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_LocusEnzymeKmKcatExp. conditionsReference
human-ACHEY72A/Y124A 70 uM 250000/min 50mM Na phosphate pH8 Barak_1994_J.Biol.Chem_269_6296
human-ACHEY72N/Y124Q 140 mM 4.1 10+5/min IS 50mM phosphate pH8 T27C Kaplan_2001_Biochemistry_40_7433
mouse-ACHEY72N/Y124Q 95 & 11 uM 94000 & 20000/min 100mM NaP pH7 T22C eq3 sch3 Radic_1993_Biochemistry_32_12074
bunfa-ACHEWT 78.8 & 6.3 uM - T25C IS 50 mM phosphate Cousin_1996_J.Biol.Chem_271_15099
chick-ACHEWT - 175000/min 100mM NaP T28C pH7.0 Vigny_1978_Eur.J.Biochem_85_317
eleel-ACHEWT 130 uM 900000 /min   Salih_1992_Biochem.J_285_451
eleel-ACHEWT - 733333/min 100mM NaP T28C pH7.0 Vigny_1978_Eur.J.Biochem_85_317
human-ACHEWT 120 uM 420000/min 50mM Na phosphate pH8 Barak_1994_J.Biol.Chem_269_6296
human-ACHEWT 140 uM 4.0 10+5 /min IS 50mM phosphate pH8 T27C Kaplan_2001_Biochemistry_40_7433
human-ACHEWT 140 & 10 uM 400000 & 50000/min 50mM NaPhosphate pH8 Kronman_1994_J.Biol.Chem_269_27819
human-ACHEWT 140 uM 370000/min IS 50mM phosphate pH8 T27C Ordentlich_1993_J.Biol.Chem_268_17083
human-ACHEWT 140 uM 400000/min 5 or 50mM Na Phosphate pH8 T27C Ordentlich_1995_J.Biol.Chem_270_2082
human-ACHEWT 140 & 50 uM 370000 & 10000/min pH8 T27C 50mM Na phosphate Shafferman_1992_EMBO.J_11_3561
human-ACHEWT 80 & 10 uM 400000 & 60000/min IS 5mM Shafferman_1994_EMBO.J_13_3448
human-ACHEWT 117 uM 390000 /min 50mM Na phosphate pH8.0 T27C Velan_1991_J.Biol.Chem_266_23977
human-BCHEWT 40 uM 0.5 10+5 /min IS 50mM phosphate pH8 T27C Kaplan_2001_Biochemistry_40_7433
mouse-ACHEWT 46 uM 140000 /min 100mM NaPhosphate Ph7.0 T22C Hosea_1995_Biochemistry_34_11528
mouse-ACHEWT 46 & 3 uM 140000 & 10000/min 100mM NaP pH7 T22C eq3 sch3 Radic_1993_Biochemistry_32_12074
mouse-BCHEWT 23 uM 40000 /min 100mM NaPhosphate Ph7.0 T22C Hosea_1995_Biochemistry_34_11528
mouse-BCHEWT 35 & 2 uM 40000 & 7000/min 100mM NaP pH7 T22C eq3 sch3 Radic_1993_Biochemistry_32_12074
ratno-ACHEWT - 220000/min 100mM NaP T28C pH7.0 Vigny_1978_Eur.J.Biochem_85_317
torca-ACHEWT - 481666/min T25C pH7.8 Taylor_1974_Mol.Pharmacol_10_78
torma-ACHEWT 81.2 & 4.2 uM - T25C IS 50 mM phosphate Cousin_1996_J.Biol.Chem_271_15099
torma-ACHEWT - 273333/min 100mM NaP T28C pH7.0 Vigny_1978_Eur.J.Biochem_85_317
human-ACHEWT 0.30 mM - IS 50mM phosphate pH8 T27C Kaplan_2001_Biochemistry_40_7433
human-ACHEWT 2.5 mM - 50mM NaPhosphate pH7.4 Loewenstein-Lichtenstein_1996_Mol.Pharmacol_50_1423

