donepezil [Ligand Id: 6599] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL502 (Aricept, D-797, Donaz, Donepezil, E-2020)
  • Acetylcholinesterase in Torpedo californica [ChEMBL: CHEMBL4780] [UniProtKB: P04058]
  • Acetylcholinesterase in Electrophorus electricus [ChEMBL: CHEMBL4078] [UniProtKB: O42275]
  • acetylcholinesterase (Yt blood group)/Acetylcholinesterase in Human [ChEMBL: CHEMBL220] [GtoPdb: 2465] [UniProtKB: P22303]
  • Acetylcholinesterase in Bovine [ChEMBL: CHEMBL4768] [UniProtKB: P23795]
  • acetylcholinesterase (Yt blood group)/Acetylcholinesterase in Mouse [ChEMBL: CHEMBL3198] [GtoPdb: 2465] [UniProtKB: P21836]
  • acetylcholinesterase (Yt blood group)/Acetylcholinesterase in Rat [ChEMBL: CHEMBL3199] [GtoPdb: 2465] [UniProtKB: P37136]
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  • carboxylesterase 1/Acyl coenzyme A:cholesterol acyltransferase in Human [ChEMBL: CHEMBL2265] [GtoPdb: 2592] [UniProtKB: P23141]
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  • beta-secretase 1/Beta-secretase 1 in Human [ChEMBL: CHEMBL4822] [GtoPdb: 2330] [UniProtKB: P56817]
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  • butyrylcholinesterase/Butyrylcholinesterase in Human [ChEMBL: CHEMBL1914] [GtoPdb: 2471] [UniProtKB: P06276]
  • Butyrylcholinesterase in Equus caballus [ChEMBL: CHEMBL5077] [UniProtKB: Q9N1N9]
  • butyrylcholinesterase/Butyrylcholinesterase in Mouse [ChEMBL: CHEMBL2528] [GtoPdb: 2471] [UniProtKB: Q03311]
  • Butyrylcholinesterase in Rat [ChEMBL: CHEMBL3403] [UniProtKB: Q9JKC1]
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  • choline O-acetyltransferase/Choline acetylase in Rat [ChEMBL: CHEMBL3945] [GtoPdb: 2480] [UniProtKB: P32738]
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  • glycogen synthase kinase 3 beta/Glycogen synthase kinase-3 beta in Human [ChEMBL: CHEMBL262] [GtoPdb: 2030] [UniProtKB: P49841]
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  • H3 receptor/Histamine H3 receptor in Human [ChEMBL: CHEMBL264] [GtoPdb: 264] [UniProtKB: Q9Y5N1]
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  • phosphodiesterase 5A/Phosphodiesterase 5A in Human [ChEMBL: CHEMBL1827] [GtoPdb: 1304] [UniProtKB: O76074]
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  • sigma non-opioid intracellular receptor 1/Sigma opioid receptor in Human [ChEMBL: CHEMBL287] [GtoPdb: 2552] [UniProtKB: Q99720]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
Acetylcholinesterase in Torpedo californica (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4780] [UniProtKB: P04058]
ChEMBL In vitro inhibition of Torpedo californica acetylcholinesterase. B 7.32 pIC50 48 nM IC50 J Med Chem (1999) 42: 730-741 [PMID:10052979]
ChEMBL Inhibition of Torpedo californica AChE (type VI-S) using acetylthiocholine iodide as substrate assessed as 5-thio-2-nitrobenzoate anion formation preincubated for 15 mins followed by substrate addition B 7.64 pIC50 23 nM IC50 Eur J Med Chem (2015) 103: 361-369 [PMID:26363872]
ChEMBL Compound was evaluated for the inhibition of acetylcholinesterase (AChE) in Torpedo californica B 7.92 pIC50 12 nM IC50 Bioorg Med Chem Lett (1998) 8: 575-580 [PMID:9871563]
Acetylcholinesterase in Electrophorus electricus (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4078] [UniProtKB: O42275]
ChEMBL Non competitive inhibition of electric eel AChE using acetylthiocholine iodide as substrate by Lineweaver-Burk plot analysis B 7.25 pKi 56 nM Ki Bioorg Med Chem (2013) 21: 5451-5460 [PMID:23810675]
ChEMBL Non-competitive inhibition of Electrophorus electricus AChE using acetylthiocholine iodide as substrate pretreated for 10 mins followed by substrate addition measured at 12 secs interval for 5 mins by Ellman's method B 7.42 pKi 38 nM Ki Eur J Med Chem (2017) 130: 440-457 [PMID:28282613]
ChEMBL Inhibition of electric eel AChE assessed as inhibition constant using acetylthiocholine iodide as substrate pretreated for 5 mins followed by substrate addition measured for 5 mins by Dixon plot analysis B 7.79 pKi 16.4 nM Ki Eur J Med Chem (2019) 174: 116-129 [PMID:31029943]
ChEMBL Inhibition of electric eel AChE pre-incubated for 3 mins before acetylthiocholine substrate addition by Lineweaver-Burk plot B 8.37 pKi 4.24 nM Ki Eur J Med Chem (2015) 97: 181-189 [PMID:25969170]
ChEMBL Inhibition of electric eel AChE using acetylthiocholine iodide as substrate preincubated for 5 mins by Ellman method B 4.58 pIC50 26100 nM IC50 Bioorg Med Chem (2015) 23: 2445-2457 [PMID:25868744]
ChEMBL Inhibition of electric eel AChE by Ellman's method B 5.14 pIC50 7230 nM IC50 Bioorg Med Chem (2014) 22: 6163-6173 [PMID:25257911]
ChEMBL Inhibition of electric eel AChE using acetylthiocholine iodide as substrate preincubated for 15 mins followed by substrate addition and measured after 15 mins under dark condition by Ellman's method B 5.55 pIC50 2800 nM IC50 Bioorg Med Chem (2019) 27: 4030-4040 [PMID:31378596]
ChEMBL Inhibition of electric eel AChE using acetylthiocholine iodide as substrate incubated for 15 to 20 mins by Ellman's method B 6.32 pIC50 480 nM IC50 Bioorg Med Chem Lett (2021) 52: 128306-128306 [PMID:34371131]
ChEMBL Inhibition of electric eel AChE using acetylthiocholine iodide as substrate preincubated for 10 mins followed by substrate addition and measured for 15 mins by Ellman's method B 6.6 pIC50 250 nM IC50 Eur J Med Chem (2022) 229: 114044-114044 [PMID:34923430]
ChEMBL Inhibition of electric eel AChE using acetylthiocholine iodide as substrate preincubated for 15 mins followed by substrate addition and measured for 5 mins by Ellmans method B 6.66 pIC50 219.7 nM IC50 Eur J Med Chem (2016) 124: 1026-1040 [PMID:27783974]
ChEMBL Inhibition of Electrophorus electricus AChE by Ellman's method B 6.92 pIC50 120 nM IC50 Bioorg Med Chem Lett (2009) 19: 5075-5077 [PMID:19643609]
ChEMBL Inhibition of electric eel AchE using acetylthiocholine iodide as substrate after 15 mins by Ellman's method B 6.92 pIC50 120 nM IC50 Eur J Med Chem (2014) 76: 314-331 [PMID:24589487]
ChEMBL Inhibition of electric eel AChE using acetylthiocholine iodide as substrate after 15 mins by Ellman method B 6.96 pIC50 110 nM IC50 Bioorg Med Chem (2015) 23: 911-923 [PMID:25678013]
ChEMBL Inhibition of Electrophorus electricus brain AChE by Ellman's method B 6.96 pIC50 110 nM IC50 Bioorg Med Chem (2008) 16: 8011-8021 [PMID:18701305]
ChEMBL Inhibition of electric eel AChE using acetylthiocholine iodide as substrate after 15 mins by Ellman's method B 6.96 pIC50 110 nM IC50 Eur J Med Chem (2015) 94: 348-366 [PMID:25778991]
ChEMBL Inhibition of electric eel AChE using acetylthiocholine iodide as substrate preincubated for 15 mins followed by substrate addition and measured for 45 mins by Ellmans microplate assay B 7 pIC50 100 nM IC50 Bioorg Med Chem (2018) 26: 1511-1522 [PMID:29429576]
ChEMBL Inhibition of electric eel AChE using ACTI as substrate preincubated for 29 mins followed by substrate addition measured at 1 min intervals for 10 mins by Ellman's assay B 7.02 pIC50 96 nM IC50 J Med Chem (2016) 59: 7683-7689 [PMID:27405689]
ChEMBL Inhibition of electric eel AChE using acetylthiocholine iodide as substrate pretreated for 10 mins followed by substrate addition measured after 20 mins by Ellman's method B 7.05 pIC50 90 nM IC50 Bioorg Med Chem (2018) 26: 3696-3706 [PMID:29886083]
ChEMBL Inhibition of Electrophorus electricus AChE using acetylthiocholine iodide as substrate after 30 mins by Ellman's method B 7.05 pIC50 90 nM IC50 Medchemcomm (2012) 3: 1098-1103
ChEMBL Inhibition of Electrophorus electricus AChE using acetylthiocholine iodide as substrate by Ellman's method B 7.1 pIC50 80 nM IC50 Eur J Med Chem (2019) 179: 680-693 [PMID:31280020]
ChEMBL Inhibition of electric eel AChE using acetylthiocholine iodide as substrate preincubated for 15 mins followed by substrate addition measured for 5 mins by UV spectrophotometric analysis B 7.17 pIC50 67 nM IC50 Eur J Med Chem (2017) 139: 612-632 [PMID:28841514]
ChEMBL Inhibition of electric eel AChE using acetylthiocholine iodide as substrate preincubated for 10 mins followed by substrate addition and measured for 10 mins by Ellman's method B 7.21 pIC50 62 nM IC50 Eur J Med Chem (2021) 212: 113124-113124 [PMID:33395623]
ChEMBL Inhibition of electric eel AChE using thiocholine iodide as substrate by Ellman's method B 7.22 pIC50 59.9 nM IC50 Bioorg Med Chem Lett (2015) 25: 5212-5216 [PMID:26454504]
ChEMBL Inhibition of electric eel AChE using acetylthiocholine iodide as substrate preincubated for 5 mins followed by substrate addition measured for 10 mins by modified Ellman's method B 7.24 pIC50 57 nM IC50 Bioorg Med Chem (2016) 24: 2352-2359 [PMID:27083471]
ChEMBL Inhibition of electric eel AChE using acetylthiocholine iodide as substrate preincubated for 5 mins followed by substrate addition measured up to 3 mins by Ellman's method B 7.29 pIC50 51 nM IC50 Eur J Med Chem (2016) 123: 282-297 [PMID:27484514]
ChEMBL Inhibition of electric eel AChE using acetylthiocholine iodide as substrate preincubated for 2 mins followed by substrate addition and measured after 2 mins by Ellman's method B 7.3 pIC50 50 nM IC50 Bioorg Med Chem (2018) 26: 3812-3824 [PMID:29960728]
ChEMBL Inhibition of electric eel AChE using acetylthiocholine iodide as substrate by Ellman's method B 7.3 pIC50 50 nM IC50 Eur J Med Chem (2017) 127: 671-690 [PMID:27823887]
ChEMBL Inhibition of electric eel AChE using acetylthiocholine chloride as substrate incubated for 5 mins followed by substrate addition measured after 180 secs by Ellman's method B 7.3 pIC50 50 nM IC50 Eur J Med Chem (2018) 157: 161-176 [PMID:30096650]
ChEMBL Inhibition of electric eel AChE using acetylthiocholine as substrate preincubated for 8 mins followed by substrate addition by Ellman's method B 7.3 pIC50 50 nM IC50 Bioorg Med Chem Lett (2016) 26: 5573-5579 [PMID:27769620]
ChEMBL Inhibition of electric eel AChE using DTNB as substrate incubated for 5 mins prior to substrate addition measured after 2 mins by Ellman's method B 7.31 pIC50 49 nM IC50 Bioorg Med Chem (2015) 23: 6389-6403 [PMID:26337018]
ChEMBL Inhibition of electric eel Ache using acetylthiocholine iodide as substrate preincubated for 5 mins followed by substrate addition and measured after 5 mins by Ellman method B 7.31 pIC50 49 nM IC50 Bioorg Med Chem (2019) 27: 3156-3166 [PMID:31176571]
ChEMBL Inhibition of electric eel AChE using acetylthiocholine iodide as substrate preincubated for 20 mins followed by substrate addition and measured every minute for 10 mins by DTNB-reagent based Ellman's method B 7.31 pIC50 49 nM IC50 Eur J Med Chem (2020) 207: 112761-112761 [PMID:32942070]
ChEMBL Inhibition of electric eel AChE using acetylthiocholine iodide as substrate preincubated for 5 mins followed by substrate addition measured after 5 mins by Ellman's method B 7.31 pIC50 49 nM IC50 Eur J Med Chem (2019) 175: 2-19 [PMID:31055149]
ChEMBL In vitro inhibition of electric eel acetylcholinesterase B 7.32 pIC50 48 nM IC50 J Med Chem (2001) 44: 2707-2718 [PMID:11495583]
ChEMBL Inhibition of electric eel AChE using acetylthiocholine iodide as substrate incubated for 5 mins by Ellman's method B 7.32 pIC50 48 nM IC50 Bioorg Med Chem (2015) 23: 1135-1148 [PMID:25624107]
ChEMBL Inhibition of electric eel AChE using acetylthiocholine iodide as substrate preincubated for 6 mins followed by substrate addition measured up to 180 secs by Ellman's method B 7.32 pIC50 47.4 nM IC50 Eur J Med Chem (2017) 139: 48-59 [PMID:28797883]
ChEMBL Inhibition of electric eel AChE using acetylthiocholine iodide as substrate preincubated for 5 mins followed by substrate addition measured after 2 mins by spectroscopy based Ellman's method B 7.33 pIC50 47 nM IC50 Eur J Med Chem (2017) 136: 36-51 [PMID:28478343]
ChEMBL Inhibition of electric eel AChE using acetylthiocholine iodide as substrate preincubated for 15 mins by Ellman's method B 7.38 pIC50 42 nM IC50 Bioorg Med Chem Lett (2015) 25: 5576-5582 [PMID:26514744]
ChEMBL Inhibition of electric eel AChE using acetylthiocholine iodide as substrate preincubated with enzyme for 5 mins prior to substrate addition measured after 5 mins by Ellman's method B 7.39 pIC50 41.1 nM IC50 Eur J Med Chem (2020) 185: 111785-111785 [PMID:31669851]
ChEMBL Inhibition of electric eel acetylcholinesterase using acetylthiocholine chloride as substrate preincubated for 15 mins followed by substrate addition by Ellman's method B 7.39 pIC50 41 nM IC50 Bioorg Med Chem (2014) 22: 1355-1361 [PMID:24461494]
ChEMBL Inhibition of electric eel AChE using acetylthiocholine iodide as substrate preincubated for 20 mins prior to substrate addition by Ellman's method B 7.39 pIC50 40.74 nM IC50 Bioorg Med Chem (2013) 21: 5451-5460 [PMID:23810675]
ChEMBL Inhibition of electric eel AChE using acetylthiocholine iodide as substrate pretreated for 6 mins followed by substrate addition measured up to 180 sec by Ellman's method B 7.4 pIC50 40.2 nM IC50 Eur J Med Chem (2017) 133: 184-196 [PMID:28388521]
ChEMBL Inhibition of electric eel AChE using acetylthiocholine iodide as substrate preincubated for 20 mins followed by substrate addition by Ellman's method B 7.4 pIC50 40 nM IC50 Bioorg Med Chem (2017) 25: 1471-1480 [PMID:28126439]
ChEMBL Inhibition of electric eel ACHE preincubated for 6 mins followed by addition of acetylcholine iodide as substrate by Ellman's method B 7.4 pIC50 40 nM IC50 Bioorg Med Chem (2016) 24: 4324-4338 [PMID:27460699]
ChEMBL Inhibition of electric eel AChE using acetylthiocholine iodide as substrate preincubated for 20 mins prior to substrate addition by Ellman's method B 7.4 pIC50 40 nM IC50 Bioorg Med Chem (2013) 21: 5451-5460 [PMID:23810675]
ChEMBL Inhibition of electric eel AChE using acetylthiocholine iodide as substrate preincubated for 6 mins followed by substrate addition measured up to 180 secs by spectrophotometric-based Ellman's method B 7.4 pIC50 40 nM IC50 Bioorg Med Chem (2016) 24: 1528-1539 [PMID:26917219]
ChEMBL Inhibition of electric eel AChE using acetylcholine iodide as substrate incubated for 20 mins prior to substrate addition by Ellman method B 7.4 pIC50 40 nM IC50 Bioorg Med Chem Lett (2013) 23: 2984-2989 [PMID:23562059]
ChEMBL Inhibition of Electric eel AChE using acetylthiocholine iodide as substrate after 10 mins measured for every mins by Ellman's method B 7.4 pIC50 40 nM IC50 Eur J Med Chem (2019) 163: 116-135 [PMID:30503937]
ChEMBL Inhibition of electric eel AChE using acetylthiocholine iodide as substrate preincubated for 5 mins followed by substrate addition measured after 2 mins by Ellman's method B 7.41 pIC50 39 nM IC50 Bioorg Med Chem (2016) 24: 3829-3841 [PMID:27353888]
ChEMBL Inhibition of electric eel AChE by Ellman's method B 7.41 pIC50 39 nM IC50 Bioorg Med Chem Lett (2020) 30: 127477-127477 [PMID:32781220]
ChEMBL Inhibition of Electric eel AChE using acetylthiocholine iodide as substrate preincubated for 5 mins followed by substrate addition measured after 2 mins by Ellman's method B 7.41 pIC50 39 nM IC50 Eur J Med Chem (2017) 125: 736-750 [PMID:27721157]
ChEMBL Inhibition of electric eel AChE preincubated for 15 mins by Ellman's method B 7.42 pIC50 38.2 nM IC50 Eur J Med Chem (2014) 87: 429-439 [PMID:25282266]
ChEMBL Inhibition of electric eel AChE using acetylthiocholine chloride as substrate preincubated for 15 mins followed by substrate addition measured every 1 min by Ellman's method B 7.42 pIC50 38 nM IC50 J Med Chem (2013) 56: 9089-9099 [PMID:24160297]
