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Kinetic parameters for mutation WT_human-ACHE
Substrate
Molecule
Km
Kcat
Exp. conditions
Reference
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
Molecule
Ki
Ksi
Ic50
Exp. conditions
Substrate
Reference
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
Send your questions or comments to :
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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