General Information of the Protein
Protein ID
PT01043
Protein Name
Urokinase-type plasminogen activator
Gene Name
PLAU
Sequence
MRALLARLLLCVLVVSDSKGSNELHQVPSNCDCLNGGTCVSNKYFSNIHWCNCPKKFGGQHCEIDKSKTCYEGNGHFYRGKASTDTMGRPCLPWNSATVLQQTYHAHRSDALQLGLGKHNYCRNPDNRRRPWCYVQVGLKLLVQECMVHDCADGKKPSSPPEELKFQCGQKTLRPRFKIIGGEFTTIENQPWFAAIYRRHRGGSVTYVCGGSLISPCWVISATHCFIDYPKKEDYIVYLGRSRLNSNTQGEMKFEVENLILHKDYSADTLAHHNDIALLKIRSKEGRCAQPSRTIQTICLPSMYNDPQFGTSCEITGFGKENSTDYLYPEQLKMTVVKLISHRECQQPHYYGSEVTTKMLCAADPQWKTDSCQGDSGGPLVCSLQGRMTLTGIVSWGRGCALKDKPGVYTRVSHFLPWIRSHTKEENGLAL
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Organism
Homo sapiens, Human
Protein Classification
Enzyme
>
Protease
>
Serine protease
>
Serine protease PA clan
>
Serine protease S1A subfamily
Function
Specifically cleaves the zymogen plasminogen to form the active enzyme plasmin.
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Uniprot ID
Primary ID:
P00749

Secondarily ID:
B4DPZ2
Q15844
Q16618
Q53XS3
Q5SWW9
Q969W6
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Ensembl ID
ENSG00000122861
HGNC ID
HGNC:9052
Subcellular Location
Secreted
Map of Molecular Bioactivity Related to the Protein
Map of Molecular Bioactivity Related to the Protein

Protein
Cell Line
Compound

Bioactivity Value:

<= 0.1 μM
> 0.1 μM and <= 10 μM
> 10 μM
Imprecise Activity
Table of Molecular Bioactivities Related to the Protein
Cell Line ID: CL000006 , HEK293
 Cell Line Info 
Compound ID Compound Name Compound Formula
CP0553142
 Compound Info 
4-[4-(3,4-Dimethoxy-phenyl)-thiazol-2-yl]-5-methylsulfanyl-thiophene-2-carboxamidine
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C17H17N3O2S3
  1
1
Ki = 58 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0165221
 Compound Info 
5-Methylsulfanyl-4-(4-phenyl-thiazol-2-yl)-thiophene-2-carboxamidine
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C15H13N3S3
  1
1
Ki = 101 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0279172
 Compound Info 
4-[4-(4-Chloro-phenyl)-thiazol-2-yl]-5-methylsulfanyl-thiophene-2-carboxamidine
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C15H12ClN3S3
  1
1
Ki = 102 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0310138
 Compound Info 
5-Methyl-4-(4-phenyl-thiazol-2-yl)-thiophene-2-carboxamidine
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C15H13N3S2
  1
1
Ki = 103 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0185927
 Compound Info 
5-Ethyl-4-(4-phenyl-thiazol-2-yl)-thiophene-2-carboxamidine
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C16H15N3S2
  1
1
Ki = 138 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0540344
 Compound Info 
4-[4-(3,4-Dimethoxy-phenyl)-thiazol-2-yl]-5-methyl-thiophene-2-carboxamidine
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C17H17N3O2S2
  1
1
Ki = 169 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0128522
 Compound Info 
2-amidino-4-iodobenzothiophene
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C9H7IN2S
  1
1
Ki = 320 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0346128
 Compound Info 
5-Methoxy-4-(4-phenyl-thiazol-2-yl)-thiophene-2-carboxamidine
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C15H13N3OS2
  1
1
Ki = 531 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0483026
 Compound Info 
4-[4-(4-Chloro-phenyl)-thiazol-2-yl]-5-methanesulfinyl-thiophene-2-carboxamidine
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C15H12ClN3OS3
  1
1
Ki = 1420 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0527481
 Compound Info 
5-(4-Methoxy-benzylsulfanyl)-4-(4-phenyl-thiazol-2-yl)-thiophene-2-carboxamidine
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C22H19N3OS3
  1
1
Ki = 1520 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0461077
 Compound Info 
5-Benzylsulfanyl-4-[4-(4-chloro-phenyl)-thiazol-2-yl]-thiophene-2-carboxamidine
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C21H16ClN3S3
  1
1
Ki = 2500 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0487121
 Compound Info 
4-[4-(4-Chloro-phenyl)-thiazol-2-yl]-5-methanesulfonyl-thiophene-2-carboxamidine
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C15H12ClN3O2S3
  1
1
Ki = 2500 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0223874
 Compound Info 
4-(4-Phenyl-thiazol-2-yl)-thiophene-2-carboxamidine
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C14H11N3S2
  1
1
Ki = 5490 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0275837
 Compound Info 
5-Methylsulfanyl-thiophene-2-carboxamidine
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C6H8N2S2
  1
1
Ki = 6000 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
Cell Line ID: CL000265 , NS0
 Cell Line Info 
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0128522
 Compound Info 
2-amidino-4-iodobenzothiophene
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C9H7IN2S
  4
1 IC50 = 210 nM
2 Ki = 79.43 nM
3 Ki = 210 nM
4 Ki = 320 nM
CP0165221
 Compound Info 
5-Methylsulfanyl-4-(4-phenyl-thiazol-2-yl)-thiophene-2-carboxamidine
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C15H13N3S3
  1
1 Ki = 90 nM
CP0275837
 Compound Info 
5-Methylsulfanyl-thiophene-2-carboxamidine
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C6H8N2S2
  1
1 Ki = 6000 nM
CP0279172
 Compound Info 
4-[4-(4-Chloro-phenyl)-thiazol-2-yl]-5-methylsulfanyl-thiophene-2-carboxamidine
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C15H12ClN3S3
  1
1 Ki = 99000 nM
Clinical Information about the Protein
Target 1 ( Urokinase-type plasminogen activator (PLAU) )
Target Type Successful Target
Disease 4 Target-related Diseases  4
1 Breast cancer [ICD-11: 2C60-2C65]
2 Reperfusion injury [ICD-11: ND56.Z]
3 Myocardial hypertrophy [ICD-11: BC45]
4 Solid tumour/cancer [ICD-11: 2A00-2F9Z]
Clinical Trial Drug(s) 3 Clinical Trial Drugs  3
1 Upamostat
 Drug Info 
Phase 2
Breast cancer
2 PMID18163548C4
 Drug Info 
Clinical trial
Reperfusion injury
3 UK-356202
 Drug Info 
Clinical trial
Myocardial hypertrophy
Discontinued Drug(s) 2 Discontinued Drugs  2
1 WX-UK1
 Drug Info 
Discontinued in Phase 1/2
Solid tumour/cancer
2 B-428
 Drug Info 
Terminated
Solid tumour/cancer