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Torpedo_number
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Kinetic parameters for torpedo number 70,121
Substrates:
Acetylthiocholine
,
Butyrylthiocholine
Inhibitors:
BW284C51
,
Decamethonium
,
Edrophonium
,
Hexamethonium
,
HuperzineA
,
Propidium
,
Tacrine
,
WT-fasciculin2
Substrates
Substrate
:
Acetylthiocholine
Gene_Locus
Enzyme
Km
Kcat
Exp. conditions
Reference
human-ACHE
Y72A/Y124A
70 uM
250000/min
50mM Na phosphate pH8
Barak_1994_J.Biol.Chem_269_6296
human-ACHE
Y72N/Y124Q
140 mM
4.1 10+5/min
IS 50mM phosphate pH8 T27C
Kaplan_2001_Biochemistry_40_7433
mouse-ACHE
Y72N/Y124Q
95 & 11 uM
94000 & 20000/min
100mM NaP pH7 T22C eq3 sch3
Radic_1993_Biochemistry_32_12074
bunfa-ACHE
WT
78.8 & 6.3 uM
-
T25C IS 50 mM phosphate
Cousin_1996_J.Biol.Chem_271_15099
chick-ACHE
WT
-
175000/min
100mM NaP T28C pH7.0
Vigny_1978_Eur.J.Biochem_85_317
eleel-ACHE
WT
130 uM
900000 /min
Salih_1992_Biochem.J_285_451
eleel-ACHE
WT
-
733333/min
100mM NaP T28C pH7.0
Vigny_1978_Eur.J.Biochem_85_317
human-ACHE
WT
120 uM
420000/min
50mM Na phosphate pH8
Barak_1994_J.Biol.Chem_269_6296
human-ACHE
WT
140 uM
4.0 10+5 /min
IS 50mM phosphate pH8 T27C
Kaplan_2001_Biochemistry_40_7433
human-ACHE
WT
140 & 10 uM
400000 & 50000/min
50mM NaPhosphate pH8
Kronman_1994_J.Biol.Chem_269_27819
human-ACHE
WT
140 uM
370000/min
IS 50mM phosphate pH8 T27C
Ordentlich_1993_J.Biol.Chem_268_17083
human-ACHE
WT
140 uM
400000/min
5 or 50mM Na Phosphate pH8 T27C
Ordentlich_1995_J.Biol.Chem_270_2082
human-ACHE
WT
140 & 50 uM
370000 & 10000/min
pH8 T27C 50mM Na phosphate
Shafferman_1992_EMBO.J_11_3561
human-ACHE
WT
80 & 10 uM
400000 & 60000/min
IS 5mM
Shafferman_1994_EMBO.J_13_3448
human-ACHE
WT
117 uM
390000 /min
50mM Na phosphate pH8.0 T27C
Velan_1991_J.Biol.Chem_266_23977
human-BCHE
WT
40 uM
0.5 10+5 /min
IS 50mM phosphate pH8 T27C
Kaplan_2001_Biochemistry_40_7433
mouse-ACHE
WT
46 uM
140000 /min
100mM NaPhosphate Ph7.0 T22C
Hosea_1995_Biochemistry_34_11528
mouse-ACHE
WT
46 & 3 uM
140000 & 10000/min
100mM NaP pH7 T22C eq3 sch3
Radic_1993_Biochemistry_32_12074
mouse-BCHE
WT
23 uM
40000 /min
100mM NaPhosphate Ph7.0 T22C
Hosea_1995_Biochemistry_34_11528
mouse-BCHE
WT
35 & 2 uM
40000 & 7000/min
100mM NaP pH7 T22C eq3 sch3
