Literature summary for 3.4.21.20 extracted from

Greco, M.N.; Hawkins, M.J.; Powell, E.T.; Almond, H.R., Jr.; Corcoran, T.W.; de Garavilla, L.; Kauffman, J.A.; Recacha, R.; Chattopadhyay, D.; Andrade-Gordon, P.; Maryanoff, B.E.
Nonpeptide inhibitors of cathepsin G: optimization of a novel beta-ketophosphonic acid lead by structure-based drug design (2002), J. Am. Chem. Soc., 124, 3810-3811.

Search for more literature for 3.4.21.20

Application

Application	Comment	Organism
pharmacology	structure-based drug design	Homo sapiens

Inhibitors

Inhibitors	Comment	Organism	Structure
bis-naphthyl beta-ketophosphoric acid	moderately potent, competitive, reversible, the R-isomer occupies the active site of the enzyme	Homo sapiens
diethyl 1-naphthylmethylphosphonate	-	Homo sapiens
additional information	structural features of inhibition, high-throughput screening of a diverse chemical library, lead structure is bis-naphthyl beta-ketophosphoric acid	Homo sapiens
[2-(3-methylcarbamoyl-naphthalen-2-yl)-1-naphthalen-1-yl-2-oxo-ethyl]-phosphonic acid	-	Homo sapiens
[2-(3-[(3-benzoylamino-propyl)-methyl-carbamoyl]-naphthalen-2-yl)-1-naphthalen-1-yl-2-oxo-ethyl]-phosphonic acid	-	Homo sapiens
[2-(3-[(piperidin-4-yl)-methyl-carbamoyl]-naphthalen-2-yl)-1-naphthalen-1-yl-2-oxo-ethyl]-phosphonic acid	reversible, selective, competitive inhibition	Homo sapiens
[2-(3-[methyl-(diphenyl-ethylcarbamoyl-methyl)-carbamoyl]-naphthalen-2-yl)-1-naphthalen-1-yl-2-oxo-ethyl]-phosphonic acid	strong inhibition	Homo sapiens
[2-(3-[methyl-(phenethylcarbamoyl-methyl)-carbamoyl]-naphthalen-2-yl)-1-naphthalen-1-yl-2-oxo-ethyl]-phosphonic acid	-	Homo sapiens
[2-[3-(benzyl-methyl-carbamoyl)-naphthalen-2-yl]-1-naphthalen-1-yl-2-oxo-ethyl]-phosphonic acid	-	Homo sapiens

Localization

Localization	Comment	Organism	GeneOntology No.	Textmining
extracellular	enzyme is released on degranulation of neutrophils	Homo sapiens	-	-

Natural Substrates/ Products (Substrates)

Natural Substrates	Organism	Comment (Nat. Sub.)	Natural Products	Comment (Nat. Pro.)	Rev.	Reac.
additional information	Homo sapiens	enzyme is involved in pathological processes of inflammation	?	-	?

Organism

Organism	UniProt	Comment	Textmining
Homo sapiens	-	-	-

Reaction

Reaction	Comment	Organism	Reaction ID
specificity similar to chymotrypsin C	active site structure	Homo sapiens	a

Source Tissue

Source Tissue	Comment	Organism	Textmining
neutrophil	polymorphonuclear leukocyte, in azurophilic granules	Homo sapiens	-

Substrates and Products (Substrate)

Substrates	Comment Substrates	Organism	Products	Comment (Products)	Rev.	Reac.
additional information	enzyme is involved in pathological processes of inflammation	Homo sapiens	?	-	?

Synonyms

Synonyms	Comment	Organism
CatG	-	Homo sapiens

Ki Value [mM]

Ki Value [mM]	Ki Value maximum [mM]	Inhibitor	Comment	Organism	Structure
additional information	-	additional information	-	Homo sapiens
0.00005	0.00006	[2-(3-[(piperidin-4-yl)-methyl-carbamoyl]-naphthalen-2-yl)1-naphthalen-1-yl-2-oxo-ethyl]-phosphonic acid	-	Homo sapiens

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Release 2023.1 (January 2023)