ChEMBL Inhibition of electric eel AChE preincubated for 5 mins followed by addition of acetylthiocholine iodide as substrate measured after 2 mins by Ellman's method B 7.42 pIC50 38 nM IC50 Eur J Med Chem (2016) 119: 260-277 [PMID:27227482]
ChEMBL Inhibition of electric eel AchE using acetylthiocholine iodide as substrate incubated for 5 mins followed by substrate addition and measured after 2 mins by Ellman's method B 7.42 pIC50 38 nM IC50 Bioorg Med Chem (2016) 24: 2777-2788 [PMID:27157006]
ChEMBL Inhibition of electric eel AChE using acetylthiocholine iodide as substrate preincubated for 5 mins followed by substrate addition measured after 5 mins by Ellman's method B 7.42 pIC50 38 nM IC50 Eur J Med Chem (2016) 107: 219-232 [PMID:26588065]
ChEMBL Inhibition of electric eel AChE using acetylthiocholine iodide as substrate preincubated for 15 mins followed by substrate addition by spectrophotometric analysis B 7.43 pIC50 37 nM IC50 Bioorg Med Chem (2017) 25: 2946-2955 [PMID:28454848]
ChEMBL Inhibition of electric eel acetylcholinesterase preincubated for 5 mins followed by addition of acetylthiocholine iodide as substrate measured after 60 to 120 mins by Ellmans method B 7.46 pIC50 35 nM IC50 Medchemcomm (2016) 7: 990-998
ChEMBL Inhibition of electric eel AChE using acetylthiocholine iodide as substrate preincubated with enzyme for 10 mins prior to substrate challenge measured after 15 mins by Ellman's method B 7.48 pIC50 33 nM IC50 Bioorg Med Chem (2014) 22: 2496-2507 [PMID:24657052]
ChEMBL Inhibition of electric eel AChE using acetylthiocholine iodide as substrate preincubated with enzyme for 6 mins followed by substrate addition and measured for 180 secs by Ellman's method B 7.49 pIC50 32 nM IC50 RSC Med Chem (2020) 11: 225-233 [PMID:33479629]
ChEMBL Inhibition of electric eel AChE using acetylthiocholine iodide as substrate measured for 6 mins by Ellman's method B 7.51 pIC50 31 nM IC50 Bioorg Med Chem (2017) 25: 3980-3988 [PMID:28587871]
ChEMBL Inhibition of electric eel acetylcholinesterase using acetylthiocholine iodide as substrate preincubated for 10 mins before substrate addition after 15 mins by Ellman's method B 7.52 pIC50 30 nM IC50 Eur J Med Chem (2014) 78: 167-177 [PMID:24681981]
ChEMBL Inhibition of electric eel acetylcholinesterase using acetylthiocholine iodide as substrate preincubated for 10 mins before substrate addition after 15 mins by Ellman's method B 7.52 pIC50 30 nM IC50 Eur J Med Chem (2014) 78: 43-53 [PMID:24675179]
ChEMBL Inhibition of electric eel AChE assessed as reduction in production of H202 using acetylcholine as substrate incubated for 15 mins followed by substrate addition by horse radish peroxidase/Amplex red reagent based fluorescence assay B 7.52 pIC50 30 nM IC50 Eur J Med Chem (2019) 177: 221-234 [PMID:31151057]
ChEMBL Inhibition of electric eel AChE using acetylthiocholine as substrate preincubated for 5 mins followed by substrate addition measured after 20 mins by Ellman's method B 7.54 pIC50 29 nM IC50 Bioorg Med Chem Lett (2020) 30: 126900-126900 [PMID:31882295]
ChEMBL Inhibition of electric eel AChE preincubated for 15 mins followed by acetylthiocholine iodide substrate addition measured for 5 mins by Ellman's spectrophotometric method B 7.54 pIC50 28.7 nM IC50 Bioorg Med Chem Lett (2016) 26: 5387-5394 [PMID:27789142]
ChEMBL Inhibition of Electrophorus electricus AChE using acetylthiocholine iodide as substrate measured after 15 mins by Ellman's method B 7.56 pIC50 27.4 nM IC50 Eur J Med Chem (2017) 126: 762-775 [PMID:27951485]
ChEMBL Inhibition of electric eel AChE using acetylthiocholine iodide as substrate by Ellman's method B 7.57 pIC50 27 nM IC50 Eur J Med Chem (2021) 216: 113310-113310 [PMID:33667847]
ChEMBL Inhibition of electric eel AChE using acetylthiocholine iodide as substrate after 15 mins by Ellman's method B 7.57 pIC50 27 nM IC50 Eur J Med Chem (2017) 135: 307-323 [PMID:28458136]
ChEMBL Inhibition of Electrophorus electricus AChE using acetylcholine iodide as substrate incubated for 15 mins by Ellman's method B 7.58 pIC50 26.4 nM IC50 Bioorg Med Chem (2020) 28: 115400-115400 [PMID:32146060]
ChEMBL Inhibition of Electrophorus electricus AChE using acetylthiocholine iodide as substrate pretreated for 10 mins followed by substrate addition measured at 12 secs interval for 5 mins by Ellman's method B 7.59 pIC50 26 nM IC50 Eur J Med Chem (2017) 130: 440-457 [PMID:28282613]
ChEMBL Inhibition of electric eel AChE using acetylthiocholine iodide as substrate preincubated for 10 mins followed by substrate addition by Ellman's method B 7.59 pIC50 26 nM IC50 Eur J Med Chem (2018) 147: 48-65 [PMID:29421570]
ChEMBL Inhibition of electric eel acetylcholine esterase using acetylcholine chloride as substrate incubated for 15 mins prior to substrate addition measured every 1 min by Ellman's assay B 7.59 pIC50 26 nM IC50 Bioorg Med Chem Lett (2012) 22: 4462-4466 [PMID:22633691]
ChEMBL Inhibition of electric eel AChE using acetylthiocholine iodide as substrate preincubated with enzyme for 20 mins followed by substrate addition and measured after 20 mins by Ellman's method B 7.59 pIC50 26 nM IC50 Eur J Med Chem (2021) 223: 113735-113735 [PMID:34371367]
ChEMBL Inhibition of electric eel AChE using acetylthiocholine iodide as substrate incubated for 5 mins followed by substrate addition measured every minute for 5 mins by Ellman's method B 7.6 pIC50 25 nM IC50 Eur J Med Chem (2019) 174: 116-129 [PMID:31029943]
ChEMBL Inhibition of electric eel AChE using acetylthiocholine iodide as substrate preincubated with enzyme for 20 mins followed by substrate addition by Ellman's method B 7.6 pIC50 25 nM IC50 Eur J Med Chem (2019) 181: 111598-111598 [PMID:31415981]
ChEMBL Inhibition of Electrophorus electricus AChE using acetylthiocholine iodide as substrate incubated for 15 mins by Ellman's method B 7.6 pIC50 25 nM IC50 Bioorg Med Chem (2021) 35: 116074-116074 [PMID:33640707]
ChEMBL Inhibition of electric eel AChE using acetylthiocholine iodide as substrate by Ellman's method B 7.62 pIC50 24 nM IC50 Eur J Med Chem (2019) 161: 292-309 [PMID:30366255]
ChEMBL Inhibition of electric eel AChE using acetylthiocholine iodide as substrate preincubated for 10 mins followed by substrate addition measured for 5 mins by Ellman's method B 7.64 pIC50 23 nM IC50 Bioorg Med Chem (2018) 26: 4952-4962 [PMID:30190181]
ChEMBL Inhibition of Electrophorus electricus AChE using acetylthiocholine iodide as substrate measured after 15 mins by Ellman's method B 7.64 pIC50 23 nM IC50 Bioorg Med Chem (2018) 26: 1885-1895 [PMID:29500132]
ChEMBL Inhibition of electric eel AChE using acetylthiocholine iodide as substrate incubated for 15 mins by Ellman's method B 7.64 pIC50 23 nM IC50 Bioorg Med Chem (2019) 27: 895-930 [PMID:30744931]
ChEMBL Inhibition of electric eel AChE pre-incubated for 5 mins before acetylthiocholine iodide substrate addition and measured after 15 mins by Ellman's method B 7.64 pIC50 23 nM IC50 Bioorg Med Chem (2019) 27: 2914-2922 [PMID:31128990]
ChEMBL Inhibition of Electrophorus electricus AChE using acetylthiocholine iodide as substrate measured after 15 mins by Ellman's method B 7.65 pIC50 22.6 nM IC50 Bioorg Med Chem (2017) 25: 714-726 [PMID:27923535]
ChEMBL Inhibition of electric eel AChE using acetylthiocholine iodide as substrate measured after 15 mins by Ellman's method B 7.65 pIC50 22.6 nM IC50 Bioorg Med Chem (2017) 25: 1997-2009 [PMID:28237559]
ChEMBL Inhibition of electric eel AChE using acetylthiocholine iodide as substrate by spectrophotometer analysis B 7.66 pIC50 22 nM IC50 Eur J Med Chem (2014) 82: 536-544 [PMID:24941128]
ChEMBL Inhibition of electric eel AChE using acetylthiocholine iodide as substrate preincubated with enzyme for 30 mins followed by substrate addition and measured for 1 min by DTNB reagent-based spectrophotometric analysis B 7.66 pIC50 22 nM IC50 Eur J Med Chem (2019) 182: 111613-111613 [PMID:31437780]
ChEMBL Inhibition of electric eel AChE using acetylthiocholine iodide as substrate preincubated for 30 mins followed by substrate addition and measured for 20 mins at 1 min interval by Ellman's method B 7.68 pIC50 21.08 nM IC50 Eur J Med Chem (2018) 150: 87-101 [PMID:29524731]
ChEMBL Inhibition of electric eel AChE using acetylthiocholine iodide as substrate preincubated for 20 mins followed by substrate addition and measured upto 5 mins by Ellman's method B 7.68 pIC50 21 nM IC50 Eur J Med Chem (2019) 177: 414-424 [PMID:31158754]
ChEMBL Inhibition of electric eel AChE using acetylthiocholine iodide as substrate preincubated for 20 mins followed by substrate addition measured for 5 mins by spectrophotometric Ellman's method B 7.68 pIC50 21 nM IC50 J Med Chem (2016) 59: 6791-6806 [PMID:27347731]
ChEMBL Inhibition of electric eel AChE using acetylthiocholine iodide as substrate after 15 mins by Ellman's method B 7.68 pIC50 21 nM IC50 Bioorg Med Chem (2018) 26: 6115-6127 [PMID:30470598]
ChEMBL Inhibition of electric eel recombinant AChE preincubated for 1 min in presence of DNTB followed by addition of acetylthiocholine iodide substrate and measured after 20 mins by Ellman's method B 7.68 pIC50 21 nM IC50 Eur J Med Chem (2021) 223: 113663-113663 [PMID:34198150]
ChEMBL Inhibition of electric eel AChE using acetylthiocholine iodide as substrate preincubated for 5 mins before substrate addition measured for 10 mins by Ellman's method B 7.69 pIC50 20.3 nM IC50 Medchemcomm (2012) 3: 627-634
ChEMBL Inhibition of electric eel AChE using acetylthiocholine iodide as substrate pretreated for 5 mins followed by substrate addition by Ellman's method B 7.7 pIC50 20 nM IC50 Eur J Med Chem (2018) 152: 600-614 [PMID:29763808]
ChEMBL Inhibition of electric eel AChE using acetylthiocholine iodide as substrate preincubated for 20 mins followed by substrate addition measured for 5 mins by spectrophotometry based Ellman method B 7.7 pIC50 20 nM IC50 Bioorg Med Chem Lett (2017) 27: 1179-1185 [PMID:28189420]
ChEMBL Inhibition of electric eel AChE preincubated for 15 mins followed by addition of acetylthiocholine iodide substrate by Ellman's method-based spectrophotometric analysis B 7.7 pIC50 20 nM IC50 Bioorg Med Chem Lett (2016) 26: 2380-2382 [PMID:27017111]
ChEMBL Inhibition of electric eel AChE using acetylthiocholine chloride by spectrophotometry B 7.7 pIC50 20 nM IC50 Medchemcomm (2013) 4: 925-931
ChEMBL Inhibition of electric eel AChE using acetylthiocholine as substrate incubated for 15 mins by Ellman's method B 7.72 pIC50 19 nM IC50 Bioorg Med Chem Lett (2017) 27: 5046-5052 [PMID:29033233]
ChEMBL Inhibition of electric eel AChE using acetylthiocholine chloride as substrate after 15 mins by Ellman's method B 7.72 pIC50 19 nM IC50 Bioorg Med Chem (2017) 25: 3006-3017 [PMID:28487125]
ChEMBL Inhibition of electric eel AChE using acetylthiocholine chloride as substrate incubated for 15 mins by Ellman's method B 7.72 pIC50 19 nM IC50 Bioorg Med Chem Lett (2017) 27: 5053-5059 [PMID:29033232]
ChEMBL Inhibition of electric eel AChE by Ellman's method B 7.72 pIC50 19 nM IC50 Eur J Med Chem (2020) 192: 112180-112180 [PMID:32131034]
ChEMBL Inhibition of electric eel AChE using acetylthiocholine iodide incubated for 15 mins as substrate by Ellman's method B 7.72 pIC50 19 nM IC50 Bioorg Med Chem Lett (2019) 29: 126625-126625 [PMID:31444085]
ChEMBL Compound was evaluated for the inhibition of acetylcholinesterase (AChE) in electric eel B 7.77 pIC50 17 nM IC50 Bioorg Med Chem Lett (1998) 8: 575-580 [PMID:9871563]
ChEMBL Inhibition of electric eel AChE using acetylthiocholine iodide as substrate preincubated for 5 mins followed by substrate addition measured at 1 to 3 mins time interval by Ellman's method B 7.79 pIC50 16.3 nM IC50 Medchemcomm (2017) 8: 1459-1467 [PMID:30108857]
ChEMBL Inhibition of electric eel AChE using acetylthiocholine iodide as substrate measured for 2 mins by Ellman's method B 7.8 pIC50 16 nM IC50 Eur J Med Chem (2016) 121: 40-46 [PMID:27214510]
ChEMBL Inhibition of Electrophorus electricus acetylcholinesterase using acetylthiocholine iodide substrate after 15 mins by spectrophotometric method B 7.82 pIC50 15 nM IC50 Bioorg Med Chem Lett (2016) 26: 2035-2039 [PMID:26947607]
ChEMBL Inhibition of Electrophorus electricus AChE using acetylthiocholine iodide as substrate measured after 15 mins by Ellman's method B 7.82 pIC50 15 nM IC50 Bioorg Med Chem (2019) 27: 991-1001 [PMID:30772129]
ChEMBL Inhibition of electric eel AChE using acetylthiocholine iodide as substrate after 2 mins by Ellman's method B 7.85 pIC50 14 nM IC50 Eur J Med Chem (2013) 68: 260-269 [PMID:23988409]
ChEMBL Inhibition of electric eel AChE using acetylthiocholine iodide substrate by Ellman method based spectrophotometry B 7.85 pIC50 14 nM IC50 Eur J Med Chem (2014) 84: 375-381 [PMID:25036795]
ChEMBL Inhibition of electric eel AChE incubated for 15 mins using acetylcholine iodide substrate by colorimetric Ellman's method B 7.85 pIC50 14 nM IC50 Eur J Med Chem (2015) 94: 195-210 [PMID:25768702]
ChEMBL Inhibition of electric eel AChE using acetylcholine as substrate preincubated for 15 mins prior to substrate addition by Ellman's method B 7.85 pIC50 14 nM IC50 Eur J Med Chem (2013) 70: 623-630 [PMID:24211638]
ChEMBL Inhibition of electric eel AChE by Ellman's method B 7.87 pIC50 13.4 nM IC50 J Med Chem (2010) 53: 5129-5143 [PMID:20575555]
ChEMBL Inhibition of electric eel AChE using acetylthiocholine iodide as substrate preincubated for 20 mins followed by substrate addition measured after 5 mins by Ellman's method B 7.89 pIC50 13 nM IC50 Eur J Med Chem (2014) 75: 82-95 [PMID:24530494]
ChEMBL Inhibition of electric eel AChE using acetylthiocholine iodide as substrate preincubated for 5 mins followed by substrate addition and measured after 2 mins by Ellman's method B 7.92 pIC50 12 nM IC50 Eur J Med Chem (2018) 158: 353-370 [PMID:30223122]
ChEMBL Inhibition of electric eel AChE using acetylthiocholine iodide as substrate incubated for 5 mins followed by substrate addition and measured after 5 mins by spectrophotometric based Ellman's method B 7.96 pIC50 11 nM IC50 Eur J Med Chem (2021) 225: 113783-113783 [PMID:34461507]
ChEMBL Inhibition of Electric eel AChE using acetylthiocholine iodide as substrate preincubated for 5 mins followed by substrate addition measured after 5 mins by Ellman's method B 7.96 pIC50 11 nM IC50 Eur J Med Chem (2017) 125: 676-695 [PMID:27721153]
ChEMBL Inhibition of electric eel AChE using acetylthiocholine as substrate preincubated for 5 mins followed by substrate addition and measured after 5 mins by Ellman's method B 7.96 pIC50 11 nM IC50 Eur J Med Chem (2021) 218: 113397-113397 [PMID:33838585]
ChEMBL Inhibition of Electrophorus electricus AChE using acetylthiocholine iodide as substrate preincubated for 5 mins followed by substrate addition and measured after 5 mins by Ellman's method B 7.96 pIC50 11 nM IC50 Eur J Med Chem (2020) 187: 111916-111916 [PMID:31812794]
ChEMBL Inhibition of Electrophorus electricus AChE after 5 mins by Ellman's method B 8 pIC50 10 nM IC50 Eur J Med Chem (2015) 92: 738-749 [PMID:25621991]
ChEMBL Inhibition of electric eel AChE using acetylthiocholine iodide as substrate preincubated for 5 mins followed by substrate addition measured up to 180 secs by spectrophotometric analysis B 8 pIC50 10 nM IC50 Eur J Med Chem (2017) 139: 68-83 [PMID:28800459]
ChEMBL Inhibition of electric eel AChE using acetylthiocholine iodide as substrate preincubated for 5 mins followed by substrate addition measured after 5 mins by Ellmans method B 8 pIC50 10 nM IC50 Bioorg Med Chem Lett (2016) 26: 4140-4145 [PMID:27445168]
