMINOGEN ACTIVATOR Deposited 1994-01-10 Assembly 1 Protein monomer Monomer;Protein × 1 PDB declaration: monomeric(1) Consistent with protein count
Chain A 26–155(130 aa)
Not recorded FUC alpha-L-fucopyranose × 1 SOLUTION NMR mmCIF provides none of the parsed conditions Resolution not provided
1VJ9 Urokinase Plasminogen Activator B-Chain-JT464 Complex Deposited 2004-02-03 Assembly 1 Protein monomer Monomer;Protein × 1 PDB declaration: monomeric(1) Consistent with protein count
Chain U 164–425(262 aa) Fragment:B Chain
Mutation:C122S SO4 SULFATE ION × 2 5IN N-(BENZYLSULFONYL)-L-SERYL-N~1~-{4-[AMINO(IMINO)METHYL]BENZYL}-O-BENZYL-L-SERINAMIDE × 1 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, HANGING DROP;pH 5.2;277 K;sodium citrate, ammonium sulfate, lithium sulfate, pH 5.2, VAPOR DIFFUSION, HANGING DROP, temperature 277K
Resolution 2.40 Å R-free 0.247
1VJA Urokinase Plasminogen Activator B-Chain-JT463 Complex Deposited 2004-02-03 Assembly 1 Protein monomer Monomer;Protein × 1 PDB declaration: monomeric(1) Consistent with protein count
Chain U 164–425(262 aa) Fragment:B Chain
Mutation:C122S SO4 SULFATE ION × 2 7IN N-(BENZYLSULFONYL)SERYL-N~1~-{4-[(Z)-AMINO(IMINO)METHYL]BENZYL}SERINAMIDE × 1 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, HANGING DROP;pH 5.2;277 K;sodium citrate, ammonium sulfate, lithium sulfate, pH 5.2, VAPOR DIFFUSION, HANGING DROP, temperature 277K
Resolution 2.00 Å R-free 0.232
1W0Z Urokinase type plasminogen activator Deposited 2004-06-15 Assembly 1 Protein monomer Monomer;Protein × 1 PDB declaration: monomeric(1) Consistent with protein count
Chain U 179–425(247 aa) Fragment:RESIDUES 179-425
Not recorded SI1 N-(BUTYLSULFONYL)-D-SERYL-N-{4-[AMINO(IMINO)METHYL]BENZYL}-L-ALANINAMIDE × 1 SO4 SULFATE ION × 2 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, SITTING DROP;277 K
Resolution 1.90 Å R-free 0.221
1W10 Urokinase type plasminogen activator Deposited 2004-06-15 Assembly 1 Protein monomer Monomer;Protein × 1 PDB declaration: monomeric(1) Consistent with protein count
Chain U 179–425(247 aa) Fragment:RESIDUES 179-425
Not recorded SJ1 N-(ISOBUTOXYCARBONYL)-D-SERYL-N-((1S)-4-{[AMINO(IMINO)METHYL]AMINO}-1-FORMYLBUTYL)-L-ALANINAMIDE × 1 SO4 SULFATE ION × 2 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, SITTING DROP;277 K
Resolution 2.00 Å
1W11 UROKINASE TYPE PLASMINOGEN ACTIVATOR Deposited 2004-06-15 Assembly 1 Protein monomer Monomer;Protein × 1 PDB declaration: monomeric(1) Consistent with protein count
Chain U 179–425(247 aa) Fragment:RESIDUES 179-425
Not recorded SO4 SULFATE ION × 2 SK1 N-(BENZYLSULFONYL)-D-SERYL-N-{4-[AMINO(IMINO)METHYL]BENZYL}-L-ALANINAMIDE × 1 X-RAY DIFFRACTION mmCIF provides none of the parsed conditions Resolution 2.00 Å R-free 0.249
1W12 UROKINASE TYPE PLASMINOGEN ACTIVATOR Deposited 2004-06-15 Assembly 1 Protein monomer Monomer;Protein × 1 PDB declaration: monomeric(1) Consistent with protein count
Chain U 179–425(247 aa) Fragment:RESIDUES 179-425
Not recorded SL1 N-((1S)-4-{[AMINO(IMINO)METHYL]AMINO}-1-FORMYLBUTYL)-2-{(3R)-3-[(BENZYLSULFONYL)AMINO]-2-OXO-5-PHENYL-2,3-DIHYDRO-1H-1,4-BENZODIAZEPIN-1-YL}ACETAMIDE × 1 X-RAY DIFFRACTION mmCIF provides none of the parsed conditions Resolution 2.40 Å R-free 0.261
1W13 UROKINASE TYPE PLASMINOGEN ACTIVATOR Deposited 2004-06-15 Assembly 1 Protein monomer Monomer;Protein × 1 PDB declaration: monomeric(1) Consistent with protein count
Chain U 179–425(247 aa) Fragment:RESIDUES 179-425
Not recorded SM1 N-(BENZYLSULFONYL)-D-SERYL-N-(4-{[AMINO(IMINO)METHYL]AMINO}BENZYL)-L-ALANINAMIDE × 1 SO4 SULFATE ION × 2 X-RAY DIFFRACTION mmCIF provides none of the parsed conditions Resolution 2.00 Å R-free 0.230
1W14 UROKINASE TYPE PLASMINOGEN ACTIVATOR Deposited 2004-06-15 Assembly 1 Protein monomer Monomer;Protein × 1 PDB declaration: monomeric(1) Consistent with protein count
Chain U 179–425(247 aa) Fragment:RESIDUES 179-425
Not recorded SO4 SULFATE ION × 2 SH1 N-[(2-PHENYLETHYL)SULFONYL]-D-SERYL-N-[(1S)-4-[(DIAMINOMETHYLENE)AMINO]-1-(HYDROXYMETHYL)BUTYL]-L-ALANINAMIDE × 1 X-RAY DIFFRACTION mmCIF provides none of the parsed conditions Resolution 2.20 Å R-free 0.253
2FD6 Structure of Human Urokinase Plasminogen Activator in Complex with Urokinase Receptor and an anti-upar antibody at 1.9 A Deposited 2005-12-13 Assembly 1 Other combination Heteromer;Protein × 4 PDB declaration: tetrameric(4) Consistent with protein count
Chain A 31–152(122 aa) Fragment:Amino terminal residues 31-152
Not recorded SO4 SULFATE ION × 1 ETX 2-ETHOXYETHANOL × 3 EDO 1,2-ETHANEDIOL × 2 PGE TRIETHYLENE GLYCOL × 1 NDG 2-acetamido-2-deoxy-alpha-D-glucopyranose × 1 PG4 TETRAETHYLENE GLYCOL × 1 X-RAY DIFFRACTION
X-ray crystallization conditions MICRODIALYSIS;pH 6.5;298 K;4% PEG4000, 5% ethylene glycol, 5% methanol, 0.05% sodium azide, 50 mM cacodylate, pH 6.5, MICRODIALYSIS, temperature 298K
Resolution 1.90 Å R-free 0.276
2FD6 Structure of Human Urokinase Plasminogen Activator in Complex with Urokinase Receptor and an anti-upar antibody at 1.9 A Deposited 2005-12-13 Assembly 2 Other combination Heteromer;Protein × 4 PDB declaration: tetrameric(4) Consistent with protein count
Chain A 31–152(122 aa) Fragment:Amino terminal residues 31-152
Not recorded SO4 SULFATE ION × 1 ETX 2-ETHOXYETHANOL × 3 EDO 1,2-ETHANEDIOL × 2 PGE TRIETHYLENE GLYCOL × 1 NDG 2-acetamido-2-deoxy-alpha-D-glucopyranose × 1 PG4 TETRAETHYLENE GLYCOL × 1 X-RAY DIFFRACTION
X-ray crystallization conditions MICRODIALYSIS;pH 6.5;298 K;4% PEG4000, 5% ethylene glycol, 5% methanol, 0.05% sodium azide, 50 mM cacodylate, pH 6.5, MICRODIALYSIS, temperature 298K
Resolution 1.90 Å R-free 0.276
2I9A Crystal structure of the free aminoterminal fragment of urokinase type plasminogen activator (ATF) Deposited 2006-09-05 Assembly 1 Protein monomer Monomer;Protein × 1 PDB declaration: monomeric(1) Consistent with protein count
Chain A 21–163(143 aa) Fragment:N-terminal fragment of urokinase, residues 21-163
Not recorded No recorded non-water small molecule X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, HANGING DROP;pH 10.5;293 K;1.2 M sodium dihydrogen phosphate, 0.8 M potassium hydrogen phosphate, 200 mM lithium sulfate, 100 mM CHES, pH 10.5, VAPOR DIFFUSION, HANGING DROP, temperature 293K
Resolution 1.90 Å R-free 0.208
2I9A Crystal structure of the free aminoterminal fragment of urokinase type plasminogen activator (ATF) Deposited 2006-09-05 Assembly 2 Protein monomer Monomer;Protein × 1 PDB declaration: monomeric(1) Consistent with protein count
Chain B 21–163(143 aa) Fragment:N-terminal fragment of urokinase, residues 21-163
Not recorded No recorded non-water small molecule X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, HANGING DROP;pH 10.5;293 K;1.2 M sodium dihydrogen phosphate, 0.8 M potassium hydrogen phosphate, 200 mM lithium sulfate, 100 mM CHES, pH 10.5, VAPOR DIFFUSION, HANGING DROP, temperature 293K
Resolution 1.90 Å R-free 0.208
2I9A Crystal structure of the free aminoterminal fragment of urokinase type plasminogen activator (ATF) Deposited 2006-09-05 Assembly 3 Protein monomer Monomer;Protein × 1 PDB declaration: monomeric(1) Consistent with protein count
Chain C 21–163(143 aa) Fragment:N-terminal fragment of urokinase, residues 21-163
Not recorded PO4 PHOSPHATE ION × 1 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, HANGING DROP;pH 10.5;293 K;1.2 M sodium dihydrogen phosphate, 0.8 M potassium hydrogen phosphate, 200 mM lithium sulfate, 100 mM CHES, pH 10.5, VAPOR DIFFUSION, HANGING DROP, temperature 293K
Resolution 1.90 Å R-free 0.208
2I9A Crystal structure of the free aminoterminal fragment of urokinase type plasminogen activator (ATF) Deposited 2006-09-05 Assembly 4 Protein monomer Monomer;Protein × 1 PDB declaration: monomeric(1) Consistent with protein count
Chain D 21–163(143 aa) Fragment:N-terminal fragment of urokinase, residues 21-163
Not recorded PO4 PHOSPHATE ION × 3 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, HANGING DROP;pH 10.5;293 K;1.2 M sodium dihydrogen phosphate, 0.8 M potassium hydrogen phosphate, 200 mM lithium sulfate, 100 mM CHES, pH 10.5, VAPOR DIFFUSION, HANGING DROP, temperature 293K
Resolution 1.90 Å R-free 0.208
2I9B Crystal structure of ATF-urokinase receptor complex Deposited 2006-09-05 Assembly 1 Other combination Heteromer;Protein × 2 PDB declaration: dimeric(2) Consistent with protein count
Chain A 21–163(143 aa) Fragment:ATF, residues 21-163
Not recorded SO4 SULFATE ION × 1 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, HANGING DROP;pH 5.5;293 K;22.5% w/v PEG3350, 200 mM ammonium sulfate, 100 mM Bis-Tris, pH 5.5, VAPOR DIFFUSION, HANGING DROP, temperature 293K
Resolution 2.80 Å R-free 0.265
2I9B Crystal structure of ATF-urokinase receptor complex Deposited 2006-09-05 Assembly 2 Other combination Heteromer;Protein × 2 PDB declaration: dimeric(2) Consistent with protein count
Chain B 21–163(143 aa) Fragment:ATF, residues 21-163
Not recorded SO4 SULFATE ION × 1 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, HANGING DROP;pH 5.5;293 K;22.5% w/v PEG3350, 200 mM ammonium sulfate, 100 mM Bis-Tris, pH 5.5, VAPOR DIFFUSION, HANGING DROP, temperature 293K
Resolution 2.80 Å R-free 0.265
