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Literature summary for 3.4.21.77 extracted from

  • Koistinen, H.; Wohlfahrt, G.; Mattsson, J.M.; Wu, P.; Lahdenperae, J.; Stenman, U.H.
    Novel small molecule inhibitors for prostate-specific antigen (2008), Prostate, 68, 1143-1151.
    View publication on PubMed

Activating Compound

Activating Compound Comment Organism Structure
B2-peptide
-
Homo sapiens

Application

Application Comment Organism
drug development compounds inhibiting the activity of prostate-specific antigen, prevent the anti-angiogenic effect of prostate-specific antigen in an angiogenesis model Homo sapiens

Cloned(Commentary)

Cloned (Comment) Organism
expressed in HUVEC cells Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
(2-methoxyphenyl)(3-phenyl-1H-1,2,4-triazol-1-yl)methanone
-
Homo sapiens
(3,4-dimethoxyphenyl)(5-(4-fluorobenzylamino)-3-phenyl-1H-1,2,4-triazol-1-yl)methanone
-
Homo sapiens
(5-amino-3-(pyridin-3-yl)-1H-1,2,4-triazol-1-yl)(2-chlorophenyl)methanone
-
Homo sapiens
(5-amino-3-(pyridin-3-yl)-1H-1,2,4-triazol-1-yl)(2-methoxyphenyl)methanone
-
Homo sapiens
(5-amino-3-(pyridin-3-yl)-1H-1,2,4-triazol-1-yl)(3,4-dimethoxyphenyl)methanone 360 nanomol inhibits by 83% Homo sapiens
(5-amino-3-(pyridin-3-yl)-1H-1,2,4-triazol-1-yl)(4-chlorophenyl)methanone
-
Homo sapiens
(5-amino-3-(pyridin-3-yl)-1H-1,2,4-triazol-1-yl)(4-fluorophenyl)methanone
-
Homo sapiens
(5-amino-3-(pyridin-3-yl)-1H-1,2,4-triazol-1-yl)(4-methoxyphenyl)methanone 360 nanomol inhibits by 56% Homo sapiens
(5-amino-3-(pyridin-3-yl)-1H-1,2,4-triazol-1-yl)(4-nitrophenyl)methanone
-
Homo sapiens
(5-amino-3-(pyridin-3-yl)-1H-1,2,4-triazol-1-yl)(p-tolyl)methanone
-
Homo sapiens
(5-amino-3-(pyridin-3-yl)-1H-1,2,4-triazol-1-yl)(phenyl)methanone
-
Homo sapiens
(5-amino-3-phenyl-1H-1,2,4-triazol-1-yl)(3,4-dimethoxyphenyl)methanone
-
Homo sapiens
1-(3-chlorobenzyl)-3-phenyl-1H-pyrazol-5-amine
-
Homo sapiens
1-benzyl-3-phenyl-1H-pyrazol-5-amine
-
Homo sapiens
2-(2-methyl-3-nitrophenyl)-4-oxo-4H-3,1-benzoxazin-6-yl acetate
-
Homo sapiens
2-(2-methyl-3-nitrophenyl)-4H-3,1-benzoxazin-4-one 360 nanomol inhibits by 61% Homo sapiens
2-(2-methylphenyl)-4H-3,1-benzoxazin-4-one
-
Homo sapiens
2-(2-nitrophenyl)-4H-3,1-benzoxazin-4-one
-
Homo sapiens
2-(3-methylphenyl)-4H-3,1-benzoxazin-4-one
-
Homo sapiens
2-(3-nitrophenyl)-4H-3,1-benzoxazin-4-one
-
Homo sapiens
2-(4-bromophenyl)quinazolin-4(3H)-one
-
Homo sapiens
2-(4-methylphenyl)-4H-3,1-benzoxazin-4-one
-
Homo sapiens
2-phenyl-4H-3,1-benzoxazin-4-one
-
Homo sapiens
2-phenylquinazolin-4(3H)-one
-
Homo sapiens
4-(4-oxo-4H-benzo[d][1,3]oxazin-2-yl)phenyl acetate
-
Homo sapiens
6-bromo-2-(2-methyl-3-nitrophenyl)-4H-3,1-benzoxazin-4-one
-
Homo sapiens

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
1.4
-
4-morpholinecarbonyl-HSSKLQ-AMC prostate-specific antigen without inhibitor Homo sapiens
1.5
-
4-morpholinecarbonyl-HSSKLQ-AMC prostate-specific antigen and inhibitor 2-(2-methyl-3-nitrophenyl)-4H-3,1-benzoxazin-4-one (25 micromol) Homo sapiens
1.6
-
4-morpholinecarbonyl-HSSKLQ-AMC prostate-specific antigen and inhibitor 2-(2-methyl-3-nitrophenyl)-4H-3,1-benzoxazin-4-one (5 micromol) Homo sapiens
2.6
-
4-morpholinecarbonyl-HSSKLQ-AMC prostate-specific antigen and inhibitor (5-amino-3-(pyridin-3-yl)-1H-1,2,4-triazol-1-yl)(4-methoxyphenyl)methanone (5 micromol) Homo sapiens
4.2
-
4-morpholinecarbonyl-HSSKLQ-AMC prostate-specific antigen and inhibitor (5-amino-3-(pyridin-3-yl)-1H-1,2,4-triazol-1-yl)(3,4-dimethoxyphenyl)methanone (5 micromol) Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Purification (Commentary)

