Kinetic parameters

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Kinetic parameters for torpedo number 72

Substrates: 1-Naphtylacetate, Acetylcholine, Acetylthiocholine, Aspirin, Benzoylcholine, Butyrylcholine, Butyrylthiocholine, Heptanoylcholine, Heroin, Hexanoylcholine, Methylprednisolone-acetate, O-Nitrophenylbutyrate, Pentanoylcholine, Procaine, Propionylcholine, Succinyldithiocholine, Tetracaine

Inhibitors: 17-desoxypancuronium, BW284C51, Chlorpromazine, Choline, Cocaine, Decamethonium, Dibucaine, Dibutyrate-pancuronium, Edrophonium, Hexamethonium, HuperzineA, Meperidine, Neostigmine~Prostigmine, Pancuronium, Physostigmine~Eserine, Procaine, Propidium, Ro-2-0683, Solanine, Succinylcholine~Suxamethonium, Tacrine, Tetracaine, Tetramethylammonium, Vecuronium, WT-fasciculin2, Win4510, Win5303

Substrates

Substrate: 1-Naphtylacetate

Gene_Locus	Enzyme	Km	Kcat	Exp. conditions	Reference
human-BCHE	D70G	370 uM	36000 /min		Lockridge_1990_Pharmacol.Ther_47_35
human-BCHE	WT	1000 uM	36000 /min		Lockridge_1990_Pharmacol.Ther_47_35

Substrate: Acetylcholine

Gene_Locus	Enzyme	Km	Kcat	Exp. conditions	Reference
human-BCHE	D70G	9000 uM	33200 /min		Lockridge_1990_Pharmacol.Ther_47_35
eleel-ACHE	WT	330 & 70 uM	960000/min	0.18MNaCl pH 7.8 T25C	Hasan_1980_J.Biol.Chem_255_3898
eleel-ACHE	WT	100 uM	960000 /min		Rosenberry_1975_Proc.Natl.Acad.Sci.U.S.A_72_3834
human-BCHE	WT	1400 uM	33200 /min		Lockridge_1990_Pharmacol.Ther_47_35

Substrate: Acetylthiocholine

Gene_Locus	Enzyme	Km	Kcat	Exp. conditions	Reference
human-ACHE	D74E	500 & 150 uM	440000 & 8000/min	pH8 T27C 50mM Na phosphate	Shafferman_1992_EMBO.J_11_3561
human-ACHE	D74G	630 & 200 uM	360000 & 10000/min	pH8 T27C 50mM Na phosphate	Shafferman_1992_EMBO.J_11_3561
human-ACHE	D74K	450 & 90 uM	350000 & 10000/min	pH8 T27C 50mM Na phosphate	Shafferman_1992_EMBO.J_11_3561
human-ACHE	D74N	600 uM	250000/min	50mM Na phosphate pH8	Barak_1994_J.Biol.Chem_269_6296
human-ACHE	D74N	580 & 200 uM	270000 & 11000/min	pH8 T27C 50mM Na phosphate	Shafferman_1992_EMBO.J_11_3561
mouse-ACHE	D74N	1300 & 140 uM	84000 & 11000/min	100mM NaP pH7 T22C eq3 sch3	Radic_1993_Biochemistry_32_12074
mouse-ACHE	Y72N/D74N/Y124Q/W286A	2100 & 300 uM	150000 & 10000/min	100mM NaP pH7 T22C eq3 sch3	Radic_1993_Biochemistry_32_12074
mouse-ACHE	Y72N/D74N/Y124Q/W286R	6100 & 730 uM	140000 & 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: Aspirin

Gene_Locus	Enzyme	Km	Kcat	Exp. conditions	Reference
human-BCHE	D70G	1600 uM	7200 /min		Lockridge_1990_Pharmacol.Ther_47_35
human-BCHE	WT	4200 uM	7200 /min		Lockridge_1990_Pharmacol.Ther_47_35