ChEMBL Inhibition of electric eel AChE preincubated for 5 mins followed by acetylthiocholine iodide substrate addition measured after 5 mins by Ellman's method B 8 pIC50 10 nM IC50 Eur J Med Chem (2016) 124: 63-81 [PMID:27560283]
ChEMBL Inhibition of Electrophorus electricus AChE using acetylthiocholine iodide as substrate preincubated for 15 mins followed by substrate addition and measured after 4 mins by Ellman's method B 8 pIC50 10 nM IC50 Bioorg Med Chem (2021) 32: 115991-115991 [PMID:33440318]
ChEMBL Inhibition of Electrophorus electricus AChE pre-incubated for 5 mins before addition of acetylthiocholine iodide substrate by Ellman's assay B 8 pIC50 10 nM IC50 Bioorg Med Chem (2015) 23: 1629-1637 [PMID:25707322]
ChEMBL Inhibition of acetylcholinesterase (AChE) in electric eel (type V-S) by modified radiometric assay B 8.04 pIC50 9.2 nM IC50 Bioorg Med Chem Lett (1992) 2: 861-864
ChEMBL Inhibition of electric eel AChE using acetylthiocholine iodide as substrate preincubated for 10 mins followed by substrate addition measured after 10 mins by Ellman's method B 8.15 pIC50 7 nM IC50 Eur J Med Chem (2017) 125: 853-864 [PMID:27744252]
ChEMBL Inhibition of electric eel AChE using acetylthiocholine iodide as substrate after 15 mins by Ellman's method B 8.17 pIC50 6.7 nM IC50 Eur J Med Chem (2012) 52: 251-262 [PMID:22503231]
ChEMBL Inhibition of electric eel AChE using acetylthiocholine iodide as substrate preincubated for 20 mins followed by substrate addition measured after 5 mins by Ellman's method B 8.17 pIC50 6.7 nM IC50 Eur J Med Chem (2014) 80: 543-561 [PMID:24813882]
ChEMBL Inhibition Assay: The inhibitory activity of the enzyme acetylcholinesterase (AChE) was evaluated by the Ellman method (Biochem. Pharmacol. 1961, 7, 88) using an electric eel as an AChE neuronal model (Electrophorus electricus) and acetylthiocholine iodide (0.35 mM) as substrate. The reaction took place in a final volume of 3 mL of a 0.1 M phosphate buffer solution, pH 8.0, containing 0.035 units of AChE and used a 0.35 mM solution of 5,5'-dithio-bis(2-nitrobenzoic acid) (DTNB) to produce the 5-thio-2-nitrobenzoic acid anion. Inhibition curves were performed in triplicate by incubating at least nine inhibitor concentrations for 10 min. A triplicate sample without inhibitor was always present so as to be aware of 100% of the AChE activity. After this time, the substrate was added to 0.35 mM acetylthiocholine iodide, from a 10 mM stock solution. Loss of color was observed at 412 nm in a spectrophotometric reader having 96 well plates. B 8.17 pIC50 6.7 nM IC50 US-8999994-B2. Derivatives of propargylamine having neuroprotective capacity for the treatment of Alzheimer's and Parkinson's diseases (2015)
ChEMBL Inhibition of Electrophorus electricus AchE using acetylthiocholine iodide as substrate preincubated for 10 mins measured after 15 mins of substrate addition by Ellman's method B 8.17 pIC50 6.7 nM IC50 J Med Chem (2011) 54: 8251-8270 [PMID:22023459]
acetylcholinesterase (Yt blood group)/Acetylcholinesterase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL220] [GtoPdb: 2465] [UniProtKB: P22303]
ChEMBL Binding affinity to CM5 sensor chip immobilized recombinant human AChE assessed as dissociation constant at 298.15 K by surface plasmon resonance assay B 8.1 pKd 8 nM Kd J Med Chem (2021) 64: 1844-1855 [PMID:33570950]
ChEMBL Mixed-type inhibition of human AChE using acetylthiocholine chloride as substrate incubated for 5 mins followed by substrate addition by Lineweaver-Burk plot analysis B 7.42 pKi 38 nM Ki Eur J Med Chem (2018) 157: 161-176 [PMID:30096650]
ChEMBL Inhibition of human recombinant AChE B 7.69 pKi 20.5 nM Ki J Med Chem (2004) 47: 6490-6498 [PMID:15588084]
ChEMBL Inhibition of AChE B 7.69 pKi 20.5 nM Ki J Med Chem (2010) 53: 5906-5914 [PMID:20420456]
ChEMBL Inhibitory potency was evaluated against recombinant human AChE B 7.69 pKi 20.5 nM Ki J Med Chem (2003) 46: 2279-2282 [PMID:12773032]
ChEMBL Mixed type inhibition of human AChE using acetylthiocholineiodide as substrate measured for every 30 sec for 5 mins by Ellman's method B 7.9 pKi 12.7 nM Ki ACS Med Chem Lett (2020) 11: 869-876 [PMID:32435398]
ChEMBL Mixed inhibition of human erythrocytes AchE using acetylthiocholine iodide as substrate incubated for 20 mins by Lineweaver-Burk plot analysis B 8 pKi 10 nM Ki ACS Med Chem Lett (2016) 7: 470-475 [PMID:27190595]
ChEMBL Inhibition of human erythrocyte AChE using acetylthiocholine iodide as substrate after 60 mins by Ellman's method B 8.14 pKi 7.2 nM Ki Bioorg Med Chem Lett (2013) 23: 702-705 [PMID:23276831]
ChEMBL Inhibition of AChE-induced amyloid beta (1-40) aggregation B 4 pIC50 >100000 nM IC50 J Med Chem (2010) 53: 5906-5914 [PMID:20420456]
ChEMBL Inhibition of AChE (unknown origin) using acetylthiocholine iodide as substrate by UV-vis spectrophotometry based Ellman's method B 5.12 pIC50 7560 nM IC50 Bioorg Med Chem Lett (2020) 30: 127370-127370 [PMID:32738978]
ChEMBL Inhibition of recombinant human AChE using ATC as substrate by DTNB-reagent based Ellman's method B 5.15 pIC50 7120 nM IC50 J Med Chem (2020) 63: 9695-9704 [PMID:32787143]
ChEMBL Inhibition of human erythrocytes BChE B 5.38 pIC50 4150 nM IC50 Eur J Med Chem (2011) 46: 2170-2184 [PMID:21459491]
ChEMBL Inhibition of human plasma BChE B 5.38 pIC50 4150 nM IC50 Eur J Med Chem (2011) 46: 2170-2184 [PMID:21459491]
ChEMBL Inhibition of human plasma AChE using acetylthiocholine iodide as substrate preincubated for 15 mins followed by substrate addition and measured after 10 mins by Ellman's method B 5.66 pIC50 2170 nM IC50 Eur J Med Chem (2020) 198: 112368-112368 [PMID:32388114]
ChEMBL Inhibition of AChE B 6.8 pIC50 160 nM IC50 Bioorg Med Chem (2008) 16: 2968-2973 [PMID:18249544]
ChEMBL Inhibition of human erythrocytic AChE using acetylthiocholine iodide as substrate preincubated for 5 mins followed by substrate addition measured up to 180 secs by spectrophotometric analysis B 6.8 pIC50 160 nM IC50 Eur J Med Chem (2017) 139: 68-83 [PMID:28800459]
ChEMBL Inhibition of human erythrocyte AChE using acetylthiocholine iodide as substrate preincubated for 10 mins followed by substrate addition and measured for 10 mins by DTNB reagent based Ellman's method B 6.83 pIC50 147.91 nM IC50 Bioorg Med Chem (2019) 27: 1327-1340 [PMID:30795991]
ChEMBL Inhibition of human erythrocyte ACHE preincubated for 6 mins followed by addition of acetylcholine iodide as substrate by Ellman's method B 6.92 pIC50 120 nM IC50 Bioorg Med Chem (2016) 24: 4324-4338 [PMID:27460699]
ChEMBL Inhibition of human acetyl cholinesterase by Ellmann's method B 6.92 pIC50 120 nM IC50 Bioorg Med Chem Lett (2010) 20: 7064-7066 [PMID:20951037]
ChEMBL Inhibition of human AChE by Ellmans test B 7.05 pIC50 90 nM IC50 J Med Chem (2010) 53: 6490-6505 [PMID:20684567]
ChEMBL Inhibition of acetylcholinesterase (unknown origin) using acetylthiocholine iodide as substrate incubated for 10 mins followed by substrate addition measured after 20 mins by UV-Vis spectrophotometric analysis B 7.05 pIC50 90 nM IC50 Bioorg Med Chem (2017) 25: 100-106 [PMID:27780618]
ChEMBL Inhibition of AChE (unknown origin) after 5 mins by Ellman's method B 7.21 pIC50 62 nM IC50 Eur J Med Chem (2014) 83: 355-365 [PMID:24980117]
ChEMBL Inhibition of AChE in human erythrocytes using acetylthiocholine iodide as substrate preincubated with enzyme for 30 mins followed by substrate addition and measured after 30 mins by Ellman's method B 7.22 pIC50 60 nM IC50 Bioorg Med Chem (2021) 46: 116385-116385 [PMID:34481338]
ChEMBL Inhibition of AChE (unknown origin) using acetylthiocholine iodide as substrate by Ellman's method B 7.23 pIC50 59 nM IC50 Eur J Med Chem (2019) 182: 111651-111651 [PMID:31479975]
ChEMBL Inhibition of AChE (unknown origin) using acetylthiocholine as substrate by Ellman's method B 7.3 pIC50 50.12 nM IC50 Bioorg Med Chem Lett (2017) 27: 4180-4184 [PMID:28751142]
ChEMBL Inhibition of human erythrocytes AChE using acetylthiocholine iodide as substrate preincubated for 5 mins followed by substrate addition measured up to 3 mins by Ellman's method B 7.32 pIC50 48 nM IC50 Eur J Med Chem (2016) 123: 282-297 [PMID:27484514]
ChEMBL Inhibition of human erythrocyte AChE using acetylthiocholine chloride as substrate incubated for 5 mins followed by substrate addition measured after 180 secs by Ellman's method B 7.32 pIC50 48 nM IC50 Eur J Med Chem (2018) 157: 161-176 [PMID:30096650]
ChEMBL Inhibition of recombinant human AChE expressed in HEK293 cells using acetylthiocholine iodide as substrate preincubated for 10 mins followed by substrate addition and measured for 10 mins by Ellman's method B 7.32 pIC50 48 nM IC50 Eur J Med Chem (2021) 212: 113124-113124 [PMID:33395623]
ChEMBL Inhibition of human recombinant AChE preincubated for 1 min in presence of DNTB followed by addition of acetylthiocholine iodide substrate and measured after 20 mins by Ellman's method B 7.36 pIC50 44 nM IC50 Eur J Med Chem (2021) 223: 113663-113663 [PMID:34198150]
ChEMBL Inhibition of human erythrocytes AChE using acetylthiocholine iodide as substrate preincubated for 10 mins followed by substrate addition by Ellman's method B 7.38 pIC50 42 nM IC50 Eur J Med Chem (2019) 183: 111707-111707 [PMID:31561043]
ChEMBL Inhibition of human AChE by Ellman's method B 7.38 pIC50 42 nM IC50 Bioorg Med Chem (2020) 28: 115721-115721 [PMID:33007563]
ChEMBL Inhibition of human erythrocyte AChE using acetylthiocholine iodide as substrate preincubated for 6 mins followed by substrate addition measured up to 180 secs by Ellman's method B 7.39 pIC50 41 nM IC50 Eur J Med Chem (2018) 146: 287-298 [PMID:29407958]
ChEMBL Inhibitory concentration required against acetylcholinesterase activity B 7.4 pIC50 40 nM IC50 J Med Chem (2001) 44: 4011-4014 [PMID:11689088]
ChEMBL Inhibition of human erythrocyte AChE using acetylthiocholine iodide as substrate preincubated for 10 mins followed by substrate addition and measured for 6 mins by Ellman's method B 7.4 pIC50 40 nM IC50 Bioorg Med Chem (2019) 27: 3650-3662 [PMID:31288978]
ChEMBL Inhibition of human AChE using acetylthiocholine iodide as substrate preincubated for 5 mins followed by substrate addition measured after 60 to 300 sec by Ellman's method B 7.4 pIC50 40 nM IC50 Medchemcomm (2015) 6: 1930-1941
ChEMBL Inhibition of human AChE using acetylthiocholine iodide as substrate treated 5 mins before substrate addition measured up to 4 mins by Ellman's method B 7.4 pIC50 40 nM IC50 Bioorg Med Chem Lett (2013) 23: 4336-4341 [PMID:23791077]
ChEMBL Inhibition of human erythrocyte AChE using acetylthiocholine iodide as substrate pretreated for 6 mins followed by substrate addition measured up to 180 sec by Ellman's method B 7.42 pIC50 37.6 nM IC50 Eur J Med Chem (2017) 133: 184-196 [PMID:28388521]
ChEMBL Inhibition of human erythrocyte AChE using acetylthiocholine iodide as substrate measured after 15 mins by Ellman's method B 7.45 pIC50 35.6 nM IC50 Eur J Med Chem (2017) 126: 762-775 [PMID:27951485]
ChEMBL Inhibition of human erythrocyte acetylcholinesterase using acetylthiocholine iodide as substrate pre-incubated for 10 mins followed by substrate addition and measured for 6 mins by Ellman's method B 7.48 pIC50 33 nM IC50 Eur J Med Chem (2019) 167: 510-524 [PMID:30784883]
ChEMBL Inhibition of human AChE using acetylthiocholine iodide as substrate incubated for 15 mins by Ellman's method B 7.49 pIC50 32 nM IC50 Bioorg Med Chem (2021) 35: 116074-116074 [PMID:33640707]
ChEMBL Inhibition of human AChE using acetylthiocholine iodide as substrate after 5 mins by DTNB method B 7.49 pIC50 32 nM IC50 Bioorg Med Chem Lett (2012) 22: 4707-4712 [PMID:22704921]
ChEMBL Inhibition of human AChE using acetylthiocholine iodide as substrate preincubated for 6 mins followed by substrate addition measured up to 180 secs by Ellman's method B 7.5 pIC50 31.8 nM IC50 Eur J Med Chem (2017) 139: 48-59 [PMID:28797883]
ChEMBL Inhibition of human erythrocytes acetylcholinesterase preincubated for 5 mins followed by addition of acetylthiocholine iodide as substrate measured after 60 to 120 mins by Ellmans method B 7.51 pIC50 30.8 nM IC50 Medchemcomm (2016) 7: 990-998
ChEMBL Inhibition of human erythrocyte AChE using acetylthiocholine chloride as substrate pretreated for 15 mins followed by substrate addition measured for 2 mins by DTNB reagent based spectrophotometric method B 7.52 pIC50 30 nM IC50 Eur J Med Chem (2017) 130: 139-153 [PMID:28242549]
ChEMBL Inhibition of AChE (unknown origin) preincubated for 30 mins followed by substrate addition acetylthiocholineiodide measured after 40 mins by Ellman's method B 7.52 pIC50 30 nM IC50 Eur J Med Chem (2020) 200: 112415-112415 [PMID:32454229]
ChEMBL Inhibition of recombinant human erythrocyte AChE using acetylthiocholine iodide as substrate preincubated for 30 mins followed by substrate addition and measured after 30 mins by spectrophotometry based Ellman's method B 7.52 pIC50 30 nM IC50 Eur J Med Chem (2020) 198: 112257-112257 [PMID:32375073]
ChEMBL Inhibition of human recombinant AChE using acetylthiocholine iodide as a substrate preincubated for 20 mins followed by substrate addition by spectrophotometric analysis B 7.57 pIC50 26.8 nM IC50 Eur J Med Chem (2021) 225: 113779-113779 [PMID:34418785]
ChEMBL Inhibition of AChE in human erythrocytes using acetylthiocholineiodide as substrate pre-incubated for 10 mins followed by substrate addition and measured for 6 mins by DTNB reagent based Ellman's method B 7.58 pIC50 26.55 nM IC50 Eur J Med Chem (2021) 215: 113224-113224 [PMID:33582578]
ChEMBL Inhibition of human erythrocytes AChE using acetylthiocholine iodide as substrate preincubated for 5 mins followed by substrate addition measured at 1 to 3 mins time interval by Ellman's method B 7.61 pIC50 24.7 nM IC50 Medchemcomm (2017) 8: 1459-1467 [PMID:30108857]
ChEMBL Inhibitory potency was evaluated against recombinant human AChE B 7.64 pIC50 23.1 nM IC50 J Med Chem (2003) 46: 2279-2282 [PMID:12773032]
ChEMBL Inhibition of human recombinant acetylcholinesterase B 7.64 pIC50 23.1 nM IC50 J Med Chem (2007) 50: 4882-4897 [PMID:17850125]
ChEMBL Inhibition of human recombinant AChE by Ellman's assay B 7.64 pIC50 23.1 nM IC50 J Med Chem (2008) 51: 7308-7312 [PMID:18954037]
ChEMBL Inhibition of human AchE B 7.64 pIC50 23 nM IC50 J Med Chem (2008) 51: 347-372 [PMID:18181565]
ChEMBL Inhibition of human AChE using acetylthiocholine iodide as substrate by Ellman's assay B 7.64 pIC50 23 nM IC50 Eur J Med Chem (2011) 46: 1682-1693 [PMID:21397996]
ChEMBL Inhibition of human recombinant AChE by Ellman's spectrophotometric assay B 7.64 pIC50 23 nM IC50 J Med Chem (2022) 65: 3962-3977 [PMID:35195417]
ChEMBL Inhibition of human recombinant AChE B 7.64 pIC50 22.91 nM IC50 J Med Chem (2004) 47: 6490-6498 [PMID:15588084]
ChEMBL Inhibition of human erythrocyte AChE using acetylthiocholine iodide as substrate preincubated for 10 mins followed by substrate addition by Ellman's method B 7.66 pIC50 22 nM IC50 Bioorg Med Chem (2016) 24: 1050-1062 [PMID:26827140]
ChEMBL Inhibitory concentration against human erythrocyte Acetylcholinesterase B 7.66 pIC50 22 nM IC50 J Med Chem (2005) 48: 986-994 [PMID:15715468]
ChEMBL Inhibition of human plasma AChE B 7.66 pIC50 22 nM IC50 Eur J Med Chem (2011) 46: 2170-2184 [PMID:21459491]
ChEMBL Inhibition of human erythrocytes AChE B 7.66 pIC50 22 nM IC50 Eur J Med Chem (2011) 46: 2170-2184 [PMID:21459491]
