Kinetic parameters for torpedo number 129

Substrates: 3,3-dimethylbutylthioacetate, Acetylthiocholine, Butyrylthiocholine

Inhibitors: BW284C51, Dibucaine, Edrophonium, Solanine, Succinylcholine~Suxamethonium, Tacrine

Substrates

Substrate: 3,3-dimethylbutylthioacetate

Gene_Locus	Enzyme	Km	Kcat	Exp. conditions	Reference
human-ACHE	V132A	210 & 30 uM	58000 & 9000/min	50mM NaPhosphate pH8	Kronman_1994_J.Biol.Chem_269_27819
human-ACHE	V132K	350 & 50 uM	30000 & 4000/min	50mM NaPhosphate pH8	Kronman_1994_J.Biol.Chem_269_27819
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	V132A	120 & 10 uM	340000 & 40000/min	50mM NaPhosphate pH8	Kronman_1994_J.Biol.Chem_269_27819
human-ACHE	V132K	900 & 140 uM	220000 & 50000/min	50mM NaPhosphate pH8	Kronman_1994_J.Biol.Chem_269_27819
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-BCHE	V127D	4.9 & 1.0 mM	-	50mM NaPhosphate pH7.4	Loewenstein-Lichtenstein_1996_Mol.Pharmacol_50_1423
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-BCHE	V127D	644 & 32 uM	-	-	Butyrylthiocholine	50mM NaPhosphate pH7.4	Loewenstein-Lichtenstein_1996_Mol.Pharmacol_50_1423
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: Dibucaine

Gene_Locus	Enzyme	Ki	Ksi	Ic50	Substrate	Exp. conditions	Reference
human-BCHE	V127D	18 & 5 uM	-	-	Butyrylthiocholine	50mM NaPhosphate pH7.4	Loewenstein-Lichtenstein_1996_Mol.Pharmacol_50_1423
human-ACHE	WT	710 uM	-	-	Acetylthiocholine	50mM NaPhosphate pH7.4	Loewenstein-Lichtenstein_1996_Mol.Pharmacol_50_1423
human-BCHE	WT	6.9 & 4.6 uM	-	-	Butyrylthiocholine	50mM NaPhosphate pH7.4	Loewenstein-Lichtenstein_1996_Mol.Pharmacol_50_1423
human-BCHE	WT	-	-	2.7 uM			Lockridge_1990_Pharmacol.Ther_47_35

Inhibitor: Edrophonium

Gene_Locus	Enzyme	Ki	Ksi	Ic50	Substrate	Exp. conditions	Reference
human-ACHE	V132A	1.2 & 0.1 uM	-	-	3.3-dimethylbutylthioacetate	50mM NaPhosphate pH8	Kronman_1994_J.Biol.Chem_269_27819
human-ACHE	V132K	90 & 20 uM	-	-	3.3-dimethylbutylthioacetate	50mM NaPhosphate pH8	Kronman_1994_J.Biol.Chem_269_27819
human-ACHE	V132A	1.2 & 0.1 uM	-	-	Acetylthiocholine	50mM NaPhosphate pH8	Kronman_1994_J.Biol.Chem_269_27819
human-ACHE	V132K	38 0 & 4.0 uM	-	-	Acetylthiocholine	50mM NaPhosphate pH8	Kronman_1994_J.Biol.Chem_269_27819
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: Solanine

Gene_Locus	Enzyme	Ki	Ksi	Ic50	Substrate	Exp. conditions	Reference
human-BCHE	V127D	4.6 & 0.7 uM	-	-	Butyrylthiocholine	50mM NaPhosphate pH7.4	Loewenstein-Lichtenstein_1996_Mol.Pharmacol_50_1423
human-BCHE	WT	3.3 & 2.8 uM	-	-	Butyrylthiocholine	50mM NaPhosphate pH7.4	Loewenstein-Lichtenstein_1996_Mol.Pharmacol_50_1423

Inhibitor: Succinylcholine~Suxamethonium

Gene_Locus	Enzyme	Ki	Ksi	Ic50	Substrate	Exp. conditions	Reference
human-BCHE	V127D	2500 & 800 uM	-	-	Butyrylthiocholine	50mM NaPhosphate pH7.4	Loewenstein-Lichtenstein_1996_Mol.Pharmacol_50_1423
human-ACHE	WT	1000 uM	-	-	Acetylthiocholine	50mM NaPhosphate pH7.4	Loewenstein-Lichtenstein_1996_Mol.Pharmacol_50_1423
human-BCHE	WT	4000 & 2600 uM	-	-	Butyrylthiocholine	50mM NaPhosphate pH7.4	Loewenstein-Lichtenstein_1996_Mol.Pharmacol_50_1423

Inhibitor: Tacrine

Gene_Locus	Enzyme	Ki	Ksi	Ic50	Substrate	Exp. conditions	Reference
human-BCHE	V127D	0.06 & 0.03 uM	-	-	Butyrylthiocholine	50mM NaPhosphate pH7.4	Loewenstein-Lichtenstein_1996_Mol.Pharmacol_50_1423
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

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