Radic_1993_Biochemistry_32_12074
ratno-ACHE
WT
-
220000/min
100mM NaP T28C pH7.0
Vigny_1978_Eur.J.Biochem_85_317
torca-ACHE
WT
-
481666/min
T25C pH7.8
Taylor_1974_Mol.Pharmacol_10_78
torma-ACHE
WT
81.2 & 4.2 uM
-
T25C IS 50 mM phosphate
Cousin_1996_J.Biol.Chem_271_15099
torma-ACHE
WT
-
273333/min
100mM NaP T28C pH7.0
Vigny_1978_Eur.J.Biochem_85_317
human-ACHE
WT
0.30 mM
-
IS 50mM phosphate pH8 T27C
Kaplan_2001_Biochemistry_40_7433
human-ACHE
WT
2.5 mM
-
50mM NaPhosphate pH7.4
Loewenstein-Lichtenstein_1996_Mol.Pharmacol_50_1423
Substrate
:
Butyrylthiocholine
Gene_Locus
Enzyme
Km
Kcat
Exp. conditions
Reference
human-ACHE
Y72N/Y124Q
0.25 mM
0.20 10+5/min
IS 50mM phosphate pH8 T27C
Kaplan_2001_Biochemistry_40_7433
human-ACHE
WT
0.30 mM
0.08 10+5/min
IS 50mM phosphate pH8 T27C
Kaplan_2001_Biochemistry_40_7433
human-ACHE
WT
2.5 mM
70000 /min
50mM NaPhosphate pH7.4
Loewenstein-Lichtenstein_1996_Mol.Pharmacol_50_1423
human-BCHE
WT
7 & 0.7 uM
24000 & 10000 /min
100mM K phosphate pH7.0 T25C
Blong_1997_Biochem.J_327_747
human-BCHE
WT
2.2 mM
-
100mM Na phosphate pH7.4 T22C
Gnatt_1994_J.Neurochem_62_749
human-BCHE
WT
0.05 mM
1.1 10+5 /min
IS 50mM phosphate pH8 T27C
Kaplan_2001_Biochemistry_40_7433
human-BCHE
WT
2.8 & 0.7 mM
98000 & 33000 /min
50mM NaPhosphate pH7.4
Loewenstein-Lichtenstein_1996_Mol.Pharmacol_50_1423
mouse-ACHE
WT
93 uM
1100 /min
100mM NaPhosphate Ph7.0 T22C
Hosea_1995_Biochemistry_34_11528
mouse-BCHE
WT
55 uM
37000 /min
100mM NaPhosphate Ph7.0 T22C
Hosea_1995_Biochemistry_34_11528
Inhibitors
Inhibitor
:
BW284C51
Gene_Locus
Enzyme
Ki
Ksi
Ic50
Substrate
Exp. conditions
Reference
human-ACHE
Y72A/Y124A
355 nM
-
-
Acetylthiocholine
50mM Na phosphate pH8
Barak_1994_J.Biol.Chem_269_6296
mouse-ACHE
Y72N/Y124Q
190 & 80 nM
460 & 130 nM
-
Acetylthiocholine
100mM NaP pH7.0 T22C eq3.gif sch3.gif
Radic_1993_Biochemistry_32_12074
bunfa-ACHE
WT
16.9 & 1.6 nM
28.9 & 0.8 nM
-
Acetylthiocholine
T25C IS 50 mM phosphate
Cousin_1996_J.Biol.Chem_271_15099
chick-ACHE
WT
240 nM
-
-
Acetylthiocholine
100mM NaCl 50mM Tris pH7.4
Eichler_1994_Mol.Pharmacol_45_335
human-ACHE
WT
10 nM
-
-
Acetylthiocholine
50mM Na phosphate pH8
Barak_1994_J.Biol.Chem_269_6296
human-ACHE
WT
170000 nM
-
-
Acetylthiocholine
T25C IS 50 mM phosphate
Kaplan_2001_Biochemistry_40_7433
