Kinetic parameters for torpedo number 278

Substrates: 3,3-dimethylbutylthioacetate, Acetylthiocholine

Inhibitors: BW284C51, Decamethonium, Edrophonium, Hexamethonium, Propidium

Substrates

Substrate: 3,3-dimethylbutylthioacetate

Gene_Locus	Enzyme	Km	Kcat	Exp. conditions	Reference
human-ACHE	E285A	230 & 30 uM	42000 & 6000/min	IS 5mM	Shafferman_1994_EMBO.J_13_3448
human-ACHE	E84Q/E285A/E292A/D349N/E358Q/E389Q/D390N	220 & 30 uM	44000 & 6000/min	IS 5mM	Shafferman_1994_EMBO.J_13_3448
human-ACHE	E84Q/E285A/E292A/D349N/E358Q	220 & 30 uM	40000 & 6000/min	IS 5mM	Shafferman_1994_EMBO.J_13_3448
human-ACHE	WT	300 & 6 mM	55000 & 10000/min	50mM NaPhosphate pH8	Kronman_1994_J.Biol.Chem_269_27819
human-ACHE	WT	450 uM	52000 /min	IS 50mM phosphate pH8 T27C	Ordentlich_1993_J.Biol.Chem_268_17083
human-ACHE	WT	300 uM	55000/min	5 or 50mM Na Phosphate pH8 T27C	Ordentlich_1995_J.Biol.Chem_270_2082
human-ACHE	WT	260 & 30 uM	46000 & 7000/min	IS 5mM	Shafferman_1994_EMBO.J_13_3448

Substrate: Acetylthiocholine

Gene_Locus	Enzyme	Km	Kcat	Exp. conditions	Reference
human-ACHE	E285A/W286A	350 uM	440000/min	50mM Na phosphate pH8	Barak_1994_J.Biol.Chem_269_6296
human-ACHE	E285A	280 uM	380000/min	50mM Na phosphate pH8	Barak_1994_J.Biol.Chem_269_6296
human-ACHE	E285A	170 & 30 uM	400000 & 60000/min	IS 5mM	Shafferman_1994_EMBO.J_13_3448
human-ACHE	E84Q/E285A/E292A/D349N/E358Q/E389Q/D390N	190 & 30 uM	380000 & 60000/min	IS 5mM	Shafferman_1994_EMBO.J_13_3448
human-ACHE	E84Q/E285A/E292A/D349N/E358Q	210 & 30 uM	400000 & 60000/min	IS 5mM	Shafferman_1994_EMBO.J_13_3448
human-ACHE	Y124A/E285A/W286A	280 uM	140000/min	50mM Na phosphate pH8	Barak_1994_J.Biol.Chem_269_6296
human-ACHE	Y72A/E285A/W286A	300 uM	200000/min	50mM Na phosphate pH8	Barak_1994_J.Biol.Chem_269_6296
human-ACHE	Y72A/E285A	240 uM	400000/min	50mM Na phosphate pH8	Barak_1994_J.Biol.Chem_269_6296
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