2I9B Crystal structure of ATF-urokinase receptor complex Deposited 2006-09-05 Assembly 3 Other combination Heteromer;Protein × 2 PDB declaration: dimeric(2) Consistent with protein count
Chain C 21–163(143 aa) Fragment:ATF, residues 21-163
Not recorded No recorded non-water small molecule X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, HANGING DROP;pH 5.5;293 K;22.5% w/v PEG3350, 200 mM ammonium sulfate, 100 mM Bis-Tris, pH 5.5, VAPOR DIFFUSION, HANGING DROP, temperature 293K
Resolution 2.80 Å R-free 0.265
2I9B Crystal structure of ATF-urokinase receptor complex Deposited 2006-09-05 Assembly 4 Other combination Heteromer;Protein × 2 PDB declaration: dimeric(2) Consistent with protein count
Chain D 21–163(143 aa) Fragment:ATF, residues 21-163
Not recorded No recorded non-water small molecule X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, HANGING DROP;pH 5.5;293 K;22.5% w/v PEG3350, 200 mM ammonium sulfate, 100 mM Bis-Tris, pH 5.5, VAPOR DIFFUSION, HANGING DROP, temperature 293K
Resolution 2.80 Å R-free 0.265
2VIN Fragment-Based Discovery of Mexiletine Derivatives as Orally Bioavailable Inhibitors of Urokinase-Type Plasminogen Activator Deposited 2007-12-05 Assembly 1 Protein monomer Monomer;Protein × 1 PDB declaration: monomeric(1) Consistent with protein count
Chain A 179–431(253 aa) Fragment:CATALYTIC DOMAIN, RESIDUES 179-431
Mutation:YES ACT ACETATE ION × 1 SO4 SULFATE ION × 1 505 (2R)-1-(2,6-dimethylphenoxy)propan-2-amine × 1 X-RAY DIFFRACTION
X-ray crystallization conditions pH 6.6;PROTEIN WAS CRYSTALLIZED FROM 22-24% PEG4000, 0.17M (NH4)2SO4, 15% GLYCEROL, 0.1M NA(CH3COO) PH=4.0; THEN SOAKED IN 0.05M COMPOUND, 27.5% PEG4000, 0.2M HEPES PH=6.6, 0.1M (NH4)(CH3COO)
Resolution 1.90 Å R-free 0.235
2VIO Fragment-Based Discovery of Mexiletine Derivatives as Orally Bioavailable Inhibitors of Urokinase-Type Plasminogen Activator Deposited 2007-12-05 Assembly 1 Protein monomer Monomer;Protein × 1 PDB declaration: monomeric(1) Consistent with protein count
Chain A 179–431(253 aa) Fragment:CATALYTIC DOMAIN, RESIDUES 179-431
Mutation:YES ACT ACETATE ION × 1 L1O 4-(2-aminoethoxy)-3,5-dichlorobenzoic acid × 1 X-RAY DIFFRACTION
X-ray crystallization conditions pH 6.6;PROTEIN WAS CRYSTALLIZED FROM 22-24% PEG4000, 0.17M (NH4)2SO4, 15% GLYCEROL, 0.1M NA(CH3COO) PH=4.0; THEN SOAKED IN 0.05M COMPOUND, 28% PEG4000, 0.29M HEPES PH=6.6, 5% GLYCEROL
Resolution 1.80 Å R-free 0.250
2VIP Fragment-Based Discovery of Mexiletine Derivatives as Orally Bioavailable Inhibitors of Urokinase-Type Plasminogen Activator Deposited 2007-12-05 Assembly 1 Protein monomer Monomer;Protein × 1 PDB declaration: monomeric(1) Consistent with protein count
Chain A 179–431(253 aa) Fragment:CATALYTIC DOMAIN, RESIDUES 179-431
Mutation:YES ACT ACETATE ION × 1 SO4 SULFATE ION × 1 L1R 4-(2-AMINOETHOXY)-3,5-DICHLORO-N-[3-(1-METHYLETHOXY)PHENYL]BENZAMIDE × 1 X-RAY DIFFRACTION
X-ray crystallization conditions pH 6.6;PROTEIN WAS CRYSTALLIZED FROM 22-24% PEG4000, 0.17M (NH4)2SO4, 15% GLYCEROL, 0.1M NA(CH3COO) PH=4.0; THEN SOAKED IN 0.01M COMPOUND, 28% PEG4000, 0.29M HEPES PH=6.6, 5% GLYCEROL, 0.001M NA(CH3COO), 0.001M (NH4)2SO4, 10% DMSO
Resolution 1.72 Å R-free 0.237
2VIQ Fragment-Based Discovery of Mexiletine Derivatives as Orally Bioavailable Inhibitors of Urokinase-Type Plasminogen Activator Deposited 2007-12-05 Assembly 1 Protein monomer Monomer;Protein × 1 PDB declaration: monomeric(1) Consistent with protein count
Chain A 179–431(253 aa) Fragment:CATALYTIC DOMAIN, RESIDUES 179-431
Mutation:YES ACT ACETATE ION × 1 D55 4-(2-aminoethoxy)-N-(2,5-diethoxyphenyl)-3,5-dimethylbenzamide × 1 X-RAY DIFFRACTION
X-ray crystallization conditions pH 6.6;PROTEIN WAS CRYSTALLIZED FROM 22-24% PEG4000, 0.17M (NH4)2SO4, 15% GLYCEROL, 0.1M NA(CH3COO) PH=4.0; THEN SOAKED IN 0.04M COMPOUND, 28% PEG4000, 5% GLYCEROL, 0.29M BISTRIS PH=6.6, 0.001M NA(CH3COO), 0.001M (NH4)2SO4
Resolution 2.00 Å R-free 0.264
2VIV Fragment-Based Discovery of Mexiletine Derivatives as Orally Bioavailable Inhibitors of Urokinase-Type Plasminogen Activator Deposited 2007-12-05 Assembly 1 Protein monomer Monomer;Protein × 1 PDB declaration: monomeric(1) Consistent with protein count
Chain A 179–431(253 aa) Fragment:CATALYTIC DOMAIN, RESIDUES 179-431
Mutation:YES ACT ACETATE ION × 1 VG2 4-(2-aminoethoxy)-N-(3-chloro-5-piperidin-1-ylphenyl)-3,5-dimethylbenzamide × 1 X-RAY DIFFRACTION
X-ray crystallization conditions pH 6.6;PROTEIN WAS CRYSTALLIZED FROM 22-24% PEG4000, 0.17M (NH4)2SO4, 15% GLYCEROL, 0.1M NA(CH3COO) PH=4.0; THEN SOAKED IN 0.04M COMPOUND, 28% PEG4000, 5% GLYCEROL, 0.29M BISTRIS PH=6.6, 0.001M NA(CH3COO), 0.001M (NH4)2SO4
Resolution 1.72 Å R-free 0.238
2VIW Fragment-Based Discovery of Mexiletine Derivatives as Orally Bioavailable Inhibitors of Urokinase-Type Plasminogen Activator Deposited 2007-12-05 Assembly 1 Protein monomer Monomer;Protein × 1 PDB declaration: monomeric(1) Consistent with protein count
Chain A 179–431(253 aa) Fragment:CATALYTIC DOMAIN, RESIDUES 179-431
Mutation:YES ACT ACETATE ION × 1 D56 4-(2-aminoethoxy)-N-(3-chloro-2-ethoxy-5-piperidin-1-ylphenyl)-3,5-dimethylbenzamide × 1 X-RAY DIFFRACTION
X-ray crystallization conditions pH 6.6;PROTEIN WAS CRYSTALLIZED FROM 22-24% PEG4000, 0.17M (NH4)2SO4, 15% GLYCEROL, 0.1M NA(CH3COO) PH=4.0; THEN SOAKED IN 0.001M COMPOUND, 28% PEG4000, 5% GLYCEROL, 0.29M BISTRIS PH=6.6, 0.001M NA(CH3COO), 0.001M (NH4)2SO4
Resolution 2.05 Å R-free 0.260
2VNT Urokinase-Type Plasminogen Activator Inhibitor Complex with a 1-(7- SULPHOAMIDOISOQUINOLINYL)GUANIDINE Deposited 2008-02-07 Assembly 1 Protein monomer Monomer;Protein × 1 PDB declaration: monomeric(1) Consistent with protein count
Chain A 156–431(276 aa) Fragment:CATALYTIC DOMAIN, RESIDUES 156-431
Not recorded QGG 1-({4-CHLORO-1-[(DIAMINOMETHYLIDENE)AMINO]ISOQUINOLIN-7-YL}SULFONYL)-D-PROLINE × 1 X-RAY DIFFRACTION mmCIF provides none of the parsed conditions Resolution 2.20 Å R-free 0.295
2VNT Urokinase-Type Plasminogen Activator Inhibitor Complex with a 1-(7- SULPHOAMIDOISOQUINOLINYL)GUANIDINE Deposited 2008-02-07 Assembly 2 Protein monomer Monomer;Protein × 1 PDB declaration: monomeric(1) Consistent with protein count
Chain B 156–431(276 aa) Fragment:CATALYTIC DOMAIN, RESIDUES 156-431
Not recorded QGG 1-({4-CHLORO-1-[(DIAMINOMETHYLIDENE)AMINO]ISOQUINOLIN-7-YL}SULFONYL)-D-PROLINE × 1 SO4 SULFATE ION × 4 X-RAY DIFFRACTION mmCIF provides none of the parsed conditions Resolution 2.20 Å R-free 0.295
2VNT Urokinase-Type Plasminogen Activator Inhibitor Complex with a 1-(7- SULPHOAMIDOISOQUINOLINYL)GUANIDINE Deposited 2008-02-07 Assembly 3 Protein monomer Monomer;Protein × 1 PDB declaration: monomeric(1) Consistent with protein count
Chain C 156–431(276 aa) Fragment:CATALYTIC DOMAIN, RESIDUES 156-431
Not recorded QGG 1-({4-CHLORO-1-[(DIAMINOMETHYLIDENE)AMINO]ISOQUINOLIN-7-YL}SULFONYL)-D-PROLINE × 1 X-RAY DIFFRACTION mmCIF provides none of the parsed conditions Resolution 2.20 Å R-free 0.295
2VNT Urokinase-Type Plasminogen Activator Inhibitor Complex with a 1-(7- SULPHOAMIDOISOQUINOLINYL)GUANIDINE Deposited 2008-02-07 Assembly 4 Protein monomer Monomer;Protein × 1 PDB declaration: monomeric(1) Consistent with protein count
Chain D 156–431(276 aa) Fragment:CATALYTIC DOMAIN, RESIDUES 156-431
Not recorded QGG 1-({4-CHLORO-1-[(DIAMINOMETHYLIDENE)AMINO]ISOQUINOLIN-7-YL}SULFONYL)-D-PROLINE × 1 SO4 SULFATE ION × 3 X-RAY DIFFRACTION mmCIF provides none of the parsed conditions Resolution 2.20 Å R-free 0.295
2VNT Urokinase-Type Plasminogen Activator Inhibitor Complex with a 1-(7- SULPHOAMIDOISOQUINOLINYL)GUANIDINE Deposited 2008-02-07 Assembly 5 Protein monomer Monomer;Protein × 1 PDB declaration: monomeric(1) Consistent with protein count
Chain E 156–431(276 aa) Fragment:CATALYTIC DOMAIN, RESIDUES 156-431
Not recorded QGG 1-({4-CHLORO-1-[(DIAMINOMETHYLIDENE)AMINO]ISOQUINOLIN-7-YL}SULFONYL)-D-PROLINE × 1 SO4 SULFATE ION × 2 X-RAY DIFFRACTION mmCIF provides none of the parsed conditions Resolution 2.20 Å R-free 0.295
2VNT Urokinase-Type Plasminogen Activator Inhibitor Complex with a 1-(7- SULPHOAMIDOISOQUINOLINYL)GUANIDINE Deposited 2008-02-07 Assembly 6 Protein monomer Monomer;Protein × 1 PDB declaration: monomeric(1) Consistent with protein count
Chain F 156–431(276 aa) Fragment:CATALYTIC DOMAIN, RESIDUES 156-431
Not recorded QGG 1-({4-CHLORO-1-[(DIAMINOMETHYLIDENE)AMINO]ISOQUINOLIN-7-YL}SULFONYL)-D-PROLINE × 1 X-RAY DIFFRACTION mmCIF provides none of the parsed conditions Resolution 2.20 Å R-free 0.295
3BT1 Structure of urokinase receptor, urokinase and vitronectin complex Deposited 2007-12-27 Assembly 1 Other combination Heteromer;Protein × 3 PDB declaration: trimeric(3) Consistent with protein count
Chain A 21–153(133 aa) Fragment:urokinase amino terminal fragment, Urokinase-type plasminogen activator long chain A, UNP residues 21-153
Not recorded NAG 2-acetamido-2-deoxy-beta-D-glucopyranose × 2 X-RAY DIFFRACTION
X-ray crystallization conditions MICRODIALYSIS;pH 7.5;295 K;12% PEG 3350, 50mM HEPES pH 7.5, MICRODIALYSIS, temperature 295K
Resolution 2.80 Å R-free 0.308
3BT2 Structure of urokinase receptor, urokinase and vitronectin complex Deposited 2007-12-27 Assembly 1 Other combination Heteromer;Protein × 5 PDB declaration: pentameric(5) Consistent with protein count