Substrate: Benzoylcholine

Gene_Locus	Enzyme	Km	Kcat	Exp. conditions	Reference
human-BCHE	D70G	22 uM	15000 /min		Lockridge_1990_Pharmacol.Ther_47_35
human-BCHE	WT	8 & 1 uM	15000 & 700 /min	100mM K phosphate pH7.0 T25C	Blong_1997_Biochem.J_327_747
human-BCHE	WT	4 uM	15000 /min		Lockridge_1990_Pharmacol.Ther_47_35

Substrate: Butyrylcholine

Gene_Locus	Enzyme	Km	Kcat	Exp. conditions	Reference
human-BCHE	D70G	1700 uM	80000 /min		Lockridge_1990_Pharmacol.Ther_47_35
human-BCHE	WT	91 uM	80000 /min		Lockridge_1990_Pharmacol.Ther_47_35

Substrate: Butyrylthiocholine

Gene_Locus	Enzyme	Km	Kcat	Exp. conditions	Reference
human-BCHE	D70G	3.8 & 0.4 mM	30000 /min	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

Substrate: Heptanoylcholine

Gene_Locus	Enzyme	Km	Kcat	Exp. conditions	Reference
human-BCHE	D70G	1110 uM	35000 /min		Lockridge_1990_Pharmacol.Ther_47_35
human-BCHE	WT	380 uM	35000 /min		Lockridge_1990_Pharmacol.Ther_47_35

Substrate: Heroin

Gene_Locus	Enzyme	Km	Kcat	Exp. conditions	Reference
human-BCHE	D70G	450 uM	500 /min		Lockridge_1990_Pharmacol.Ther_47_35
human-BCHE	WT	110 uM	500 /min		Lockridge_1990_Pharmacol.Ther_47_35

Substrate: Hexanoylcholine

Gene_Locus	Enzyme	Km	Kcat	Reference
human-BCHE	D70G	820 uM	-	Lockridge_1990_Pharmacol.Ther_47_35
human-BCHE	WT	-	36000 /min	Lockridge_1990_Pharmacol.Ther_47_35
human-BCHE	WT	570 uM	36000 /min	Lockridge_1990_Pharmacol.Ther_47_35

Substrate: Methylprednisolone-acetate

Gene_Locus	Enzyme	Km	Kcat	Exp. conditions	Reference
human-BCHE	D70G	-	25 /min		Lockridge_1990_Pharmacol.Ther_47_35
human-BCHE	WT	1000 uM	25 /min		Lockridge_1990_Pharmacol.Ther_47_35

Substrate: O-Nitrophenylbutyrate

Gene_Locus	Enzyme	Km	Kcat	Exp. conditions	Reference
human-BCHE	D70G	400 uM	48000 /min		Lockridge_1990_Pharmacol.Ther_47_35
human-BCHE	WT	110 & 20 uM	36000 & 5000 /min	100mM K phosphate pH7.0 T25C	Blong_1997_Biochem.J_327_747
human-BCHE	WT	330 uM	48000 /min		Lockridge_1990_Pharmacol.Ther_47_35

Substrate: Pentanoylcholine

Gene_Locus	Enzyme	Km	Kcat	Exp. conditions	Reference
human-BCHE	D70G	1500 uM	63000 /min		Lockridge_1990_Pharmacol.Ther_47_35
human-BCHE	WT	720 uM	63000 /min		Lockridge_1990_Pharmacol.Ther_47_35

Substrate: Procaine

Gene_Locus	Enzyme	Km	Kcat	Exp. conditions	Reference
human-BCHE	D70G	100 uM	255 /min		Lockridge_1990_Pharmacol.Ther_47_35
human-BCHE	WT	66 uM	255 /min		Lockridge_1990_Pharmacol.Ther_47_35

Substrate: Propionylcholine

Gene_Locus	Enzyme	Km	Kcat	Exp. conditions	Reference
human-BCHE	D70G	3100 uM	55000 /min		Lockridge_1990_Pharmacol.Ther_47_35
human-BCHE	WT	970 uM	55000 /min		Lockridge_1990_Pharmacol.Ther_47_35