Inhibitors

Inhibitor: BW284C51

Gene_Locus	Enzyme	Ki	Ksi	Ic50	Substrate	Exp. conditions	Reference
human-ACHE	E285A/W286A	2220 nM	-	-	Acetylthiocholine	50mM Na phosphate pH8	Barak_1994_J.Biol.Chem_269_6296
human-ACHE	E285A	21 nM	-	-	Acetylthiocholine	50mM Na phosphate pH8	Barak_1994_J.Biol.Chem_269_6296
human-ACHE	Y124A/E285A/W286A	3500 nM	-	-	Acetylthiocholine	50mM Na phosphate pH8	Barak_1994_J.Biol.Chem_269_6296
human-ACHE	Y72A/E285A/W286A	3870 nM	-	-	Acetylthiocholine	50mM Na phosphate pH8	Barak_1994_J.Biol.Chem_269_6296
human-ACHE	Y72A/E285A	140 nM	-	-	Acetylthiocholine	50mM Na phosphate pH8	Barak_1994_J.Biol.Chem_269_6296
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	E285A/W286A	280 uM	-	-	Acetylthiocholine	50mM Na phosphate pH8	Barak_1994_J.Biol.Chem_269_6296
human-ACHE	E285A	26 uM	-	-	Acetylthiocholine	50mM Na phosphate pH8	Barak_1994_J.Biol.Chem_269_6296
human-ACHE	Y124A/E285A/W286A	790 uM	-	-	Acetylthiocholine	50mM Na phosphate pH8	Barak_1994_J.Biol.Chem_269_6296
human-ACHE	Y72A/E285A/W286A	340 uM	-	-	Acetylthiocholine	50mM Na phosphate pH8	Barak_1994_J.Biol.Chem_269_6296
human-ACHE	Y72A/E285A	370 uM	-	-	Acetylthiocholine	50mM Na phosphate pH8	Barak_1994_J.Biol.Chem_269_6296
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	E285A/W286A	0.6 uM	-	-	Acetylthiocholine	50mM Na phosphate pH8	Barak_1994_J.Biol.Chem_269_6296
human-ACHE	E285A	0.8 uM	-	-	Acetylthiocholine	50mM Na phosphate pH8	Barak_1994_J.Biol.Chem_269_6296
human-ACHE	E285A	1.00 & 0.15 uM	-	-	Acetylthiocholine	IS 150mM	Shafferman_1994_EMBO.J_13_3448
human-ACHE	E84Q/E285A/E292A/D349N/E358Q/E389Q/D390N	1.40 & 0.20 uM	-	-	Acetylthiocholine	IS 5mM	Shafferman_1994_EMBO.J_13_3448
human-ACHE	E84Q/E285A/E292A/D349N/E358Q	1.70 & 0.25 uM	-	-	Acetylthiocholine	IS 150 mM	Shafferman_1994_EMBO.J_13_3448
human-ACHE	Y124A/E285A/W286A	0.6 uM	-	-	Acetylthiocholine	50mM Na phosphate pH8	Barak_1994_J.Biol.Chem_269_6296
human-ACHE	Y72A/E285A/W286A	0.6 uM	-	-	Acetylthiocholine	50mM Na phosphate pH8	Barak_1994_J.Biol.Chem_269_6296
human-ACHE	Y72A/E285A	0.6 uM	-	-	Acetylthiocholine	50mM Na phosphate pH8	Barak_1994_J.Biol.Chem_269_6296
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	E285A/W286A	1.8 mM	-	-	Acetylthiocholine	50mM Na phosphate pH8	Barak_1994_J.Biol.Chem_269_6296
human-ACHE	E285A	1.3 mM	-	-	Acetylthiocholine	50mM Na phosphate pH8	Barak_1994_J.Biol.Chem_269_6296
human-ACHE	Y124A/E285A/W286A	2.1 mM	-	-	Acetylthiocholine	50mM Na phosphate pH8	Barak_1994_J.Biol.Chem_269_6296
human-ACHE	Y72A/E285A/W286A	3.3 mM	-	-	Acetylthiocholine	50mM Na phosphate pH8	Barak_1994_J.Biol.Chem_269_6296
human-ACHE	Y72A/E285A	2.2 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: Propidium

Gene_Locus	Enzyme	Ki	Ksi	Ic50	Substrate	Exp. conditions	Reference
human-ACHE	E285A/W286A	133 uM	-	-	Acetylthiocholine	50mM Na phosphate pH8	Barak_1994_J.Biol.Chem_269_6296
human-ACHE	E285A	6.5 uM	-	-	Acetylthiocholine	50mM Na phosphate pH8	Barak_1994_J.Biol.Chem_269_6296
human-ACHE	Y124A/E285A/W286A	110 uM	-	-	Acetylthiocholine	50mM Na phosphate pH8	Barak_1994_J.Biol.Chem_269_6296
human-ACHE	Y72A/E285A/W286A	138 uM	-	-	Acetylthiocholine	50mM Na phosphate pH8	Barak_1994_J.Biol.Chem_269_6296
human-ACHE	Y72A/E285A	14 uM	-	-	Acetylthiocholine	50mM Na phosphate pH8	Barak_1994_J.Biol.Chem_269_6296
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

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.

For technical information about these pages see:
ESTHER Home Page and ACEDB Home Page
AcePerl Lincoln Stein Home Page

webmaster

Acknowledgements and disclaimer