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Literature summary for 3.4.21.37 extracted from

  • Macdonald, S.J.; Dowle, M.D.; Harrison, L.A.; Clarke, G.D.; Inglis, G.G.; Johnson, M.R.; Shah, P.; Smith, R.A.; Amour, A.; Fleetwood, G.; Humphreys, D.C.; Molloy, C.R.; Dixon, M.; Godward, R.E.; Wonacott, A.J.; Singh, O.M.; Hodgson, S.T.; Hardy, G.W.
    Discovery of further pyrrolidine trans-lactams as inhibitors of human neutrophil elastase (HNE) with potential as development candidates and the crystal structure of HNE complexed with an inhibitor (GW475151) (2002), J. Med. Chem., 45, 3878-3890.
    View publication on PubMed

Crystallization (Commentary)

Crystallization (Comment) Organism
hanging drop vapour diffusion method Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
GW311616
-
Homo sapiens
GW447631 i.e. (3S,3aS,6aR)-4-(5-cyclopropylaminomethyl-pyrazine-2-carbonyl)-3-isopropyl-1-methanesulfonyl-hexahydropyrrolo[3,2-b]pyrrol-2-one hydrochloride Homo sapiens
GW469002 i.e. (3S,3aS,6R)-4-[1-(2,2-dimethyl-propyl)azetidine-3-carbonyl]-3-isopropyl-1-methanesulfonyl-hexahydro-pyrrolo-[3,2-b]pyrrol-2-one Homo sapiens
GW475151 i.e. (3S,3aS,6aR)-3-isopropyl-1-methanesulfonyl-4-(2-pyrrolidin-1-ylmethyl-oxazole-4-carbonyl)hexahydro-pyrrolo-[3,2-b]pyrrol-2-one hydrochloride Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
methoxysuccinyl-Ala-Ala-Pro-Val-4-methylcoumarin 7-amide + H2O
-
Homo sapiens methoxysuccinyl-Ala-Ala-Pro-Val + 7-amino-4-methylcoumarin
-
?

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.000000014
-
GW447631 pH 7.4, 30°C Homo sapiens
0.00000016
-
GW475151 pH 7.4, 30°C Homo sapiens
0.00000031
-
GW311616 pH 7.4, 30°C Homo sapiens
0.00000173
-
GW469002 pH 7.4, 30°C Homo sapiens