Substrate: Butyrylthiocholine
Gene_LocusEnzymeKmKcatExp. conditionsReference
human-ACHEY72N/Y124Q 0.25 mM 0.20 10+5/min IS 50mM phosphate pH8 T27C Kaplan_2001_Biochemistry_40_7433
human-ACHEWT 0.30 mM 0.08 10+5/min IS 50mM phosphate pH8 T27C Kaplan_2001_Biochemistry_40_7433
human-ACHEWT 2.5 mM 70000 /min 50mM NaPhosphate pH7.4 Loewenstein-Lichtenstein_1996_Mol.Pharmacol_50_1423
human-BCHEWT 7 & 0.7 uM 24000 & 10000 /min 100mM K phosphate pH7.0 T25C Blong_1997_Biochem.J_327_747
human-BCHEWT 2.2 mM - 100mM Na phosphate pH7.4 T22C Gnatt_1994_J.Neurochem_62_749
human-BCHEWT 0.05 mM 1.1 10+5 /min IS 50mM phosphate pH8 T27C Kaplan_2001_Biochemistry_40_7433
human-BCHEWT 2.8 & 0.7 mM 98000 & 33000 /min 50mM NaPhosphate pH7.4 Loewenstein-Lichtenstein_1996_Mol.Pharmacol_50_1423
mouse-ACHEWT 93 uM 1100 /min 100mM NaPhosphate Ph7.0 T22C Hosea_1995_Biochemistry_34_11528
mouse-BCHEWT 55 uM 37000 /min 100mM NaPhosphate Ph7.0 T22C Hosea_1995_Biochemistry_34_11528


Inhibitors

Inhibitor: BW284C51
Gene_LocusEnzymeKiKsiIc50SubstrateExp. conditionsReference
human-ACHEY72A/Y124A 355 nM - - Acetylthiocholine 50mM Na phosphate pH8 Barak_1994_J.Biol.Chem_269_6296
mouse-ACHEY72N/Y124Q 190 & 80 nM 460 & 130 nM - Acetylthiocholine 100mM NaP pH7.0 T22C eq3.gif sch3.gif Radic_1993_Biochemistry_32_12074
bunfa-ACHEWT 16.9 & 1.6 nM 28.9 & 0.8 nM - Acetylthiocholine T25C IS 50 mM phosphate Cousin_1996_J.Biol.Chem_271_15099
chick-ACHEWT 240 nM - - Acetylthiocholine 100mM NaCl 50mM Tris pH7.4 Eichler_1994_Mol.Pharmacol_45_335
human-ACHEWT 10 nM - - Acetylthiocholine 50mM Na phosphate pH8 Barak_1994_J.Biol.Chem_269_6296
human-ACHEWT 170000 nM - - Acetylthiocholine T25C IS 50 mM phosphate Kaplan_2001_Biochemistry_40_7433
human-ACHEWT 0.13 uM - - Butyrylthiocholine 50mM NaPhosphate pH7.4 Loewenstein-Lichtenstein_1996_Mol.Pharmacol_50_1423
human-ACHEWT - - 50 nM Acetylthiocholine pH8 T27C 50mM Na phosphate Shafferman_1992_EMBO.J_11_3561
human-BCHEWT 14000 nM - - Acetylthiocholine T25C IS 50 mM phosphate Kaplan_2001_Biochemistry_40_7433
mouse-ACHEWT 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-BCHEWT 11300 & 400 nM 42000000 & 5000000 nM - Acetylthiocholine 100mM NaP pH7.0 T22C eq3.gif sch3.gif Radic_1993_Biochemistry_32_12074
torma-ACHEWT 15.1 & 0.7 nM 63.6 & 8.4 nM - Acetylthiocholine T25C IS 50 mM phosphate Cousin_1996_J.Biol.Chem_271_15099
torma-ACHEWT 2 nM - - Acetylthiocholine 100mM NaCl 50mM Tris pH7.4 Eichler_1994_Mol.Pharmacol_45_335
human-BCHEWT 480 & 110 uM - - Butyrylthiocholine 50mM NaPhosphate pH7.4 Loewenstein-Lichtenstein_1996_Mol.Pharmacol_50_1423