Substrate: Succinyldithiocholine

Gene_Locus	Enzyme	Km	Kcat	Exp. conditions	Reference
human-BCHE	D70G	1080 uM	600 /min		Lockridge_1990_Pharmacol.Ther_47_35
human-BCHE	WT	35 uM	600 /min		Lockridge_1990_Pharmacol.Ther_47_35

Substrate: Tetracaine

Gene_Locus	Enzyme	Km	Kcat	Exp. conditions	Reference
human-BCHE	D70G	8 uM	74 /min		Lockridge_1990_Pharmacol.Ther_47_35
human-BCHE	WT	0.14 uM	74 /min		Lockridge_1990_Pharmacol.Ther_47_35

Inhibitors

Inhibitor: 17-desoxypancuronium

Gene_Locus	Enzyme	Ki	Ksi	Ic50	Substrate	Exp. conditions	Reference
human-BCHE	D70G	-	-	24 uM			Lockridge_1990_Pharmacol.Ther_47_35
human-BCHE	WT	-	-	0.13 uM			Lockridge_1990_Pharmacol.Ther_47_35

Inhibitor: BW284C51

Gene_Locus	Enzyme	Ki	Ksi	Ic50	Substrate	Exp. conditions	Reference
human-ACHE	D74E	-	-	500 nM	Acetylthiocholine	pH8 T27C 50mM Na phosphate	Shafferman_1992_EMBO.J_11_3561
human-ACHE	D74G	-	-	4000 nM	Acetylthiocholine	pH8 T27C 50mM Na phosphate	Shafferman_1992_EMBO.J_11_3561
human-ACHE	D74K	-	-	64000 nM	Acetylthiocholine	pH8 T27C 50mM Na phosphate	Shafferman_1992_EMBO.J_11_3561
human-ACHE	D74N	2450 nM	-	-	Acetylthiocholine	50mM Na phosphate pH8	Barak_1994_J.Biol.Chem_269_6296
human-ACHE	D74N	-	-	5650 nM	Acetylthiocholine	pH8 T27C 50mM Na phosphate	Shafferman_1992_EMBO.J_11_3561
mouse-ACHE	D74N	1900 & 400 nM	23000 & 6000 nM	-	Acetylthiocholine	100mM NaP pH7.0 T22C eq3.gif sch3.gif	Radic_1993_Biochemistry_32_12074
mouse-ACHE	Y72N/D74N/Y124Q/W286A	170000 & 6000 nM	690000 & 18000 nM	-	Acetylthiocholine	100mM NaP pH7.0 T22C eq3.gif sch3.gif	Radic_1993_Biochemistry_32_12074
mouse-ACHE	Y72N/D74N/Y124Q/W286R	780000 & 28000 nM	1000000 & 240000 nM	-	Acetylthiocholine	100mM NaP pH7.0 T22C eq3.gif sch3.gif	Radic_1993_Biochemistry_32_12074
human-BCHE	D70G	2540 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: Chlorpromazine

Gene_Locus	Enzyme	Ki	Ksi	Ic50	Substrate	Exp. conditions	Reference
human-BCHE	D70G	-	-	74 uM			Lockridge_1990_Pharmacol.Ther_47_35
mouse-ACHE	WT	26 & 8 uM	410 & 290 uM	-	Acetylthiocholine	100mM NaP pH7.0 T22C	Radic_1993_Biochemistry_32_12074
mouse-BCHE	WT	2.1 & 0.9 uM	8.5 & 4.0 uM	-	Acetylthiocholine	100mM NaP pH7.0 T22C	Radic_1993_Biochemistry_32_12074
human-BCHE	WT	-	-	4.4 uM			Lockridge_1990_Pharmacol.Ther_47_35

Inhibitor: Choline

Gene_Locus	Enzyme	Ki	Ksi	Ic50	Substrate	Exp. conditions	Reference
human-BCHE	D70G	-	-	59 mM			Lockridge_1990_Pharmacol.Ther_47_35
human-BCHE	WT	-	-	30 mM			Lockridge_1990_Pharmacol.Ther_47_35