Chain A 21–153(133 aa) Fragment:urokinase amino terminal fragment, Urokinase-type plasminogen activator long chain A, UNP residues 21-153
Not recorded NAG 2-acetamido-2-deoxy-beta-D-glucopyranose × 1 X-RAY DIFFRACTION
X-ray crystallization conditions MICRODIALYSIS;pH 7.5;295 K;8% PEG 4000, 2.5% ethanol, 0.05% sodium azide, 50mM cacodylate pH 6.5, pH 7.5, MICRODIALYSIS, temperature 295K
Resolution 2.50 Å R-free 0.272
3BT2 Structure of urokinase receptor, urokinase and vitronectin complex Deposited 2007-12-27 Assembly 2 Other combination Heteromer;Protein × 4 PDB declaration: tetrameric(4) Consistent with protein count
Chain A 21–153(133 aa) Fragment:urokinase amino terminal fragment, Urokinase-type plasminogen activator long chain A, UNP residues 21-153
Not recorded NAG 2-acetamido-2-deoxy-beta-D-glucopyranose × 1 X-RAY DIFFRACTION
X-ray crystallization conditions MICRODIALYSIS;pH 7.5;295 K;8% PEG 4000, 2.5% ethanol, 0.05% sodium azide, 50mM cacodylate pH 6.5, pH 7.5, MICRODIALYSIS, temperature 295K
Resolution 2.50 Å R-free 0.272
3KGP Crystal Structures of Urokinase-type Plasminogen Activator in Complex with 4-(Aminomethyl) Benzoic Acid and 4-(Aminomethyl-phenyl)-methanol Deposited 2009-10-29 Assembly 1 Protein monomer Monomer;Protein × 1 PDB declaration: monomeric(1) Consistent with protein count
Chain A 179–431(253 aa) Fragment:C-terminal domain, UNP residues 179-431
Mutation:C122A, N145Q 4AZ 4-(aminomethyl)benzoic acid × 1 SO4 SULFATE ION × 1 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, SITTING DROP;pH 4.6;298 K;0.05M sodium citrate, 1.95M (NH4)2SO4, 0.05% NaN3, 5% PEG 400, pH 4.60, VAPOR DIFFUSION, SITTING DROP, temperature 298K
Resolution 2.35 Å R-free 0.274
3KHV Crystal Structures of Urokinase-type Plasminogen Activator in Complex with 4-(Aminomethyl) Benzoic Acid and 4-(Aminomethyl-phenyl)-methanol Deposited 2009-10-30 Assembly 1 Protein monomer Monomer;Protein × 1 PDB declaration: monomeric(1) Consistent with protein count
Chain A 179–431(253 aa) Fragment:C-terminal domain, UNP residues 179-431
Mutation:C122A, N145Q 4AL [4-(aminomethyl)phenyl]methanol × 1 SO4 SULFATE ION × 1 PGE TRIETHYLENE GLYCOL × 1 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, SITTING DROP;pH 4.6;298 K;0.05M sodium citrate, 1.95M (NH4)2SO4, 0.05% NaN3, 5% PEG 400, pH 4.60, VAPOR DIFFUSION, SITTING DROP, temperature 298K
Resolution 2.35 Å R-free 0.293
3KID The Crystal Structures of 2-Aminobenzothiazole-based Inhibitors in Complexes with Urokinase-type Plasminogen Activator Deposited 2009-11-01 Assembly 1 Protein monomer Monomer;Protein × 1 PDB declaration: monomeric(1) Consistent with protein count
Chain U 179–431(253 aa) Fragment:C-terminal domain, UNP residues 179-431
Mutation:C122A, N145Q 2BS ethyl 2-amino-1,3-benzothiazole-6-carboxylate × 1 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, SITTING DROP;pH 4.6;298 K;0.05M sodium citrate, 1.95M (NH4)2SO4, 0.05% NaN3, 5% PEG 400, pH 4.60, VAPOR DIFFUSION, SITTING DROP, temperature 298K
Resolution 2.71 Å R-free 0.275
3M61 Crystal structure of complex of urokinase and a upain-1 variant(W3A) in pH4.6 condition Deposited 2010-03-15 Assembly 1 Protein heterocomplex Heteromer;Protein × 2 PDB declaration: dimeric(2) Consistent with protein count
Chain U 179–431(253 aa) Fragment:C-terminal domain, UNP residues 179-431
Mutation:C122A, N145Q No recorded non-water small molecule X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, SITTING DROP;pH 4.6;298 K;2.0M ammonium sulfate, 50mM sodium citrate pH 4.60, 5% PEG 400, VAPOR DIFFUSION, SITTING DROP, temperature 298K
Resolution 1.68 Å R-free 0.243
3MHW The complex crystal Structure of Urokianse and 2-Aminobenzothiazole Deposited 2010-04-09 Assembly 1 Protein monomer Monomer;Protein × 1 PDB declaration: monomeric(1) Consistent with protein count
Chain U 179–425(247 aa) Fragment:C-terminal domain, UNP residues 179-425
Mutation:C122S SO4 SULFATE ION × 1 ABV 1,3-benzothiazol-2-amine × 1 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, SITTING DROP;pH 4.6;298 K;0.05M sodium citrate, 1.95M (NH4)2SO4, 0.05% NaN3, 5% PEG 400, pH 4.6, VAPOR DIFFUSION, SITTING DROP, temperature 298K
Resolution 1.45 Å R-free 0.234
3MWI The complex crystal Structure of Urokianse and 5-nitro-1H-indole-2-amidine Deposited 2010-05-06 Assembly 1 Protein monomer Monomer;Protein × 1 PDB declaration: monomeric(1) Consistent with protein count
Chain U 179–424(246 aa) Fragment:C-terminal domain, UNP residues 179-424
Mutation:C122A B25 5-nitro-1H-indole-2-carboximidamide × 1 SO4 SULFATE ION × 2 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, SITTING DROP;pH 4.6;298 K;0.05M sodium citrate, 1.95M (NH4)2SO4, 0.05% NaN3, 5% PEG 400, pH 4.6, VAPOR DIFFUSION, SITTING DROP, temperature 298K
Resolution 2.03 Å R-free 0.297
3OX7 The crystal structure of uPA complex with peptide inhibitor MH027 at pH4.6 Deposited 2010-09-21 Assembly 1 Protein heterocomplex Heteromer;Protein × 2 PDB declaration: dimeric(2) Consistent with protein count
Chain U 179–431(253 aa) Fragment:C-TERMINAL DOMAIN, RESIDUES 179-431
Mutation:C122A, N145Q SO4 SULFATE ION × 1 PG4 TETRAETHYLENE GLYCOL × 1 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, HANGING DROP;pH 4.6;298 K;0.05M SODIUM CITRATE, 1.95M (NH4)2SO4, 0.05% NAN3, 5% PEG 400, pH 4.6, VAPOR DIFFUSION, HANGING DROP, temperature 298K
Resolution 1.58 Å R-free 0.230
3OY5 The crystal structure of uPA complex with peptide inhibitor MH027 at pH7.4 Deposited 2010-09-22 Assembly 1 Protein heterocomplex Heteromer;Protein × 2 PDB declaration: dimeric(2) Consistent with protein count
Chain U 179–431(253 aa) Fragment:C-TERMINAL DOMAIN, UNP residues 179-431
Mutation:C122A, N145Q SO4 SULFATE ION × 1 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, SITTING DROP;pH 7.4;298 K;100mM Tris-Hcl, 2.0M (NH4)2SO4, 0.05% NAN3, 5% PEG 400, pH 7.4, VAPOR DIFFUSION, SITTING DROP, temperature 298K
Resolution 2.31 Å R-free 0.231
3OY6 The crystal structure of uPA complex with peptide inhibitor MH036 at pH4.6 Deposited 2010-09-22 Assembly 1 Protein heterocomplex Heteromer;Protein × 2 PDB declaration: dimeric(2) Consistent with protein count
Chain U 179–431(253 aa) Fragment:C-TERMINAL DOMAIN, UNP residues 179-431
Mutation:C122A, N145Q No recorded non-water small molecule X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, SITTING DROP;pH 7.4;298 K;0.05M SODIUM CITRATE, 1.95M (NH4)2SO4, 0.05% NAN3, 5% PEG 400, pH 7.4, VAPOR DIFFUSION, SITTING DROP, temperature 298K
Resolution 2.31 Å R-free 0.263
3QN7 Potent and selective bicyclic peptide inhibitor (UK18) of human urokinase-type plasminogen activator(uPA) Deposited 2011-02-08 Assembly 1 Protein heterocomplex Heteromer;Protein × 2 PDB declaration: dimeric(2) Consistent with protein count
Chain A 179–431(253 aa) Fragment:Catalytic domain, Urokinase-type plasminogen activator chain B
Mutation:C122A, N145Q ZBR 1,3,5-tris(bromomethyl)benzene × 1 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, HANGING DROP;pH 4.3;293 K;2M ammonium sulfate, 0.05M sodium citrate, 5%(v/v) PEG 400, pH 4.3, VAPOR DIFFUSION, HANGING DROP, temperature 293K
Resolution 1.90 Å R-free 0.252
3U73 Crystal structure of stabilized human uPAR mutant in complex with ATF Deposited 2011-10-13 Assembly 1 Other combination Heteromer;Protein × 2 PDB declaration: dimeric(2) Consistent with protein count
Chain A 21–152(132 aa)
Not recorded No recorded non-water small molecule X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, SITTING DROP;pH 7.4;295 K;0.2M NaCl, 100mM HEPES, pH7.4, 1.8 M ammonium sulfate, vapor diffusion, sitting drop, temperature 295.0K
Resolution 3.19 Å R-free 0.258
4DVA The crystal structure of human urokinase-type plasminogen activator catalytic domain Deposited 2012-02-23 Assembly 1 Protein monomer Monomer;Protein × 1 PDB declaration: monomeric(1) Consistent with protein count
Chain U 179–424(246 aa) Fragment:catalytic domain
Mutation:C122A, N145Q SO4 SULFATE ION × 2 P6G HEXAETHYLENE GLYCOL × 2 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, SITTING DROP;pH 4.6;298 K;2.0M ammonium sulfate, 50mM sodium citrate, 5% PEG400, pH 4.6, VAPOR DIFFUSION, SITTING DROP, temperature 298K
Resolution 1.94 Å R-free 0.244
4DW2 The crystal structure of uPA in complex with the Fab fragment of mAb-112 Deposited 2012-02-24 Assembly 1 Protein heterocomplex Heteromer;Protein × 3 PDB declaration: trimeric(3) Consistent with protein count
Chain U 179–424(246 aa) Fragment:catalytic domain, UNP RESIDUES 179-424
Mutation:C122A, N145Q SO4 SULFATE ION × 1 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, SITTING DROP;pH 8;298 K;25% (w/v) PEG 2000 MME, 100mM Tris-HCl (pH 8.0), 0.21M ammonium sulfate, VAPOR DIFFUSION, SITTING DROP, temperature 298K
Resolution 2.97 Å R-free 0.300
4FU7 Crystal Structure of the Urokinase Deposited 2012-06-28 Assembly 1 Protein monomer Monomer;Protein × 1 PDB declaration: monomeric(1) Consistent with protein count
Chain A 179–424(246 aa)
Not recorded SO4 SULFATE ION × 3 ACT ACETATE ION × 1 1UP 2-[(7-carbamimidoyl-2-methoxynaphthalen-1-yl)oxy]acetamide × 1 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, HANGING DROP;298 K;0.15 M Li2SO4, 20% polyethylene glycol MW 4000 in succinate buffer, pH 4.8-6.0, VAPOR DIFFUSION, HANGING DROP, temperature 298K