Inhibitor: Decamethonium
Gene_LocusEnzymeKiKsiIc50SubstrateExp. conditionsReference
human-ACHEY72A/Y124A 22 uM - - Acetylthiocholine 50mM Na phosphate pH8 Barak_1994_J.Biol.Chem_269_6296
human-ACHEY72N/Y124Q 200 uM - - Acetylthiocholine T25C IS 50 mM phosphate Kaplan_2001_Biochemistry_40_7433
mouse-ACHEY72N/Y124Q 130 & 14 uM 510 & 180 uM - Acetylthiocholine 100mM NaP pH7.0 T22C eq3.gif sch3.gif Radic_1993_Biochemistry_32_12074
bunfa-ACHEWT 8.2 & 1.2 uM 47.5 & 3.5 uM - Acetylthiocholine T25C IS 50 mM phosphate Cousin_1996_J.Biol.Chem_271_15099
chick-ACHEWT 23.6 uM - - Acetylthiocholine 100mM NaCl 50mM Tris pH7.4 Eichler_1994_Mol.Pharmacol_45_335
human-ACHEWT 6 uM - - Acetylthiocholine 50mM Na phosphate pH8 Barak_1994_J.Biol.Chem_269_6296
human-ACHEWT 360 uM - - Acetylthiocholine T25C IS 50 mM phosphate Kaplan_2001_Biochemistry_40_7433
human-ACHEWT 6.0 uM 5.7 uM - Acetylthiocholine 5 or 50mM Na Phosphate pH8 T27C Ordentlich_1995_J.Biol.Chem_270_2082
human-ACHEWT - - 8.5 uM Acetylthiocholine pH8 T27C 50mM Na phosphate Shafferman_1992_EMBO.J_11_3561
human-BCHEWT 2.5 uM - - Acetylthiocholine T25C IS 50 mM phosphate Kaplan_2001_Biochemistry_40_7433
mouse-ACHEWT 3.5 & 1.6 uM 31 & 16 uM - Acetylthiocholine 100mM NaP pH7.0 T22C eq3.gif sch3.gif Radic_1993_Biochemistry_32_12074
mouse-BCHEWT 10 & 1.1 uM 42 & 25 uM - Acetylthiocholine 100mM NaP pH7.0 T22C eq3.gif sch3.gif Radic_1993_Biochemistry_32_12074
torma-ACHEWT 1.3 & 0.2 uM 7.0 & 1.3 uM - Acetylthiocholine T25C IS 50 mM phosphate Cousin_1996_J.Biol.Chem_271_15099
torma-ACHEWT 0.34 uM - - Acetylthiocholine 100mM NaCl 50mM Tris pH7.4 Eichler_1994_Mol.Pharmacol_45_335
human-BCHEWT - - 13 uM   Lockridge_1990_Pharmacol.Ther_47_35

