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Target Report Card

Target Name and Classification

Target ID CHEMBL3475
Preferred Name Plasminogen activator inhibitor-1
Synonyms Endothelial plasminogen activator inhibitor | PAI | PAI-1 | PAI1 | PLANH1 | Plasminogen activator inhibitor 1 | SERPINE1 | Serpin E1
Organism Homo sapiens
Species Group No
Protein Target Classification
  • secreted protein

Target Components

Component Description Relationship Accession
Plasminogen activator inhibitor 1 SINGLE PROTEIN P05121

Approved Drugs and Clinical Candidates

ChEMBL ID Name Mechanism of Action Max Phase References
CHEMBL325424 ALEPLASININ Plasminogen activator inhibitor-1 inhibitor 1 PubMed

Target Associated Bioactivities

Target Associated Assays

Target Ligand Efficiencies

Target Associated Compound Properties

Target Cross References - Gene

Array Express ENSG00000106366
Ensembl ENSG00000106366
GO Cellular Component GO:0005576 (extracellular region)
GO:0005615 (extracellular space)
GO:0005886 (plasma membrane)
GO:0031012 (extracellular matrix)
GO:0031093 (platelet alpha granule lumen)
GO:0070062 (extracellular exosome)
GO Molecular Function GO:0002020 (protease binding)
GO:0004867 (serine-type endopeptidase inhibitor activity)
GO:0005102 (receptor binding)
GO:0005515 (protein binding)
GO:0030414 (peptidase inhibitor activity)
GO Biological Process GO:0001300 (chronological cell aging)
GO:0001525 (angiogenesis)
GO:0002576 (platelet degranulation)
GO:0007623 (circadian rhythm)
GO:0010466 (negative regulation of peptidase activity)
GO:0010469 (regulation of receptor activity)
GO:0010757 (negative regulation of plasminogen activation)
GO:0010951 (negative regulation of endopeptidase activity)
GO:0014912 (negative regulation of smooth muscle cell migration)
GO:0030194 (positive regulation of blood coagulation)
GO:0030195 (negative regulation of blood coagulation)
GO:0030198 (extracellular matrix organization)
GO:0030336 (negative regulation of cell migration)
GO:0032757 (positive regulation of interleukin-8 production)
GO:0033629 (negative regulation of cell adhesion mediated by integrin)
GO:0035491 (positive regulation of leukotriene production involved in inflammatory response)
GO:0042730 (fibrinolysis)
GO:0045766 (positive regulation of angiogenesis)
GO:0045944 (positive regulation of transcription from RNA polymerase II promoter)
GO:0048260 (positive regulation of receptor-mediated endocytosis)
GO:0050729 (positive regulation of inflammatory response)
GO:0050829 (defense response to Gram-negative bacterium)
GO:0051918 (negative regulation of fibrinolysis)
GO:0061044 (negative regulation of vascular wound healing)
GO:0061045 (negative regulation of wound healing)
GO:0071222 (cellular response to lipopolysaccharide)
GO:0071277 (cellular response to calcium ion)
GO:0090026 (positive regulation of monocyte chemotaxis)
GO:0090399 (replicative senescence)
GO:0097187 (dentinogenesis)
GO:1901331 (positive regulation of odontoblast differentiation)
GO:1902042 (negative regulation of extrinsic apoptotic signaling pathway via death domain receptors)
GO:2000098 (negative regulation of smooth muscle cell-matrix adhesion)
GO:2000352 (negative regulation of endothelial cell apoptotic process)
Wikipedia Plasminogen_activator_inhibitor-1

Target Cross References - Protein

canSAR P05121
CGD Plasminogen activator inhibitor-1 deficiency
Human Protein Atlas ENSG00000106366
IntAct P05121
Open Targets ENSG00000106366
PharmGKB PA261
Reactome R-HSA-114608 (Platelet degranulation.)
R-HSA-1368108 (BMAL1:CLOCK,NPAS2 activates circadian gene expression.)
R-HSA-2173796 (SMAD2/SMAD3:SMAD4 heterotrimer regulates transcription.)
R-HSA-3000178 (ECM proteoglycans.)
R-HSA-75205 (Dissolution of Fibrin Clot.)
UniProt B7Z4S0 F8WD53 P05121

Target Cross References - Domain

InterPro IPR000215 (Serpin_fam.)
IPR023795 (Serpin_CS.)
IPR023796 (Serpin_dom.)
IPR036186 (Serpin_sf.)
Pfam PF00079 (Serpin)

Target Cross References - Structure

PDBe 1A7C 1B3K 1C5G 1DB2 1DVM 1DVN 1LJ5 1OC0 3CVM 3EOX 3PB1 3Q02 3Q03 3R4L 3UT3 4AQH 4G8O 4G8R 4IC0 5BRR 9PAI
CREDO 1A7C 1B3K 1C5G 1DB2 1DVM 1DVN 1LJ5 1OC0 3CVM 3EOX 3PB1 3Q02 3Q03 3R4L 3UT3 4AQH 4G8O 4G8R 4IC0 5BRR 9PAI