ChEMBL Ex vivo inhibition of human erythrocyte Acetylcholinesterase. B 7.66 pIC50 22 nM IC50 J Med Chem (2002) 45: 3684-3691 [PMID:12166941]
ChEMBL Anticholinesterase activity against human erythrocyte AChE B 7.66 pIC50 22 nM IC50 J Med Chem (2006) 49: 2174-2185 [PMID:16570913]
ChEMBL Inhibition of acetylcholine esterase (unknown origin) using acetylthiocholine as substrate incubated for 15 mins prior to substrate addition measured after 5 mins by spectrophotometry B 7.68 pIC50 21 nM IC50 Eur J Med Chem (2013) 63: 854-868 [PMID:23603045]
ChEMBL Inhibition of human serum AChE using acetylthiocholine iodide as substrate preincubated for 20 mins followed by substrate addition measured for 3 mins by Ellman's method B 7.69 pIC50 20.3 nM IC50 Eur J Med Chem (2017) 141: 197-210 [PMID:29031067]
ChEMBL Inhibition of human recombinant AChE preincubated for 20 mins before substrate addition by Ellman's method B 7.7 pIC50 20 nM IC50 Bioorg Med Chem (2010) 18: 1749-1760 [PMID:20171894]
ChEMBL Inhibition of human recombinant AChE by Ellman's method B 7.7 pIC50 20 nM IC50 Eur J Med Chem (2009) 44: 1341-1348 [PMID:18396354]
ChEMBL Inhibition of human erythrocyte AChE using acetylthiocholine chloride as substrate incubated for 15 mins by Ellman's method B 7.72 pIC50 19 nM IC50 Bioorg Med Chem Lett (2017) 27: 5053-5059 [PMID:29033232]
ChEMBL Inhibition of human AChE using acetylthiocholine iodide as substrate preincubated with enzyme for 5 mins followed by substrate addition and measured after 5 mins by Ellman's method B 7.74 pIC50 18 nM IC50 Eur J Med Chem (2021) 223: 113735-113735 [PMID:34371367]
ChEMBL In vitro inhibition of human recombinant AChE. B 7.74 pIC50 18 nM IC50 Bioorg Med Chem Lett (2002) 12: 2565-2568 [PMID:12182861]
ChEMBL Inhibition of human recombinant AChE after 20 mins using acetylthiocholine iodide as a substrate by Ellman's assay B 7.74 pIC50 18 nM IC50 J Med Chem (2011) 54: 2627-2645 [PMID:21417225]
ChEMBL Inhibition of human erythrocytes AChE by Ellman's method B 7.75 pIC50 17.76 nM IC50 Bioorg Med Chem Lett (2020) 30: 127659-127659 [PMID:33137375]
ChEMBL Inhibition of human AChE using acetylthiocholineiodide as substrate measured for every 30 sec for 5 mins by Ellman's method B 7.79 pIC50 16.1 nM IC50 ACS Med Chem Lett (2020) 11: 869-876 [PMID:32435398]
ChEMBL Inhibitory concentration against acetylcholinesterase (AChE) from human erythrocytes B 7.8 pIC50 16 nM IC50 J Med Chem (1999) 42: 730-741 [PMID:10052979]
ChEMBL Inhibition of human AChE using acetylthiocholine iodide as substrate preincubated for 20 mins followed by substrate addition and measured upto 5 mins by Ellman's method B 7.8 pIC50 16 nM IC50 Eur J Med Chem (2019) 177: 414-424 [PMID:31158754]
ChEMBL Inhibition of recombinant human AChE expressed in HEK293 cells preincubated for 15 mins B 7.8 pIC50 16 nM IC50 J Med Chem (2014) 57: 10455-10463 [PMID:25418133]
ChEMBL In vitro inhibition of acetylcholinesterase from human erythrocytes B 7.8 pIC50 16 nM IC50 J Med Chem (2001) 44: 2707-2718 [PMID:11495583]
ChEMBL Inhibition of human recombinant AChE by spectrophotometric Ellman's method B 7.82 pIC50 15 nM IC50 J Med Chem (2015) 58: 5561-5578 [PMID:26107513]
ChEMBL Inhibition of human recombinant AChE using acetylthiocholine iodide as substrate preincubated for 5 mins followed by substrate addition by Ellman's method B 7.85 pIC50 14 nM IC50 Eur J Med Chem (2015) 103: 302-311 [PMID:26363866]
ChEMBL Inhibition of human erythrocyte AChE using acetylthiocholine as substrate measured after 5 mins by Ellman's method B 7.85 pIC50 14 nM IC50 Eur J Med Chem (2020) 191: 112140-112140 [PMID:32088494]
ChEMBL Inhibition of human erythrocytes AChE assessed as reduction in 5-thio-2-nitrobenzoate anion formation using acetylthiocholine iodide as substrate preincubated for 5 mins followed by substrate addition by Ellman's method B 7.92 pIC50 12.1 nM IC50 Eur J Med Chem (2019) 182: 111596-111596 [PMID:31419776]
ChEMBL Inhibition of human erythrocyte AChE using acetylthiocholine iodide as substrate after 15 mins by Ellman's method B 7.92 pIC50 12 nM IC50 Eur J Med Chem (2017) 135: 307-323 [PMID:28458136]
ChEMBL Inhibition of AChE in human erythrocytes using acetylthiocholine iodide as substrate after 15 mins by Ellman's method B 7.92 pIC50 12 nM IC50 Eur J Med Chem (2015) 94: 348-366 [PMID:25778991]
ChEMBL Inhibition of human erythrocyte AChE preincubated for 15 mins by Ellman's method B 7.93 pIC50 11.7 nM IC50 Eur J Med Chem (2014) 87: 429-439 [PMID:25282266]
ChEMBL Inhibition of human erythrocytes AchE using acetylthiocholine iodide as substrate incubated for 20 mins by Ellman method B 7.96 pIC50 11 nM IC50 ACS Med Chem Lett (2016) 7: 470-475 [PMID:27190595]
ChEMBL Inhibition of AChE in human erythrocytes using acetylthiocholine chloride as substrate measured after 15 mins by Ellman's method B 7.96 pIC50 11 nM IC50 Eur J Med Chem (2017) 130: 379-392 [PMID:28279845]
ChEMBL Inhibition of human erythrocyte AChE using acetylthiocholine chloride as substrate preincubated for 15 mins followed by substrate addition measured every 1 min by Ellman's method B 7.96 pIC50 11 nM IC50 J Med Chem (2013) 56: 9089-9099 [PMID:24160297]
ChEMBL Inhibition of human erythrocyte AChE using acetylthiocholine chloride by spectrophotometry B 7.96 pIC50 11 nM IC50 Medchemcomm (2013) 4: 925-931
ChEMBL Inhibition of human erythrocytes AchE using acetylthiocholine iodide as substrate after 15 mins by Ellman's method B 7.96 pIC50 11 nM IC50 Eur J Med Chem (2014) 76: 314-331 [PMID:24589487]
ChEMBL Inhibition of human erythrocytes AChE using acetylthiocholine iodide as substrate measured after 15 mins by Ellman's method B 7.96 pIC50 11 nM IC50 Eur J Med Chem (2020) 187: 111958-111958 [PMID:31865014]
ChEMBL Inhibition of human erythrocyte acetylcholinesterase using acetylthiocholine chloride as substrate preincubated for 15 mins followed by substrate addition by Ellman's method B 7.96 pIC50 11 nM IC50 Bioorg Med Chem (2014) 22: 1355-1361 [PMID:24461494]
ChEMBL Inhibition of human erythrocyte AChE using ATCI as substrate preincubated for 30 mins followed by substrate addition measured after 30 mins by Ellman assay B 8 pIC50 10 nM IC50 J Med Chem (2016) 59: 5823-5846 [PMID:27253679]
ChEMBL Inhibition of human AChE using acetylthiocholine as substrate by Ellman's method B 8 pIC50 10 nM IC50 Eur J Med Chem (2014) 73: 56-72 [PMID:24378710]
ChEMBL Inhibition of purified human erythrocyte AChE using acetylcholine as substrate by Ellman's method B 8 pIC50 10 nM IC50 Eur J Med Chem (2013) 67: 64-74 [PMID:23838422]
ChEMBL Inhibition of recombinant human AChE expressed in HEK293 cells using acetylthiocholine iodide as substrate pretreated for 5 mins followed by substrate addition measured for 5 mins by UV-Vis spectrophotometric method B 8 pIC50 10 nM IC50 Eur J Med Chem (2017) 130: 60-72 [PMID:28242552]
ChEMBL Inhibition of human erythrocyte AChE using acetylthiocholine as substrate by Ellman method B 8 pIC50 10 nM IC50 Eur J Med Chem (2012) 57: 296-301 [PMID:23078965]
ChEMBL Inhibition of human erythrocyte AChE using acetylthiocholine iodide as substrate preincubated for 6 mins followed by substrate addition measured up to 180 secs by spectrophotometric-based Ellman's method B 8 pIC50 10 nM IC50 Bioorg Med Chem (2016) 24: 1528-1539 [PMID:26917219]
ChEMBL Inhibition of human AChE using acetylthiocholine iodide as substrate pretreated for 5 mins followed by substrate addition measured after 5 mins by Ellman's method B 8 pIC50 10 nM IC50 Eur J Med Chem (2018) 158: 781-800 [PMID:30245401]
ChEMBL Inhibition of recombinant human AChE expressed in HEK293 cells using acetylthiocholine iodide as substrate pretreated for 5 mins followed by substrate addition and measured for 5 mins by Ellman's method B 8 pIC50 10 nM IC50 Eur J Med Chem (2018) 156: 534-553 [PMID:30025348]
ChEMBL Inhibition of recombinant human AChE using acetylthiocholine iodide as substrate measured after 7 mins by Ellman's method B 8 pIC50 10 nM IC50 Eur J Med Chem (2021) 222: 113541-113541 [PMID:34116326]
ChEMBL Inhibition of human erythrocyte AChE using acetylthiocholine as substrate by Ellman's assay B 8 pIC50 10 nM IC50 Eur J Med Chem (2019) 166: 90-107 [PMID:30685536]
ChEMBL Inhibition of human recombinant AChE using acetylthiocholine iodide as substrate preincubated for 5 mins followed by substrate addition measured for 5 mins by Ellman's method B 8 pIC50 10 nM IC50 Eur J Med Chem (2016) 121: 376-386 [PMID:27267007]
ChEMBL Inhibition of acetylcholinesterase (unknown origin) B 8.05 pIC50 9 nM IC50 J Med Chem (2020) 63: 15187-15217 [PMID:33111525]
ChEMBL Inhibition of AChE in human erythrocytes by Ellman's method B 8.05 pIC50 9 nM IC50 Eur J Med Chem (2020) 192: 112180-112180 [PMID:32131034]
ChEMBL Inhibition of human recombinant AChE expressed in HEK293 cells using acetylthiocholine iodide as substrate preincubated for 30 mins followed by substrate addition measured after 30 mins by Ellman's method B 8.05 pIC50 9 nM IC50 Eur J Med Chem (2016) 121: 864-879 [PMID:26471320]
ChEMBL Inhibition of AChE in human erythrocytes by Ellman's method B 8.09 pIC50 8.2 nM IC50 J Med Chem (2010) 53: 5129-5143 [PMID:20575555]
ChEMBL Concentration required to inhibit 50% of Acetylcholinesterase obtained from human erythrocytes was determined in vitro B 8.1 pIC50 8 nM IC50 J Med Chem (1995) 38: 1084-1089 [PMID:7707311]
ChEMBL Inhibition of human recombinant AChE using acetylthiocholine iodide substrate incubated for 15 mins by spectrophotometry based Ellman's method B 8.1 pIC50 8 nM IC50 Bioorg Med Chem (2014) 22: 5141-5154 [PMID:25189690]
ChEMBL Inhibition of AChE B 8.1 pIC50 8 nM IC50 Eur J Med Chem (2010) 45: 1167-1172 [PMID:20053484]
ChEMBL Compound was evaluated for the inhibition of acetylcholinesterase (AChE) in human erythrocytes B 8.1 pIC50 8 nM IC50 Bioorg Med Chem Lett (1998) 8: 575-580 [PMID:9871563]
ChEMBL Evaluated for the in vitro inhibition of the Acetylcholinesterase (AChE) from human erythrocytes B 8.1 pIC50 8 nM IC50 J Med Chem (1994) 37: 2721-2734 [PMID:8064800]
ChEMBL Inhibition against Acetylcholinesterase (AChE) B 8.1 pIC50 8 nM IC50 J Med Chem (1996) 39: 380-387 [PMID:8558505]
ChEMBL Inhibition of recombinant AChE in human erythrocytes using acetylthiocholine iodide as substrate incubated for 20 mins by Ellman's method B 8.13 pIC50 7.39 nM IC50 Eur J Med Chem (2022) 229: 114045-114045 [PMID:34922191]
ChEMBL Inhibition of human erythrocyte AChE using acetylthiocholine iodide as substrate peincubated for 5 mins followed by substrate addition by DTNB-reagent based Ellman's method B 8.15 pIC50 7 nM IC50 Eur J Med Chem (2021) 210: 113059-113059 [PMID:33310288]
ChEMBL Inhibition of AchE (unknown origin) B 8.15 pIC50 7 nM IC50 ACS Med Chem Lett (2016) 7: 341-344 [PMID:27096037]
ChEMBL Inhibition of human recombinant AChE using acetylthiocholine as substrate by UV-visible spectrophotometric Ellman's method B 8.16 pIC50 6.87 nM IC50 Bioorg Med Chem Lett (2018) 28: 2910-2913 [PMID:30017317]
ChEMBL Inhibition of human recombinant AChE expressed in HEK293 cells using acetylthiocholine iodide as substrate by Ellman's method B 8.21 pIC50 6.2 nM IC50 Medchemcomm (2019) 10: 1018-1026 [PMID:31304000]
ChEMBL Inhibition of human recombinant AChE preincubated for 5 mins followed by acetylthiocholine iodide substrate addition measured after 5 mins by Ellman's method B 8.22 pIC50 6 nM IC50 Eur J Med Chem (2016) 124: 63-81 [PMID:27560283]
ChEMBL Inhibition of human erythrocyte AChE pre-incubated for 5 mins before acetylthiocholine iodide substrate by Ellman' method B 8.22 pIC50 6 nM IC50 J Med Chem (2015) 58: 3172-3187 [PMID:25793650]
ChEMBL Inhibition of human recombinant AChE after 5 mins by Ellman's method B 8.22 pIC50 6 nM IC50 Eur J Med Chem (2015) 92: 738-749 [PMID:25621991]
ChEMBL Inhibition of human recombinant AChE pre-incubated for 5 mins before addition of acetylthiocholine iodide substrate by Ellman's assay B 8.22 pIC50 6 nM IC50 Bioorg Med Chem (2015) 23: 1629-1637 [PMID:25707322]
ChEMBL Inhibition of human erythrocytes AChE using acetylthiocholine iodide as substrate preincubated for 5 mins followed by substrate addition measured at 1 min time interval for 10 mins by Ellman's method B 8.22 pIC50 6 nM IC50 Eur J Med Chem (2019) 162: 234-248 [PMID:30447434]
ChEMBL Inhibition of AChE-induced amyloid beta aggregation B 8.22 pIC50 6 nM IC50 Bioorg Med Chem Lett (2011) 21: 2687-2691 [PMID:21216144]
ChEMBL Inhibition of AChE (unknown origin) using acetylthiocholine iodide as substrate preincubated for 15 mins followed by substrate addition and measured after 30 mins by Ellman's method B 8.22 pIC50 6 nM IC50 RSC Med Chem (2020) 11: 307-316 [PMID:33479638]
ChEMBL Inhibition of recombinant human AChE using ATCI as substrate incubated for 5 mins followed by substrate addition and measured after 5 mins by spectrophotometric based Ellman's method B 8.22 pIC50 6 nM IC50 Eur J Med Chem (2020) 207: 112743-112743 [PMID:32882609]
ChEMBL Inhibition of AChE (unknown origin) B 8.24 pIC50 5.7 nM IC50 Bioorg Med Chem (2013) 21: 676-683 [PMID:23273608]
ChEMBL Inhibition of human acetylcholinesterase B 8.24 pIC50 5.7 nM IC50 Bioorg Med Chem (2019) 27: 895-930 [PMID:30744931]
ChEMBL Inhibition of recombinant human AChE using acetylthiocholine iodide as substrate pretreated for 5 mins followed by substrate addition measured for 5 mins by Ellman's method B 8.24 pIC50 5.7 nM IC50 Eur J Med Chem (2018) 145: 431-444 [PMID:29335209]
ChEMBL Inhibition of AChE (unknown origin) B 8.24 pIC50 5.7 nM IC50 Eur J Med Chem (2018) 147: 48-65 [PMID:29421570]
ChEMBL Inhibition of human AChE using acetylthiocholine iodide as substrate preincubated for 5 mins followed by substrate addition measured over 5 mins by UV-Vis spectrophotometric analysis B 8.24 pIC50 5.7 nM IC50 Eur J Med Chem (2017) 139: 773-791 [PMID:28863358]
ChEMBL Inhibition of recombinant human AChE using acetylthiocholine iodide as substrate preincubated for 5 mins followed by substrate addition and measured for 5 mins by Ellman's method B 8.24 pIC50 5.7 nM IC50 Bioorg Med Chem (2019) 27: 931-943 [PMID:30765302]
ChEMBL Inhibition of recombinant human AChE using acetylthiocholine iodide as substrate preincubated with enzyme for 5 mins prior to substrate addition measured after 5 mins by Ellman's method B 8.25 pIC50 5.59 nM IC50 Eur J Med Chem (2020) 185: 111785-111785 [PMID:31669851]
GtoPdb - - 8.3 pIC50 - - - J Med Chem (2006) 49: 2174-85 [PMID:16570913];
Eur J Pharmacol (1994) 270: 189-93 [PMID:8039548];
J Med Chem (1992) 35: 584-9 [PMID:1738151]
ChEMBL Inhibition of human recombinant AChE expressed in HEK293 cells using acetylthiocholine iodide as substrate incubated for 10 mins by Ellman's method B 8.3 pIC50 5 nM IC50 Bioorg Med Chem (2021) 30: 115940-115940 [PMID:33340937]
ChEMBL Inhibition of acetylcholinesterase (AChE) of human red blood cell (type XIII) by modified radiometric AChE assay B 8.63 pIC50 2.33 nM IC50 Bioorg Med Chem Lett (1992) 2: 861-864
ChEMBL Inhibition of acetylcholinesterase (unknown origin) B 8.7 pIC50 2 nM IC50 Bioorg Med Chem (2013) 21: 146-152 [PMID:23199476]
ChEMBL In vitro reversal of vecuronium-induced neuromuscular block in guinea pig hemi-diaphragm. F 7.37 pEC50 43 nM EC50 Bioorg Med Chem Lett (2002) 12: 2565-2568 [PMID:12182861]
Acetylcholinesterase in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4768] [UniProtKB: P23795]
ChEMBL Inhibition of fetal Bovine serum AChE B 8.54 pKi 2.9 nM Ki J Med Chem (2003) 46: 1-4 [PMID:12502352]
