Mutation

Kinetic parameters

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Kinetic parameters for mutation WT_human-ACHE

Substrate

MoleculeKmKcatExp. conditionsReference
3,3-dimethylbutylthioacetate 300 & 6 mM 55000 & 10000/min 50mM NaPhosphate pH8 Kronman_1994_J.Biol.Chem_269_27819
3,3-dimethylbutylthioacetate 450 uM 52000 /min IS 50mM phosphate pH8 T27C Ordentlich_1993_J.Biol.Chem_268_17083
3,3-dimethylbutylthioacetate 300 uM 55000/min 5 or 50mM Na Phosphate pH8 T27C Ordentlich_1995_J.Biol.Chem_270_2082
3,3-dimethylbutylthioacetate 260 & 30 uM 46000 & 7000/min IS 5mM Shafferman_1994_EMBO.J_13_3448
Acetylthiocholine 120 uM 420000/min 50mM Na phosphate pH8 Barak_1994_J.Biol.Chem_269_6296
Acetylthiocholine 140 uM 4.0 10+5 /min IS 50mM phosphate pH8 T27C Kaplan_2001_Biochemistry_40_7433
Acetylthiocholine 140 & 10 uM 400000 & 50000/min 50mM NaPhosphate pH8 Kronman_1994_J.Biol.Chem_269_27819
Acetylthiocholine 140 uM 370000/min IS 50mM phosphate pH8 T27C Ordentlich_1993_J.Biol.Chem_268_17083
Acetylthiocholine 140 uM 400000/min 5 or 50mM Na Phosphate pH8 T27C Ordentlich_1995_J.Biol.Chem_270_2082
Acetylthiocholine 140 & 50 uM 370000 & 10000/min pH8 T27C 50mM Na phosphate Shafferman_1992_EMBO.J_11_3561
Acetylthiocholine 80 & 10 uM 400000 & 60000/min IS 5mM Shafferman_1994_EMBO.J_13_3448
Acetylthiocholine 117 uM 390000 /min 50mM Na phosphate pH8.0 T27C Velan_1991_J.Biol.Chem_266_23977
Butyrylthiocholine 0.30 mM 0.08 10+5/min IS 50mM phosphate pH8 T27C Kaplan_2001_Biochemistry_40_7433
Butyrylthiocholine 2.5 mM 70000 /min 50mM NaPhosphate pH7.4 Loewenstein-Lichtenstein_1996_Mol.Pharmacol_50_1423
Paranitrophenylacetate 5600 uM 110000 /min IS 50mM phosphate pH8 T27C Ordentlich_1993_J.Biol.Chem_268_17083
S-N-Propylthioacetate 11000 uM 11000 /min IS 50mM phosphate pH8 T27C Ordentlich_1993_J.Biol.Chem_268_17083

