General Information of the Protein
Protein ID
PT01859
Protein Name
Kallikrein-1
Secondarily
Protein Name
Kidney/pancreas/salivary gland kallikrein
Tissue kallikrein
Gene Name
KLK1
Sequence
MWFLVLCLALSLGGTGAAPPIQSRIVGGWECEQHSQPWQAALYHFSTFQCGGILVHRQWVLTAAHCISDNYQLWLGRHNLFDDENTAQFVHVSESFPHPGFNMSLLENHTRQADEDYSHDLMLLRLTEPADTITDAVKVVELPTEEPEVGSTCLASGWGSIEPENFSFPDDLQCVDLKILPNDECKKAHVQKVTDFMLCVGHLEGGKDTCVGDSGGPLMCDGVLQGVTSWGYVPCGTPNKPSVAVRVLSYVKWIEDTIAENS
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Organism
Homo sapiens, Human
Protein Classification
Enzyme
>
Protease
>
Serine protease
>
Serine protease PA clan
>
Serine protease S1A subfamily
Function
Glandular kallikreins cleave Met-Lys and Arg-Ser bonds in kininogen to release Lys-bradykinin.
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Uniprot ID
Primary ID:
P06870

Secondarily ID:
Q66US9
Q86U61
Q8TCV8
Q9BS53
Q9NQU4
Q9UD19
Q9UMJ1
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Ensembl ID
ENSG00000167748
HGNC ID
HGNC:6357
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: CL000013 , Sf9
 Cell Line Info 
Compound ID Compound Name Compound Formula
CP0542345
 Compound Info 
N-(4-carbamimidoylphenyl)-3-ethoxy-2-hydroxybenzamide;hydrochloride
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C16H18ClN3O3
  1
1
IC50 = 125.89 nM
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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 = 251.19 nM
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CP0415993
 Compound Info 
N-(4-carbamimidoyl-3-fluorophenyl)-2-hydroxy-3-methoxybenzamide;formic acid
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C16H16FN3O5
  1
1
IC50 = 251.19 nM
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CP0532836
 Compound Info 
N-(4-carbamimidoylphenyl)-2-hydroxy-3-methoxybenzamide
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C15H15N3O3
  1
1
IC50 = 316.23 nM
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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 = 398.11 nM
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CP0552469
 Compound Info 
3-(1-hydroxy-3,4-dihydro-2,1-benzoxaborinin-3-yl)benzenecarboximidamide;hydrochloride
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C15H16BClN2O2
  1
1
IC50 = 501.19 nM
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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 = 630.96 nM
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CP0867278
 Compound Info 
N-(4-carbamimidoylphenyl)-3-chloro-2-hydroxybenzamide 2,2,2-trifluoroacetate
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C16H13ClF3N3O4
  1
1
IC50 = 630.96 nM
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CP0415994
 Compound Info 
N-(4-carbamimidoyl-3-chlorophenyl)-2-hydroxy-3-methoxybenzamide;formic acid
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C16H16ClN3O5
  1
1
IC50 = 1258.93 nM
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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 = 1584.89 nM
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CP0564667
 Compound Info 
4-[(6-chloro-1H-benzimidazol-2-yl)methylamino]benzenecarboximidamide;hydrochloride
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C15H15Cl2N5
  1
1
IC50 = 1995.26 nM
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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 = 1995.26 nM
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CP0252871
 Compound Info 
N-(4-carbamimidoylphenyl)-2-hydroxy-3-methylbenzamide
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C15H15N3O2
  1
1
IC50 = 3162.28 nM
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CP0530148
 Compound Info 
N-(4-carbamimidoyl-2-fluorophenyl)-2-hydroxybenzamide;formic acid
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C15H14FN3O4
  1
1
IC50 = 3162.28 nM
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CP0473980
 Compound Info 
N-(4-carbamimidoylphenyl)-2,3-dihydroxybenzamide;2,2,2-trifluoroacetic acid
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C16H14F3N3O5
  1
1
IC50 = 3981.07 nM
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CP0526053
 Compound Info 
4-[(1-hydroxy-3H-2,1-benzoxaborol-3-yl)methyl]benzenecarboximidamide;hydrochloride
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C15H16BClN2O2
  1
1
IC50 = 5011.87 nM
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CP0415992
 Compound Info 
N-(4-carbamimidoyl-2-methylphenyl)-2-hydroxybenzamide;formic acid
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C16H17N3O4
  1
1
IC50 = 5011.87 nM
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CP0384146
 Compound Info 
formic acid;4-[(6-methyl-1H-benzimidazol-2-yl)methylamino]benzenecarboximidamide
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C17H19N5O2
  1
1
IC50 = 6309.57 nM
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CP0413003
 Compound Info 
4-[(1-methylbenzimidazol-2-yl)methylamino]benzenecarboximidamide