ChEMBL Dissociation constant for inhibition of fetal bovine serum Acetylcholinesterase B 8.54 pKi 2.9 nM Ki J Med Chem (2005) 48: 1919-1929 [PMID:15771436]
ChEMBL Inhibition of bovine erythrocyte AChE by Ellman's assay B 7.72 pIC50 19 nM IC50 J Med Chem (2008) 51: 3588-3598 [PMID:18517184]
ChEMBL Compound was evaluated for the inhibition of acetylcholinesterase (AChE) in bovine erythrocytes B 8.1 pIC50 8 nM IC50 Bioorg Med Chem Lett (1998) 8: 575-580 [PMID:9871563]
ChEMBL Compound was evaluated for the inhibition of acetylcholinesterase (AChE) in bovine brain B 8.22 pIC50 6 nM IC50 Bioorg Med Chem Lett (1998) 8: 575-580 [PMID:9871563]
ChEMBL Inhibition of bovine acetylcholinesterase using acetylcholine iodide as substrate incubated for 20 mins prior to substrate addition measured after 3 mins by Ellman's method B 8.38 pIC50 4.2 nM IC50 Bioorg Med Chem (2013) 21: 146-152 [PMID:23199476]
acetylcholinesterase (Yt blood group)/Acetylcholinesterase in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3198] [GtoPdb: 2465] [UniProtKB: P21836]
ChEMBL Inhibition of AchE in albino LACA mouse brain using acetylthiocholine iodide as substrate incubated for 10 mins measured for 2 mins by Ellman's method B 4.84 pIC50 14550 nM IC50 Bioorg Med Chem (2018) 26: 215-224 [PMID:29195794]
ChEMBL Inhibition of mouse AChE using acetylthiocholine iodide as substrate incubated for 20 mins by Ellman's method B 5.21 pIC50 6100 nM IC50 J Med Chem (2021) 64: 7483-7506 [PMID:34024109]
ChEMBL Inhibition of acetylcholinesterase in Albino LACA mouse brain homogenates using acetylthiocholine iodide as substrate measured for 2 mins by Ellman's method B 5.74 pIC50 1820 nM IC50 Bioorg Med Chem (2016) 24: 4587-4599 [PMID:27519464]
ChEMBL In Vitro Pharmacodynamic Assay: Modified Ellman method (Alvin V. et al. JWS-USC-75-IX Improves Information Processing and Cognitive Function in Animal Models[J]. Journal of Pharmacology and experimental therapeutics, 2010, 336(3): 751) was employed in the test, for testing the inhibition effect of a series of compounds of formula (I) on acetylcholinesterase, so that active AchEIs were screened out, and their activity were evaluated via the IC50 value of inhibition of the series of compounds of formula (I) on the enzyme. B 7.03 pIC50 94 nM IC50 US-9346818-B2. Benzodioxole derivative and preparation method and use thereof (2016)
ChEMBL Inhibition of mouse brain AChE using acetylthiocholine iodide as substrate measured after 30 mins by Ellman's method B 7.08 pIC50 84 nM IC50 Eur J Med Chem (2019) 168: 207-220 [PMID:30822710]
ChEMBL Inhibition of mouse brain homogenate AChE using acetylthiocholine iodide as substrate measured after 15 mins in presence of BChE inhibitor methopropazine hydrochloride by DTNB reagent based colorimetric method B 7.92 pIC50 11.9 nM IC50 Bioorg Med Chem Lett (2019) 29: 1593-1596 [PMID:31078410]
ChEMBL Inhibition of AChE in mouse cortical homogenate using acetylthiocholine iodide as substrate incubated for 20 mins by Ellman's method B 8.21 pIC50 6.22 nM IC50 Eur J Med Chem (2022) 229: 114045-114045 [PMID:34922191]
ChEMBL Inhibition of AChE in mouse brain homogenate using acetylthiocholine as substrate preincubated for 300 secs followed by substrate addition by Ellman's method B 8.24 pIC50 5.7 nM IC50 J Med Chem (2018) 61: 119-139 [PMID:29227101]
acetylcholinesterase (Yt blood group)/Acetylcholinesterase in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3199] [GtoPdb: 2465] [UniProtKB: P37136]
ChEMBL Inhibition of AChE in rat brain using acetylthiocholine iodide as substrate by Ellman's UV-vis spectrophotometric method B 6.92 pIC50 120 nM IC50 Bioorg Med Chem Lett (2020) 30: 127404-127404 [PMID:32717612]
ChEMBL Inhibition of rat cortex AChE using acetylthiocholine iodide as substrate by Ellman's method B 7.37 pIC50 42.82 nM IC50 Eur J Med Chem (2021) 226: 113827-113827 [PMID:34530383]
ChEMBL Inhibition of rat brain acetylcholine esterase in presence of acetylcholine substrate by chemiluminescent assay B 7.4 pIC50 40 nM IC50 Eur J Med Chem (2008) 43: 657-661 [PMID:17624631]
ChEMBL Inhibition of rat cortex homogenate AChE using acetylthiocholine chloride as substrate incubated for 15 mins by Ellman's method B 7.43 pIC50 37 nM IC50 Bioorg Med Chem Lett (2017) 27: 5053-5059 [PMID:29033232]
ChEMBL Inhibition of 5% rat cortex homogenate AChE using acetylthiocholine chloride as substrate after 15 mins by Ellman's method B 7.43 pIC50 37 nM IC50 Bioorg Med Chem (2017) 25: 3006-3017 [PMID:28487125]
ChEMBL Inhibition of acetylcholinesterase in Wistar rat brain homogenate by Ellman's method B 7.45 pIC50 35.48 nM IC50 Bioorg Med Chem (2008) 16: 9911-9924 [PMID:18976927]
ChEMBL Inhibition of AChE in Sprague-Dawley rat cortices using acetylthiocholine iodide as substrate by Ellman's method B 7.49 pIC50 32 nM IC50 Bioorg Med Chem (2013) 21: 676-683 [PMID:23273608]
ChEMBL Inhibition of AchE in rat cortex by Ellman's method B 7.57 pIC50 26.8 nM IC50 Bioorg Med Chem (2008) 16: 7646-7653 [PMID:18662884]
ChEMBL Inhibition of AChE activity in rat brain homogenate using acetylthiocholine as substrate by Ellman's method B 7.67 pIC50 21.5 nM IC50 Bioorg Med Chem (2012) 20: 521-530 [PMID:22172310]
ChEMBL Inhibition of AchE in Rattus norvegicus (rat) cortex homogenates by Ellman's method B 7.67 pIC50 21.5 nM IC50 Med Chem Res (2013) 22: 1648-1659
ChEMBL Inhibitory activity against Acetylcholinesterase (AChE) in rat brain hippocampal crude homogenate B 7.7 pIC50 20 nM IC50 Bioorg Med Chem Lett (1999) 9: 3279-3284 [PMID:10612585]
ChEMBL Inhibition of AChE in rat brain cortex homogenates using acetylthiocholine iodide as substrate in presence of BuChE inhibitor tetraisopropyl pyrophosphoramide measured after 15 mins by Ellman's method B 7.72 pIC50 19 nM IC50 Eur J Med Chem (2017) 126: 762-775 [PMID:27951485]
ChEMBL In vitro inhibitory concentration against rat cortex acetylcholinesterase B 7.8 pIC50 16 nM IC50 Bioorg Med Chem Lett (2005) 15: 3834-3837 [PMID:15993600]
ChEMBL Inhibition of acetylcholinesterase in Rattus norvegicus (rat) cortex by Ellman method B 7.8 pIC50 16 nM IC50 Med Chem Res (2013) 22: 2328-2345
ChEMBL Inhibition of acetylcholinesterase in Rattus norvegicus (rat) cortex by Ellman method B 7.8 pIC50 15.85 nM IC50 Med Chem Res (2013) 22: 2328-2345
ChEMBL Inhibition of rat cortex homogenate AchE using acetylthiocholine iodide as substrate after 15 mins by Ellman's method B 7.82 pIC50 15 nM IC50 Eur J Med Chem (2014) 76: 314-331 [PMID:24589487]
ChEMBL Inhibition of rat cortex homogenate acetylcholinesterase by Ellman's method B 7.82 pIC50 15 nM IC50 Eur J Med Chem (2021) 216: 113310-113310 [PMID:33667847]
ChEMBL Inhibition of rat cortex AChE using acetylthiocholine iodide as substrate measured after 15 mins by Ellman's method B 7.82 pIC50 15 nM IC50 Eur J Med Chem (2020) 187: 111958-111958 [PMID:31865014]
ChEMBL Inhibition of AChE from rat cortex homogenate using acetylthiocholine iodide as substrate after 15 mins by Ellman method B 7.82 pIC50 15 nM IC50 Bioorg Med Chem (2015) 23: 911-923 [PMID:25678013]
ChEMBL Inhibition of AChE in rat cortex using acetylthiocholine iodide as substrate after 15 mins by Ellman's method B 7.82 pIC50 15 nM IC50 Eur J Med Chem (2015) 94: 348-366 [PMID:25778991]
ChEMBL Inhibition of rat cortex homogenate AChE using acetylthiocholine iodide as substrate after 15 mins in presence of BuChE inhibitor iso-OMPA by Ellman's method B 7.82 pIC50 15 nM IC50 Eur J Med Chem (2017) 135: 307-323 [PMID:28458136]
ChEMBL Inhibition of rat cortex AChE using acetylthiocholine iodide as substrate after 15 mins by Ellman's method B 7.82 pIC50 15 nM IC50 Bioorg Med Chem (2018) 26: 6115-6127 [PMID:30470598]
ChEMBL Inhibition of rat brain AChE using acetylthiocholine iodide as substrate by spectroscopic method B 7.9 pIC50 12.7 nM IC50 Bioorg Med Chem (2017) 25: 6273-6285 [PMID:29089261]
ChEMBL Inhibition of AChE in rat cortex after 15 mins by modified Ellman's method B 7.92 pIC50 12 nM IC50 Bioorg Med Chem (2009) 17: 6692-6698 [PMID:19692250]
ChEMBL Inhibition of AChE in rat cortex after 15 mins by modified Ellman method B 7.92 pIC50 12 nM IC50 Eur J Med Chem (2009) 44: 7-17 [PMID:18436348]
ChEMBL Inhibition of AChE in rat cortex homogenates using acetylthiocholine iodide substrate incubated for 15 mins by UV spectroscopy based Ellman's method B 7.96 pIC50 11 nM IC50 Bioorg Med Chem (2014) 22: 4717-4725 [PMID:25082512]
ChEMBL Inhibition of rat cortex homogenate acetylcholinesterase by spectrophotometric method B 8 pIC50 10 nM IC50 Bioorg Med Chem (2020) 28: 115820-115820 [PMID:33120080]
ChEMBL Inhibition of AChE in rat cortex preincubated for 20 mins by Ellman method B 8.1 pIC50 7.86 nM IC50 Bioorg Med Chem (2009) 17: 1600-1613 [PMID:19162488]
ChEMBL Inhibitory concentration in vitro and ex vivo for anti-AChE activity in rat brain B 8.24 pIC50 5.7 nM IC50 Bioorg Med Chem Lett (1992) 2: 871-876
ChEMBL Inhibition of rat cortex AChE B 8.24 pIC50 5.7 nM IC50 J Med Chem (2008) 51: 3588-3598 [PMID:18517184]
ChEMBL Inhibition of AChE in rat cortex homogenates using acetylthiocholine iodide as substrate after 15 mins by Ellman's method B 8.3 pIC50 5 nM IC50 Bioorg Med Chem (2011) 19: 7158-7167 [PMID:22019465]
ChEMBL Inhibition of rat cortex homogenate acetylcholinesterase using acetylthiocholine iodide as substrate incubated for 20 mins by Ellman's method B 8.7 pIC50 2 nM IC50 J Med Chem (2021) 64: 1844-1855 [PMID:33570950]
ChEMBL In vitro inhibitory effect on rat Acetylcholinesterase B 8.77 pIC50 1.7 nM IC50 J Med Chem (1995) 38: 2969-2973 [PMID:7636858]
carboxylesterase 1/Acyl coenzyme A:cholesterol acyltransferase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2265] [GtoPdb: 2592] [UniProtKB: P23141]
ChEMBL Inhibition of human carboxylesterase 1 using o-nitrophenylacetate as substrate by spectrophotometry analysis B 4 pIC50 >100000 nM IC50 Bioorg Med Chem (2016) 24: 1050-1062 [PMID:26827140]
beta-secretase 1/Beta-secretase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4822] [GtoPdb: 2330] [UniProtKB: P56817]
ChEMBL Inhibition of BACE1 B 5.49 pIC50 3200 nM IC50 Bioorg Med Chem Lett (2012) 22: 4707-4712 [PMID:22704921]
ChEMBL Inhibition of human BACE-1 using MOCA-SEV-NL-DAEFR-DNP-RR as substrate preincubated with substrate followed by enzyme addition by FRET assay B 6.44 pIC50 362 nM IC50 Eur J Med Chem (2019) 183: 111707-111707 [PMID:31561043]
ChEMBL Inhibition of human BACE-1 by FRET assay B 6.44 pIC50 362 nM IC50 Bioorg Med Chem (2020) 28: 115721-115721 [PMID:33007563]
ChEMBL Inhibition of human BACE1 using as 7-Methoxycoumarin-4-acetyl-[Asn670, Leu671]-Amyloid beta/A4 precursor protein 770 fragment 667-676-(2,4-dinitrophenyl) Lys-Arg-Arg amide trifluoroacetate salt as substrate incubated for 2 hrs by FRET based florescence assay B 6.62 pIC50 240 nM IC50 Eur J Med Chem (2019) 167: 510-524 [PMID:30784883]
ChEMBL Inhibition of BACE1 (unknown origin) B 6.77 pIC50 169 nM IC50 Eur J Med Chem (2017) 138: 738-747 [PMID:28728106]
butyrylcholinesterase/Butyrylcholinesterase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1914] [GtoPdb: 2471] [UniProtKB: P06276]
ChEMBL Non competitive inhibition of human serum BChE using butyrylthiocholine iodide as substrate by Lineweaver-Burk plot analysis B 4.9 pKi 12540 nM Ki Bioorg Med Chem (2013) 21: 5451-5460 [PMID:23810675]
ChEMBL Inhibition of human serum BChE using butyrylthiocholine iodide as substrate after 10 mins measured for every mins by Ellman's method B 4.82 pIC50 15240 nM IC50 Eur J Med Chem (2019) 163: 116-135 [PMID:30503937]
ChEMBL Inhibition of human serum BChE using butyrylthiocholine iodide as substrate preincubated for 20 mins prior to substrate addition by Ellman's method B 4.82 pIC50 15240 nM IC50 Bioorg Med Chem (2013) 21: 5451-5460 [PMID:23810675]
ChEMBL Inhibition of human serum BChE using butyrylthiolcholine iodide as substrate incubated for 20 mins prior to substrate addition by Ellman's method B 4.82 pIC50 15240 nM IC50 Bioorg Med Chem Lett (2013) 23: 2984-2989 [PMID:23562059]
ChEMBL Inhibition of human plasma BuChE using butyrylthiocholine as substrate measured after 5 mins by Ellman's method B 4.84 pIC50 14400 nM IC50 Eur J Med Chem (2020) 191: 112140-112140 [PMID:32088494]
ChEMBL Inhibition of human BuChE using S-butyrylthiocholine iodide as substrate treated 5 mins before substrate addition measured up to 4 mins by Ellman's method B 4.87 pIC50 13600 nM IC50 Bioorg Med Chem Lett (2013) 23: 4336-4341 [PMID:23791077]
ChEMBL Inhibition of human serum BuChE using butyrylthiocholine iodide as substrate preincubated with enzyme for 5 mins followed by substrate addition and measured after 5 mins by Ellman's method B 4.93 pIC50 11860 nM IC50 Eur J Med Chem (2021) 223: 113735-113735 [PMID:34371367]
ChEMBL Inhibition of human plasma BChE using butyrylthiocholine iodide as substrate preincubated for 10 mins followed by substrate addition and measured at 6 mins by Ellman's method B 4.99 pIC50 10240 nM IC50 Bioorg Med Chem (2019) 27: 3650-3662 [PMID:31288978]
ChEMBL Inhibition of human BChE by Ellman's method B 5 pIC50 10050 nM IC50 Bioorg Med Chem (2007) 15: 6596-6607 [PMID:17681794]
ChEMBL Inhibition of recombinant human serum BuChE using butyrylthiocholine iodide as substrate pretreated for 5 mins followed by substrate addition measured for 5 mins by Ellman's method B 5.04 pIC50 9140 nM IC50 Eur J Med Chem (2018) 145: 431-444 [PMID:29335209]
ChEMBL Inhibition of recombinant human BuChE using butyrylthiocholine iodide as substrate preincubated for 5 mins followed by substrate addition and measured for 5 mins by Ellman's method B 5.04 pIC50 9140 nM IC50 Bioorg Med Chem (2019) 27: 931-943 [PMID:30765302]
ChEMBL Inhibition of human serum BuChE using butyrylthiocholine iodide as substrate preincubated for 5 mins followed by substrate addition measured over 5 mins by UV-Vis spectrophotometric analysis B 5.04 pIC50 9140 nM IC50 Eur J Med Chem (2017) 139: 773-791 [PMID:28863358]
ChEMBL Inhibition of human serum BuChE using S-butyrylthiocholine iodide as substrate preincubated for 6 mins followed by substrate addition measured up to 180 secs by Ellman's method B 5.06 pIC50 8700 nM IC50 Eur J Med Chem (2017) 139: 48-59 [PMID:28797883]
ChEMBL Inhibition of human serum butyrylcholinesterase preincubated for 5 mins followed by addition of S-butyrylthiocholine iodide as substrate measured after 60 to 120 mins by Ellmans method B 5.08 pIC50 8280 nM IC50 Medchemcomm (2016) 7: 990-998
ChEMBL Inhibitory concentration against Butyrylcholinesterase (BuChE) from human serum B 5.09 pIC50 8200 nM IC50 J Med Chem (1999) 42: 730-741 [PMID:10052979]
ChEMBL Inhibition of butyrylcholinesterase from human serum B 5.09 pIC50 8200 nM IC50 J Med Chem (2001) 44: 2707-2718 [PMID:11495583]
ChEMBL Inhibition of recombinant human BuChE expressed in HEK293 cells preincubated for 15 mins B 5.09 pIC50 8200 nM IC50 J Med Chem (2014) 57: 10455-10463 [PMID:25418133]
ChEMBL Inhibition of human BChE using butyrylthiocholine iodide as substrate preincubated followed by substrate addition by Ellman's method B 5.12 pIC50 7600 nM IC50 Bioorg Med Chem (2016) 24: 1050-1062 [PMID:26827140]
ChEMBL Inhibition of human serum BChE by Ellman's method B 5.12 pIC50 7600 nM IC50 Eur J Med Chem (2020) 192: 112180-112180 [PMID:32131034]
ChEMBL Inhibition of human recombinant BChE B 5.12 pIC50 7585.78 nM IC50 J Med Chem (2004) 47: 6490-6498 [PMID:15588084]