Resolution 2.00 Å R-free 0.223
4FU8 Crystal Structure of the Urokinase Deposited 2012-06-28 Assembly 1 Protein monomer Monomer;Protein × 1 PDB declaration: monomeric(1) Consistent with protein count
Chain A 179–424(246 aa)
Not recorded 2UP naphthalene-2-carboximidamide × 1 ACT ACETATE ION × 2 SIN SUCCINIC ACID × 1 SO4 SULFATE ION × 4 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, HANGING DROP;298 K;0.15 M Li2SO4, 20% polyethylene glycol MW 4000 in succinate buffer, pH 4.8-6.0, VAPOR DIFFUSION, HANGING DROP, temperature 298.0K
Resolution 2.20 Å R-free 0.239
4FU9 Crystal Structure of the Urokinase Deposited 2012-06-28 Assembly 1 Protein monomer Monomer;Protein × 1 PDB declaration: monomeric(1) Consistent with protein count
Chain A 179–424(246 aa)
Not recorded SO4 SULFATE ION × 3 SIN SUCCINIC ACID × 1 GOL GLYCEROL × 6 ACT ACETATE ION × 2 675 6-[(Z)-AMINO(IMINO)METHYL]-N-PHENYL-2-NAPHTHAMIDE × 1 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, HANGING DROP;298 K;0.15 M Li2SO4, 20% polyethylene glycol MW 4000 in succinate buffer, pH 4.8-6.0, VAPOR DIFFUSION, HANGING DROP, temperature 291 - 298.0K
Resolution 1.60 Å R-free 0.182
4FUB Crystal Structure of the Urokinase Deposited 2012-06-28 Assembly 1 Protein monomer Monomer;Protein × 1 PDB declaration: monomeric(1) Consistent with protein count
Chain A 179–424(246 aa)
Not recorded 4UP 6-[(2S,3S)-3-phenyloxiran-2-yl]naphthalene-2-carboximidamide × 1 SO4 SULFATE ION × 1 SIN SUCCINIC ACID × 1 GOL GLYCEROL × 6 15P POLYETHYLENE GLYCOL (N=34) × 1 ACT ACETATE ION × 5 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, HANGING DROP;298 K;0.15 M Li2SO4, 20% polyethylene glycol MW 4000 in succinate buffer, pH 4.8-6.0, VAPOR DIFFUSION, HANGING DROP, temperature 298.0K
Resolution 1.90 Å R-free 0.187
4FUC Crystal Structure of the Urokinase Deposited 2012-06-28 Assembly 1 Protein monomer Monomer;Protein × 1 PDB declaration: monomeric(1) Consistent with protein count
Chain A 179–424(246 aa)
Not recorded 239 6-[(Z)-AMINO(IMINO)METHYL]-N-[4-(AMINOMETHYL)PHENYL]-2-NAPHTHAMIDE × 1 SIN SUCCINIC ACID × 1 SO4 SULFATE ION × 4 ACT ACETATE ION × 1 GOL GLYCEROL × 8 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, HANGING DROP;298 K;0.15 M Li2SO4, 20% polyethylene glycol MW 4000 in succinate buffer, pH 4.8-6.0, VAPOR DIFFUSION, HANGING DROP, temperature 298.0K
Resolution 1.72 Å R-free 0.187
4FUD Crystal Structure of the Urokinase Deposited 2012-06-28 Assembly 1 Protein monomer Monomer;Protein × 1 PDB declaration: monomeric(1) Consistent with protein count
Chain A 179–424(246 aa)
Not recorded 6UP 8-aminonaphthalene-2-carboximidamide × 1 SIN SUCCINIC ACID × 3 SO4 SULFATE ION × 4 NA SODIUM ION × 1 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, HANGING DROP;298 K;0.15 M Li2SO4, 20% polyethylene glycol MW 4000 in succinate buffer, pH 4.8-6.0, VAPOR DIFFUSION, HANGING DROP, temperature 298.0K
Resolution 2.00 Å R-free 0.220
4FUE Crystal Structure of the Urokinase Deposited 2012-06-28 Assembly 1 Protein monomer Monomer;Protein × 1 PDB declaration: monomeric(1) Consistent with protein count
Chain A 179–424(246 aa)
Not recorded 7UP 6-(1,2,3,4-tetrahydroisoquinolin-6-ylethynyl)naphthalene-2-carboximidamide × 1 SIN SUCCINIC ACID × 1 SO4 SULFATE ION × 2 GOL GLYCEROL × 3 ACT ACETATE ION × 2 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, HANGING DROP;298 K;0.15 M Li2SO4, 20% polyethylene glycol MW 4000 in succinate buffer, pH 4.8-6.0, VAPOR DIFFUSION, HANGING DROP, temperature 298.0K
Resolution 2.00 Å R-free 0.190
4FUF Crystal Structure of the Urokinase Deposited 2012-06-28 Assembly 1 Protein monomer Monomer;Protein × 1 PDB declaration: monomeric(1) Consistent with protein count
Chain A 179–424(246 aa)
Not recorded 8UP 8-(3-bromopropoxy)-7-methoxynaphthalene-2-carboximidamide × 1 SIN SUCCINIC ACID × 1 SO4 SULFATE ION × 3 GOL GLYCEROL × 4 ACT ACETATE ION × 3 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, HANGING DROP;298 K;0.15 M Li2SO4, 20% polyethylene glycol MW 4000 in succinate buffer, pH 4.8-6.0, VAPOR DIFFUSION, HANGING DROP, temperature 298.0K
Resolution 2.00 Å R-free 0.202
4FUG Crystal Structure of the Urokinase Deposited 2012-06-28 Assembly 1 Protein monomer Monomer;Protein × 1 PDB declaration: monomeric(1) Consistent with protein count
Chain A 179–424(246 aa)
Not recorded 9UP methyl (7-carbamimidoylnaphthalen-1-yl)carbamate × 1 SO4 SULFATE ION × 4 GOL GLYCEROL × 2 ACT ACETATE ION × 2 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, HANGING DROP;298 K;0.15 M Li2SO4, 20% polyethylene glycol MW 4000 in succinate buffer, pH 4.8-6.0, VAPOR DIFFUSION, HANGING DROP, temperature 298.0K
Resolution 1.80 Å R-free 0.203
4FUH Crystal Structure of the Urokinase Deposited 2012-06-28 Assembly 1 Protein monomer Monomer;Protein × 1 PDB declaration: monomeric(1) Consistent with protein count
Chain A 179–424(246 aa)
Not recorded 1U2 6-[(phenylcarbamoyl)amino]naphthalene-2-carboximidamide × 1 SO4 SULFATE ION × 4 ACT ACETATE ION × 1 GOL GLYCEROL × 7 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, HANGING DROP;298 K;0.15 M Li2SO4, 20% polyethylene glycol MW 4000 in succinate buffer, pH 4.8-6.0, VAPOR DIFFUSION, HANGING DROP, temperature 298.0K
Resolution 1.60 Å R-free 0.183
4FUI Crystal Structure of the Urokinase Deposited 2012-06-28 Assembly 1 Protein monomer Monomer;Protein × 1 PDB declaration: monomeric(1) Consistent with protein count
Chain A 179–424(246 aa)
Not recorded UI3 7-METHOXY-8-[1-(METHYLSULFONYL)-1H-PYRAZOL-4-YL]NAPHTHALENE-2-CARBOXIMIDAMIDE × 1 SO4 SULFATE ION × 3 GOL GLYCEROL × 4 NA SODIUM ION × 1 SIN SUCCINIC ACID × 1 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, HANGING DROP;298 K;0.15 M Li2SO4, 20% polyethylene glycol MW 4000 in succinate buffer, pH 4.8-6.0, VAPOR DIFFUSION, HANGING DROP, temperature 298.0K
Resolution 2.00 Å R-free 0.209
4FUJ Crystal Structure of the Urokinase Deposited 2012-06-28 Assembly 1 Protein monomer Monomer;Protein × 1 PDB declaration: monomeric(1) Consistent with protein count
Chain A 179–424(246 aa)
Not recorded 1U9 6-{(E)-2-[3-(2-hydroxyethyl)phenyl]ethenyl}naphthalene-2-carboximidamide × 1 SIN SUCCINIC ACID × 1 SO4 SULFATE ION × 2 ACT ACETATE ION × 2 GOL GLYCEROL × 3 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, HANGING DROP;298 K;0.15 M Li2SO4, 20% polyethylene glycol MW 4000 in succinate buffer, pH 4.8-6.0, VAPOR DIFFUSION, HANGING DROP, temperature 291 - 298.0K
Resolution 2.05 Å R-free 0.205
4GLY Human urokinase-type plasminogen activator uPA in complex with the two-disulfide bridge peptide UK504 Deposited 2012-08-15 Assembly 1 Protein heterocomplex Heteromer;Protein × 2 PDB declaration: dimeric(2) Consistent with protein count
Chain A 179–423(245 aa) Fragment:CATALYTIC DOMAIN, UROKINASE-TYPE PLASMINOGEN ACTIVATOR
Mutation:C122A, N145Q SO4 SULFATE ION × 4 NA SODIUM ION × 2 CL CHLORIDE ION × 3 P6G HEXAETHYLENE GLYCOL × 1 GOL GLYCEROL × 1 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, HANGING DROP;pH 4.6;293 K;1.8M Ammonium sulfate, 5% PEG400, 0.05% Sodium azide, pH 4.6, VAPOR DIFFUSION, HANGING DROP, temperature 293K
Resolution 1.52 Å R-free 0.204
4H42 Synthesis of a Weak Basic uPA Inhibitor and Crystal Structure of Complex with uPA Deposited 2012-09-14 Assembly 1 Protein monomer Monomer;Protein × 1 PDB declaration: monomeric(1) Consistent with protein count
Chain U 179–426(248 aa) Fragment:human urokinase-type plasminogen activator catalytic domain
Mutation:C122A, N145Q 11E N-[(2-amino-1,3-benzothiazol-6-yl)carbonyl]glycine × 1 PG6 1-(2-METHOXY-ETHOXY)-2-{2-[2-(2-METHOXY-ETHOXY]-ETHOXY}-ETHANE × 1 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, SITTING DROP;pH 4.6;298 K;2.0 M ammonium sulfate, 50 mM sodium citrate pH 4.6 and 5% PEG400, VAPOR DIFFUSION, SITTING DROP, temperature 298K
Resolution 2.01 Å R-free 0.285
4JK5 Human urokinase-type Plasminogen Activator (uPA) in complex with a bicyclic peptide inhibitor (UK18-D-Ser) Deposited 2013-03-09 Assembly 1 Protein heterocomplex Heteromer;Protein × 2 PDB declaration: dimeric(2) Consistent with protein count
Chain A 179–423(245 aa) Fragment:Catalytic domain
Mutation:C122A, N145Q SO4 SULFATE ION × 4 CL CHLORIDE ION × 2 P6G HEXAETHYLENE GLYCOL × 1 ZBR 1,3,5-tris(bromomethyl)benzene × 1 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, HANGING DROP;pH 4.9;293 K;50mM Na3(cit) pH 4.9, 5% v/v PEG400, 1.8M (NH4)2SO4, 0.05% NaN3, VAPOR DIFFUSION, HANGING DROP, temperature 293K
Resolution 1.55 Å R-free 0.213
4JK6 Human urokinase-type Plasminogen Activator (uPA) in complex with a bicyclic peptide inhibitor (UK18-D-Aba) Deposited 2013-03-09 Assembly 1 Protein heterocomplex Heteromer;Protein × 2 PDB declaration: dimeric(2) Consistent with protein count
Chain A 179–423(245 aa) Fragment:Catalytic domain
Mutation:C299A, N322Q SO4 SULFATE ION × 4 CL CHLORIDE ION × 1 P6G HEXAETHYLENE GLYCOL × 1 ZBR 1,3,5-tris(bromomethyl)benzene × 1 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, HANGING DROP;pH 4.9;293 K;50mM Na3(cit) pH 4.9, 5% v/v PEG400, 1.8M (NH4)2SO4, 0.05% NaN3, VAPOR DIFFUSION, HANGING DROP, temperature 293K
Resolution 2.20 Å R-free 0.205