Inhibitor: Edrophonium
Gene_LocusEnzymeKiKsiIc50SubstrateExp. conditionsReference
human-ACHEY72A/Y124A 0.2 uM - - Acetylthiocholine 50mM Na phosphate pH8 Barak_1994_J.Biol.Chem_269_6296
human-ACHEY72N/Y124Q 1.1 uM - - Acetylthiocholine T25C IS 50 mM phosphate Kaplan_2001_Biochemistry_40_7433
human-ACHEWT 0.6 & 0.1 uM - - 3.3-dimethylbutylthioacetate 50mM NaPhosphate pH8 Kronman_1994_J.Biol.Chem_269_27819
bunfa-ACHEWT 0.6 & 0.0 uM 9.9 & 4.2 uM - Acetylthiocholine T25C IS 50 mM phosphate Cousin_1996_J.Biol.Chem_271_15099
chick-ACHEWT 0.23 uM - - Acetylthiocholine 100mM NaCl 50mM Tris pH7.4 Eichler_1994_Mol.Pharmacol_45_335
human-ACHEWT 0.75 uM - - Acetylthiocholine 50mM Na phosphate pH8 Barak_1994_J.Biol.Chem_269_6296
human-ACHEWT 50 uM - - Acetylthiocholine T25C IS 50 mM phosphate Kaplan_2001_Biochemistry_40_7433
human-ACHEWT 0.7 & 0.1 uM - - Acetylthiocholine 50mM NaPhosphate pH8 Kronman_1994_J.Biol.Chem_269_27819
human-ACHEWT 0.3 uM - - Acetylthiocholine IS 50mM phosphate pH8 T27C Ordentlich_1993_J.Biol.Chem_268_17083
human-ACHEWT 0.6 uM 4.8 uM - Acetylthiocholine 5 or 50mM Na Phosphate pH8 T27C Ordentlich_1995_J.Biol.Chem_270_2082
human-ACHEWT - - 1.5 uM Acetylthiocholine pH8 T27C 50mM Na phosphate Shafferman_1992_EMBO.J_11_3561
human-ACHEWT 0.32 & 0.05 uM - - Acetylthiocholine IS 5mM Shafferman_1994_EMBO.J_13_3448
human-BCHEWT 50 uM - - Acetylthiocholine T25C IS 50 mM phosphate Kaplan_2001_Biochemistry_40_7433
mouse-ACHEWT 0.30 & 0.1O uM 6.4 & 0.6 uM - Acetylthiocholine 100mM NaP pH7.0 T22C Radic_1993_Biochemistry_32_12074
mouse-BCHEWT 110 & 37 uM 1400 & 700 uM - Acetylthiocholine 100mM NaP pH7.0 T22C Radic_1993_Biochemistry_32_12074
torma-ACHEWT 0.3 & 0.0 uM - - Acetylthiocholine T25C IS 50 mM phosphate Cousin_1996_J.Biol.Chem_271_15099
torma-ACHEWT 0.15 uM - - Acetylthiocholine 100mM NaCl 50mM Tris pH7.4 Eichler_1994_Mol.Pharmacol_45_335
human-ACHEWT 0.4 uM - - Paranitrophenylacetate IS 50mM phosphate pH8 T27C Ordentlich_1993_J.Biol.Chem_268_17083
human-ACHEWT 0.24 uM - - S-N-Propylthioacetate IS 50mM phosphate pH8 T27C Ordentlich_1993_J.Biol.Chem_268_17083

Inhibitor: Hexamethonium
Gene_LocusEnzymeKiKsiIc50SubstrateExp. conditionsReference
human-ACHEY72A/Y124A 0.2 mM - - Acetylthiocholine 50mM Na phosphate pH8 Barak_1994_J.Biol.Chem_269_6296
chick-ACHEWT 242 uM - - Acetylthiocholine 100mM NaCl 50mM Tris pH7.4 Eichler_1994_Mol.Pharmacol_45_335
human-ACHEWT 0.2 mM - - Acetylthiocholine 50mM Na phosphate pH8 Barak_1994_J.Biol.Chem_269_6296
torma-ACHEWT 84 uM - - Acetylthiocholine 100mM NaCl 50mM Tris pH7.4 Eichler_1994_Mol.Pharmacol_45_335

Inhibitor: HuperzineA
Gene_LocusEnzymeKiKsiIc50SubstrateExp. conditionsReference
human-ACHEY72N/Y124Q 90 nM - - Acetylthiocholine T25C IS 50 mM phosphate Kaplan_2001_Biochemistry_40_7433
human-ACHEWT 16 & 1 nM 12 & 4 nM - Acetylthiocholine 50mM Na phosphate pH8 T22C Ariel_1998_Biochem.J_335_95
human-ACHEWT 16 nM - - Acetylthiocholine T25C IS 50 mM phosphate Kaplan_2001_Biochemistry_40_7433
human-BCHEWT 50000 nM - - Acetylthiocholine T25C IS 50 mM phosphate Kaplan_2001_Biochemistry_40_7433