ChEMBL Inhibition of human recombinant BuChE expressed in HEK293 cells using S-butyrylthiocholine iodide as substrate preincubated for 30 mins followed by substrate addition measured after 30 mins by Ellman's method B 5.12 pIC50 7500 nM IC50 Eur J Med Chem (2016) 121: 864-879 [PMID:26471320]
ChEMBL Inhibition of human BuChE preincubated for 20 mins before substrate addition by Ellman's method B 5.13 pIC50 7420 nM IC50 Bioorg Med Chem (2010) 18: 1749-1760 [PMID:20171894]
ChEMBL Inhibitory potency was evaluated against isolated Butyrylcholinesterase B 5.13 pIC50 7420 nM IC50 J Med Chem (2003) 46: 2279-2282 [PMID:12773032]
ChEMBL Inhibition of human recombinant butyrylcholinesterase B 5.13 pIC50 7420 nM IC50 J Med Chem (2007) 50: 4882-4897 [PMID:17850125]
ChEMBL Inhibition of human serum BChE by Ellman's assay B 5.13 pIC50 7420 nM IC50 J Med Chem (2008) 51: 7308-7312 [PMID:18954037]
ChEMBL Inhibition of human serum BChE by Ellman's method B 5.13 pIC50 7420 nM IC50 Eur J Med Chem (2009) 44: 1341-1348 [PMID:18396354]
ChEMBL Inhibition of human BChE using butyrylthiocholine iodide as substrate by Ellman's method B 5.13 pIC50 7400 nM IC50 Eur J Med Chem (2011) 46: 1682-1693 [PMID:21397996]
ChEMBL Inhibition of human BChE using butyrylthiocholineiodide as substrate incubated for 10 mins by Ellman's method B 5.14 pIC50 7300 nM IC50 Bioorg Med Chem (2021) 30: 115940-115940 [PMID:33340937]
ChEMBL Inhibition of human recombinant BuChE using butyrylthiocholine iodide substrate incubated for 15 mins by spectrophotometry based Ellman's method B 5.15 pIC50 7100 nM IC50 Bioorg Med Chem (2014) 22: 5141-5154 [PMID:25189690]
ChEMBL Inhibition of BChE B 5.15 pIC50 7000 nM IC50 Bioorg Med Chem Lett (2011) 21: 2687-2691 [PMID:21216144]
ChEMBL Inhibition of human serum BChE using butyrylthiocholine iodide as a substrate preincubated for 20 mins followed by substrate addition by spectrophotometric analysis B 5.16 pIC50 6980 nM IC50 Eur J Med Chem (2021) 225: 113779-113779 [PMID:34418785]
ChEMBL Inhibition of BuChE (unknown origin) after 5 mins by Ellman's method B 5.16 pIC50 6920 nM IC50 Eur J Med Chem (2014) 83: 355-365 [PMID:24980117]
ChEMBL Inhibition of recombinant human BChE using butyrylthiocholine iodide as substrate preincubated for 10 mins followed by substrate addition and measured for 10 mins by Ellman's method B 5.19 pIC50 6400 nM IC50 Eur J Med Chem (2021) 212: 113124-113124 [PMID:33395623]
ChEMBL Inhibition of human BChE using butyrylthiocholine iodide as substrate preincubated for 10 mins before substrate addition after 15 mins by Ellman's method B 5.2 pIC50 6370 nM IC50 Eur J Med Chem (2014) 78: 43-53 [PMID:24675179]
ChEMBL Inhibition of human BChE using butyrylthiocholine iodide as substrate preincubated for 10 mins before substrate addition after 15 mins by Ellman's method B 5.2 pIC50 6370 nM IC50 Eur J Med Chem (2014) 78: 167-177 [PMID:24681981]
ChEMBL Inhibition of human serum BuChE using S-butyrylthiocholine iodide as substrate preincubated for 5 mins followed by substrate addition by Ellman's method B 5.25 pIC50 5600 nM IC50 Eur J Med Chem (2015) 103: 302-311 [PMID:26363866]
ChEMBL Inhibition of BuChE (unknown origin) preincubated for 30 mins followed by substrate addition acetylthiocholineiodide measured after 40 mins by Ellman's method B 5.27 pIC50 5400 nM IC50 Eur J Med Chem (2020) 200: 112415-112415 [PMID:32454229]
ChEMBL Inhibition of human BuChE using butyrylthiocholine iodide as substrate incubated for 15 mins by Ellman's method B 5.29 pIC50 5120 nM IC50 Eur J Med Chem (2019) 183: 111737-111737 [PMID:31581002]
ChEMBL Inhibition of human serum BuChE using butylthiocholine chloride as substrate pretreated for 15 mins followed by substrate addition measured for 2 mins by DTNB reagent based spectrophotometric method B 5.3 pIC50 >5000 nM IC50 Eur J Med Chem (2017) 130: 139-153 [PMID:28242549]
ChEMBL Inhibition of human BChE using butyrylthiocholine as substrate preincubated for 20 mins followed by substrate addition and measured upto 5 mins by Ellman's method B 5.32 pIC50 4800 nM IC50 Eur J Med Chem (2019) 177: 414-424 [PMID:31158754]
ChEMBL Inhibition of human serum BuChE by spectrophotometric Ellman's method B 5.32 pIC50 4800 nM IC50 J Med Chem (2015) 58: 5561-5578 [PMID:26107513]
ChEMBL Inhibition of human serum BChE using butyrylthiocholine iodide as substrate preincubated for 10 mins followed by substrate addition and measured for 10 mins by DTNB reagent based Ellman's method B 5.32 pIC50 4786.3 nM IC50 Bioorg Med Chem (2019) 27: 1327-1340 [PMID:30795991]
ChEMBL Inhibition of human serum BChE using butyrylthiocholine chloride as substrate incubated for 15 mins by Ellman's method B 5.32 pIC50 4760 nM IC50 Bioorg Med Chem Lett (2017) 27: 5053-5059 [PMID:29033232]
ChEMBL Inhibition of human serum BCHE preincubated for 6 mins followed by addition of S-butyrylcholine iodide as substrate by Ellman's method B 5.32 pIC50 4760 nM IC50 Bioorg Med Chem (2016) 24: 4324-4338 [PMID:27460699]
ChEMBL Inhibition of human serum BChE using S-butyrylthiocholine iodide as substrate preincubated for 5 mins followed by substrate addition measured up to 180 secs by spectrophotometric analysis B 5.36 pIC50 4380 nM IC50 Eur J Med Chem (2017) 139: 68-83 [PMID:28800459]
ChEMBL Inhibitory concentration against human plasma Butyrylcholinesterase B 5.38 pIC50 4150 nM IC50 J Med Chem (2005) 48: 986-994 [PMID:15715468]
ChEMBL Anticholinesterase activity against human plasma BChE B 5.38 pIC50 4150 nM IC50 J Med Chem (2006) 49: 2174-2185 [PMID:16570913]
ChEMBL Ex vivo inhibition of human plasma Butyrylcholinesterase. B 5.38 pIC50 4150 nM IC50 J Med Chem (2002) 45: 3684-3691 [PMID:12166941]
ChEMBL Inhibition of BChE (unknown origin) B 5.38 pIC50 4150 nM IC50 Eur J Med Chem (2018) 156: 598-617 [PMID:30031971]
ChEMBL Inhibition of human BChE after 20 mins using butyrylthiocholine iodide as a substrate by Ellman's assay B 5.41 pIC50 3900 nM IC50 J Med Chem (2011) 54: 2627-2645 [PMID:21417225]
ChEMBL Inhibition of human BuChE using S-butyrylthiocholine iodide as substrate preincubated for 5 mins followed by substrate addition measured after 60 to 300 sec by Ellman's method B 5.44 pIC50 3600 nM IC50 Medchemcomm (2015) 6: 1930-1941
ChEMBL Inhibition of BuChE in human serum using butyrylthiocholine chloride as substrate measured after 15 mins by Ellman's method B 5.49 pIC50 3200 nM IC50 Eur J Med Chem (2017) 130: 379-392 [PMID:28279845]
ChEMBL Inhibition of human serum BChE using acetylthiocholine iodide as substrate measured after 15 mins by Ellman's method B 5.49 pIC50 3200 nM IC50 Eur J Med Chem (2020) 187: 111958-111958 [PMID:31865014]
ChEMBL Inhibition of human serum BuChE using s-butyrylthiocholine iodide as substrate preincubated for 5 mins followed by substrate addition measured up to 3 mins by Ellman's method B 5.5 pIC50 3170 nM IC50 Eur J Med Chem (2016) 123: 282-297 [PMID:27484514]
ChEMBL Inhibition of human serum BuChE using butyrylthiocholine iodide as substrate incubated for 5 mins followed by substrate addition measured after 180 secs by Ellman's method B 5.5 pIC50 3170 nM IC50 Eur J Med Chem (2018) 157: 161-176 [PMID:30096650]
ChEMBL Concentration required to inhibit 50% of Butyrylcholinesterase obtained from human serum was determined in vitro B 5.54 pIC50 2900 nM IC50 J Med Chem (1995) 38: 1084-1089 [PMID:7707311]
ChEMBL Inhibition of human BChE using butyrylthiocholineiodide as substrate measured for every 30 sec for 5 mins by Ellman's method B 5.54 pIC50 2900 nM IC50 ACS Med Chem Lett (2020) 11: 869-876 [PMID:32435398]
ChEMBL Inhibition of human serum BuChE using S-butyrylthiocholine iodide as substrate preincubated for 6 mins followed by substrate addition measured up to 180 secs by spectrophotometric-based Ellman's method B 5.56 pIC50 2740 nM IC50 Bioorg Med Chem (2016) 24: 1528-1539 [PMID:26917219]
ChEMBL Inhibition of human serum BuChE using butyrylthiocholine as substrate preincubated for 5 mins followed by substrate addition measured for 5 mins by Ellman's method B 5.6 pIC50 2500 nM IC50 Eur J Med Chem (2016) 121: 376-386 [PMID:27267007]
ChEMBL Inhibition of human serum BChE using butyrylthiocholine as substrate by Ellman method B 5.6 pIC50 2500 nM IC50 Eur J Med Chem (2012) 57: 296-301 [PMID:23078965]
ChEMBL Inhibition of human plasma BuChE using butyrylthiocholine as substrate by Ellman's method B 5.6 pIC50 2500 nM IC50 Eur J Med Chem (2013) 67: 64-74 [PMID:23838422]
ChEMBL Inhibition of human serum BuChE using butyrylthiocholine iodide as substrate pretreated for 5 mins followed by substrate addition measured for 5 mins by UV-Vis spectrophotometric method B 5.6 pIC50 2500 nM IC50 Eur J Med Chem (2017) 130: 60-72 [PMID:28242552]
ChEMBL Inhibition of human serum BuChE using butyrylthiocholine as substrate pretreated for 5 mins followed by substrate addition measured after 5 mins by Ellman's method B 5.6 pIC50 2500 nM IC50 Eur J Med Chem (2018) 158: 781-800 [PMID:30245401]
ChEMBL Inhibition of human serum BuChE using butyrylthiocholine as substrate pretreated for 5 mins followed by substrate addition and measured for 5 mins by Ellman's method B 5.6 pIC50 2500 nM IC50 Eur J Med Chem (2018) 156: 534-553 [PMID:30025348]
ChEMBL Inhibition of human serum BChE using butyrylthiocholine iodide as substrate preincubated for 10 mins followed by substrate addition by Ellman's method B 5.62 pIC50 2420 nM IC50 Eur J Med Chem (2019) 183: 111707-111707 [PMID:31561043]
ChEMBL Inhibition of human BChE by Ellman's method B 5.62 pIC50 2420 nM IC50 Bioorg Med Chem (2020) 28: 115721-115721 [PMID:33007563]
ChEMBL Inhibition of butyrylcholinesterase (unknown origin) B 5.7 pIC50 2000 nM IC50 Bioorg Med Chem (2013) 21: 146-152 [PMID:23199476]
ChEMBL Inhibition of human serum butyrylcholinesterase using BTCI as substrate pre-incubated for 10 mins followed by substrate addition and measured for 6 mins by Ellman's method B 5.85 pIC50 1400 nM IC50 Eur J Med Chem (2019) 167: 510-524 [PMID:30784883]
ChEMBL Inhibition of BuChE in human serum using butyrylthiocholineiodide as substrate pre-incubated for 10 mins followed by substrate addition and measured for 6 mins by DTNB reagent based Ellman's method B 5.92 pIC50 1210 nM IC50 Eur J Med Chem (2021) 215: 113224-113224 [PMID:33582578]
ChEMBL Inhibition of human serum BChE by Ellman's assay B 6.03 pIC50 930 nM IC50 J Med Chem (2008) 51: 3588-3598 [PMID:18517184]
ChEMBL Inhibition of butyrylcholinesterase (unknown origin) using butyrylthiocholine chloride as substrate incubated for 10 mins followed by substrate addition measured after 20 mins by UV-Vis spectrophotometric analysis B 6.89 pIC50 130 nM IC50 Bioorg Med Chem (2017) 25: 100-106 [PMID:27780618]
ChEMBL Inhibition of recombinant human BuChe using S-butyrylthiocholine iodide as substrate measured after 7 mins by Ellman's method B 6.93 pIC50 117 nM IC50 Eur J Med Chem (2021) 222: 113541-113541 [PMID:34116326]
ChEMBL Inhibition of human BChE by Ellman's method B 7.7 pIC50 20 nM IC50 Bioorg Med Chem (2014) 22: 6163-6173 [PMID:25257911]
ChEMBL Inhibition of human Cholinesterase B 7.85 pIC50 14 nM IC50 Bioorg Med Chem (2019) 27: 895-930 [PMID:30744931]
Butyrylcholinesterase in Equus caballus (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5077] [UniProtKB: Q9N1N9]
ChEMBL Inhibition of Equine Butyrylcholinesterase B 6.19 pKi 640 nM Ki J Med Chem (2003) 46: 1-4 [PMID:12502352]
ChEMBL Dissociation constant for inhibition of equine Butyrylcholinesterase (BuChE) B 6.19 pKi 640 nM Ki J Med Chem (2005) 48: 1919-1929 [PMID:15771436]
ChEMBL Inhibition of equine serum BChE using butyrylthiocholine iodide as substrate after 15 mins by Ellman's method B 5.13 pIC50 7400 nM IC50 Eur J Med Chem (2012) 52: 251-262 [PMID:22503231]
ChEMBL Inhibition Assay: The inhibitory activity of the enzyme acetylcholinesterase (AChE) was evaluated by the Ellman method (Biochem. Pharmacol. 1961, 7, 88) using an electric eel as an AChE neuronal model (Electrophorus electricus) and acetylthiocholine iodide (0.35 mM) as substrate. The reaction took place in a final volume of 3 mL of a 0.1 M phosphate buffer solution, pH 8.0, containing 0.035 units of AChE and used a 0.35 mM solution of 5,5'-dithio-bis(2-nitrobenzoic acid) (DTNB) to produce the 5-thio-2-nitrobenzoic acid anion. Inhibition curves were performed in triplicate by incubating at least nine inhibitor concentrations for 10 min. A triplicate sample without inhibitor was always present so as to be aware of 100% of the AChE activity. After this time, the substrate was added to 0.35 mM acetylthiocholine iodide, from a 10 mM stock solution. Loss of color was observed at 412 nm in a spectrophotometric reader having 96 well plates. B 5.13 pIC50 7400 nM IC50 US-8999994-B2. Derivatives of propargylamine having neuroprotective capacity for the treatment of Alzheimer's and Parkinson's diseases (2015)
ChEMBL Inhibition of (BChE) Butyrylcholinesterase of horse serum B 5.38 pIC50 4166.7 nM IC50 Bioorg Med Chem Lett (1992) 2: 861-864
ChEMBL Inhibition of equine BChE preincubated for 15 mins by Ellman's method B 5.47 pIC50 3365.4 nM IC50 Eur J Med Chem (2014) 87: 429-439 [PMID:25282266]
ChEMBL Compound was evaluated for the in vitro inhibition of the Butyrylcholinesterase from horse serum B 5.54 pIC50 2900 nM IC50 J Med Chem (1994) 37: 2721-2734 [PMID:8064800]
butyrylcholinesterase/Butyrylcholinesterase in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2528] [GtoPdb: 2471] [UniProtKB: Q03311]
ChEMBL Inhibition of BuChE in mouse brain homogenate using butyrylthiocholine as substrate preincubated for 300 secs followed by substrate addition by Ellman's method B 5.15 pIC50 7138 nM IC50 J Med Chem (2018) 61: 119-139 [PMID:29227101]
ChEMBL Inhibition of BuChE in mouse serum using butyrylthiocholine iodide as substrate incubated for 20 mins by Ellman's method B 5.7 pIC50 1992 nM IC50 Eur J Med Chem (2022) 229: 114045-114045 [PMID:34922191]
Butyrylcholinesterase in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3403] [UniProtKB: Q9JKC1]
ChEMBL Inhibition of rat serum butyrylcholinesterase using butyrylthiocholine iodide as substrate incubated for 15 mins by Ellman's method B 4.67 pIC50 21400 nM IC50 Bioorg Med Chem (2019) 27: 895-930 [PMID:30744931]
ChEMBL Inhibition of rat serum BuChE measured after 15 mins by Ellman's method B 4.67 pIC50 21400 nM IC50 Bioorg Med Chem (2017) 25: 714-726 [PMID:27923535]
ChEMBL Inhibition of rat serum BuChE using butyrylthiocholine iodide as substrate after 15 mins by Ellman's method B 4.68 pIC50 20700 nM IC50 Eur J Med Chem (2014) 76: 314-331 [PMID:24589487]
ChEMBL Inhibition of rat serum BuChE by Ellman's method B 4.68 pIC50 20700 nM IC50 Eur J Med Chem (2021) 216: 113310-113310 [PMID:33667847]
ChEMBL Inhibition of rat serum BChE using acetylthiocholine iodide as substrate measured after 15 mins by Ellman's method B 4.68 pIC50 20700 nM IC50 Eur J Med Chem (2020) 187: 111958-111958 [PMID:31865014]
ChEMBL Inhibition of rat serum BChE using butyrylthiocholine iodide as substrate by Ellman's method B 4.89 pIC50 12773 nM IC50 Eur J Med Chem (2021) 226: 113827-113827 [PMID:34530383]
ChEMBL Inhibition of rat serum BuChE using S-butyrylthiocholine iodide as substrate incubated for 8 mins by Ellman's method B 4.97 pIC50 10833.33 nM IC50 J Med Chem (2021) 64: 1844-1855 [PMID:33570950]
ChEMBL In vitro inhibitory concentration against butyrylcholinesterase was determined using rat serum homogenate B 5.12 pIC50 7600 nM IC50 Bioorg Med Chem Lett (2005) 15: 3834-3837 [PMID:15993600]
ChEMBL Inhibitory concentration was determined in in vitro for Butyrylcholinesterase in rat plasma B 5.15 pIC50 7138 nM IC50 Bioorg Med Chem Lett (1992) 2: 871-876
