General Information of the Protein
Protein ID
PT02196
Protein Name
Plasma kallikrein
Secondarily
Protein Name
Fletcher factor
Kininogenin
Plasma prekallikrein
Gene Name
KLKB1
Secondarily
Gene Name
KLK3
Sequence
MILFKQATYFISLFATVSCGCLTQLYENAFFRGGDVASMYTPNAQYCQMRCTFHPRCLLFSFLPASSINDMEKRFGCFLKDSVTGTLPKVHRTGAVSGHSLKQCGHQISACHRDIYKGVDMRGVNFNVSKVSSVEECQKRCTSNIRCQFFSYATQTFHKAEYRNNCLLKYSPGGTPTAIKVLSNVESGFSLKPCALSEIGCHMNIFQHLAFSDVDVARVLTPDAFVCRTICTYHPNCLFFTFYTNVWKIESQRNVCLLKTSESGTPSSSTPQENTISGYSLLTCKRTLPEPCHSKIYPGVDFGGEELNVTFVKGVNVCQETCTKMIRCQFFTYSLLPEDCKEEKCKCFLRLSMDGSPTRIAYGTQGSSGYSLRLCNTGDNSVCTTKTSTRIVGGTNSSWGEWPWQVSLQVKLTAQRHLCGGSLIGHQWVLTAAHCFDGLPLQDVWRIYSGILNLSDITKDTPFSQIKEIIIHQNYKVSEGNHDIALIKLQAPLNYTEFQKPICLPSKGDTSTIYTNCWVTGWGFSKEKGEIQNILQKVNIPLVTNEECQKRYQDYKITQRMVCAGYKEGGKDACKGDSGGPLVCKHNGMWRLVGITSWGEGCARREQPGVYTKVAEYMDWILEKTQSSDGKAQMQSPA
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Organism
Homo sapiens, Human
Protein Classification
Enzyme
>
Protease
>
Serine protease
>
Serine protease PA clan
>
Serine protease S1A subfamily
Function
Participates in the surface-dependent activation of blood coagulation. Activates, in a reciprocal reaction, coagulation factor XII/F12 after binding to negatively charged surfaces. Releases bradykinin from HMW kininogen and may also play a role in the renin-angiotensin system by converting prorenin into renin.
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Uniprot ID
Primary ID:
P03952

Secondarily ID:
A6NH96
B2R8H9
Q17RE8
Q17RE9
Q4W5C3
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HGNC ID
HGNC:6371
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: CL000265 , NS0
 Cell Line Info 
Compound ID Compound Name Compound Formula
CP0239863
 Compound Info 
2-[(3-chlorophenyl)methoxy]-4-(1-hydroxy-3,4-dihydro-2,1-benzoxaborinin-3-yl)benzenecarboximidamide;hydrochloride
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C22H21BCl2N2O3
  1
1
IC50 = 5.012 nM
 Bioactivity Info 
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CP0438055
 Compound Info 
4-[1-hydroxy-7-(trifluoromethyl)-3,4-dihydro-2,1-benzoxaborinin-3-yl]-2-(pyridin-3-ylmethoxy)benzenecarboximidamide;hydrochloride
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C22H20BClF3N3O3
  1
1
IC50 = 10 nM
 Bioactivity Info 
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CP0164331
 Compound Info 
4-[(3R)-1-hydroxy-7-(trifluoromethyl)-3,4-dihydro-2,1-benzoxaborinin-3-yl]-2-(pyridin-3-ylmethoxy)benzenecarboximidamide;hydrochloride
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C22H20BClF3N3O3
  1
1
IC50 = 19.95 nM
 Bioactivity Info 
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CP0250361
 Compound Info 
2-[(2-chlorophenyl)methoxy]-4-(1-hydroxy-3,4-dihydro-2,1-benzoxaborinin-3-yl)benzenecarboximidamide;hydrochloride
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C22H21BCl2N2O3
  1
1
IC50 = 50.12 nM
 Bioactivity Info 
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CP0239864
 Compound Info 
4-[(1-hydroxy-3H-2,1-benzoxaborol-3-yl)methyl]-2-(pyridin-3-ylmethoxy)benzenecarboximidamide;hydrochloride
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C21H21BClN3O3
  1
1
IC50 = 79.43 nM
 Bioactivity Info 
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CP0354488
 Compound Info 
4-(1-hydroxy-8-methyl-3,4-dihydro-2,1-benzoxaborinin-3-yl)-2-(pyridin-3-ylmethoxy)benzenecarboximidamide;hydrochloride
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C22H23BClN3O3
  1
1
IC50 = 79.43 nM
 Bioactivity Info 
