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| ChEMBL ligand: CHEMBL502 (D-797, Donaz, Donepezil, Donepezilo) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| phosphodiesterase 4D/3`,5`-cyclic-AMP phosphodiesterase 4D in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL288] [GtoPdb: 1303] [UniProtKB: Q08499] | ||||||||
| ChEMBL | Inhibition of PDE4D7 (unknown origin) | B | 4.44 | pIC50 | 36000 | nM | IC50 | Eur J Med Chem (2022) 238: 114503-114503 [PMID:35689855] |
| nicotinic acetylcholine receptor ε subunit/Acetylcholine receptor subunit epsilon in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2484] [GtoPdb: 477] [UniProtKB: Q04844] | ||||||||
| ChEMBL | Inhibition of human AChE by Ellman's method | B | 7.49 | pIC50 | 32.36 | nM | IC50 | Eur J Med Chem (2022) 230: 114098-114098 [PMID:35026532] |
| 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 electrical eel AChE using acetylthiocholine chloride as substrate preincubated for 15 mins followed by substrate addition and measured after 30 mins by DTNB reagent based Ellman's method | B | 5.14 | pIC50 | 7300 | nM | IC50 | Bioorg Med Chem (2023) 78: 117132-117132 [PMID:36542960] |
| 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 30 mins by Ellman's method | B | 5.49 | pIC50 | 3210 | nM | IC50 | Eur J Med Chem (2024) 271: 116388-116388 [PMID:38614062] |
| 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 every min for 10 mins by DTNB based Ellman's assay | B | 7.18 | pIC50 | 66 | nM | IC50 | Bioorg Med Chem (2024) 101: 117649-117649 [PMID:38401458] |
| 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 ATCI and BTCI as substrate preincubated for 5 mins followed by substrate addition and measured after 3 mins by DTNB-reagent based Ellman's method | B | 7.28 | pIC50 | 52 | nM | IC50 | Bioorg Med Chem (2023) 78: 117146-117146 [PMID:36580744] |
| 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 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 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 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 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 Electrophorus electricus AchE | B | 7.31 | pIC50 | 49 | nM | IC50 | Eur J Med Chem (2021) 221: 113492-113492 [PMID:33984802] |
| 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 | 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 | 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 Electrophorus electricus AchE using acetylcholine iodide as substrate incubated for 10 mins followed by substrate addition measured at 0 to 180 secs by Ellman's method | B | 7.33 | pIC50 | 47 | nM | IC50 | Eur J Med Chem (2022) 234: 114210-114210 [PMID:35303485] |
| 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 with enzyme for 20 mins followed by substrate addition and measured after 10 mins by Ellman's method | B | 7.35 | pIC50 | 45 | nM | IC50 | Eur J Med Chem (2022) 238: 114503-114503 [PMID:35689855] |
| 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 AChE using acetylthiocholine iodide as substrate preincubated for 5 mins followed by substrate addition by DTNB reagent based Ellman's method | B | 7.39 | pIC50 | 41 | nM | IC50 | Eur J Med Chem (2022) 242: 114630-114630 [PMID:35987018] |
| 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 | B | 7.4 | pIC50 | 40 | nM | IC50 | Bioorg Med Chem Lett (2022) 61: 128602-128602 [PMID:35124202] |
| 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 | B | 7.4 | pIC50 | 40 | nM | IC50 | Bioorg Med Chem (2023) 80: 117178-117178 [PMID:36706609] |
| 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 | 7.4 | pIC50 | 40 | nM | IC50 | Eur J Med Chem (2022) 229: 114095-114095 [PMID:34995924] |
| 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 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 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 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 using acetylthiocholine iodine as substrate preincubated for 20 mins followed by substrate addition and measured after 20 mins by DTNB reagent based Ellman's method | B | 7.4 | pIC50 | 40 | nM | IC50 | Eur J Med Chem (2022) 242: 114689-114689 [PMID:36007469] |
| 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 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 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 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 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 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 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 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 preincubated with enzyme for 10 mins followed by substrate addition and measured every 1 min for 20 mins by spectrophotometric analysis | B | 7.51 | pIC50 | 31 | nM | IC50 | Eur J Med Chem (2023) 259: 115670-115670 [PMID:37515920] |
| 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 Electrophorus electricus AchE using acetylthiocholine iodide as substrate preincubated for 10 mins followed by substrate addition by spectrophotometric based Ellman's method | B | 7.52 | pIC50 | 30 | nM | IC50 | Bioorg Med Chem (2022) 71: 116952-116952 [PMID:35930852] |