human-ACHE
WT
0.13 uM
-
-
Butyrylthiocholine
50mM NaPhosphate pH7.4
Loewenstein-Lichtenstein_1996_Mol.Pharmacol_50_1423
human-ACHE
WT
-
-
50 nM
Acetylthiocholine
pH8 T27C 50mM Na phosphate
Shafferman_1992_EMBO.J_11_3561
human-BCHE
WT
14000 nM
-
-
Acetylthiocholine
T25C IS 50 mM phosphate
Kaplan_2001_Biochemistry_40_7433
mouse-ACHE
WT
2.8 & 1.0 nM
4.8 & 1.8 nM
-
Acetylthiocholine
100mM NaP pH7.0 T22C eq3.gif sch3.gif
Radic_1993_Biochemistry_32_12074
mouse-BCHE
WT
11300 & 400 nM
42000000 & 5000000 nM
-
Acetylthiocholine
100mM NaP pH7.0 T22C eq3.gif sch3.gif
Radic_1993_Biochemistry_32_12074
torma-ACHE
WT
15.1 & 0.7 nM
63.6 & 8.4 nM
-
Acetylthiocholine
T25C IS 50 mM phosphate
Cousin_1996_J.Biol.Chem_271_15099
torma-ACHE
WT
2 nM
-
-
Acetylthiocholine
100mM NaCl 50mM Tris pH7.4
Eichler_1994_Mol.Pharmacol_45_335
human-BCHE
WT
480 & 110 uM
-
-
Butyrylthiocholine
50mM NaPhosphate pH7.4
Loewenstein-Lichtenstein_1996_Mol.Pharmacol_50_1423
Inhibitor
:
Decamethonium
Gene_Locus
Enzyme
Ki
Ksi
Ic50
Substrate
Exp. conditions
Reference
human-ACHE
Y72A/Y124A
22 uM
-
-
Acetylthiocholine
50mM Na phosphate pH8
Barak_1994_J.Biol.Chem_269_6296
human-ACHE
Y72N/Y124Q
200 uM
-
-
Acetylthiocholine
T25C IS 50 mM phosphate
Kaplan_2001_Biochemistry_40_7433
mouse-ACHE
Y72N/Y124Q
130 & 14 uM
510 & 180 uM
-
Acetylthiocholine
100mM NaP pH7.0 T22C eq3.gif sch3.gif
Radic_1993_Biochemistry_32_12074
bunfa-ACHE
WT
8.2 & 1.2 uM
47.5 & 3.5 uM
-
Acetylthiocholine
T25C IS 50 mM phosphate
Cousin_1996_J.Biol.Chem_271_15099
chick-ACHE
WT
23.6 uM
-
-
Acetylthiocholine
100mM NaCl 50mM Tris pH7.4
Eichler_1994_Mol.Pharmacol_45_335
human-ACHE
WT
6 uM
-
-
Acetylthiocholine
50mM Na phosphate pH8
Barak_1994_J.Biol.Chem_269_6296
human-ACHE
WT
360 uM
-
-
Acetylthiocholine
T25C IS 50 mM phosphate
Kaplan_2001_Biochemistry_40_7433
human-ACHE
WT
6.0 uM
5.7 uM
-
Acetylthiocholine
5 or 50mM Na Phosphate pH8 T27C
Ordentlich_1995_J.Biol.Chem_270_2082
human-ACHE
WT
-
-
8.5 uM
Acetylthiocholine
pH8 T27C 50mM Na phosphate
Shafferman_1992_EMBO.J_11_3561
human-BCHE
WT
2.5 uM
-
-
Acetylthiocholine
T25C IS 50 mM phosphate
Kaplan_2001_Biochemistry_40_7433
mouse-ACHE
WT
3.5 & 1.6 uM
31 & 16 uM
-
Acetylthiocholine
100mM NaP pH7.0 T22C eq3.gif sch3.gif
Radic_1993_Biochemistry_32_12074