Inhibitor: Cocaine

Gene_Locus	Enzyme	Ki	Ksi	Ic50	Substrate	Exp. conditions	Reference
human-BCHE	D70G	3200 & 100 uM	-	-	Butyrylthiocholine	50mM NaPhosphate pH7.4	Loewenstein-Lichtenstein_1996_Mol.Pharmacol_50_1423
human-ACHE	WT	3900 uM	-	-	Acetylthiocholine	50mM NaPhosphate pH7.4	Loewenstein-Lichtenstein_1996_Mol.Pharmacol_50_1423
human-BCHE	WT	390 & 30 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	D74E	-	-	68 uM	Acetylthiocholine	pH8 T27C 50mM Na phosphate	Shafferman_1992_EMBO.J_11_3561
human-ACHE	D74G	-	-	850 uM	Acetylthiocholine	pH8 T27C 50mM Na phosphate	Shafferman_1992_EMBO.J_11_3561
human-ACHE	D74K	-	-	7080 uM	Acetylthiocholine	pH8 T27C 50mM Na phosphate	Shafferman_1992_EMBO.J_11_3561
human-ACHE	D74N	850 uM	-	-	Acetylthiocholine	50mM Na phosphate pH8	Barak_1994_J.Biol.Chem_269_6296
human-ACHE	D74N	-	-	850 uM	Acetylthiocholine	pH8 T27C 50mM Na phosphate	Shafferman_1992_EMBO.J_11_3561
mouse-ACHE	D74N	830 & 130 uM	3000 & 670 uM	-	Acetylthiocholine	100mM NaP pH7.0 T22C eq3.gif sch3.gif	Radic_1993_Biochemistry_32_12074
mouse-ACHE	Y72N/D74N/Y124Q/W286A	16000 & 1000 uM	55000 & 35000 uM	-	Acetylthiocholine	100mM NaP pH7.0 T22C eq3.gif sch3.gif	Radic_1993_Biochemistry_32_12074
mouse-ACHE	Y72N/D74N/Y124Q/W286R	50000 & 18000 uM	40000 & 35000 uM	-	Acetylthiocholine	100mM NaP pH7.0 T22C eq3.gif sch3.gif	Radic_1993_Biochemistry_32_12074
human-BCHE	D70G	-	-	1800 uM			Lockridge_1990_Pharmacol.Ther_47_35
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: Dibucaine

Gene_Locus	Enzyme	Ki	Ksi	Ic50	Substrate	Exp. conditions	Reference
human-BCHE	D70G	182 & 100 uM	-	-	Butyrylthiocholine	50mM NaPhosphate pH7.4	Loewenstein-Lichtenstein_1996_Mol.Pharmacol_50_1423
human-BCHE	D70G	-	-	54 uM			Lockridge_1990_Pharmacol.Ther_47_35
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: Dibutyrate-pancuronium

Gene_Locus	Enzyme	Ki	Ksi	Ic50	Substrate	Exp. conditions	Reference
human-BCHE	D70G	-	-	4.2 uM			Lockridge_1990_Pharmacol.Ther_47_35
human-BCHE	WT	-	-	0.015 uM			Lockridge_1990_Pharmacol.Ther_47_35