| 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 | B | 7.54 | pIC50 | 29 | nM | IC50 | Eur J Med Chem (2020) 186: 111893-111893 [PMID:31761383] |
| ChEMBL | Inhibition of electric eel AChE using acetylthiocholine iodide as substrate preincubated for 20 mins followed by substrate addition and measured after 20 mins by DTNB reagent based Ellman's method | B | 7.54 | pIC50 | 29 | nM | IC50 | Eur J Med Chem (2023) 257: 115502-115502 [PMID:37224761] |
| 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 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 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 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 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 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 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 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 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 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 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 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 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 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 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 with compounds for 20 mins followed by substrate addition and measured after 5 mins by Ellman's method | B | 7.68 | pIC50 | 21 | nM | IC50 | Eur J Med Chem (2023) 259: 115695-115695 [PMID:37567058] |
| 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 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 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 ATC and BTC iodide as substrate preincubated for 5 mins followed by substrate addition and measured after 2 mins by DTNB reagent based assay | B | 7.68 | pIC50 | 21 | nM | IC50 | Eur J Med Chem (2022) 244: 114806-114806 [PMID:36223681] |
| ChEMBL | Inhibition of electric eel AChE using acetylthiocholine iodide as substrate preincubated for 20 mins followed by substrate addition and measured after 10 mins by DTNB-reagent based Ellman's method | B | 7.68 | pIC50 | 21 | nM | IC50 | Eur J Med Chem (2024) 270: 116353-116353 [PMID:38579622] |
| ChEMBL | Inhibition of electric eel AChE assessed as residual enzyme activity using acetylthiocholine iodide as substrate and measured for 10 mins by Ellman's colorimetric assay | B | 7.68 | pIC50 | 21 | nM | IC50 | Bioorg Med Chem (2024) 110: 117829-117829 [PMID:39002183] |
| 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 preincubated for 20 mins followed by substrate addition by DTNB reagent based Ellman's method | B | 7.7 | pIC50 | 20 | nM | IC50 | Eur J Med Chem (2023) 250: 115169-115169 [PMID:36753881] |
| 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 chloride by spectrophotometry | B | 7.7 | pIC50 | 20 | nM | IC50 | Medchemcomm (2013) 4: 925-931 |
| 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 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 using acetylthiocholine iodide as substrate incubated for 30 min by DTNB reagent based Ellman's method | B | 7.7 | pIC50 | 20 | nM | IC50 | RSC Med Chem (2024) 15: 2922-2936 [PMID:39149109] |
| ChEMBL | Inhibition of electric eel AChE using acetylthiocholine iodide as substrate preincubated with enzyme for 20 mins followed by substrate addition and measured for 10 mins by Ellman's method | B | 7.7 | pIC50 | 20 | nM | IC50 | Eur J Med Chem (2024) 266: 116131-116131 [PMID:38215587] |
| ChEMBL | Inhibition of electric eel AChE using acetylthiocholine iodide as substrate preincubated for 15 mins followed by substrate addition by Ellman's method | B | 7.7 | pIC50 | 20 | nM | IC50 | Eur J Med Chem (2022) 244: 114841-114841 [PMID:36257284] |
| ChEMBL | Inhibition of electric eel AChE using acetylthiocholine iodide as substrate pre-incubated for 30 mins followed by substrate addition and measured after 5 mins by DTNB reagent based Ellman's method | B | 7.7 | pIC50 | 20 | nM | IC50 | Eur J Med Chem (2024) 264: 116013-116013 [PMID:38052155] |
| 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 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 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 | 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 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 | 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 as substrate by Ellman's method | B | 7.77 | pIC50 | 17 | nM | IC50 | Eur J Med Chem (2024) 276: 116592-116592 [PMID:39013357] |
| 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 electric eel AChE using acetylthiocholine iodide as substrate preincubated for 20 mins followed by substrate addition and measured after 5 mins by DTNB-reagent based Ellman's method | B | 7.8 | pIC50 | 16 | nM | IC50 | Eur J Med Chem (2022) 227: 113973-113973 [PMID:34752955] |
| ChEMBL | Inhibition of electric eel AChE by Ellman's method | B | 7.82 | pIC50 | 15 | nM | IC50 | Eur J Med Chem (2022) 230: 114098-114098 [PMID:35026532] |