4K24 Structure of anti-uPAR Fab ATN-658 in complex with uPAR Deposited 2013-04-08 Assembly 1 Other combination Heteromer;Protein × 5 PDB declaration: pentameric(5) Consistent with protein count
Chain A 21–153(133 aa) Fragment:UNP residues 21-153
Not recorded MAN alpha-D-mannopyranose × 1 NAG 2-acetamido-2-deoxy-beta-D-glucopyranose × 1 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, SITTING DROP;pH 7.5;295 K;0.1M HEPES pH 7.5, 55%(v/v) Tacsimate, 2%(v/v) 2-methyl-1,3-propanediol, vapor diffusion, sitting drop, temperature 295K
Resolution 4.50 Å R-free 0.275
4MNV Crystal structure of bicyclic peptide UK729 bound as an acyl-enzyme intermediate to urokinase-type plasminogen activator (uPA) Deposited 2013-09-11 Assembly 1 Protein heterocomplex Heteromer;Protein × 3 PDB declaration: trimeric(3) Consistent with protein count
Chain A 179–423(245 aa) Fragment:catalytic domain (UNP residues 179-423)
Mutation:C122A, N145Q SO4 SULFATE ION × 1 ACT ACETATE ION × 2 ZBR 1,3,5-tris(bromomethyl)benzene × 1 GOL GLYCEROL × 1 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, HANGING DROP;pH 4.25;291 K;21% PEG4000, 16% glycerol, 0.17 M ammonium sulfate, 0.1 M sodium acetate, pH 4.25, VAPOR DIFFUSION, HANGING DROP, temperature 291K
Resolution 1.80 Å R-free 0.216
4MNW Crystal structure of urokinase-type plasminogen activator (uPA) complexed with bicyclic peptide UK749 Deposited 2013-09-11 Assembly 1 Protein heterocomplex Heteromer;Protein × 2 PDB declaration: dimeric(2) Consistent with protein count
Chain A 179–423(245 aa) Fragment:catalytic domain (UNP residues 179-423)
Mutation:C122A, N145Q SO4 SULFATE ION × 2 GOL GLYCEROL × 5 ACT ACETATE ION × 1 ZBR 1,3,5-tris(bromomethyl)benzene × 1 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, HANGING DROP;pH 4.5;291 K;22% PEG4000, 15% glycerol, 0.17 M ammonium sulfate, 0.1 M sodium acetate, pH 4.5, VAPOR DIFFUSION, HANGING DROP, temperature 291K
Resolution 1.49 Å R-free 0.171
4MNX Crystal structure of urokinase-type plasminogen activator (uPA) complexed with bicyclic peptide UK811 Deposited 2013-09-11 Assembly 1 Protein heterocomplex Heteromer;Protein × 2 PDB declaration: dimeric(2) Consistent with protein count
Chain A 179–423(245 aa) Fragment:catalytic domain (UNP residues 179-423)
Mutation:C122A, N145Q SO4 SULFATE ION × 2 GOL GLYCEROL × 1 29N 1,1',1''-(1,3,5-triazinane-1,3,5-triyl)tripropan-1-one × 1 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, HANGING DROP;pH 4.5;291 K;22% PEG4000, 15% glycerol, 0.17 M ammonium sulfate, 0.1 M sodium acetate, pH 4.5, VAPOR DIFFUSION, HANGING DROP, temperature 291K
Resolution 1.85 Å R-free 0.227
4MNY Crystal structure of urokinase-type plasminogen activator (uPA) complexed with bicyclic peptide UK903 Deposited 2013-09-11 Assembly 1 Protein heterocomplex Heteromer;Protein × 2 PDB declaration: dimeric(2) Consistent with protein count
Chain A 179–423(245 aa) Fragment:catalytic domain (UNP residues 179-423)
Mutation:C122A, N145Q SO4 SULFATE ION × 2 ACT ACETATE ION × 2 GOL GLYCEROL × 2 29O N,N',N''-benzene-1,3,5-triyltris(2-bromoacetamide) × 1 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, HANGING DROP;pH 4.25;291 K;20% PEG4000, 16% glycerol, 0.17 M ammonium sulfate, 0.1 M sodium acetate, pH 4.25, VAPOR DIFFUSION, HANGING DROP, temperature 291K
Resolution 1.70 Å R-free 0.215
4MNY Crystal structure of urokinase-type plasminogen activator (uPA) complexed with bicyclic peptide UK903 Deposited 2013-09-11 Assembly 2 Protein heterocomplex Heteromer;Protein × 2 PDB declaration: dimeric(2) Consistent with protein count
Chain B 179–423(245 aa) Fragment:catalytic domain (UNP residues 179-423)
Mutation:C122A, N145Q SO4 SULFATE ION × 2 ACT ACETATE ION × 3 GOL GLYCEROL × 1 29O N,N',N''-benzene-1,3,5-triyltris(2-bromoacetamide) × 1 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, HANGING DROP;pH 4.25;291 K;20% PEG4000, 16% glycerol, 0.17 M ammonium sulfate, 0.1 M sodium acetate, pH 4.25, VAPOR DIFFUSION, HANGING DROP, temperature 291K
Resolution 1.70 Å R-free 0.215
4OS1 Crystal structure of urokinase-type plasminogen activator (uPA) complexed with bicyclic peptide UK601 (bicyclic 1) Deposited 2014-02-12 Assembly 1 Protein heterocomplex Heteromer;Protein × 2 PDB declaration: dimeric(2) Consistent with protein count
Chain A 179–423(245 aa) Fragment:catalytic domain (UNP residues 179-423)
Mutation:C122A, N145Q SO4 SULFATE ION × 2 ACT ACETATE ION × 1 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, HANGING DROP;pH 4.5;291 K;21% PEG4000, 15% glycerol, 0.17 M ammonium sulfate, 0.1 M sodium acetate, pH 4.5, VAPOR DIFFUSION, HANGING DROP, temperature 291K
Resolution 2.20 Å R-free 0.227
4OS2 Crystal structure of urokinase-type plasminogen activator (uPA) complexed with bicyclic peptide UK602 (bicyclic 1) Deposited 2014-02-12 Assembly 1 Protein heterocomplex Heteromer;Protein × 2 PDB declaration: dimeric(2) Consistent with protein count
Chain A 179–423(245 aa) Fragment:catalytic domain (UNP residues 179-423)
Mutation:C122A, N145Q SO4 SULFATE ION × 2 ACT ACETATE ION × 2 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, HANGING DROP;pH 4.5;291 K;21% PEG4000, 15% glycerol, 0.17 M ammonium sulfate, 0.1 M sodium acetate, pH 4.5, VAPOR DIFFUSION, HANGING DROP, temperature 291K
Resolution 1.79 Å R-free 0.207
4OS4 Crystal structure of urokinase-type plasminogen activator (uPA) complexed with bicyclic peptide UK603 (bicyclic 1) Deposited 2014-02-12 Assembly 1 Protein heterocomplex Heteromer;Protein × 2 PDB declaration: dimeric(2) Consistent with protein count
Chain A 179–423(245 aa) Fragment:catalytic domain (UNP residues 179-423)
Mutation:C122A, N145Q SO4 SULFATE ION × 2 GOL GLYCEROL × 1 ACT ACETATE ION × 1 CL CHLORIDE ION × 1 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, HANGING DROP;pH 4.5;291 K;21% PEG4000, 15% glycerol, 0.17 M ammonium sulfate, 0.1 M sodium acetate, pH 4.5, VAPOR DIFFUSION, HANGING DROP, temperature 291K
Resolution 2.00 Å R-free 0.214
4OS5 Crystal structure of urokinase-type plasminogen activator (uPA) complexed with bicyclic peptide UK603 (bicyclic 2) Deposited 2014-02-12 Assembly 1 Protein heterocomplex Heteromer;Protein × 2 PDB declaration: dimeric(2) Consistent with protein count
Chain A 179–423(245 aa) Fragment:catalytic domain (UNP residues 179-423)
Mutation:C122A, N145Q SO4 SULFATE ION × 2 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, HANGING DROP;pH 4.5;291 K;21% PEG4000, 15% glycerol, 0.17 M ammonium sulfate, 0.1 M sodium acetate, pH 4.5, VAPOR DIFFUSION, HANGING DROP, temperature 291K
Resolution 2.26 Å R-free 0.200
4OS6 Crystal structure of urokinase-type plasminogen activator (uPA) complexed with bicyclic peptide UK604 (bicyclic 2) Deposited 2014-02-12 Assembly 1 Protein heterocomplex Heteromer;Protein × 2 PDB declaration: dimeric(2) Consistent with protein count
Chain A 179–423(245 aa) Fragment:catalytic domain (UNP residues 179-423)
Mutation:C122A, N145Q SO4 SULFATE ION × 2 ACT ACETATE ION × 1 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, HANGING DROP;pH 4.5;291 K;21% PEG4000, 15% glycerol, 0.17 M ammonium sulfate, 0.1 M sodium acetate, pH 4.5, VAPOR DIFFUSION, HANGING DROP, temperature 291K
Resolution 1.75 Å R-free 0.186
4OS7 Crystal structure of urokinase-type plasminogen activator (uPA) complexed with bicyclic peptide UK607 (bicyclic) Deposited 2014-02-12 Assembly 1 Protein heterocomplex Heteromer;Protein × 2 PDB declaration: dimeric(2) Consistent with protein count
Chain A 179–423(245 aa) Fragment:catalytic domain (UNP residues 179-423)
Mutation:C122A, N145Q SO4 SULFATE ION × 3 ACT ACETATE ION × 1 GOL GLYCEROL × 1 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, HANGING DROP;pH 4.5;291 K;21% PEG4000, 15% glycerol, 0.17 M ammonium sulfate, 0.1 M sodium acetate, pH 4.5, VAPOR DIFFUSION, HANGING DROP, temperature 291K
Resolution 2.00 Å R-free 0.198
4X0W The crystal structure of mupain-1-17 in complex with murinised human uPA Deposited 2014-11-24 Assembly 1 Protein heterocomplex Heteromer;Protein × 2 PDB declaration: dimeric(2) Consistent with protein count
Chain U 179–425(247 aa) Fragment:UNP RESIDUES 179-425
Mutation:H99Y, C122A, N145Q MRZ piperidine-1-carboximidamide × 1 SO4 SULFATE ION × 1 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, SITTING DROP;pH 4.6;298 K;2.0 M ammonium sulfate, 50 mM sodium citrate pH 4.6, 5% PEG 400
Resolution 2.10 Å R-free 0.272
4X1N The crystal structure of mupain-1-16 in complex with murinised human uPA at pH7.4 Deposited 2014-11-25 Assembly 1 Protein heterocomplex Heteromer;Protein × 2 PDB declaration: dimeric(2) Consistent with protein count
Chain U 179–425(247 aa) Fragment:UNP RESIDUES 179-425
Mutation:C299A, H272Y, N322Q MRZ piperidine-1-carboximidamide × 1 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, SITTING DROP;pH 4.6;298 K;2.0M ammonium sulfate, 50mM sodium citrate pH 4.6, 5% PEG 400
Resolution 1.80 Å R-free 0.276
4X1P The crystal structure of mupain-1-17 in complex with murinised human uPA at pH4.6 Deposited 2014-11-25 Assembly 1 Protein heterocomplex Heteromer;Protein × 2 PDB declaration: dimeric(2) Consistent with protein count
Chain U 179–425(247 aa) Fragment:catalytic domain (UNP RESIDUES 179-425)