mouse-BCHE
WT
10 & 1.1 uM
42 & 25 uM
-
Acetylthiocholine
100mM NaP pH7.0 T22C eq3.gif sch3.gif
Radic_1993_Biochemistry_32_12074
torma-ACHE
WT
1.3 & 0.2 uM
7.0 & 1.3 uM
-
Acetylthiocholine
T25C IS 50 mM phosphate
Cousin_1996_J.Biol.Chem_271_15099
torma-ACHE
WT
0.34 uM
-
-
Acetylthiocholine
100mM NaCl 50mM Tris pH7.4
Eichler_1994_Mol.Pharmacol_45_335
human-BCHE
WT
-
-
13 uM
Lockridge_1990_Pharmacol.Ther_47_35
Inhibitor
:
Edrophonium
Gene_Locus
Enzyme
Ki
Ksi
Ic50
Substrate
Exp. conditions
Reference
human-ACHE
Y72A/Y124A
0.2 uM
-
-
Acetylthiocholine
50mM Na phosphate pH8
Barak_1994_J.Biol.Chem_269_6296
human-ACHE
Y72N/Y124Q
1.1 uM
-
-
Acetylthiocholine
T25C IS 50 mM phosphate
Kaplan_2001_Biochemistry_40_7433
human-ACHE
WT
0.6 & 0.1 uM
-
-
3.3-dimethylbutylthioacetate
50mM NaPhosphate pH8
Kronman_1994_J.Biol.Chem_269_27819
bunfa-ACHE
WT
0.6 & 0.0 uM
9.9 & 4.2 uM
-
Acetylthiocholine
T25C IS 50 mM phosphate
Cousin_1996_J.Biol.Chem_271_15099
chick-ACHE
WT
0.23 uM
-
-
Acetylthiocholine
100mM NaCl 50mM Tris pH7.4
Eichler_1994_Mol.Pharmacol_45_335
human-ACHE
WT
0.75 uM
-
-
Acetylthiocholine
50mM Na phosphate pH8
Barak_1994_J.Biol.Chem_269_6296
human-ACHE
WT
50 uM
-
-
Acetylthiocholine
T25C IS 50 mM phosphate
Kaplan_2001_Biochemistry_40_7433
human-ACHE
WT
0.7 & 0.1 uM
-
-
Acetylthiocholine
50mM NaPhosphate pH8
Kronman_1994_J.Biol.Chem_269_27819
human-ACHE
WT
0.3 uM
-
-
Acetylthiocholine
IS 50mM phosphate pH8 T27C
Ordentlich_1993_J.Biol.Chem_268_17083
human-ACHE
WT
0.6 uM
4.8 uM
-
Acetylthiocholine
5 or 50mM Na Phosphate pH8 T27C
Ordentlich_1995_J.Biol.Chem_270_2082
human-ACHE
WT
-
-
1.5 uM
Acetylthiocholine
pH8 T27C 50mM Na phosphate
Shafferman_1992_EMBO.J_11_3561
human-ACHE
WT
0.32 & 0.05 uM
-
-
Acetylthiocholine
IS 5mM
Shafferman_1994_EMBO.J_13_3448
human-BCHE
WT
50 uM
-
-
Acetylthiocholine
T25C IS 50 mM phosphate
Kaplan_2001_Biochemistry_40_7433
mouse-ACHE
WT
0.30 & 0.1O uM
6.4 & 0.6 uM
-
Acetylthiocholine
100mM NaP pH7.0 T22C
Radic_1993_Biochemistry_32_12074
mouse-BCHE
WT
110 & 37 uM
1400 & 700 uM
-
Acetylthiocholine
100mM NaP pH7.0 T22C
Radic_1993_Biochemistry_32_12074
torma-ACHE
WT
0.3 & 0.0 uM
-
-
Acetylthiocholine
T25C IS 50 mM phosphate
Cousin_1996_J.Biol.Chem_271_15099
torma-ACHE
WT
0.15 uM
-
-
Acetylthiocholine
100mM NaCl 50mM Tris pH7.4