Inhibitor: Propidium
Gene_LocusEnzymeKiKsiIc50SubstrateExp. conditionsReference
human-ACHEY72A/Y124A 7 uM - - Acetylthiocholine 50mM Na phosphate pH8 Barak_1994_J.Biol.Chem_269_6296
mouse-ACHEY72N/Y124Q 35 & 7 uM 120 & 44 uM - Acetylthiocholine 100mM NaP pH7.0 T22C eq3.gif sch3.gif Radic_1993_Biochemistry_32_12074
bunfa-ACHEWT 46.0 & 3.6 uM 250.0 & 60.0 uM - Acetylthiocholine T25C IS 50 mM phosphate Cousin_1996_J.Biol.Chem_271_15099
chick-ACHEWT >1000 uM - - Acetylthiocholine 100mM NaCl 50mM Tris pH7.4 Eichler_1994_Mol.Pharmacol_45_335
human-ACHEWT 1.4 uM - - Acetylthiocholine 50mM Na phosphate pH8 Barak_1994_J.Biol.Chem_269_6296
human-ACHEWT 0.6 uM 0.9 uM - Acetylthiocholine 5 or 50mM Na Phosphate pH8 T27C Ordentlich_1995_J.Biol.Chem_270_2082
human-ACHEWT - - 1.5 uM Acetylthiocholine pH8 T27C 50mM Na phosphate Shafferman_1992_EMBO.J_11_3561
mouse-ACHEWT 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-BCHEWT 5.3 & 1.8 uM 26 & 18 uM - Acetylthiocholine 100mM NaP pH7.0 T22C eq3.gif sch3.gif Radic_1993_Biochemistry_32_12074
torma-ACHEWT 2.0 & 0.2 uM 3.6 & 0.4 uM - Acetylthiocholine T25C IS 50 mM phosphate Cousin_1996_J.Biol.Chem_271_15099
torma-ACHEWT 2.8 uM - - Acetylthiocholine 100mM NaCl 50mM Tris pH7.4 Eichler_1994_Mol.Pharmacol_45_335

Inhibitor: Tacrine
Gene_LocusEnzymeKiKsiIc50SubstrateExp. conditionsReference
human-ACHEY72N/Y124Q 55 nM - - Acetylthiocholine T25C IS 50 mM phosphate Kaplan_2001_Biochemistry_40_7433
human-ACHEWT 85 & 12 nM 90 & 20 nM - Acetylthiocholine 50mM Na phosphate pH8 T22C Ariel_1998_Biochem.J_335_95
human-ACHEWT 12 nM - - Acetylthiocholine T25C IS 50 mM phosphate Kaplan_2001_Biochemistry_40_7433
human-ACHEWT 0.21 uM - - Acetylthiocholine 50mM NaPhosphate pH7.4 Loewenstein-Lichtenstein_1996_Mol.Pharmacol_50_1423
human-BCHEWT 12 nM - - Acetylthiocholine T25C IS 50 mM phosphate Kaplan_2001_Biochemistry_40_7433
mouse-ACHEWT 40 & 10 nM 130 & 50 nM - Acetylthiocholine 100mM NaP pH7.0 T22C Radic_1993_Biochemistry_32_12074
mouse-BCHEWT 17 & 4 nM 47 & 22 nM - Acetylthiocholine 100mM NaP pH7.0 T22C Radic_1993_Biochemistry_32_12074
human-BCHEWT 0.06 & 0.03 uM - - Butyrylthiocholine 50mM NaPhosphate pH7.4 Loewenstein-Lichtenstein_1996_Mol.Pharmacol_50_1423

Inhibitor: WT-fasciculin2
Gene_LocusEnzymeKiKsiIc50SubstrateExp. conditionsReference
mouse-ACHEY72N/Y124Q - 95 & 10 nM - Acetylthiocholine 100mM NaP pH7.0 T37C eq4 sch4 meth6 Radic_1994_J.Biol.Chem_269_11233
bunfa-ACHEWT - 50.7 & 2.6 nM - Acetylthiocholine T25C IS 50 mM phosphate Cousin_1996_J.Biol.Chem_271_15099
mouse-ACHEWT - 2.3 & 0.6 pM - Acetylthiocholine 50mM NaP pH8.0 Marchot_1997_J.Biol.Chem_272_3502
mouse-ACHEWT - 6.3 pM - Acetylthiocholine 100mM NaP pH7.0 T37C eq4 sch4 meth5 Radic_1994_J.Biol.Chem_269_11233
mouse-BCHEWT - 290000 & 30000 nM - Acetylthiocholine 100mM NaP pH7.0 T37C eq4 sch4 meth6 Radic_1994_J.Biol.Chem_269_11233
torma-ACHEWT - 0.14 & 0.04 nM - Acetylthiocholine T25C IS 50 mM phosphate Cousin_1996_J.Biol.Chem_271_15099

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