Mutation

Kinetic parameters

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Kinetic parameters for mutation Y337A_human-ACHE

Substrate

MoleculeKmKcatExp. conditionsReference
3,3-dimethylbutylthioacetate 500 uM 83000 /min IS 50mM phosphate pH8 T27C Ordentlich_1993_J.Biol.Chem_268_17083
3,3-dimethylbutylthioacetate 200 uM 20000/min 5 or 50mM Na Phosphate pH8 T27C Ordentlich_1995_J.Biol.Chem_270_2082
Acetylthiocholine 100 uM 100000/min 50mM Na phosphate pH8 Barak_1994_J.Biol.Chem_269_6296
Acetylthiocholine 90 uM 1.4 10+5/min IS 50mM phosphate pH8 T27C Kaplan_2001_Biochemistry_40_7433
Acetylthiocholine 140 uM 100000 /min IS 50mM phosphate pH8 T27C Ordentlich_1993_J.Biol.Chem_268_17083
Acetylthiocholine 100 uM 100000/min 5 or 50mM Na Phosphate pH8 T27C Ordentlich_1995_J.Biol.Chem_270_2082
Acetylthiocholine 140 & 30 uM 100000 & 10000/min pH8 T27C 50mM Na phosphate Shafferman_1992_EMBO.J_11_3561
Butyrylthiocholine 0.24 mM 0.03 10+5/min IS 50mM phosphate pH8 T27C Kaplan_2001_Biochemistry_40_7433
Paranitrophenylacetate 5400 uM 96000 /min IS 50mM phosphate pH8 T27C Ordentlich_1993_J.Biol.Chem_268_17083
S-N-Propylthioacetate 10000 uM 15000 /min IS 50mM phosphate pH8 T27C Ordentlich_1993_J.Biol.Chem_268_17083

Inhibitor

MoleculeKiKsiIc50Exp. conditionsSubstrateReference
BW284C51 51 nM - - 50mM Na phosphate pH8 Acetylthiocholine Barak_1994_J.Biol.Chem_269_6296
BW284C51 - - 650 nM pH8 T27C 50mM Na phosphate Acetylthiocholine Shafferman_1992_EMBO.J_11_3561
Decamethonium 0.9 uM - - 50mM Na phosphate pH8 Acetylthiocholine Barak_1994_J.Biol.Chem_269_6296
Decamethonium 0.9 uM 3.9 uM - 5 or 50mM Na Phosphate pH8 T27C Acetylthiocholine Ordentlich_1995_J.Biol.Chem_270_2082
Decamethonium - - 6.8 uM pH8 T27C 50mM Na phosphate Acetylthiocholine Shafferman_1992_EMBO.J_11_3561
Edrophonium 17.1 uM - - 3-dimethylbutylthioacetate 3 IS 50mM phosphate pH8 T27C
Edrophonium 5.7 uM - - 50mM Na phosphate pH8 Acetylthiocholine Barak_1994_J.Biol.Chem_269_6296
Edrophonium 11.2 uM - - IS 50mM phosphate pH8 T27C Acetylthiocholine Ordentlich_1993_J.Biol.Chem_268_17083
Edrophonium 5.7 uM 21 uM - 5 or 50mM Na Phosphate pH8 T27C Acetylthiocholine Ordentlich_1995_J.Biol.Chem_270_2082
Edrophonium - - 22.5 uM pH8 T27C 50mM Na phosphate Acetylthiocholine Shafferman_1992_EMBO.J_11_3561
Edrophonium 4.2 uM - - IS 50mM phosphate pH8 T27C Paranitrophenylacetate Ordentlich_1993_J.Biol.Chem_268_17083
Edrophonium 3 uM - - IS 50mM phosphate pH8 T27C S-N-Propylthioacetate Ordentlich_1993_J.Biol.Chem_268_17083
Hexamethonium 0.08 mM - - 50mM Na phosphate pH8 Acetylthiocholine Barak_1994_J.Biol.Chem_269_6296
HuperzineA 4900 nM - - 50mM Na phosphate pH8 T22C Acetylthiocholine Ariel_1998_Biochem.J_335_95
Propidium 0.9 uM - - 50mM Na phosphate pH8 Acetylthiocholine Barak_1994_J.Biol.Chem_269_6296
Propidium 0.9 uM 3.7 uM - 5 or 50mM Na Phosphate pH8 T27C Acetylthiocholine Ordentlich_1995_J.Biol.Chem_270_2082
Propidium - - 1.5 uM pH8 T27C 50mM Na phosphate Acetylthiocholine Shafferman_1992_EMBO.J_11_3561
Tacrine 8 & 2 nM 8 & 2 nM - 50mM Na phosphate pH8 T22C Acetylthiocholine Ariel_1998_Biochem.J_335_95

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Mail to: Nicolas Lenfant, Thierry Hotelier, Yves Bourne, Pascale Marchot and Arnaud Chatonnet.
Please cite: Lenfant 2013 Nucleic.Acids.Res. or Marchot Chatonnet 2012 Prot.Pept Lett.
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