Literature summary for 3.4.21.73 extracted from

Joossens, J.; Van der Veken, P.; Surpateanu, G.; Lambeir, A.M.; El-Sayed, I.; Ali, O.M.; Augustyns, K.; Haemers, A.
Diphenyl phosphonate inhibitors for the urokinase-type plasminogen activator: optimization of the P4 position (2006), J. Med. Chem., 49, 5785-5793.

Search for more literature for 3.4.21.73

Inhibitors

Inhibitors	Comment	Organism	Structure
1-[(N-benzylsulfonyl-D-seryl)-L-alanyl]amino-2-(4-guanidinophenyl)ethanephosphonate trifluoroacetate	-	Mus musculus
di-(4-acetamidophenyl) 1-[(N-benzyloxycarbonyl-D-seryl)-Lalanyl]amino-2-[4-(guanidino)phenyl]-ethanephosphonate trifluoroacetate	-	Mus musculus
diphenyl 1-[(N-2-acetoadamantanyl-D-seryl)-L-alanyl]amino-2-(4-guanidinophenyl)ethanephosphonate trifluoroacetate	-	Mus musculus
diphenyl 1-[(N-2-acetothiophenyl-D-seryl)-L-alanyl]amino-2-(4-guanidinophenyl)ethanephosphonate trifluoroacetate	-	Mus musculus
diphenyl 1-[(N-benzenesulfonyl-D-seryl)-L-alanyl]amino-2-(4-guanidinophenyl)ethanephosphonate trifluoroacetate	-	Mus musculus
diphenyl 1-[(N-benzoyloxycarbonyl-D-seryl)-L-alanyl]amino-2-(4-guanidinophenyl)ethanephosphonate trifluoroacetate	-	Mus musculus
diphenyl 1-[(N-benzoylsulfonyl-D-seryl)-L-alanyl]amino-2-(4-guanidinophenyl)ethanephosphonate trifluoroacetate	-	Mus musculus
diphenyl 1-[(N-naphtalenesulfonyl-D-seryl)-L-alanyl]amino-2-(4-guanidinophenyl)ethanephosphonate trifluoroacetate	-	Mus musculus
diphenyl 1-[(N-o,o-dimethylbenzoyl-D-seryl)-L-alanyl]amino-2-(4-guanidinophenyl)ethanephosphonate trifluoroacetate	-	Mus musculus
diphenyl 1-[(N-o-methylbenzoyl-D-seryl)-L-alanyl]amino-2-(4-guanidinophenyl)ethanephosphonate trifluoroacetate	-	Mus musculus
diphenyl 1-[(N-p-bromobenzenesulfonyl-D-seryl)-L-alanyl]-amino-2-(4-guanidinophenyl)ethane-phosphonate trifluoroacetate	-	Mus musculus
diphenyl 1-[(N-p-cyanobenzenesulfonyl-D-seryl)-L-alanyl]-amino-2-(4-guanidinophenyl)ethane-phosphonate trifluoroacetate	-	Mus musculus
diphenyl 1-[(N-p-methoxybenzenesulfonyl-D-seryl)-L-alanyl]-amino-2-(4-guanidinophenyl)ethane-phosphonate trifluoroacetate	-	Mus musculus
diphenyl 1-[(N-p-methylbenzoyl-D-seryl)-L-alanyl]amino-2-(4-guanidinophenyl)ethanephosphonate trifluoroacetate	-	Mus musculus
diphenyl 1-[(N2-thiophenesulfonyl-D-seryl)-L-alanyl]amino-2-(4-guanidinophenyl)ethanephosphonate trifluoroacetate	-	Mus musculus
tripeptidyl diphenyl phosphonates	irreversible inhibition	Mus musculus

KM Value [mM]

KM Value [mM]	KM Value Maximum [mM]	Substrate	Comment	Organism	Structure
0.08	-	L-pyroGlu-Gly-L-Arg-p-NA	pH 8.8, 37°C	Mus musculus

Organism

Organism	UniProt	Comment	Textmining
Mus musculus	-	-	-

Source Tissue

Source Tissue	Comment	Organism	Textmining
commercial preparation	-	Mus musculus	-

Substrates and Products (Substrate)

Substrates	Comment Substrates	Organism	Products	Comment (Products)	Rev.	Reac.
L-pyroGlu-Gly-L-Arg-4-nitroanilide + H2O	chromogenic substrate S-2444	Mus musculus	L-pyroGlu-Gly-L-Arg + 4-nitroaniline	-	?