Eichler_1994_Mol.Pharmacol_45_335
human-ACHE
WT
0.4 uM
-
-
Paranitrophenylacetate
IS 50mM phosphate pH8 T27C
Ordentlich_1993_J.Biol.Chem_268_17083
human-ACHE
WT
0.24 uM
-
-
S-N-Propylthioacetate
IS 50mM phosphate pH8 T27C
Ordentlich_1993_J.Biol.Chem_268_17083
Inhibitor
:
Hexamethonium
Gene_Locus
Enzyme
Ki
Ksi
Ic50
Substrate
Exp. conditions
Reference
human-ACHE
Y72A/Y124A
0.2 mM
-
-
Acetylthiocholine
50mM Na phosphate pH8
Barak_1994_J.Biol.Chem_269_6296
chick-ACHE
WT
242 uM
-
-
Acetylthiocholine
100mM NaCl 50mM Tris pH7.4
Eichler_1994_Mol.Pharmacol_45_335
human-ACHE
WT
0.2 mM
-
-
Acetylthiocholine
50mM Na phosphate pH8
Barak_1994_J.Biol.Chem_269_6296
torma-ACHE
WT
84 uM
-
-
Acetylthiocholine
100mM NaCl 50mM Tris pH7.4
Eichler_1994_Mol.Pharmacol_45_335
Inhibitor
:
HuperzineA
Gene_Locus
Enzyme
Ki
Ksi
Ic50
Substrate
Exp. conditions
Reference
human-ACHE
Y72N/Y124Q
90 nM
-
-
Acetylthiocholine
T25C IS 50 mM phosphate
Kaplan_2001_Biochemistry_40_7433
human-ACHE
WT
16 & 1 nM
12 & 4 nM
-
Acetylthiocholine
50mM Na phosphate pH8 T22C
Ariel_1998_Biochem.J_335_95
human-ACHE
WT
16 nM
-
-
Acetylthiocholine
T25C IS 50 mM phosphate
Kaplan_2001_Biochemistry_40_7433
human-BCHE
WT
50000 nM
-
-
Acetylthiocholine
T25C IS 50 mM phosphate
Kaplan_2001_Biochemistry_40_7433
Inhibitor
:
Propidium
Gene_Locus
Enzyme
Ki
Ksi
Ic50
Substrate
Exp. conditions
Reference
human-ACHE
Y72A/Y124A
7 uM
-
-
Acetylthiocholine
50mM Na phosphate pH8
Barak_1994_J.Biol.Chem_269_6296
mouse-ACHE
Y72N/Y124Q
35 & 7 uM
120 & 44 uM
-
Acetylthiocholine
100mM NaP pH7.0 T22C eq3.gif sch3.gif
Radic_1993_Biochemistry_32_12074
bunfa-ACHE
WT
46.0 & 3.6 uM
250.0 & 60.0 uM
-
Acetylthiocholine
T25C IS 50 mM phosphate
Cousin_1996_J.Biol.Chem_271_15099
chick-ACHE
WT
>1000 uM
-
-
Acetylthiocholine
100mM NaCl 50mM Tris pH7.4
Eichler_1994_Mol.Pharmacol_45_335
human-ACHE
WT
1.4 uM
-
-
Acetylthiocholine
50mM Na phosphate pH8
Barak_1994_J.Biol.Chem_269_6296
human-ACHE
WT
0.6 uM
0.9 uM
-
Acetylthiocholine
5 or 50mM Na Phosphate pH8 T27C
Ordentlich_1995_J.Biol.Chem_270_2082
human-ACHE
WT
-
-
1.5 uM
Acetylthiocholine
pH8 T27C 50mM Na phosphate
Shafferman_1992_EMBO.J_11_3561
mouse-ACHE
WT
2.2 & 0.7 uM
5.3 & 1.8 uM
-
Acetylthiocholine
100mM NaP pH7.0 T22C eq3.gif sch3.gif
Radic_1993_Biochemistry_32_12074