Mutation:H99Y, C122A, N145Q SO4 SULFATE ION × 2 PGE TRIETHYLENE GLYCOL × 2 MRZ piperidine-1-carboximidamide × 1 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, SITTING DROP;pH 4.6;298 K;2.0M ammonium sulfate, 50mM sodium citrate pH 4.6, 5% PEG400
Resolution 1.60 Å R-free 0.211
4X1Q The crystal structure of mupain-1 in complex with murinised human uPA at pH7.4 Deposited 2014-11-25 Assembly 1 Protein heterocomplex Heteromer;Protein × 2 PDB declaration: dimeric(2) Consistent with protein count
Chain U 179–425(247 aa) Fragment:catalytic domain (UNP RESIDUES 179-425)
Mutation:H99Y, C122A, N145Q No recorded non-water small molecule X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, SITTING DROP;pH 4.6;298 K;2.0M ammonium sulfate, 50mM sodium citrate pH 4.6, 5% PEG 400
Resolution 2.28 Å R-free 0.287
4X1R The crystal structure of mupain-1-12 in complex with murinised human uPA at pH7.4 Deposited 2014-11-25 Assembly 1 Protein heterocomplex Heteromer;Protein × 2 PDB declaration: dimeric(2) Consistent with protein count
Chain U 179–425(247 aa) Fragment:catalytic domain (UNP RESIDUES 179-425)
Mutation:H99Y, C122A, N145Q PL0 1-phenylguanidine × 1 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, SITTING DROP;pH 4.6;298 K;2.0M ammonium sulfate, 50mM sodium citrate pH 4.6, 5% PEG 400
Resolution 2.10 Å R-free 0.273
4X1S The crystal structure of mupain-1-16-D9A in complex with murinised human uPA at pH7.4 Deposited 2014-11-25 Assembly 1 Protein heterocomplex Heteromer;Protein × 2 PDB declaration: dimeric(2) Consistent with protein count
Chain U 179–425(247 aa) Fragment:catalytic domain (UNP RESIDUES 179-425)
Mutation:H99Y, C122A, N145Q MRZ piperidine-1-carboximidamide × 1 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, SITTING DROP;pH 4.6;298 K;2.0M ammonium sulfate, 50mM sodium citrate pH 4.6, 5% PEG 400
Resolution 1.90 Å R-free 0.249
4XSK Structure of PAItrap, an uPA mutant Deposited 2015-01-22 Assembly 1 Protein monomer Monomer;Protein × 1 PDB declaration: monomeric(1) Consistent with protein count
Chain U 179–424(246 aa) Fragment:UNP RESIDUES 162-407
Mutation:G37R, C122A, N145Q, S195A, R217L SO4 SULFATE ION × 2 PGE TRIETHYLENE GLYCOL × 2 GOL GLYCEROL × 2 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, SITTING DROP;pH 4.6;298 K;2.2 M ammonium sulfate, 5% PEG 400, 50 mM sodium citrate (pH 4.6)
Resolution 1.50 Å R-free 0.209
4ZHL The crystal structure of mupain-1-IG in complex with murinised human uPA at pH7.4 Deposited 2015-04-25 Assembly 1 Protein heterocomplex Heteromer;Protein × 2 PDB declaration: dimeric(2) Consistent with protein count
Chain U 179–425(247 aa) Fragment:UNP RESIDUES 179-425
Mutation:H99Y, C122A, N145Q No recorded non-water small molecule X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, SITTING DROP;pH 4.6;298 K;2.0M ammonium sulfate, 50mM sodium citrate, pH 4.6, 5% polyethylene glycol (PEG) 400
Resolution 2.06 Å R-free 0.262
4ZHM The crystal structure of mupain-1--16-IG in complex with murinised human uPA at pH7.4 Deposited 2015-04-25 Assembly 1 Protein heterocomplex Heteromer;Protein × 2 PDB declaration: dimeric(2) Consistent with protein count
Chain U 179–425(247 aa) Fragment:UNP RESIDUES 179-425
Mutation:H99Y, C122A, N145Q MRZ piperidine-1-carboximidamide × 1 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, SITTING DROP;pH 4.6;298 K;2.0M ammonium sulfate, 50mM sodium citrate, pH 4.6, 5% polyethylene glycol (PEG) 400
Resolution 1.90 Å R-free 0.264
4ZKN The crystal structure of upain-1-W3A in complex with uPA at pH5.5 Deposited 2015-04-30 Assembly 1 Protein heterocomplex Heteromer;Protein × 2 PDB declaration: dimeric(2) Consistent with protein count
Chain U 179–425(247 aa) Fragment:UNP residues 179-425
Mutation:C122A, N145Q SO4 SULFATE ION × 1 PG4 TETRAETHYLENE GLYCOL × 2 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, SITTING DROP;pH 4.6;298 K;50 mM sodium citrate pH 4.6, 2.0 M ammonium sulfate supplemented with 5% PEG 400
Resolution 1.36 Å R-free 0.265
4ZKO The crystal structure of upain-1-W3A in complex with uPA at pH7.4 Deposited 2015-04-30 Assembly 1 Protein heterocomplex Heteromer;Protein × 3 PDB declaration: trimeric(3) Consistent with protein count
Chain U 179–425(247 aa) Fragment:UNP residues 179-425
Mutation:C122A, N145Q SO4 SULFATE ION × 1 P6G HEXAETHYLENE GLYCOL × 1 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, SITTING DROP;pH 4.6;298 K;50 mM sodium citrate pH 4.6, 2.0 M ammonium sulfate supplemented with 5% PEG 400
Resolution 1.29 Å R-free 0.225
4ZKR The crystal structure of upain-1-W3A in complex with uPA at pH9.0 Deposited 2015-04-30 Assembly 1 Protein heterocomplex Heteromer;Protein × 2 PDB declaration: dimeric(2) Consistent with protein count
Chain U 179–425(247 aa) Fragment:UNP residues 179-425
Mutation:C122A, N145Q SO4 SULFATE ION × 1 P6G HEXAETHYLENE GLYCOL × 1 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, SITTING DROP;298 K;50 mM sodium citrate pH 4.6, 2.0 M ammonium sulfate supplemented with 5% PEG400
Resolution 1.36 Å R-free 0.234
4ZKS The crystal structure of upain-1-W3A in complex with inactive uPA (uPA-S195A) at pH7.4 Deposited 2015-04-30 Assembly 1 Protein heterocomplex Heteromer;Protein × 2 PDB declaration: dimeric(2) Consistent with protein count
Chain U 179–425(247 aa) Fragment:UNP residues 179-425
Mutation:C122A, N145Q, S195A No recorded non-water small molecule X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, SITTING DROP;pH 4.6;298 K;50 mM sodium citrate pH 4.6, 2.0 M ammonium sulfate supplemented with 5% PEG400
Resolution 1.85 Å R-free 0.245
5HGG Crystal structure of uPA in complex with a camelid-derived antibody fragment Deposited 2016-01-08 Assembly 1 Protein heterocomplex Heteromer;Protein × 4 PDB declaration: tetrameric(4) Consistent with protein count
Chain A 179–424(246 aa) Fragment:UNP residues 179-424
Chain B 179–424(246 aa) Fragment:UNP residues 179-424
Mutation:C122A, N145Q Mutation:C122A, N145Q GOL GLYCEROL × 5 SO4 SULFATE ION × 2 TWN (3S)-3-[(2S,3S,4R)-3,4-DIMETHYLTETRAHYDROFURAN-2-YL]BUTYL LAURATE × 3 MES 2-(N-MORPHOLINO)-ETHANESULFONIC ACID × 1 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, HANGING DROP;pH 6.25;289 K;Sodium Phosphate dibasic, Ammonium Sulfate, MES, Tween 20
Resolution 1.97 Å R-free 0.196
5WXF Crystal structure of uPA in complex with upain-2-2 Deposited 2017-01-07 Assembly 1 Protein heterocomplex Heteromer;Protein × 2 PDB declaration: dimeric(2) Consistent with protein count
Chain U 179–431(253 aa)
Mutation:C299A/N322Q SO4 SULFATE ION × 1 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, SITTING DROP;298 K;50 mM sodium citrate, pH 4.6, and 2.0 M ammonium sulfate supplemented with 5% polyethylene glycol 400
Resolution 1.46 Å R-free 0.245
5WXO Crystal structure of uPA in complex with upain-2-2-W3A Deposited 2017-01-08 Assembly 1 Protein heterocomplex Heteromer;Protein × 2 PDB declaration: dimeric(2) Consistent with protein count
Chain U 179–431(253 aa)
Mutation:C299A/N322Q No recorded non-water small molecule X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, SITTING DROP;298 K;50mM sodium citrate, pH 4.6, 2.0M ammonium sulfate supplemented with 5% polyethylene glycol 400
Resolution 1.64 Å R-free 0.221
5WXP Crystal structure of uPA in complex with upain-2-3-W3A Deposited 2017-01-08 Assembly 1 Protein heterocomplex Heteromer;Protein × 2 PDB declaration: dimeric(2) Consistent with protein count
Chain U 179–431(253 aa)
Mutation:C299A/N322Q ALA ALANINE × 1 CYS CYSTEINE × 1 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, SITTING DROP;298 K;50mM sodium citrate, pH 4.6, 2.0M ammonium sulfate supplemented with 5% polyethylene glycol 400
Resolution 1.75 Å R-free 0.249
5WXQ Crystal structure of uPA in complex with upain-2-4 Deposited 2017-01-08 Assembly 1 Protein heterocomplex Heteromer;Protein × 2 PDB declaration: dimeric(2) Consistent with protein count
Chain U 179–431(253 aa)
Mutation:C299A/N322Q No recorded non-water small molecule X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, SITTING DROP;298 K;50mM sodium citrate, pH 4.6, 2.0M ammonium sulfate supplemented with 5% polyethylene glycol 400
Resolution 1.79 Å R-free 0.212
5WXR Crystal structure of uPA in complex with upain-2-4-W3A Deposited 2017-01-08 Assembly 1 Protein heterocomplex Heteromer;Protein × 2 PDB declaration: dimeric(2) Consistent with protein count
Chain U 179–431(253 aa)
Mutation:C299A/N322Q No recorded non-water small molecule X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, SITTING DROP;298 K;50mM sodium citrate, pH 4.6, 2.0M ammonium sulfate supplemented with 5% polyethylene glycol 400
Resolution 1.75 Å R-free 0.234
5WXS Crystal structure of uPA in complex with S2444 Deposited 2017-01-08 Assembly 1 Protein monomer Monomer;Protein × 1 PDB declaration: monomeric(1) Consistent with protein count
Chain U 179–431(253 aa)
Mutation:C299A/N322Q 7YF (2R)-N-[2-[[(2S)-5-carbamimidamido-1-oxidanylidene-pentan-2-yl]amino]-2-oxidanylidene-ethyl]-5-oxidanylidene-1,2-dihydropyrrole-2-carboxamide × 1 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, SITTING DROP;298 K;50mM sodium citrate, pH 4.6, 2.0M ammonium sulfate supplemented with 5% polyethylene glycol 400
Resolution 2.30 Å R-free 0.266
5WXT Crystal structure of uPA-S195A in complex with S2444 Deposited 2017-01-08 Assembly 1 Protein monomer Monomer;Protein × 1 PDB declaration: monomeric(1) Consistent with protein count