Purification (Comment) Organism
from seminal plasma Homo sapiens

Source Tissue

Source Tissue Comment Organism Textmining
seminal plasma
-
Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
4-morpholinecarbonyl-HSSKLQ-AMC + H2O
-
Homo sapiens ?
-
?
additional information proteolytic activity of prostate-specific antigen is essential for inhibition of angiogenesis Homo sapiens ?
-
?

Synonyms

Synonyms Comment Organism
KLK3
-
Homo sapiens
prostate-specific antigen
-
Homo sapiens
PSA
-
Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0003
-
-
Homo sapiens 2-(2-methyl-3-nitrophenyl)-4H-3,1-benzoxazin-4-one
0.0005
-
-
Homo sapiens (5-amino-3-(pyridin-3-yl)-1H-1,2,4-triazol-1-yl)(3,4-dimethoxyphenyl)methanone
0.0009
-
-
Homo sapiens (5-amino-3-(pyridin-3-yl)-1H-1,2,4-triazol-1-yl)(4-methoxyphenyl)methanone
0.0022
-
-
Homo sapiens (5-amino-3-(pyridin-3-yl)-1H-1,2,4-triazol-1-yl)(4-chlorophenyl)methanone
0.0038
-
-
Homo sapiens (5-amino-3-(pyridin-3-yl)-1H-1,2,4-triazol-1-yl)(p-tolyl)methanone
0.0041
-
-
Homo sapiens (5-amino-3-(pyridin-3-yl)-1H-1,2,4-triazol-1-yl)(4-fluorophenyl)methanone
0.0054
-
-
Homo sapiens 2-(2-methyl-3-nitrophenyl)-4-oxo-4H-3,1-benzoxazin-6-yl acetate
0.0096
-
-
Homo sapiens (5-amino-3-(pyridin-3-yl)-1H-1,2,4-triazol-1-yl)(phenyl)methanone
0.0142
-
-
Homo sapiens 2-(2-nitrophenyl)-4H-3,1-benzoxazin-4-one
0.0163
-
-
Homo sapiens (5-amino-3-(pyridin-3-yl)-1H-1,2,4-triazol-1-yl)(2-chlorophenyl)methanone
0.0169
-
-
Homo sapiens (5-amino-3-phenyl-1H-1,2,4-triazol-1-yl)(3,4-dimethoxyphenyl)methanone
0.0291
-
-
Homo sapiens 2-(2-methylphenyl)-4H-3,1-benzoxazin-4-one
0.0298
-
-
Homo sapiens (5-amino-3-(pyridin-3-yl)-1H-1,2,4-triazol-1-yl)(2-methoxyphenyl)methanone
0.049
-
-
Homo sapiens 6-bromo-2-(2-methyl-3-nitrophenyl)-4H-3,1-benzoxazin-4-one
0.08
-
-
Homo sapiens (2-methoxyphenyl)(3-phenyl-1H-1,2,4-triazol-1-yl)methanone
0.08
-
-
Homo sapiens (3,4-dimethoxyphenyl)(5-(4-fluorobenzylamino)-3-phenyl-1H-1,2,4-triazol-1-yl)methanone
0.08
-
-
Homo sapiens (5-amino-3-(pyridin-3-yl)-1H-1,2,4-triazol-1-yl)(4-nitrophenyl)methanone
0.08
-
-
Homo sapiens 1-(3-chlorobenzyl)-3-phenyl-1H-pyrazol-5-amine
0.08
-
-
Homo sapiens 1-benzyl-3-phenyl-1H-pyrazol-5-amine
0.08
-
-
Homo sapiens 2-(3-methylphenyl)-4H-3,1-benzoxazin-4-one
0.08
-
-
Homo sapiens 2-(3-nitrophenyl)-4H-3,1-benzoxazin-4-one
0.08
-
-
Homo sapiens 2-(4-bromophenyl)quinazolin-4(3H)-one
0.08
-
-
Homo sapiens 2-(4-methylphenyl)-4H-3,1-benzoxazin-4-one
0.08
-
-
Homo sapiens 2-phenyl-4H-3,1-benzoxazin-4-one
0.08
-
-
Homo sapiens 2-phenylquinazolin-4(3H)-one
0.08
-
-
Homo sapiens 4-(4-oxo-4H-benzo[d][1,3]oxazin-2-yl)phenyl acetate