mouse-BCHE
WT
5.3 & 1.8 uM
26 & 18 uM
-
Acetylthiocholine
100mM NaP pH7.0 T22C eq3.gif sch3.gif
Radic_1993_Biochemistry_32_12074
torma-ACHE
WT
2.0 & 0.2 uM
3.6 & 0.4 uM
-
Acetylthiocholine
T25C IS 50 mM phosphate
Cousin_1996_J.Biol.Chem_271_15099
torma-ACHE
WT
2.8 uM
-
-
Acetylthiocholine
100mM NaCl 50mM Tris pH7.4
Eichler_1994_Mol.Pharmacol_45_335
Inhibitor
:
Tacrine
Gene_Locus
Enzyme
Ki
Ksi
Ic50
Substrate
Exp. conditions
Reference
human-ACHE
Y72N/Y124Q
55 nM
-
-
Acetylthiocholine
T25C IS 50 mM phosphate
Kaplan_2001_Biochemistry_40_7433
human-ACHE
WT
85 & 12 nM
90 & 20 nM
-
Acetylthiocholine
50mM Na phosphate pH8 T22C
Ariel_1998_Biochem.J_335_95
human-ACHE
WT
12 nM
-
-
Acetylthiocholine
T25C IS 50 mM phosphate
Kaplan_2001_Biochemistry_40_7433
human-ACHE
WT
0.21 uM
-
-
Acetylthiocholine
50mM NaPhosphate pH7.4
Loewenstein-Lichtenstein_1996_Mol.Pharmacol_50_1423
human-BCHE
WT
12 nM
-
-
Acetylthiocholine
T25C IS 50 mM phosphate
Kaplan_2001_Biochemistry_40_7433
mouse-ACHE
WT
40 & 10 nM
130 & 50 nM
-
Acetylthiocholine
100mM NaP pH7.0 T22C
Radic_1993_Biochemistry_32_12074
mouse-BCHE
WT
17 & 4 nM
47 & 22 nM
-
Acetylthiocholine
100mM NaP pH7.0 T22C
Radic_1993_Biochemistry_32_12074
human-BCHE
WT
0.06 & 0.03 uM
-
-
Butyrylthiocholine
50mM NaPhosphate pH7.4
Loewenstein-Lichtenstein_1996_Mol.Pharmacol_50_1423
Inhibitor
:
WT-fasciculin2
Gene_Locus
Enzyme
Ki
Ksi
Ic50
Substrate
Exp. conditions
Reference
mouse-ACHE
Y72N/Y124Q
-
95 & 10 nM
-
Acetylthiocholine
100mM NaP pH7.0 T37C eq4 sch4 meth6
Radic_1994_J.Biol.Chem_269_11233
bunfa-ACHE
WT
-
50.7 & 2.6 nM
-
Acetylthiocholine
T25C IS 50 mM phosphate
Cousin_1996_J.Biol.Chem_271_15099
mouse-ACHE
WT
-
2.3 & 0.6 pM
-
Acetylthiocholine
50mM NaP pH8.0
Marchot_1997_J.Biol.Chem_272_3502
mouse-ACHE
WT
-
6.3 pM
-
Acetylthiocholine
100mM NaP pH7.0 T37C eq4 sch4 meth5
Radic_1994_J.Biol.Chem_269_11233
mouse-BCHE
WT
-
290000 & 30000 nM
-
Acetylthiocholine
100mM NaP pH7.0 T37C eq4 sch4 meth6
Radic_1994_J.Biol.Chem_269_11233
torma-ACHE
WT
-
0.14 & 0.04 nM
-
Acetylthiocholine
T25C IS 50 mM phosphate
Cousin_1996_J.Biol.Chem_271_15099
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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and
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