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C16H17N5
  1
1
IC50 = 6309.57 nM
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CP0539517
 Compound Info 
2-ethoxy-4-[(5-phenyl-1H-imidazol-2-yl)methylamino]benzenecarboximidamide;formic acid
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C20H23N5O3
  1
1
IC50 = 6309.57 nM
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CP0483322
 Compound Info 
4-[[(1-hydroxy-3H-2,1-benzoxaborol-7-yl)amino]methyl]benzenecarboximidamide;hydrochloride
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C15H17BClN3O2
  1
1
IC50 = 7943.28 nM
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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 > 10000 nM
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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
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1
IC50 > 10000 nM
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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 > 10000 nM
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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 > 10000 nM
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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 > 10000 nM
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CP0470987
 Compound Info 
4-[(1-hydroxy-3,4-dihydro-2,1-benzoxaborinin-3-yl)methylamino]benzenecarboximidamide;hydrochloride
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C16H19BClN3O2
  1
1
IC50 > 10000 nM
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CP0477253
 Compound Info 
4-(1-hydroxy-3,4-dihydro-2,1-benzoxaborinin-3-yl)benzenecarboximidamide;hydrochloride
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C15H16BClN2O2
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1
IC50 = 10000 nM
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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 > 10000 nM
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CP0526031
 Compound Info 
4-[(1-hydroxy-3H-2,1-benzoxaborol-6-yl)methoxy]benzenecarboximidamide;hydrochloride
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C15H16BClN2O3
  1
1
IC50 = 10000 nM
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CP0528487
 Compound Info 
2-(1,3-oxazol-2-ylmethoxy)-4-[(5-phenyl-1H-imidazol-2-yl)methylamino]benzenecarboximidamide
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C21H20N6O2
  1
1
IC50 = 12589.25 nM
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CP0530147
 Compound Info 
N-(4-carbamimidoyl-3-fluorophenyl)-2-hydroxybenzamide;formic acid
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C15H14FN3O4
  1
1
IC50 = 12589.25 nM
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CP0903118
 Compound Info 
N-(4-carbamimidoylphenyl)-2-hydroxybenzamide formate
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C15H15N3O4
  1
1
IC50 = 12589.25 nM
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CP0530238
 Compound Info 
2-[2-carbamimidoyl-5-[(5-phenyl-1H-imidazol-2-yl)methylamino]phenoxy]-N-cyclopropylacetamide
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C22H24N6O2
  1
1
IC50 = 15848.93 nM
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CP0539518
 Compound Info 
4-[(5-phenyl-1H-imidazol-2-yl)methylamino]-2-(pyridin-2-ylmethoxy)benzenecarboximidamide;hydrochloride
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C23H23ClN6O
  1
1
IC50 = 19952.62 nM
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CP0417036
 Compound Info 
4-[(5-phenyl-1H-imidazol-2-yl)methylamino]benzenecarboximidamide
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C17H17N5
  1
1
IC50 = 25118.86 nM
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CP0543042
 Compound Info 
4-[(5-phenyl-1H-imidazol-2-yl)methylamino]-2-phenylmethoxybenzenecarboximidamide
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C24H23N5O
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1
IC50 = 25118.86 nM
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CP0536722
 Compound Info 
4-[(1-hydroxy-3H-2,1-benzoxaborol-6-yl)oxy]benzenecarboximidamide;hydrochloride
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C14H14BClN2O3
  1
1
IC50 = 25118.86 nM
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CP0530236
 Compound Info 
4-[(6-methoxy-1H-benzimidazol-2-yl)methylamino]benzenecarboximidamide
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C16H17N5O
  1
1
IC50 = 31622.78 nM
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CP0539519
 Compound Info 
2-[2-carbamimidoyl-5-[(5-phenyl-1H-imidazol-2-yl)methylamino]phenoxy]-N-methylacetamide;formic acid
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C21H24N6O4
  1
1
IC50 = 31622.78 nM
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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 = 31622.78 nM
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CP0384147
 Compound Info 
4-[(5-phenyl-1H-imidazol-2-yl)methylamino]-2-(pyrimidin-2-ylmethoxy)benzenecarboximidamide;hydrochloride