Inhibitor

MoleculeKiKsiIc50Exp. conditionsSubstrateReference
BW284C51 10 nM - - 50mM Na phosphate pH8 Acetylthiocholine Barak_1994_J.Biol.Chem_269_6296
BW284C51 170000 nM - - T25C IS 50 mM phosphate Acetylthiocholine Kaplan_2001_Biochemistry_40_7433
BW284C51 0.13 uM - - 50mM NaPhosphate pH7.4 Butyrylthiocholine Loewenstein-Lichtenstein_1996_Mol.Pharmacol_50_1423
BW284C51 - - 50 nM pH8 T27C 50mM Na phosphate Acetylthiocholine Shafferman_1992_EMBO.J_11_3561
Bambuterol - - 41000 & 5000 nM 50mM KP pH8 T37C Acetylthiocholine Tunek_1988_Drug.Metab.Dispos_16_759
Cocaine 3900 uM - - 50mM NaPhosphate pH7.4 Acetylthiocholine Loewenstein-Lichtenstein_1996_Mol.Pharmacol_50_1423
Decamethonium 6 uM - - 50mM Na phosphate pH8 Acetylthiocholine Barak_1994_J.Biol.Chem_269_6296
Decamethonium 360 uM - - T25C IS 50 mM phosphate Acetylthiocholine Kaplan_2001_Biochemistry_40_7433
Decamethonium 6.0 uM 5.7 uM - 5 or 50mM Na Phosphate pH8 T27C Acetylthiocholine Ordentlich_1995_J.Biol.Chem_270_2082
Decamethonium - - 8.5 uM pH8 T27C 50mM Na phosphate Acetylthiocholine Shafferman_1992_EMBO.J_11_3561
Dibucaine 710 uM - - 50mM NaPhosphate pH7.4 Acetylthiocholine Loewenstein-Lichtenstein_1996_Mol.Pharmacol_50_1423
Edrophonium 0.6 & 0.1 uM - - 50mM NaPhosphate pH8 3.3-dimethylbutylthioacetate Kronman_1994_J.Biol.Chem_269_27819
Edrophonium 0.75 uM - - 50mM Na phosphate pH8 Acetylthiocholine Barak_1994_J.Biol.Chem_269_6296
Edrophonium 50 uM - - T25C IS 50 mM phosphate Acetylthiocholine Kaplan_2001_Biochemistry_40_7433
Edrophonium 0.7 & 0.1 uM - - 50mM NaPhosphate pH8 Acetylthiocholine Kronman_1994_J.Biol.Chem_269_27819
Edrophonium 0.3 uM - - IS 50mM phosphate pH8 T27C Acetylthiocholine Ordentlich_1993_J.Biol.Chem_268_17083
Edrophonium 0.6 uM 4.8 uM - 5 or 50mM Na Phosphate pH8 T27C Acetylthiocholine Ordentlich_1995_J.Biol.Chem_270_2082
Edrophonium - - 1.5 uM pH8 T27C 50mM Na phosphate Acetylthiocholine Shafferman_1992_EMBO.J_11_3561
Edrophonium 0.32 & 0.05 uM - - IS 5mM Acetylthiocholine Shafferman_1994_EMBO.J_13_3448
Edrophonium 0.4 uM - - IS 50mM phosphate pH8 T27C Paranitrophenylacetate Ordentlich_1993_J.Biol.Chem_268_17083
Edrophonium 0.24 uM - - IS 50mM phosphate pH8 T27C S-N-Propylthioacetate Ordentlich_1993_J.Biol.Chem_268_17083
Hexamethonium 0.2 mM - - 50mM Na phosphate pH8 Acetylthiocholine Barak_1994_J.Biol.Chem_269_6296
HuperzineA 16 & 1 nM 12 & 4 nM - 50mM Na phosphate pH8 T22C Acetylthiocholine Ariel_1998_Biochem.J_335_95
HuperzineA 16 nM - - T25C IS 50 mM phosphate Acetylthiocholine Kaplan_2001_Biochemistry_40_7433
HuperzineA 400000 nM - - T25C IS 50 mM phosphate Acetylthiocholine Kaplan_2001_Biochemistry_40_7433
Propidium 1.4 uM - - 50mM Na phosphate pH8 Acetylthiocholine Barak_1994_J.Biol.Chem_269_6296
Propidium 0.6 uM 0.9 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
Succinylcholine~Suxamethonium 1000 uM - - 50mM NaPhosphate pH7.4 Acetylthiocholine Loewenstein-Lichtenstein_1996_Mol.Pharmacol_50_1423
Tacrine 85 & 12 nM 90 & 20 nM - 50mM Na phosphate pH8 T22C Acetylthiocholine Ariel_1998_Biochem.J_335_95
Tacrine 12 nM - - T25C IS 50 mM phosphate Acetylthiocholine Kaplan_2001_Biochemistry_40_7433
Tacrine 0.21 uM - - 50mM NaPhosphate pH7.4 Acetylthiocholine Loewenstein-Lichtenstein_1996_Mol.Pharmacol_50_1423

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Please cite: Lenfant 2013 Nucleic.Acids.Res. or Marchot Chatonnet 2012 Prot.Pept Lett.
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