Inhibitor: Edrophonium

Gene_Locus	Enzyme	Ki	Ksi	Ic50	Substrate	Exp. conditions	Reference
human-ACHE	D74E	-	-	3 uM	Acetylthiocholine	pH8 T27C 50mM Na phosphate	Shafferman_1992_EMBO.J_11_3561
human-ACHE	D74G	-	-	7.5 uM	Acetylthiocholine	pH8 T27C 50mM Na phosphate	Shafferman_1992_EMBO.J_11_3561
human-ACHE	D74K	-	-	6 uM	Acetylthiocholine	pH8 T27C 50mM Na phosphate	Shafferman_1992_EMBO.J_11_3561
human-ACHE	D74N	3.5 uM	-	-	Acetylthiocholine	50mM Na phosphate pH8	Barak_1994_J.Biol.Chem_269_6296
human-ACHE	D74N	-	-	10.5 uM	Acetylthiocholine	pH8 T27C 50mM Na phosphate	Shafferman_1992_EMBO.J_11_3561
mouse-ACHE	Y72N/D74N/Y124Q/W286A	17 & 3 uM	>120 uM	-	Acetylthiocholine	100mM NaP pH7.0 T22C eq3.gif sch3.gif	Radic_1993_Biochemistry_32_12074
mouse-ACHE	Y72N/D74N/Y124Q/W286R	28 & 6 uM	-	-	Acetylthiocholine	100mM NaP pH7.0 T22C eq3.gif sch3.gif	Radic_1993_Biochemistry_32_12074
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	D74N	2.0 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	D74N	17 & 2 nM	25 & 5 nM	-	Acetylthiocholine	50mM Na phosphate pH8 T22C	Ariel_1998_Biochem.J_335_95
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: Meperidine

Gene_Locus	Enzyme	Ki	Ksi	Ic50	Substrate	Exp. conditions	Reference
human-BCHE	D70G	-	-	1800 uM			Lockridge_1990_Pharmacol.Ther_47_35
human-BCHE	WT	-	-	760 uM			Lockridge_1990_Pharmacol.Ther_47_35

Inhibitor: Neostigmine~Prostigmine

Gene_Locus	Enzyme	Ki	Ksi	Ic50	Substrate	Exp. conditions	Reference
human-BCHE	D70G	-	-	24 uM			Lockridge_1990_Pharmacol.Ther_47_35
human-BCHE	WT	-	-	0.13 uM			Lockridge_1990_Pharmacol.Ther_47_35

Inhibitor: Pancuronium

Gene_Locus	Enzyme	Ki	Ksi	Ic50	Substrate	Exp. conditions	Reference
human-BCHE	D70G	-	-	22 uM			Lockridge_1990_Pharmacol.Ther_47_35
human-BCHE	WT	-	-	0.15 uM			Lockridge_1990_Pharmacol.Ther_47_35

Inhibitor: Physostigmine~Eserine

Gene_Locus	Enzyme	Ki	Ksi	Ic50	Substrate	Exp. conditions	Reference
human-BCHE	D70G	-	-	270 nM			Lockridge_1990_Pharmacol.Ther_47_35
human-BCHE	WT	-	-	14 nM			Lockridge_1990_Pharmacol.Ther_47_35

Inhibitor: Procaine

Gene_Locus	Enzyme	Ki	Ksi	Ic50	Substrate	Exp. conditions	Reference
human-BCHE	D70G	-	-	590 uM			Lockridge_1990_Pharmacol.Ther_47_35
human-BCHE	WT	-	-	44 uM			Lockridge_1990_Pharmacol.Ther_47_35

Inhibitor: Propidium

Gene_Locus	Enzyme	Ki	Ksi	Ic50	Substrate	Exp. conditions	Reference
human-ACHE	D74E	-	-	2.25 uM	Acetylthiocholine	pH8 T27C 50mM Na phosphate	Shafferman_1992_EMBO.J_11_3561
human-ACHE	D74G	-	-	90 uM	Acetylthiocholine	pH8 T27C 50mM Na phosphate	Shafferman_1992_EMBO.J_11_3561
human-ACHE	D74K	-	-	54.0 uM	Acetylthiocholine	pH8 T27C 50mM Na phosphate	Shafferman_1992_EMBO.J_11_3561
human-ACHE	D74N	7.8 uM	-	-	Acetylthiocholine	50mM Na phosphate pH8	Barak_1994_J.Biol.Chem_269_6296
human-ACHE	D74N	-	-	6.15 uM	Acetylthiocholine	pH8 T27C 50mM Na phosphate	Shafferman_1992_EMBO.J_11_3561
mouse-ACHE	D74N	8.7 & 2.1 uM	34 & 11 uM	-	Acetylthiocholine	100mM NaP pH7.0 T22C eq3.gif sch3.gif	Radic_1993_Biochemistry_32_12074
mouse-ACHE	Y72N/D74N/Y124Q/W286A	1100 & 430 uM	2700 & 1200 uM	-	Acetylthiocholine	100mM NaP pH7.0 T22C eq3.gif sch3.gif	Radic_1993_Biochemistry_32_12074
mouse-ACHE	Y72N/D74N/Y124Q/W286R	1900 & 760 uM	3200 & 1600 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: Ro-2-0683