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CP0477255
 Compound Info 
4-[(6-fluoro-1-hydroxy-3H-2,1-benzoxaborol-3-yl)methyl]-2-(pyridin-3-ylmethoxy)benzenecarboximidamide;hydrochloride
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C21H20BClFN3O3
  1
1
IC50 = 79.43 nM
 Bioactivity Info 
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CP0360969
 Compound Info 
4-(1-hydroxy-3,4-dihydro-2,1-benzoxaborinin-3-yl)-2-(pyridin-3-ylmethoxy)benzenecarboximidamide;hydrochloride
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C21H21BClN3O3
  1
1
IC50 = 100 nM
 Bioactivity Info 
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CP0340135
 Compound Info 
4-[[1-hydroxy-6-(trifluoromethyl)-3H-2,1-benzoxaborol-3-yl]methyl]-2-(pyridin-3-ylmethoxy)benzenecarboximidamide;hydrochloride
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C22H20BClF3N3O3
  1
1
IC50 = 199.53 nM
 Bioactivity Info 
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CP0354490
 Compound Info 
4-(6-chloro-7-fluoro-1-hydroxy-3,4-dihydro-2,1-benzoxaborinin-3-yl)-2-(pyridin-3-ylmethoxy)benzenecarboximidamide;hydrochloride
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C21H19BCl2FN3O3
  1
1
IC50 = 199.53 nM
 Bioactivity Info 
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CP0360971
 Compound Info 
4-[(3S)-1-hydroxy-7-(trifluoromethyl)-3,4-dihydro-2,1-benzoxaborinin-3-yl]-2-(pyridin-3-ylmethoxy)benzenecarboximidamide;hydrochloride
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C22H20BClF3N3O3
  1
1
IC50 = 398.11 nM
 Bioactivity Info 
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CP0340136
 Compound Info 
4-[(5-fluoro-1-hydroxy-3H-2,1-benzoxaborol-3-yl)methyl]-2-(pyridin-3-ylmethoxy)benzenecarboximidamide;hydrochloride
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C21H20BClFN3O3
  1
1
IC50 = 794.33 nM
 Bioactivity Info 
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CP0360970
 Compound Info 
4-[(1-hydroxy-5-methyl-3H-2,1-benzoxaborol-3-yl)methyl]-2-(pyridin-3-ylmethoxy)benzenecarboximidamide;hydrochloride
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C22H23BClN3O3
  1
1
IC50 = 794.33 nM
 Bioactivity Info 
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CP0477254
 Compound Info 
4-(7-fluoro-1-hydroxy-3,4-dihydro-2,1-benzoxaborinin-3-yl)-2-(pyridin-3-ylmethoxy)benzenecarboximidamide;hydrochloride
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C21H20BClFN3O3
  1
1
IC50 = 794.33 nM
 Bioactivity Info 
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CP0239865
 Compound Info 
4-[(1-hydroxy-5-methoxy-3H-2,1-benzoxaborol-3-yl)methyl]-2-(pyridin-3-ylmethoxy)benzenecarboximidamide;hydrochloride
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C22H23BClN3O4
  1
1
IC50 = 1258.93 nM
 Bioactivity Info 
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CP0063723
 Compound Info 
4-[(5-phenyl-1H-imidazol-2-yl)methylamino]-2-(pyridin-3-ylmethoxy)benzenecarboximidamide
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C23H22N6O
  1
1
IC50 = 6309.57 nM
 Bioactivity Info 
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Cell Line ID: CL000013 , Sf9
 Cell Line Info 
Clinical Information about the Protein
Target 1 ( Plasma kallikrein (KLKB1) )
Target Type Successful Target
Disease 1 Target-related Disease  1
1 Hereditary angioedema [ICD-11: 4A00.14]
Approved Drug(s) 1 Approved Drug  1
1 Berotralstat
 Drug Info 
Approved
Hereditary angioedema
Target 2 ( Plasma kallikrein messenger RNA (KLKB1 mRNA) )
Target Type Clinical trial Target