ChEMBL Inhibition of rat serum BChE B 5.15 pIC50 7138 nM IC50 J Med Chem (2008) 51: 3588-3598 [PMID:18517184]
ChEMBL Inhibition of rat plasma butyrylcholine esterase in presence of butyrylcholine substrate by chemiluminescent assay B 5.28 pIC50 5300 nM IC50 Eur J Med Chem (2008) 43: 657-661 [PMID:17624631]
ChEMBL Inhibition of rat cortex homogenate BuChE by spectrophotometric method B 5.3 pIC50 5010 nM IC50 Bioorg Med Chem (2020) 28: 115820-115820 [PMID:33120080]
ChEMBL Inhibition of BChE in rat serum after 15 mins by modified Ellman's method B 5.33 pIC50 4670 nM IC50 Bioorg Med Chem (2009) 17: 6692-6698 [PMID:19692250]
ChEMBL Inhibition of rat serum BChE using butyrylthiocholine chloride as substrate incubated for 15 mins by Ellman's method B 5.35 pIC50 4420 nM IC50 Bioorg Med Chem Lett (2017) 27: 5053-5059 [PMID:29033232]
ChEMBL Inhibition of BuchE in rat serum by Ellman's method B 5.49 pIC50 3260 nM IC50 Bioorg Med Chem (2008) 16: 7646-7653 [PMID:18662884]
ChEMBL Inhibition of BChE in rat serum after 15 mins by modified Ellman method B 5.56 pIC50 2770 nM IC50 Eur J Med Chem (2009) 44: 7-17 [PMID:18436348]
ChEMBL Inhibition of BChE in rat serum using butyrylthiocholine iodide substrate incubated for 15 mins by UV spectroscopy based Ellman's method B 5.89 pIC50 1280 nM IC50 Bioorg Med Chem (2014) 22: 4717-4725 [PMID:25082512]
choline O-acetyltransferase/Choline acetylase in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3945] [GtoPdb: 2480] [UniProtKB: P32738]
ChEMBL In vitro inhibitory activity against acetylcholinesterase B 8.28 pIC50 5.3 nM IC50 J Med Chem (1992) 35: 584-589 [PMID:1738151]
Cholinesterase in Equus caballus (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5763] [UniProtKB: P81908]
ChEMBL Non-competitive inhibition of horse serum BuChE using butyrylthiocoline iodide as substrate incubated for 20 mins by Lineweaver-Burk plot analysis B 5.67 pKi 2140 nM Ki ACS Med Chem Lett (2016) 7: 470-475 [PMID:27190595]
ChEMBL Inhibition of equine serum BuChE using butyrylthiocholine iodide as substrate preincubated for 20 mins followed by substrate addition and measured after 20 mins by Ellman's method B 4.93 pIC50 11810 nM IC50 Eur J Med Chem (2018) 147: 194-204 [PMID:29438888]
ChEMBL Inhibition of equine serum BuChE using butyrylthiocholine chloride as substrate incubated for 15 to 20 mins by Ellman's method B 4.97 pIC50 10600 nM IC50 Bioorg Med Chem Lett (2021) 52: 128306-128306 [PMID:34371131]
ChEMBL Inhibition of equine serum BuChE using butyrylthiocholine iodide as substrate preincubated with enzyme for 20 mins followed by substrate addition by Ellman's method B 4.98 pIC50 10380 nM IC50 Eur J Med Chem (2019) 181: 111598-111598 [PMID:31415981]
ChEMBL Inhibition of equine serum BuChE using butyrylthiocholine iodide as substrate preincubated with enzyme for 20 mins followed by addition of substrate and measured after 20 mins by DTNB reagent based Ellman's method B 4.98 pIC50 10380 nM IC50 Eur J Med Chem (2020) 201: 112273-112273 [PMID:32569925]
ChEMBL Inhibition of equine serum BuChE using butyrylthiocholine iodide as substrate preincubated with enzyme for 20 mins followed by substrate addition and measured after 20 mins by Ellman's method B 5.03 pIC50 9240 nM IC50 Eur J Med Chem (2021) 223: 113735-113735 [PMID:34371367]
ChEMBL Inhibition of equine serum BuChE using butyrylthiocholine iodide as substrate measured for 6 mins by Ellman's method B 5.06 pIC50 8730 nM IC50 Bioorg Med Chem (2017) 25: 3980-3988 [PMID:28587871]
ChEMBL Inhibition of equine serum BuChE using butyrylthiocholine iodide as substrate pretreated for 5 mins followed by substrate addition measured after 5 mins by Ellman's method B 5.06 pIC50 8710 nM IC50 Eur J Med Chem (2019) 175: 2-19 [PMID:31055149]
ChEMBL Inhibition of equine serum BuChE using DTNB as substrate incubated for 5 mins prior to substrate addition measured after 2 mins by Ellman's method B 5.06 pIC50 8710 nM IC50 Bioorg Med Chem (2015) 23: 6389-6403 [PMID:26337018]
ChEMBL Inhibition of equine serum BuChE using butyrylthiocholine iodide as substrate preincubated for 5 mins followed by substrate addition and measured after 5 mins by Ellman method B 5.06 pIC50 8710 nM IC50 Bioorg Med Chem (2019) 27: 3156-3166 [PMID:31176571]
ChEMBL Inhibition of equine serum BuChE by Ellman's method B 5.07 pIC50 8416 nM IC50 Bioorg Med Chem Lett (2020) 30: 127477-127477 [PMID:32781220]
ChEMBL Inhibition of equine serum BChE using butyrylcholine chloride as substrate preincubated for 15 mins followed by substrate addition and measured after 15 mins under dark condition by Ellman's method B 5.08 pIC50 8400 nM IC50 Bioorg Med Chem (2019) 27: 4030-4040 [PMID:31378596]
ChEMBL Inhibition of equine serum BuChE using S-butyrylthiocholine iodide as substrate preincubated with enzyme for 30 mins followed by substrate addition and measured after 30 mins by Ellman's method B 5.1 pIC50 7870 nM IC50 Eur J Med Chem (2019) 177: 198-211 [PMID:31136894]
ChEMBL Inhibition of horse serum butyrylcholinesterase using butyrylthiocholine iodide as substrate preincubated for 5 mins followed by substrate addition measured after 5 mins by Ellman's method B 5.11 pIC50 7690 nM IC50 Eur J Med Chem (2016) 107: 219-232 [PMID:26588065]
ChEMBL Inhibition of equine serum BuChE using butyrylthiocholine iodide as substrate measured for 2 mins by Ellman's method B 5.13 pIC50 7400 nM IC50 Eur J Med Chem (2016) 121: 40-46 [PMID:27214510]
ChEMBL Inhibition of equine serum BuChE using butyrylthiocholine iodide as substrate preincubated for 20 mins followed by substrate addition measured after 25 mins by Ellman's method B 5.13 pIC50 7400 nM IC50 Eur J Med Chem (2014) 80: 543-561 [PMID:24813882]
ChEMBL Inhibition of equine serum BuchE using butyrylthiocholine iodide as substrate preincubated for 10 mins measured after 15 mins of substrate addition by Ellman's method B 5.13 pIC50 7400 nM IC50 J Med Chem (2011) 54: 8251-8270 [PMID:22023459]
ChEMBL Inhibition of equine serum BChE using butyrylthiocholine iodide as substrate by spectrophotometer analysis B 5.14 pIC50 7300 nM IC50 Eur J Med Chem (2014) 82: 536-544 [PMID:24941128]
ChEMBL Inhibition of equine serum BuChE pre-incubated for 5 mins before butyrylthiocholine iodide substrate addition and measured after 15 mins by Ellman's method B 5.14 pIC50 7200 nM IC50 Bioorg Med Chem (2019) 27: 2914-2922 [PMID:31128990]
ChEMBL Inhibition of equine serum BuChE pre-incubated for 5 mins before butyrylthiocholine iodide substrate by Ellman' method B 5.15 pIC50 7000 nM IC50 J Med Chem (2015) 58: 3172-3187 [PMID:25793650]
ChEMBL Inhibition of horse serum BChE using butrylthiocholine iodide as substrate preincubated for 5 mins followed by substrate addition measured for 10 mins by modified Ellman's method B 5.19 pIC50 6500 nM IC50 Bioorg Med Chem (2016) 24: 2352-2359 [PMID:27083471]
ChEMBL Inhibition of equine BuChE using ACTI as substrate preincubated for 29 mins followed by substrate addition measured at 1 min intervals for 10 mins by Ellman's assay B 5.23 pIC50 5910 nM IC50 J Med Chem (2016) 59: 7683-7689 [PMID:27405689]
ChEMBL Inhibition of equine serum BChE using S-butyrylthiocholine iodide as substrate preincubated for 20 mins followed by substrate addition and measured every minute for 10 mins by DTNB-reagent based Ellman's method B 5.26 pIC50 5520 nM IC50 Eur J Med Chem (2020) 207: 112761-112761 [PMID:32942070]
ChEMBL Inhibition of equine serum BuChE using S-butyrylthiocholine iodide as substrate after 30 mins by Ellman's method B 5.26 pIC50 5520 nM IC50 Medchemcomm (2012) 3: 1098-1103
ChEMBL Inhibition of equine serum BChE using butyrylthiocholine iodide as substrate preincubated for 15 mins prior to substrate addition by Ellman's method B 5.27 pIC50 5380 nM IC50 Eur J Med Chem (2013) 70: 623-630 [PMID:24211638]
ChEMBL Inhibition of equine serum BuChE using butyrylthiocholine iodide substrate by Ellman method based spectrophotometry B 5.27 pIC50 5380 nM IC50 Eur J Med Chem (2014) 84: 375-381 [PMID:25036795]
ChEMBL Inhibition of equine serum BChE using butyrylthiocholine iodide as substrate after 2 mins by Ellman's method B 5.27 pIC50 5380 nM IC50 Eur J Med Chem (2013) 68: 260-269 [PMID:23988409]
ChEMBL Inhibition of BuChE in equine serum using Butyrylthiocholine iodide as substrate by Ellman's method B 5.28 pIC50 5200 nM IC50 Eur J Med Chem (2019) 179: 680-693 [PMID:31280020]
ChEMBL Inhibition of equine serum BChE using butyrylthiocholine iodide as substrate by Ellman's method B 5.31 pIC50 4900 nM IC50 Medchemcomm (2019) 10: 1018-1026 [PMID:31304000]
ChEMBL Inhibition of equine serum BuChE using butyrylthiocholine chloride as substrate after 15 mins by Ellman's method B 5.32 pIC50 4760 nM IC50 Bioorg Med Chem (2017) 25: 3006-3017 [PMID:28487125]
ChEMBL Inhibition of equine serum BChE by Ellman's method B 5.32 pIC50 4760 nM IC50 Eur J Med Chem (2020) 192: 112180-112180 [PMID:32131034]
ChEMBL Inhibition of equine serum BuChE using butyrylthiocholine iodide as substrate incubated for 15 mins by Ellman's method B 5.32 pIC50 4760 nM IC50 Eur J Med Chem (2019) 180: 238-252 [PMID:31310916]
ChEMBL Inhibition of equine serum BuChE using S-butyrylthiocholine iodide as susbtrate preincubated for 6 mins followed by substrate addition measured up to 3 mins by Ellman's method B 5.32 pIC50 4760 nM IC50 Eur J Med Chem (2019) 178: 726-739 [PMID:31229875]
ChEMBL Inhibition of equine serum BuChE using S-butyrylthiocholine chloride as substrate incubated for 15 mins by Ellman's method B 5.32 pIC50 4760 nM IC50 Bioorg Med Chem Lett (2019) 29: 126625-126625 [PMID:31444085]
ChEMBL Inhibition of equine butyrylcholinesterase using butyrylthiocholine iodide as substrate incubated for 15 mins by Ellman's method B 5.32 pIC50 4760 nM IC50 Eur J Med Chem (2019) 183: 111737-111737 [PMID:31581002]
ChEMBL Inhibition of equine serum BuChE using butyrylthiocholine chloride as substrate measured after 15 mins by Ellman's method B 5.32 pIC50 4760 nM IC50 Eur J Med Chem (2017) 130: 379-392 [PMID:28279845]
ChEMBL Inhibition of equine serum BChE using butyrylthiocholine chloride as substrate incubated for 15 mins by Ellman's method B 5.32 pIC50 4760 nM IC50 Bioorg Med Chem Lett (2017) 27: 5053-5059 [PMID:29033232]
ChEMBL Inhibition of equine serum BuChE using butyrylthiocholine iodide as substrate pretreated for 10 mins followed by substrate addition measured at 12 secs interval for 5 mins by Ellman's method B 5.33 pIC50 4690 nM IC50 Eur J Med Chem (2017) 130: 440-457 [PMID:28282613]
ChEMBL Inhibition of equine serum BuChE using acetylthiocholine iodide as substrate preincubated for 10 mins followed by substrate addition by Ellman's method B 5.33 pIC50 4690 nM IC50 Eur J Med Chem (2018) 147: 48-65 [PMID:29421570]
ChEMBL Inhibition of equine serum butyrylcholinesterase using butyrylthiocholine chloride as substrate incubated for 15 mins prior to substrate addition measured every 1 min by Ellman's assay B 5.33 pIC50 4660 nM IC50 Bioorg Med Chem Lett (2012) 22: 4462-4466 [PMID:22633691]
ChEMBL Inhibition of equine serum BuChE using s-butyrylthiocholine iodide as substrate preincubated for 6 mins followed by substrate addition measured up to 180 sec by Ellman's method B 5.35 pIC50 4500 nM IC50 Eur J Med Chem (2017) 133: 184-196 [PMID:28388521]
ChEMBL Inhibition of horse serum BChE using butyrylthiocholine iodide as substrate preincubated for 5 mins by Ellman method B 5.35 pIC50 4460 nM IC50 Bioorg Med Chem (2015) 23: 2445-2457 [PMID:25868744]
ChEMBL Inhibition of equine serum butyrylcholinesterase preincubated for 5 mins followed by addition of S-butyrylthiocholine iodide as substrate measured after 60 to 120 mins by Ellmans method B 5.38 pIC50 4170 nM IC50 Medchemcomm (2016) 7: 990-998
ChEMBL Inhibition of equine serum BuChE using S-butyrylthiocholine iodide as substrate preincubated for 6 mins followed by substrate addition measured up to 180 secs by spectrophotometric-based Ellman's method B 5.42 pIC50 3790 nM IC50 Bioorg Med Chem (2016) 24: 1528-1539 [PMID:26917219]
ChEMBL Inhibition of equine serum BuChE using thiocholine iodide as substrate by Ellman's method B 5.44 pIC50 3620 nM IC50 Bioorg Med Chem Lett (2015) 25: 5212-5216 [PMID:26454504]
ChEMBL Inhibition of equine BuChE using butyrylthiocholine iodide as substrate after 5 mins by DTNB method B 5.44 pIC50 3600 nM IC50 Bioorg Med Chem Lett (2012) 22: 4707-4712 [PMID:22704921]
ChEMBL Inhibition of equine serum BChE using butyrylthiocholine iodide as substrate preincubated for 10 mins followed by substrate addition and measured for 10 mins by Ellman's method B 5.45 pIC50 3550 nM IC50 Eur J Med Chem (2021) 212: 113124-113124 [PMID:33395623]
ChEMBL Inhibition of equine serum BuChE using butyrylthiocholine chloride as substrate preincubated for 15 mins followed by substrate addition and measured after 4 mins by Ellman's method B 5.45 pIC50 3540 nM IC50 Bioorg Med Chem (2021) 32: 115991-115991 [PMID:33440318]
ChEMBL Inhibition of equine serum butyrylcholinesterase using butyrylthiocholine chloride as substrate preincubated for 15 mins followed by substrate addition by Ellman's method B 5.46 pIC50 3490 nM IC50 Bioorg Med Chem (2014) 22: 1355-1361 [PMID:24461494]
ChEMBL Inhibition of equine serum BuChE using butyrylthiocholine iodide as substrate pretreated for 5 mins followed by substrate addition by Ellman's method B 5.47 pIC50 3400 nM IC50 Eur J Med Chem (2018) 152: 600-614 [PMID:29763808]
ChEMBL Inhibition of equine serum BuChE using butyrylthiocholine chloride as substrate preincubated for 15 mins followed by substrate addition measured every 1 min by Ellman's method B 5.47 pIC50 3365 nM IC50 J Med Chem (2013) 56: 9089-9099 [PMID:24160297]
ChEMBL Inhibition of equine serum BChE using butyrylthiocholine iodide as substrate preincubated for 5 mins followed by substrate addition measured every minute for 10 mins by Ellman's method B 5.47 pIC50 3365 nM IC50 Eur J Med Chem (2018) 145: 165-190 [PMID:29324339]
ChEMBL Inhibition of equine BCHE preincubated for 6 mins followed by addition of S-butyrylcholine iodide as substrate by Ellman's method B 5.47 pIC50 3360 nM IC50 Bioorg Med Chem (2016) 24: 4324-4338 [PMID:27460699]
ChEMBL Inhibition of equine serum BuChE using butyrylthiocholine iodide as substrate preincubated for 5 mins followed by substrate addition measured after 2 mins by Ellman's method B 5.47 pIC50 3360 nM IC50 Bioorg Med Chem (2016) 24: 3829-3841 [PMID:27353888]
ChEMBL Inhibition of equine serum butyrylcholine esterase incubated for 15 mins using S-butyrylthiocholine chloride substrate by colorimetric Ellman's method B 5.48 pIC50 3310 nM IC50 Eur J Med Chem (2015) 94: 195-210 [PMID:25768702]
ChEMBL Inhibition of equine serum BChE using butyrylthiocholine iodide as substrate preincubated for 2 mins followed by substrate addition and measured after 2 mins by Ellman's method B 5.49 pIC50 3200 nM IC50 Bioorg Med Chem (2018) 26: 3812-3824 [PMID:29960728]
ChEMBL Inhibition of equine serum BuChE using butyrylthiocholine iodide as substrate incubated for 5 mins followed by substrate addition and measured after 2 mins by Ellman's method B 5.5 pIC50 3140 nM IC50 Bioorg Med Chem (2016) 24: 2777-2788 [PMID:27157006]
ChEMBL Inhibition of equine serum BuChE using acetylthiocholine iodide as substrate preincubated for 15 mins followed by substrate addition by spectrophotometric analysis B 5.51 pIC50 3060 nM IC50 Bioorg Med Chem (2017) 25: 2946-2955 [PMID:28454848]