Gene_Locus	Enzyme	Ki	Ksi	Ic50	Substrate	Exp. conditions	Reference
human-BCHE	D70G	-	-	170 nM			Lockridge_1990_Pharmacol.Ther_47_35
human-BCHE	WT	-	-	1.4 nM			Lockridge_1990_Pharmacol.Ther_47_35

Inhibitor: Solanine

Gene_Locus	Enzyme	Ki	Ksi	Ic50	Substrate	Exp. conditions	Reference
human-BCHE	D70G	78.0 & 2.5 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	D70G	52000 & 13000 uM	-	-	Butyrylthiocholine	50mM NaPhosphate pH7.4	Loewenstein-Lichtenstein_1996_Mol.Pharmacol_50_1423
human-BCHE	D70G	-	-	9500 uM			Lockridge_1990_Pharmacol.Ther_47_35
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-ACHE	D74N	4600 & 700 nM	65000 & 15000 nM	-	Acetylthiocholine	50mM Na phosphate pH8 T22C	Ariel_1998_Biochem.J_335_95
human-BCHE	D70G	9.1 & 2.4 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

Inhibitor: Tetracaine

Gene_Locus	Enzyme	Ki	Ksi	Ic50	Substrate	Exp. conditions	Reference
human-BCHE	D70G	-	-	6.3 uM			Lockridge_1990_Pharmacol.Ther_47_35
human-BCHE	WT	-	-	0.28 uM			Lockridge_1990_Pharmacol.Ther_47_35

Inhibitor: Tetramethylammonium

Gene_Locus	Enzyme	Ki	Ksi	Ic50	Substrate	Exp. conditions	Reference
human-BCHE	D70G	-	-	71 mM			Lockridge_1990_Pharmacol.Ther_47_35
human-BCHE	WT	-	-	28 mM			Lockridge_1990_Pharmacol.Ther_47_35

Inhibitor: Vecuronium

Gene_Locus	Enzyme	Ki	Ksi	Ic50	Substrate	Exp. conditions	Reference
human-BCHE	D70G	-	-	1.7 uM			Lockridge_1990_Pharmacol.Ther_47_35
human-BCHE	WT	-	-	0.34 uM			Lockridge_1990_Pharmacol.Ther_47_35

Inhibitor: WT-fasciculin2

Gene_Locus	Enzyme	Ki	Ksi	Ic50	Substrate	Exp. conditions	Reference
mouse-ACHE	D74N	-	83 pM	-	Acetylthiocholine	100mM NaP pH7.0 T37C eq4 sch4 meth5	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

Inhibitor: Win4510

Gene_Locus	Enzyme	Ki	Ksi	Ic50	Substrate	Exp. conditions	Reference
human-BCHE	D70G	-	-	5.4 uM			Lockridge_1990_Pharmacol.Ther_47_35
human-BCHE	WT	-	-	0.15 uM			Lockridge_1990_Pharmacol.Ther_47_35

Inhibitor: Win5303

Gene_Locus	Enzyme	Ki	Ksi	Ic50	Substrate	Exp. conditions	Reference
human-BCHE	D70G	-	-	21 uM			Lockridge_1990_Pharmacol.Ther_47_35
human-BCHE	WT	-	-	0.79 uM			Lockridge_1990_Pharmacol.Ther_47_35

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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