Chain U 179–431(253 aa)
Mutation:C299A/N322Q/S376A 7YR 5-oxo-D-prolylglycyl-N-(4-nitrophenyl)-L-argininamide × 1 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, SITTING DROP;298 K;50 mM sodium citrate, pH 4.6, and 2.0 M ammonium sulfate supplemented with 5% polyethylene glycol 400
Resolution 2.10 Å R-free 0.266
5XG4 Crystal structure of uPA in complex with quercetin Deposited 2017-04-11 Assembly 1 Protein monomer Monomer;Protein × 1 PDB declaration: monomeric(1) Consistent with protein count
Chain U 179–424(246 aa) Fragment:UNP residues 179-424
Not recorded QUE 3,5,7,3',4'-PENTAHYDROXYFLAVONE × 1 PG6 1-(2-METHOXY-ETHOXY)-2-{2-[2-(2-METHOXY-ETHOXY]-ETHOXY}-ETHANE × 1 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, SITTING DROP;298 K;50mM sodium citrate at pH 4.6, 1.95M (NH4)2SO4, 0.03% NaN3, 5% PEG 400
Resolution 3.00 Å R-free 0.258
5YC6 The crystal structure of uPA in complex with 4-Bromobenzylamirne at pH4.6 Deposited 2017-09-06 Assembly 1 Protein monomer Monomer;Protein × 1 PDB declaration: monomeric(1) Consistent with protein count
Chain U 179–424(246 aa) Fragment:Urokinase-type plasminogen activator chain B, UNP residues 179-324
Not recorded PZH 1-(4-BROMOPHENYL)METHANAMINE × 1 SO4 SULFATE ION × 1 PGE TRIETHYLENE GLYCOL × 2 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, SITTING DROP;298 K;50mM sodium citrate (pH 4.6), 2.0M ammonium sulfate supplemented with 5% PEG 400
Resolution 1.18 Å R-free 0.228
5YC7 The crystal structure of uPA in complex with 4-Bromobenzylamirne at pH7.4 Deposited 2017-09-06 Assembly 1 Protein monomer Monomer;Protein × 1 PDB declaration: monomeric(1) Consistent with protein count
Chain U 179–424(246 aa) Fragment:Urokinase-type plasminogen activator chain B, UNP residues 179-324
Not recorded PZH 1-(4-BROMOPHENYL)METHANAMINE × 1 SO4 SULFATE ION × 1 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, SITTING DROP;298 K;50mM sodium citrate (pH 4.6), 2.0M ammonium sulfate supplemented with 5% PEG 400
Resolution 2.00 Å R-free 0.262
5Z1C The crystal structure of uPA in complex with 4-Iodobenzylamine at pH7.4 Deposited 2017-12-25 Assembly 1 Protein monomer Monomer;Protein × 1 PDB declaration: monomeric(1) Consistent with protein count
Chain U 179–423(245 aa)
Mutation:C299U,N322U ZXI 1-(4-iodophenyl)methanamine × 1 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, SITTING DROP;298 K;50mM sodium citrate (pH 4.6), 2.0M ammonium sulfate supplemented with 5% PEG 400
Resolution 1.45 Å R-free 0.143
5ZA7 uPA-HMA Deposited 2018-02-06 Assembly 1 Protein monomer Monomer;Protein × 1 PDB declaration: monomeric(1) Consistent with protein count
Chain U 179–431(253 aa)
Mutation:C122A, N145Q HMX 3-azanyl-5-(azepan-1-yl)-N-[bis(azanyl)methylidene]-6-chloranyl-pyrazine-2-carboxamide × 1 SO4 SULFATE ION × 1 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, SITTING DROP;298 K;50mM sodium citrate pH 4.6, 1.95M (NH4)2SO4, 0.03% NaN3, 5% PEG 400
Resolution 1.70 Å R-free 0.227
5ZA8 uPA-BB2-27F Deposited 2018-02-06 Assembly 1 Protein monomer Monomer;Protein × 1 PDB declaration: monomeric(1) Consistent with protein count
Chain U 179–431(253 aa)
Mutation:C122A, N145Q 27I 3-azanyl-5-(azepan-1-yl)-N-carbamimidoyl-6-(1-methylpyrazol-4-yl)pyrazine-2-carboxamide × 1 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, SITTING DROP;298 K;50mM sodium citrate pH 4.6, 1.95M (NH4)2SO4, 0.03% NaN3, 5% PEG 400
Resolution 1.90 Å R-free 0.233
5ZA9 uPA-BB2-50F Deposited 2018-02-07 Assembly 1 Protein monomer Monomer;Protein × 1 PDB declaration: monomeric(1) Consistent with protein count
Chain U 179–431(253 aa)
Mutation:C122A, N145Q 50I 3-azanyl-5-(azepan-1-yl)-6-(1-benzofuran-2-yl)-Ncarbamimidoyl-pyrazine-2-carboxamide × 1 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, SITTING DROP;298 K;50mM sodium citrate pH 4.6, 1.95M (NH4)2SO4, 0.03% NaN3, 5% PEG 400
Resolution 1.62 Å R-free 0.236
5ZAE uPA-6F-HMA Deposited 2018-02-07 Assembly 1 Protein monomer Monomer;Protein × 1 PDB declaration: monomeric(1) Consistent with protein count
Chain U 179–431(253 aa)
Mutation:C122A, N145Q EAU 3-azanyl-5-(azepan-1-yl)-N-carbamimidoyl-6-(furan-2-yl)pyrazine-2-carboxamide × 1 SO4 SULFATE ION × 1 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, SITTING DROP;298 K;50mM sodium citrate pH 4.6, 1.95M (NH4)2SO4, 0.03% NaN3, 5% PEG 400
Resolution 1.73 Å R-free 0.276
5ZAF uPA-BB2-28F Deposited 2018-02-07 Assembly 1 Protein monomer Monomer;Protein × 1 PDB declaration: monomeric(1) Consistent with protein count
Chain U 162–414(253 aa)
Mutation:C122A, N145Q 28I 3-azanyl-5-(azepan-1-yl)-N-carbamimidoyl-6-(furan-3-yl)pyrazine-2-carboxamide × 1 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, SITTING DROP;298 K;50mM sodium citrate pH 4.6, 1.95M (NH4)2SO4, 0.03% NaN3, 5% PEG 400
Resolution 1.65 Å R-free 0.236
5ZAG uPA-BB2-94F Deposited 2018-02-07 Assembly 1 Protein monomer Monomer;Protein × 1 PDB declaration: monomeric(1) Consistent with protein count
Chain U 179–431(253 aa)
Mutation:C122A, N145Q 94I 3-azanyl-5-(azepan-1-yl)-N-carbamimidoyl-6-pyrimidin-5-yl-pyrazine-2-carboxamide × 1 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, SITTING DROP;298 K;50mM sodium citrate pH 4.6, 1.95M (NH4)2SO4, 0.03% NaN3, 5% PEG 400
Resolution 1.95 Å R-free 0.225
5ZAH uPA-BB2-30F Deposited 2018-02-07 Assembly 1 Protein monomer Monomer;Protein × 1 PDB declaration: monomeric(1) Consistent with protein count
Chain U 179–431(253 aa)
Mutation:C122A, N145Q 30I 3-azanyl-5-(azepan-1-yl)-N-carbamimidoyl-6-(2-methoxypyrimidin-5-yl)pyrazine-2-carboxamide × 1 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, SITTING DROP;298 K;50mM sodium citrate pH 4.6, 1.95M (NH4)2SO4, 0.03% NaN3, 5% PEG 400
Resolution 2.98 Å R-free 0.268
5ZAJ uPA-31F Deposited 2018-02-07 Assembly 1 Protein monomer Monomer;Protein × 1 PDB declaration: monomeric(1) Consistent with protein count
Chain U 179–431(253 aa)
Mutation:C122A, N145Q 32I 3-azanyl-5-(azepan-1-yl)-N-carbamimidoyl-6-(2,4-dimethoxypyrimidin-5-yl)pyrazine-2-carboxamide × 1 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, SITTING DROP;298 K;50mM sodium citrate pH 4.6, 1.95M (NH4)2SO4, 0.03% NaN3, 5% PEG 400
Resolution 1.65 Å R-free 0.239
5ZC5 uPA-NU-09F Deposited 2018-02-15 Assembly 1 Protein monomer Monomer;Protein × 1 PDB declaration: monomeric(1) Consistent with protein count
Chain U 179–431(253 aa)
Mutation:C122A, N145Q 09I 3-azanyl-5-(azepan-1-yl)-N-carbamimidoyl-6-(4-fluoranyl-1-benzofuran-2-yl)pyrazine-2-carboxamide × 1 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, SITTING DROP;298 K;50mM sodium citrate pH 4.6, 1.95M (NH4)2SO4, 0.03% NaN3, 5% PEG 400
Resolution 1.90 Å R-free 0.235
6AG2 uPA-HMA Deposited 2018-08-09 Assembly 1 Protein monomer Monomer;Protein × 1 PDB declaration: monomeric(1) Consistent with protein count
Chain U 179–431(253 aa)
Mutation:C122A, N145Q 9X9 3,5-bis(azanyl)-N-carbamimidoyl-6-(2-methoxypyrimidin-5-yl)pyrazine-2-carboxamide × 1 SO4 SULFATE ION × 1 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, SITTING DROP;298 K;2.0M ammonium sulfate, 50mM sodium citrate (pH 4.6), 5% PEG 400
Resolution 1.77 Å R-free 0.252
6AG3 Crystal structure of uPA in complex with 3,5-bis(azanyl)-N-carbamimidoyl-6-(2,4-dimethoxypyrimidin-5-yl)pyrazine-2-carboxamide Deposited 2018-08-09 Assembly 1 Protein monomer Monomer;Protein × 1 PDB declaration: monomeric(1) Consistent with protein count
Chain U 179–431(253 aa)
Mutation:C122A, N145Q 9XC 3,5-bis(azanyl)-N-carbamimidoyl-6-(2,4-dimethoxypyrimidin-5-yl)pyrazine-2-carboxamide × 1 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, SITTING DROP;298 K;50mM sodium citrate, pH 4.6, 2.0M ammonium sulfate supplemented with 5% polyethylene glycol 400
Resolution 2.48 Å R-free 0.267
6AG7 The crystal structure of uPA in complex with HMA-55F Deposited 2018-08-09 Assembly 1 Protein monomer Monomer;Protein × 1 PDB declaration: monomeric(1) Consistent with protein count
Chain U 179–423(245 aa)
Not recorded H55 3,5-diamino-N-carbamimidoyl-6-(1-methyl-1H-pyrazol-4-yl)pyrazine-2-carboxamide × 1 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, SITTING DROP;298 K;50 mM sodium citrate, pH 4.6, and 2.0 M ammonium sulfate supplemented with 5% polyethylene glycol 400
Resolution 1.90 Å R-free 0.228
6AG9 Crystal structure of uPA in complex with 3,5-bis(azanyl)-6-(1-benzofuran-2-yl)-N-carbamimidoyl-pyrazine-2- carboxamide Deposited 2018-08-09 Assembly 1 Protein monomer Monomer;Protein × 1 PDB declaration: monomeric(1) Consistent with protein count
Chain U 179–431(253 aa)
Mutation:C122A, N145Q 9XF 3,5-bis(azanyl)-6-(1-benzofuran-2-yl)-N-carbamimidoyl-pyrazine-2-carboxamide × 1 SO4 SULFATE ION × 1 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, SITTING DROP;298 K;50mM sodium citrate, pH 4.6, 2.0M ammonium sulfate supplemented with 5% polyethylene glycol 400
Resolution 1.63 Å R-free 0.206
6JYP Crystal structure of uPA_H99Y in complex with 3-azanyl-5-(azepan-1-yl)-N-[bis(azanyl)methylidene]-6-chloranyl-pyrazine-2-carboxamide Deposited 2019-04-27 Assembly 1 Protein monomer Monomer;Protein × 1 PDB declaration: monomeric(1) Consistent with protein count
Chain U 179–424(246 aa)