Synonyms

Synonyms	Comment	Organism
uPA	-	Mus musculus
Urokinase-type plasminogen activator	-	Mus musculus

Temperature Optimum [°C]

Temperature Optimum [°C]	Temperature Optimum Maximum [°C]	Comment	Organism
37	-	assay at	Mus musculus

pH Optimum

pH Optimum Minimum	pH Optimum Maximum	Comment	Organism
8.8	-	assay at	Mus musculus

IC50 Value

IC50 Value	IC50 Value Maximum	Comment	Organism	Inhibitor	Structure
0.0000015	-	pH 8.8, 37°C	Mus musculus	diphenyl 1-[(N2-thiophenesulfonyl-D-seryl)-L-alanyl]amino-2-(4-guanidinophenyl)ethanephosphonate trifluoroacetate
0.0000026	-	pH 8.8, 37°C	Mus musculus	diphenyl 1-[(N-benzenesulfonyl-D-seryl)-L-alanyl]amino-2-(4-guanidinophenyl)ethanephosphonate trifluoroacetate
0.0000035	-	pH 8.8, 37°C	Mus musculus	1-[(N-benzylsulfonyl-D-seryl)-L-alanyl]amino-2-(4-guanidinophenyl)ethanephosphonate trifluoroacetate
0.0000043	-	pH 8.8, 37°C	Mus musculus	diphenyl 1-[(N-benzoyloxycarbonyl-D-seryl)-L-alanyl]amino-2-(4-guanidinophenyl)ethanephosphonate trifluoroacetate
0.0000044	-	pH 8.8, 37°C	Mus musculus	diphenyl 1-[(N-o-methylbenzoyl-D-seryl)-L-alanyl]amino-2-(4-guanidinophenyl)ethanephosphonate trifluoroacetate
0.000005	-	pH 8.8, 37°C	Mus musculus	diphenyl 1-[(N-benzoylsulfonyl-D-seryl)-L-alanyl]amino-2-(4-guanidinophenyl)ethanephosphonate trifluoroacetate
0.0000058	-	pH 8.8, 37°C	Mus musculus	diphenyl 1-[(N-p-methoxybenzenesulfonyl-D-seryl)-L-alanyl]-amino-2-(4-guanidinophenyl)ethane-phosphonate trifluoroacetate
0.0000058	-	pH 8.8, 37°C	Mus musculus	diphenyl 1-[(N-naphthalenesulfonyl-D-seryl)-L-alanyl]amino-2-(4-guanidinophenyl)ethanephosphonate trifluoroacetate
0.000006	-	pH 8.8, 37°C	Mus musculus	diphenyl 1-[(N-o,o-dimethylbenzoyl-D-seryl)-L-alanyl]amino-2-(4-guanidinophenyl)ethanephosphonate trifluoroacetate
0.0000062	-	pH 8.8, 37°C	Mus musculus	diphenyl 1-[(N-p-cyanobenzenesulfonyl-D-seryl)-L-alanyl]-amino-2-(4-guanidinophenyl)ethane-phosphonate trifluoroacetate
0.0000066	-	pH 8.8, 37°C	Mus musculus	diphenyl 1-[(N-p-bromobenzenesulfonyl-D-seryl)-L-alanyl]-amino-2-(4-guanidinophenyl)ethane-phosphonate trifluoroacetate
0.0000067	-	pH 8.8, 37°C	Mus musculus	di-(4-acetamidophenyl) 1-[(N-benzyloxycarbonyl-D-seryl)-Lalanyl]amino-2-[4-(guanidino)phenyl]-ethanephosphonate trifluoroacetate
0.0000069	-	pH 8.8, 37°C	Mus musculus	diphenyl 1-[(N-2-acetothiophenyl-D-seryl)-L-alanyl]amino-2-(4-guanidinophenyl)ethanephosphonate trifluoroacetate
0.000007	-	pH 8.8, 37°C	Mus musculus	diphenyl 1-[(N-p-methylbenzoyl-D-seryl)-L-alanyl]amino-2-(4-guanidinophenyl)ethanephosphonate trifluoroacetate
0.000008	-	pH 8.8, 37°C	Mus musculus	diphenyl 1-[(N-2-acetoadamantanyl-D-seryl)-L-alanyl]amino-2-(4-guanidinophenyl)ethanephosphonate trifluoroacetate

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Release 2023.1 (January 2023)