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C22H22ClN7O
  1
1
IC50 = 39810.72 nM
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CP0491838
 Compound Info 
4-(1H-benzimidazol-2-ylmethylamino)benzenecarboximidamide
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C15H15N5
  1
1
IC50 = 39810.72 nM
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CP0438054
 Compound Info 
4-[(1-hydroxy-3H-2,1-benzoxaborol-6-yl)oxymethyl]benzenecarboximidamide;hydrochloride
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C15H16BClN2O3
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1
IC50 = 39810.72 nM
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CP0491840
 Compound Info 
2-(2-cyclopropylethoxy)-4-[(5-phenyl-1H-imidazol-2-yl)methylamino]benzenecarboximidamide
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C22H25N5O
  1
1
IC50 = 50118.72 nM
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CP0559459
 Compound Info 
2-(cyclopropylmethoxy)-4-[(5-phenyl-1H-imidazol-2-yl)methylamino]benzenecarboximidamide;formic acid
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C22H25N5O3
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1
IC50 = 50118.72 nM
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CP0560119
 Compound Info 
2-[2-carbamimidoyl-5-[(5-phenyl-1H-imidazol-2-yl)methylamino]phenoxy]acetamide;formic acid
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C20H22N6O4
  1
1
IC50 > 50118.72 nM
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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
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1
IC50 = 63095.73 nM
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CP0559458
 Compound Info 
4-(1H-imidazol-2-ylmethylamino)benzenecarboximidamide;hydrochloride
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C11H14ClN5
  1
1
IC50 = 63095.73 nM
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CP0485771
 Compound Info 
4-(2-hydroxyoxaborinan-6-yl)benzenecarboximidamide;hydrochloride
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C11H16BClN2O2
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1
IC50 = 63095.73 nM
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CP0417037
 Compound Info 
2-[2-(dimethylamino)ethoxy]-4-[(5-phenyl-1H-imidazol-2-yl)methylamino]benzenecarboximidamide
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C21H26N6O
  1
1
IC50 = 79432.82 nM
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CP0491839
 Compound Info 
formic acid;2-(2-methylpropoxy)-4-[(5-phenyl-1H-imidazol-2-yl)methylamino]benzenecarboximidamide
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C22H27N5O3
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1
IC50 = 79432.82 nM
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CP0530237
 Compound Info 
2-(2-hydroxyethoxy)-4-[(5-phenyl-1H-imidazol-2-yl)methylamino]benzenecarboximidamide;hydrochloride
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C19H22ClN5O2
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1
IC50 = 79432.82 nM
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CP0526032
 Compound Info 
4-(1-hydroxy-3H-2,1-benzoxaborol-3-yl)benzenecarboximidamide;hydrochloride
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C14H14BClN2O2
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1
IC50 = 79432.82 nM
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CP0556536
 Compound Info 
2-[(2-chlorophenyl)methoxy]-4-[(5-phenyl-1H-imidazol-2-yl)methylamino]benzenecarboximidamide
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C24H22ClN5O
  1
1
IC50 > 2511.89 nM
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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 >= 3981.07 nM
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CP0536799
 Compound Info 
2-[(4-chlorophenyl)methoxy]-4-[(5-phenyl-1H-imidazol-2-yl)methylamino]benzenecarboximidamide
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C24H22ClN5O
  1
1
IC50 > 5011.87 nM
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CP0543040
 Compound Info 
2-[(3-chlorophenyl)methoxy]-4-[(5-phenyl-1H-imidazol-2-yl)methylamino]benzenecarboximidamide
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C24H22ClN5O
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1
IC50 > 5011.87 nM
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CP0528488
 Compound Info 
2-[2-carbamimidoyl-5-[(5-phenyl-1H-imidazol-2-yl)methylamino]phenoxy]-N-(cyclopropylmethyl)acetamide
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C23H26N6O2
  1
1
IC50 > 6309.57 nM
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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
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1
IC50 >= 6309.57 nM
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Clinical Information about the Protein
Target 1 ( Tissue kallikrein (KLK1) )
Target Type Literature-reported Target