Mutation:H99Y,C122A,N145Q HMX 3-azanyl-5-(azepan-1-yl)-N-[bis(azanyl)methylidene]-6-chloranyl-pyrazine-2-carboxamide × 1 SO4 SULFATE ION × 1 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, SITTING DROP;298 K;0.05M sodium citrate at pH 4.6, 1.95M (NH4)2SO4, 0.03% NaN3, 5% PEG 400
Resolution 2.25 Å R-free 0.254
6JYQ Crystal structure of uPA_H99Y in complex with 3-azanyl-5-(azepan-1-yl)-N-carbamimidoyl-6-(furan-2-yl)pyrazine-2-carboxamide Deposited 2019-04-27 Assembly 1 Protein monomer Monomer;Protein × 1 PDB declaration: monomeric(1) Consistent with protein count
Chain U 179–424(246 aa)
Mutation:H99Y,C122A,N145Q EAU 3-azanyl-5-(azepan-1-yl)-N-carbamimidoyl-6-(furan-2-yl)pyrazine-2-carboxamide × 1 SO4 SULFATE ION × 1 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, SITTING DROP;298 K;0.05M sodium citrate at pH 4.6, 1.95M (NH4)2SO4, 0.03% NaN3, 5% PEG 400
Resolution 1.75 Å R-free 0.263
6L04 Crystal structure of uPA_H99Y in complex with 31F Deposited 2019-09-26 Assembly 1 Protein monomer Monomer;Protein × 1 PDB declaration: monomeric(1) Consistent with protein count
Chain U 179–423(245 aa)
Mutation:H99Y,C122A,N145Q 32I 3-azanyl-5-(azepan-1-yl)-N-carbamimidoyl-6-(2,4-dimethoxypyrimidin-5-yl)pyrazine-2-carboxamide × 1 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, SITTING DROP;298 K;50mM sodium citrate at pH 4.6, 1.95M (NH4)2SO4, 0.03% NaN3, 5% PEG 400
Resolution 2.21 Å R-free 0.217
6L05 Crystal structure of uPA_H99Y in complex with 50F Deposited 2019-09-26 Assembly 1 Protein monomer Monomer;Protein × 1 PDB declaration: monomeric(1) Consistent with protein count
Chain U 179–423(245 aa)
Mutation:H99Y,C122A,N145Q 50I 3-azanyl-5-(azepan-1-yl)-6-(1-benzofuran-2-yl)-Ncarbamimidoyl-pyrazine-2-carboxamide × 1 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, SITTING DROP;298 K;50mM sodium citrate at pH 4.6, 1.95M (NH4)2SO4, 0.03% NaN3, 5% PEG 400
Resolution 2.49 Å R-free 0.261
6NMB Tranexamic Acid is an Active Site Inhibitor of Urokinase Plasminogen Activator Deposited 2019-01-10 Assembly 1 Protein monomer Monomer;Protein × 1 PDB declaration: monomeric(1) Consistent with protein count
Chain A 164–431(268 aa) Fragment:UNP residues 164-431
Not recorded NO3 NITRATE ION × 1 AMH TRANS-4-AMINOMETHYLCYCLOHEXANE-1-CARBOXYLIC ACID × 1 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, HANGING DROP;pH 8.5;293 K;0.03 M sodium nitrate, 0.03 M sodium phosphate, 0.03 M ammonium sulfate, 0.1 M Tris bicine, 25% v/v PEG500, 10% v/v PEG20000
Resolution 2.30 Å R-free 0.271
6NMB Tranexamic Acid is an Active Site Inhibitor of Urokinase Plasminogen Activator Deposited 2019-01-10 Assembly 2 Protein monomer Monomer;Protein × 1 PDB declaration: monomeric(1) Consistent with protein count
Chain B 164–431(268 aa) Fragment:UNP residues 164-431
Not recorded NO3 NITRATE ION × 1 AMH TRANS-4-AMINOMETHYLCYCLOHEXANE-1-CARBOXYLIC ACID × 1 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, HANGING DROP;pH 8.5;293 K;0.03 M sodium nitrate, 0.03 M sodium phosphate, 0.03 M ammonium sulfate, 0.1 M Tris bicine, 25% v/v PEG500, 10% v/v PEG20000
Resolution 2.30 Å R-free 0.271
6NMB Tranexamic Acid is an Active Site Inhibitor of Urokinase Plasminogen Activator Deposited 2019-01-10 Assembly 3 Protein monomer Monomer;Protein × 1 PDB declaration: monomeric(1) Consistent with protein count
Chain C 164–431(268 aa) Fragment:UNP residues 164-431
Not recorded NO3 NITRATE ION × 1 AMH TRANS-4-AMINOMETHYLCYCLOHEXANE-1-CARBOXYLIC ACID × 1 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, HANGING DROP;pH 8.5;293 K;0.03 M sodium nitrate, 0.03 M sodium phosphate, 0.03 M ammonium sulfate, 0.1 M Tris bicine, 25% v/v PEG500, 10% v/v PEG20000
Resolution 2.30 Å R-free 0.271
6NMB Tranexamic Acid is an Active Site Inhibitor of Urokinase Plasminogen Activator Deposited 2019-01-10 Assembly 4 Protein monomer Monomer;Protein × 1 PDB declaration: monomeric(1) Consistent with protein count
Chain D 164–431(268 aa) Fragment:UNP residues 164-431
Not recorded NO3 NITRATE ION × 1 AMH TRANS-4-AMINOMETHYLCYCLOHEXANE-1-CARBOXYLIC ACID × 1 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, HANGING DROP;pH 8.5;293 K;0.03 M sodium nitrate, 0.03 M sodium phosphate, 0.03 M ammonium sulfate, 0.1 M Tris bicine, 25% v/v PEG500, 10% v/v PEG20000
Resolution 2.30 Å R-free 0.271
6XVD Crystal structure of complex of urokinase and a upain-1 variant(W3F) in pH7.4 condition Deposited 2020-01-21 Assembly 1 Protein heterocomplex Heteromer;Protein × 2 PDB declaration: dimeric(2) Consistent with protein count
Chain U 162–414(253 aa)
Not recorded No recorded non-water small molecule X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, SITTING DROP;pH 4.5;293 K;0.05 M sodium citrate at pH 4.5, 1.95 M (NH4)2SO4, 0.05% NaN3, and 5% PEG400
Resolution 1.40 Å R-free 0.203
7DZD Crystal structure of uPA in complex with cleaved camostat Deposited 2021-01-25 Assembly 1 Protein monomer Monomer;Protein × 1 PDB declaration: monomeric(1) Consistent with protein count
Chain U 179–423(245 aa)
Mutation:C122A,N145Q GBS 4-carbamimidamidobenzoic acid × 1 PGE TRIETHYLENE GLYCOL × 2 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, SITTING DROP;298 K;2.0M ammonium sulfate, 50mM sodium citrate pH 4.6, 5% PEG 400
Resolution 2.00 Å R-free 0.231
7VM4 Crystal structure of uPA in complex with nafamostat Deposited 2021-10-07 Assembly 1 Protein monomer Monomer;Protein × 1 PDB declaration: monomeric(1) Consistent with protein count
Chain U 179–423(245 aa)
Not recorded GBS 4-carbamimidamidobenzoic acid × 1 PGE TRIETHYLENE GLYCOL × 2 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, SITTING DROP;298 K;2.0 M ammonium sulfate, 5% PEG400, 20 mM sodium citrate, pH 4.6
Resolution 2.01 Å R-free 0.224
7VM5 Crystal structure of uPA in complex with 4-guanidinobenzoic acid Deposited 2021-10-07 Assembly 1 Protein monomer Monomer;Protein × 1 PDB declaration: monomeric(1) Consistent with protein count
Chain U 179–424(246 aa)
Not recorded PGE TRIETHYLENE GLYCOL × 1 GBS 4-carbamimidamidobenzoic acid × 1 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, SITTING DROP;pH 4.6;298 K;2.0 M ammonium sulfate, 5% PEG 400, 20 mM sodium citrate, pH 4.6
Resolution 1.97 Å R-free 0.247
7VM6 Crystal structure of uPA in complex with 6-amidino-2-naphthol Deposited 2021-10-07 Assembly 1 Protein monomer Monomer;Protein × 1 PDB declaration: monomeric(1) Consistent with protein count
Chain U 179–426(248 aa)
Not recorded 7R8 6-oxidanylnaphthalene-2-carboximidamide × 1 SO4 SULFATE ION × 1 PGE TRIETHYLENE GLYCOL × 1 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, SITTING DROP;pH 4.6;298 K;2.0 M ammonium sulfate, 5% PEG 400, 20 mM sodium citrate, pH 4.6
Resolution 1.79 Å R-free 0.243
7VM7 Crystal structure of inactive uPA in complex with nafamostat Deposited 2021-10-07 Assembly 1 Protein monomer Monomer;Protein × 1 PDB declaration: monomeric(1) Consistent with protein count
Chain U 179–423(245 aa)
Not recorded 7RF (6-carbamimidoylnaphthalen-2-yl) 4-carbamimidamidobenzoate × 1 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, SITTING DROP;pH 4.6;298 K;2.0 M ammonium sulfate, 5% PEG 400, 20 mM sodium citrate, pH 4.6
Resolution 1.87 Å R-free 0.242
7ZRR Crystal structure of human Urokinase-type plasminogen activator in complex with bicycle peptide inhibitor UK965 Deposited 2022-05-05 Assembly 1 Protein heterocomplex Heteromer;Protein × 2 PDB declaration: dimeric(2) Consistent with protein count
Chain A 154–431(278 aa)
Not recorded 1PE PENTAETHYLENE GLYCOL × 1 EDO 1,2-ETHANEDIOL × 2 NH2 AMINO GROUP × 1 ZBR 1,3,5-tris(bromomethyl)benzene × 1 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, SITTING DROP;pH 4.3;293 K;5% PEG400, 50mM Citrato pH 4.3, 1.8 M (NH4)2SO4, 20% Ethylene glycol
Resolution 1.64 Å R-free 0.239
7ZRT Crystal structure of human Urokinase-type plasminogen activator in complex with bicycle peptide inhibitor UK970 Deposited 2022-05-05 Assembly 1 Protein heterocomplex Heteromer;Protein × 2 PDB declaration: dimeric(2) Consistent with protein count
Chain A 162–414(253 aa)
Not recorded SO4 SULFATE ION × 2 PEG DI(HYDROXYETHYL)ETHER × 2 EDO 1,2-ETHANEDIOL × 3 1PE PENTAETHYLENE GLYCOL × 1 ZBR 1,3,5-tris(bromomethyl)benzene × 1 X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION, SITTING DROP;pH 4.3;293 K;7% PEG400, 50mM Citrato, 1.8 M (NH4)2SO4; 20% Ethylene glycol
Resolution 1.80 Å R-free 0.229
9PYF uPA Inhibitory Fab AB2 Complex Deposited 2025-08-07 Assembly 1 Protein heterocomplex Heteromer;Protein × 3 PDB declaration: trimeric(3) Consistent with protein count
Chain F 156–425(270 aa)
Mutation:C122A No recorded non-water small molecule X-RAY DIFFRACTION
X-ray crystallization conditions VAPOR DIFFUSION;298.15 K;For crystallization purposes, uPA was co-incubated with AB2 in a 1:1 stoichiometric ratio for 1h and co-purified using size-exclusion chromatography. The complex co-eluted was concentrated to 15 mg/mL.Crystallization drops were produced by mixing 0.1 uL of uPA-AB2 solution with 0.1 uL of the respective crystallization solution. A single crystal was produced using a solution containing 0.2 M diammonium hydrogen citrate (Salt) and 20 percent PEG 3350 and incubating the experiment for 14 days at room temperature.
Resolution 2.90 Å R-free 0.300