ChEMBL Inhibition of recombinant equine serum BuChE using butyryl thiocholine iodide as substrate preincubated for 30 mins followed by substrate addition and measured after 30 mins by spectrophotometry based Ellman's method B 5.54 pIC50 2890 nM IC50 Eur J Med Chem (2020) 198: 112257-112257 [PMID:32375073]
ChEMBL Inhibition of equine serum BChE using S-butyrylthiocholine iodide as substrate preincubated for 5 mins followed by substrate addition measured up to 180 secs by spectrophotometric analysis B 5.54 pIC50 2890 nM IC50 Eur J Med Chem (2017) 139: 68-83 [PMID:28800459]
ChEMBL Inhibition of equine serum BuChE using S-butylthiocholine iodide as substrate preincubated for 10 mins followed by substrate addition measured after 10 mins by Ellman's method B 5.54 pIC50 2870 nM IC50 Eur J Med Chem (2017) 125: 853-864 [PMID:27744252]
ChEMBL Inhibition of equine serum BuChE using butyrylthiocholine iodide as substrate preincubated for 5 mins followed by substrate addition measured after 2 mins by spectroscopy based Ellman's method B 5.57 pIC50 2720 nM IC50 Eur J Med Chem (2017) 136: 36-51 [PMID:28478343]
ChEMBL Inhibition of horse serum butyrylcholine esterase in presence of acetylcholine substrate by chemiluminescent assay B 5.57 pIC50 2700 nM IC50 Eur J Med Chem (2008) 43: 657-661 [PMID:17624631]
ChEMBL Inhibition of equine serum BChE using butyrylthiocholine iodide as substrate preincubated for 10 mins followed by substrate addition and measured after 15 mins by Ellman's method B 5.58 pIC50 2660 nM IC50 Eur J Med Chem (2022) 229: 114044-114044 [PMID:34923430]
ChEMBL Inhibition of equine serum BuChE using butyrylthiocholine as substrate preincubated for 5 mins followed by substrate addition measured after 20 mins by Ellman's method B 5.59 pIC50 2600 nM IC50 Bioorg Med Chem Lett (2020) 30: 126900-126900 [PMID:31882295]
ChEMBL Inhibition of equine serum BuChE preincubated for 5 mins followed by addition of butyrylthiocholine iodide as substrate measured after 2 mins by Ellman's method B 5.59 pIC50 2580 nM IC50 Eur J Med Chem (2016) 119: 260-277 [PMID:27227482]
ChEMBL Inhibition of horse serum BuChE using butyrylthiocholine as substrate by Ellman's method B 5.6 pIC50 2500 nM IC50 Eur J Med Chem (2014) 73: 56-72 [PMID:24378710]
ChEMBL Inhibition of equine serum BuChE using s-butyrylthiocholine iodide as substrate preincubated for 5 mins followed by substrate addition measured up to 3 mins by Ellman's method B 5.61 pIC50 2480 nM IC50 Eur J Med Chem (2016) 123: 282-297 [PMID:27484514]
ChEMBL Inhibition of equine serum BuChE using butyrylthiocholine iodide as substrate incubated for 5 mins followed by substrate addition measured after 180 secs by Ellman's method B 5.61 pIC50 2480 nM IC50 Eur J Med Chem (2018) 157: 161-176 [PMID:30096650]
ChEMBL Inhibition of equine serum BuChE using butyrylthiocholine iodide as substrate preincubated with enzyme for 6 mins followed by substrate addition and measured for 180 secs by Ellman's method B 5.61 pIC50 2470 nM IC50 RSC Med Chem (2020) 11: 225-233 [PMID:33479629]
ChEMBL Inhibition of equine serum BChE using butyrylthiocholine iodide as substrate preincubated for 20 mins followed by substrate addition measured for 5 mins by spectrophotometric Ellman's method B 5.64 pIC50 2310 nM IC50 J Med Chem (2016) 59: 6791-6806 [PMID:27347731]
ChEMBL Inhibition of equine serum BCHE using butyrylthiocholine iodide as substrate preincubated for 20 mins followed by substrate addition measured for 5 mins by spectrophotometry based Ellman method B 5.64 pIC50 2300 nM IC50 Bioorg Med Chem Lett (2017) 27: 1179-1185 [PMID:28189420]
ChEMBL Inhibition of equine serum BChE using butyrylthiocholine as substrate preincubated for 20 mins followed by substrate addition and measured upto 5 mins by Ellman's method B 5.64 pIC50 2300 nM IC50 Eur J Med Chem (2019) 177: 414-424 [PMID:31158754]
ChEMBL Inhibition of equine serum BChE using butyrylthiocholine iodide as substrate incubated for 5 mins followed by substrate addition measured for 5 mins by Ellman's method B 5.66 pIC50 2200 nM IC50 Eur J Med Chem (2019) 174: 116-129 [PMID:31029943]
ChEMBL Inhibition of equine serum BChE using butyrylthiocholine iodide as substrate preincubated with enzyme for 30 mins followed by substrate addition and measured after 30 mins by Ellman's method B 5.67 pIC50 2160 nM IC50 Bioorg Med Chem (2021) 46: 116385-116385 [PMID:34481338]
ChEMBL Inhibition of equine serum BuChE using butyrylthiocholine iodide as substrate by Ellman's method B 5.68 pIC50 2100 nM IC50 Eur J Med Chem (2019) 161: 292-309 [PMID:30366255]
ChEMBL Inhibition of horse serum BChE by Ellman's spectrophotometric assay B 5.68 pIC50 2100 nM IC50 J Med Chem (2022) 65: 3962-3977 [PMID:35195417]
ChEMBL Inhibition of equine serum BChE using butyrylthiocholine iodide as substrate incubated for 5 mins by Ellman's method B 5.72 pIC50 1911 nM IC50 Bioorg Med Chem (2015) 23: 1135-1148 [PMID:25624107]
ChEMBL Inhibition of equine butyrylcholinesterase using butyrylthiocholine as substrate incubated for 20 mins prior to substrate addition measured after 3 mins by Ellman's method B 5.72 pIC50 1900 nM IC50 Bioorg Med Chem (2013) 21: 146-152 [PMID:23199476]
ChEMBL Inhibition of equine serum BChE using butyrylthiocholine chloride as substrate preincubated for 5 mins followed by substrate addition measured after 5 mins by Ellmans method B 5.74 pIC50 1830 nM IC50 Bioorg Med Chem Lett (2016) 26: 4140-4145 [PMID:27445168]
ChEMBL Inhibition of equine serum BuChE using butyrylthiocholine iodide as substrate preincubated for 5 mins followed by substrate addition measured after 5 mins by Ellman's method B 5.74 pIC50 1830 nM IC50 Eur J Med Chem (2017) 125: 676-695 [PMID:27721153]
ChEMBL Inhibition of equine serum BuChE preincubated for 5 mins followed by butyrylthiocholine iodide substrate addition measured after 5 mins by Ellman's method B 5.74 pIC50 1830 nM IC50 Eur J Med Chem (2016) 124: 63-81 [PMID:27560283]
ChEMBL Inhibition of equine serum BuChE after 5 mins by Ellman's method B 5.74 pIC50 1830 nM IC50 Eur J Med Chem (2015) 92: 738-749 [PMID:25621991]
ChEMBL Inhibition of equine serum BChE using butyrylthiocholine iodide as substrate preincubated with enzyme for 5 mins prior to substrate addition measured after 5 mins by Ellman's method B 5.74 pIC50 1830 nM IC50 Eur J Med Chem (2020) 185: 111785-111785 [PMID:31669851]
ChEMBL Inhibition of equine serum BuChE using butyrylthiocholine chloride as substrate pre-incubated for 5 mins followed by substrate addition and measured after 5 mins by Ellman's method B 5.74 pIC50 1830 nM IC50 Eur J Med Chem (2020) 187: 111916-111916 [PMID:31812794]
ChEMBL Inhibition of BuChE in horse serum pre-incubated for 5 mins before addition of butyrylthiocholine iodide substrate by Ellman's assay B 5.74 pIC50 1830 nM IC50 Bioorg Med Chem (2015) 23: 1629-1637 [PMID:25707322]
ChEMBL Inhibition of equine serum BuChE using butyrylthiocholine as substrate preincubated for 5 mins followed by substrate addition and measured after 5 mins by Ellman's method B 5.74 pIC50 1830 nM IC50 Eur J Med Chem (2021) 218: 113397-113397 [PMID:33838585]
ChEMBL Inhibition of equine serum BuChE using BTC as substrate preincubated with enzyme for 5 mins followed by substrate addition for 5 mins by Ellman's method B 5.74 pIC50 1830 nM IC50 Eur J Med Chem (2021) 225: 113792-113792 [PMID:34530376]
ChEMBL Inhibition of equine serum BuChE using butyrylthiocholine as substrate incubated for 5 mins followed by substrate addition and measured after 5 mins by spectrophotometric based Ellman's method B 5.74 pIC50 1830 nM IC50 Eur J Med Chem (2021) 225: 113783-113783 [PMID:34461507]
ChEMBL Inhibition of BuChE in equine serum using butyrylthiocholine iodide as substrate preincubated with enzyme for 10 mins prior to substrate challenge measured after 15 mins by Ellman's method B 5.74 pIC50 1820 nM IC50 Bioorg Med Chem (2014) 22: 2496-2507 [PMID:24657052]
ChEMBL Inhibition of horse serum BuChE using acetylthiocholine as substrate after 60 mins by FRET assay B 5.87 pIC50 1340 nM IC50 Bioorg Med Chem Lett (2018) 28: 2910-2913 [PMID:30017317]
ChEMBL Inhibition of recombinant equine BChE by Ellman's method B 5.89 pIC50 1300 nM IC50 Bioorg Med Chem (2021) 46: 116355-116355 [PMID:34391122]
ChEMBL Inhibition of horse serum BuChE using butyrylthiocoline iodide as substrate incubated for 20 mins by Ellman method B 5.9 pIC50 1270 nM IC50 ACS Med Chem Lett (2016) 7: 470-475 [PMID:27190595]
ChEMBL Inhibition of equine serum BuChE using BTCI as substrate preincubated for 30 mins followed by substrate addition measured after 30 mins by Ellman assay B 5.9 pIC50 1260 nM IC50 J Med Chem (2016) 59: 5823-5846 [PMID:27253679]
ChEMBL Inhibition of equine serum BuChE using butyrylthiocholine iodide as substrate preincubated for 30 mins followed by substrate addition and measured for 1 min by DTNB reagent-based spectrophotometric analysis B 6.03 pIC50 941 nM IC50 Eur J Med Chem (2019) 182: 111613-111613 [PMID:31437780]
ChEMBL Inhibition of equine serum BuChE using butyrylthiocholine iodide as substrate preincubated for 20 mins followed by substrate addition measured after 25 mins by Ellman's method B 6.08 pIC50 840 nM IC50 Eur J Med Chem (2014) 75: 82-95 [PMID:24530494]
ChEMBL Inhibition of equine serum BuChE by Ellman's method B 6.08 pIC50 840 nM IC50 J Med Chem (2010) 53: 5129-5143 [PMID:20575555]
ChEMBL Inhibition of equine serum BuChE using butyrylthiocholine iodide as substrate preincubated for 15 mins by Ellman's method B 6.27 pIC50 540 nM IC50 Bioorg Med Chem Lett (2015) 25: 5576-5582 [PMID:26514744]
ChEMBL Inhibition of equine serum BChE using butyrylthiocholine iodide as substrate preincubated for 10 mins followed by substrate addition measured for 5 mins by Ellman's method B 6.46 pIC50 350 nM IC50 Eur J Med Chem (2018) 155: 49-60 [PMID:29857276]
ChEMBL Inhibition of equine serum BuChE using butyrylthiocholine iodide as substrate preincubated for 10 mins followed by substrate addition measured for 5 mins by Ellman's method B 6.46 pIC50 350 nM IC50 Bioorg Med Chem (2018) 26: 4952-4962 [PMID:30190181]
ChEMBL Inhibition of horse serum BuChE using acetylthiocholine as substrate by UV-visible spectrophotometric Ellman's method B 6.64 pIC50 231 nM IC50 Bioorg Med Chem Lett (2018) 28: 2910-2913 [PMID:30017317]
ChEMBL Inhibition of horse serum BChE using butyrylthiocholine iodide as substrate pretreated for 10 mins followed by substrate addition measured after 20 mins by Ellman's method B 6.89 pIC50 130 nM IC50 Bioorg Med Chem (2018) 26: 3696-3706 [PMID:29886083]
ChEMBL Inhibition of equine serum BuChE using S-butyrylthiocholine iodide as substrate preincubated for 6 mins followed by substrate addition measured up to 180 secs by Ellman's method B 8.34 pIC50 4.6 nM IC50 Eur J Med Chem (2017) 139: 48-59 [PMID:28797883]
glycogen synthase kinase 3 beta/Glycogen synthase kinase-3 beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL262] [GtoPdb: 2030] [UniProtKB: P49841]
ChEMBL Inhibition of human recombinant GSK-3beta using prephosphorylated polypeptide as substrate incubated for 30 mins in presence of ATP by Kinase-Glo luminescence assay B 4 pIC50 >100000 nM IC50 J Med Chem (2021) 64: 7483-7506 [PMID:34024109]
ChEMBL Inhibition of human recombinant N-terminal His-tagged GSK3beta expressed in Escherichia coli using RRRPASVPPSPSLS RHS(pS)HQRR as substrate incubated for 30 mins in presence of ATP by Kinase-Glo reagent based luminescence assay B 5 pIC50 >10000 nM IC50 Eur J Med Chem (2021) 223: 113663-113663 [PMID:34198150]
ChEMBL Inhibition of recombinant human N-terminal His6-tagged GSK3beta H350L mutant expressed in baculovirus infected Sf21 cells using prephosphorylated polypeptide as substrate incubated for 1 min followed by substrate addition and measured after 30 mins by Kinase-Glo luminescence assay B 6 pIC50 >1000 nM IC50 Bioorg Med Chem (2021) 30: 115940-115940 [PMID:33340937]
Kv11.1/HERG in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809]
ChEMBL Inhibition of hERG expressed in CHO-K1 cells assessed as reduction in thallium influx incubated for 30 minutes by FLIPR B 5.06 pIC50 8718 nM IC50 Eur J Med Chem (2021) 226: 113827-113827 [PMID:34530383]
ChEMBL Inhibition of human ERG B 5.7 pIC50 1995.26 nM IC50 Eur J Med Chem (2011) 46: 618-630 [PMID:21185626]
H3 receptor/Histamine H3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL264] [GtoPdb: 264] [UniProtKB: Q9Y5N1]
ChEMBL Inhibition of histamine H3 receptor B 6.46 pIC50 350 nM IC50 Bioorg Med Chem (2008) 16: 2968-2973 [PMID:18249544]
Monoamine oxidase B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2039] [GtoPdb: 2490] [UniProtKB: P27338]
ChEMBL Inhibition of human recombinant MAOB using p-tyramine as substrate preincubated for 30 mins followed by substrate addition measured for 1 hr by horse-radish peroxidase/amplex red-based fluorometric method B 4.82 pIC50 15200 nM IC50 Eur J Med Chem (2016) 121: 864-879 [PMID:26471320]
ChEMBL Inhibition of human recombinant MAO-B using tyramine as substrate preincubated for 30 mins followed by substrate addition measured for 1 hr by fluorometric assay B 4.82 pIC50 15000 nM IC50 Eur J Med Chem (2014) 75: 82-95 [PMID:24530494]
Monoamine oxidase B in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2993] [GtoPdb: 2490] [UniProtKB: P19643]
ChEMBL Inhibition of rat liver mitochondrial MAO-B using [14C]-phenylethylamine after 30 mins by scintillation counting B 4.82 pIC50 15000 nM IC50 J Med Chem (2011) 54: 8251-8270 [PMID:22023459]
ChEMBL Inhibition of mitochondrial MAO-B in rat liver homogenates using [14C]-phenylethylamine as substrate preincubated for 30 mins by liquid scintillation counting B 4.82 pIC50 15000 nM IC50 Eur J Med Chem (2012) 52: 251-262 [PMID:22503231]
ChEMBL Inhibition of MAO-B in rat liver homogenate using [14C]-phenylethylamine as substrate preincubated for 30 mins followed by substrate addition measured after 4 mins by liquid scintillation counting analysis B 4.82 pIC50 15000 nM IC50 Eur J Med Chem (2014) 80: 543-561 [PMID:24813882]
ABCB1/P-glycoprotein 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4302] [GtoPdb: 768] [UniProtKB: P08183]
ChEMBL Inhibition of human recombinant MDR1 in cell membrane fraction preincubated for 5 mins measured after 40 mins by Pgp-Glo luciferase assay B 4.46 pIC50 34850 nM IC50 Bioorg Med Chem Lett (2015) 25: 297-301 [PMID:25499431]
phosphodiesterase 5A/Phosphodiesterase 5A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1827] [GtoPdb: 1304] [UniProtKB: O76074]
ChEMBL Inhibition of PDE5A (unknown origin) B 4 pIC50 >100000 nM IC50 Bioorg Med Chem Lett (2020) 30: 127097-127097 [PMID:32171616]
Sigma-1 receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4153] [UniProtKB: Q60492]
ChEMBL Displacement of [3H]DTG from S1R in P2 fraction of Hartley guinea pig whole brain after 90 mins by liquid scintillation counting method B 7.84 pKi 14.6 nM Ki Eur J Med Chem (2018) 158: 353-370 [PMID:30223122]
sigma non-opioid intracellular receptor 1/Sigma opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL287] [GtoPdb: 2552] [UniProtKB: Q99720]
ChEMBL Displacement of [3H]DTG from sigma 1 receptor (unknown origin) B 7.84 pKi 14.6 nM Ki Bioorg Med Chem (2013) 21: 2764-2771 [PMID:23582449]
ChEMBL Inhibition of [3H]DTG binding to sigma 1 receptor (unknown origin) B 7.84 pKi 14.6 nM Ki J Med Chem (2020) 63: 15187-15217 [PMID:33111525]

ChEMBL data shown on this page come from version 33:

Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]