The Ligandable Human Proteome

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Urokinase-type plasminogen activator

Serine proteases, trypsin domain

IndexLigand NameStructurePDB codeligand desolvation
1qggUROKINASE-TYPE PLASMINOGEN ACTIVATOR INHIBITOR COMPLEX WITH A 1-(7- SULPHOAMIDOISOQUINOLINYL)GUANIDINE2vnt87.77
2ui2Substituted 2-Naphthamidine Inhibitors of Urokinase1sqo85.39
3amrUROKINASE PLASMINOGEN ACTIVATOR B-CHAIN-AMILORIDE COMPLEX1f5l84.2
49upCrystal Structure of the Urokinase4fug83.06
54pgUrokinase plasminogen activator B-chain-GPPE complex2r2w82.6
68upCrystal Structure of the Urokinase4fuf79.94
71upCrystal Structure of the Urokinase4fu779.58
8239Crystal Structure of the Urokinase4fuc78.29
9135ENGINEERING INHIBITORS HIGHLY SELECTIVE FOR THE S1 SITES OF SER190 TRYPSIN-LIKE SERINE PROTEASE DRUG TARGETS1gja78.16
10ui3Substituted 2-Naphthamidine Inhibitors of Urokinase1sqt77.82
11ui3Crystal Structure of the Urokinase4fui76.89
12134ENGINEERING INHIBITORS HIGHLY SELECTIVE FOR THE S1 SITES OF SER190 TRYPSIN-LIKE SERINE PROTEASE DRUG TARGETS1gj976.7
1311eSynthesis of a Weak Basic uPA Inhibitor and Crystal Structure of Complex with uPA4h4276.34
14136ENGINEERING INHIBITORS HIGHLY SELECTIVE FOR THE S1 SITES OF SER190 TRYPSIN-LIKE SERINE PROTEASE DRUG TARGETS1gjd76.14
15hmxuPA-HMA5za775.89
16queCrystal structure of uPA in complex with quercetin5xg475.15
17239Substituted 2-Naphthamidine Inhibitors of Urokinase1owh75.09
189x9uPA-HMA6ag274.71
199xfCrystal structure of uPA in complex with 3,5-bis(azanyl)-6-(1-benzofuran-2-yl)-N-carbamimidoyl-pyrazine-2- carboxamide6ag974.71
20eauuPA-6F-HMA5zae74.51
217upCrystal Structure of the Urokinase4fue74.03
22133ENGINEERING INHIBITORS HIGHLY SELECTIVE FOR THE S1 SITES OF SER190 TRYPSIN-LIKE SERINE PROTEASE DRUG TARGETS1gj872.52
23l1rFragment-Based Discovery of Mexiletine Derivatives as Orally Bioavailable Inhibitors of Urokinase-Type Plasminogen Activator2vip72.23
24cr9Dissecting and Designing Inhibitor Selectivity Determinants at the S1 site Using an Artificial Ala190 Protease (Ala190 uPA)1o5c72.21
2509iuPA-NU-09F5zc571.8
26655Elaborate Manifold of Short Hydrogen Bond Arrays Mediating Binding of Active Site-Directed Serine Protease Inhibitors1o3p71.62
27d55Fragment-Based Discovery of Mexiletine Derivatives as Orally Bioavailable Inhibitors of Urokinase-Type Plasminogen Activator2viq71.25
2832iuPA-31F5zaj71.21
29ui1Substituted 2-Naphthamidine Inhibitors of Urokinase1sqa70.92
30h55The crystal structure of uPA in complex with HMA-55F6ag770.79
31745Substituted 2-Naphthamadine inhibitors of Urokinase1u6q70.13
3294iuPA-BB2-94F5zag69.17
33426Substituted 2-Naphthamidine Inhibitors of Urokinase1owi69.14
34d56Fragment-Based Discovery of Mexiletine Derivatives as Orally Bioavailable Inhibitors of Urokinase-Type Plasminogen Activator2viw68.78
351u9Crystal Structure of the Urokinase4fuj68.44
3650iuPA-BB2-50F5za968.34
3728iuPA-BB2-28F5zaf67.15
3827iuPA-BB2-27F5za866.78
39123A NOVEL SERINE PROTEASE INHIBITION MOTIF INVOLVING A MULTI-CENTERED SHORT HYDROGEN BONDING NETWORK AT THE ACTIVE SITE1gi966.08
4030iuPA-BB2-30F5zah65.61
41497Substituted 2-Naphthamidine inhibitors of urokinase1owd64.3
42303Substituted 2-Naphthamidine Inhibitors of Urokinase1owk64.19
43vg2Fragment-Based Discovery of Mexiletine Derivatives as Orally Bioavailable Inhibitors of Urokinase-Type Plasminogen Activator2viv63.21
449xcCrystal structure of uPA in complex with 3,5-bis(azanyl)-N-carbamimidoyl-6-(2,4-dimethoxypyrimidin-5-yl)pyrazine-2-carboxamide6ag359.7