| 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 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 electric eel AChE by Ellman's method | B | 7.83 | pIC50 | 14.79 | nM | IC50 | Eur J Med Chem (2022) 230: 114098-114098 [PMID:35026532] |
| 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 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 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 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 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 chloride as substrate by Ellman's method | B | 7.89 | pIC50 | 13 | nM | IC50 | Eur J Med Chem (2023) 251: 115253-115253 [PMID:36921526] |
| 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 15 mins by Ellman's method | B | 7.96 | pIC50 | 11 | nM | IC50 | RSC Med Chem (2024) 15: 2037-2044 [PMID:38911155] |
| 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 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 and measured after 5 mins by DTNB reagent based Ellman's method | B | 7.96 | pIC50 | 11 | nM | IC50 | Eur J Med Chem (2023) 261: 115832-115832 [PMID:37837674] |
| 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 electric eel AChE using acetylthiocholine iodide as substrate preincubated for 5 mins followed by substrate addition and measured after 5 mins by DTNB-reagent based Ellman's method | B | 8 | pIC50 | 10 | nM | IC50 | Eur J Med Chem (2023) 249: 115135-115135 [PMID:36696766] |
| 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 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 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 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 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 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 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 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] |
| 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) |
| 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 plasma BChE | B | 5.38 | pIC50 | 4150 | nM | IC50 | Eur J Med Chem (2011) 46: 2170-2184 [PMID:21459491] |
| 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 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 human AChE using acetylthiocholine iodide as substrate measured after 15 to 20 mins by DTNB reagent based Ellman's method | B | 6.66 | pIC50 | 220 | nM | IC50 | Eur J Med Chem (2023) 262: 115880-115880 [PMID:37871406] |
| 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 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 human AChE by Ellmans test | B | 7.05 | pIC50 | 90 | nM | IC50 | J Med Chem (2010) 53: 6490-6505 [PMID:20684567] |
| ChEMBL | Inhibition of human acetylcholinesterase using acetylthiocholine iodide as substrate incubated for 15 mins by Ellman's method | B | 7.06 | pIC50 | 87 | nM | IC50 | RSC Med Chem (2022) 13: 1644-1656 [PMID:36561075] |
| ChEMBL | Inhibition of AChE (unknown origin) by Ellman's method | B | 7.1 | pIC50 | 80 | nM | IC50 | Bioorg Med Chem Lett (2024) 98: 129566-129566 [PMID:38008338] |
| ChEMBL | Inhibition of AChE (unknown origin) by Ellman's method | B | 7.1 | pIC50 | 79 | nM | IC50 | RSC Med Chem (2024) 15: 207-222 [PMID:38283217] |
| 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 human recombinant AChe using acetylthiocholine iodide as substrate incubated for 10 mins by DTNB reagent based Ellman's method | B | 7.22 | pIC50 | 60 | nM | IC50 | J Med Chem (2022) 65: 12292-12318 [PMID:36084304] |
| 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 iodide as substrate incubated for 5 mins by Ellman's method | B | 7.23 | pIC50 | 59 | nM | IC50 | Eur J Med Chem (2022) 227: 113964-113964 [PMID:34743062] |
| ChEMBL | Inhibition of C-terminal 6His-tagged human recombinant AChE (32 to 614 residues) expressed in HEK293 cells using acetylthiocholine iodide as substrate preincubated for 5 mins followed by substrate addition by Ellman's method | B | 7.27 | pIC50 | 54 | nM | IC50 | Eur J Med Chem (2022) 231: 114152-114152 [PMID:35101650] |
| 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 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 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 iodide as substrate preincubated for 30 mins followed by substrate addition by DTNB based Ellman's colorimetric method | B | 7.33 | pIC50 | 47 | nM | IC50 | Eur J Med Chem (2024) 271: 116409-116409 [PMID:38663285] |
| ChEMBL | Inhibition of human AChE using ATC and BTC iodide as substrate preincubated for 5 mins followed by substrate addition and measured after 2 mins by DTNB reagent based assay | B | 7.36 | pIC50 | 44 | nM | IC50 | Eur J Med Chem (2022) 244: 114806-114806 [PMID:36223681] |
| 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 erythrocyte AChE using acetylthiocholine iodide as substrate preincubated for 30 mins followed by substrate addition and measured after 30 mins by DTNB based Ellman's method | B | 7.37 | pIC50 | 43 | nM | IC50 | Eur J Med Chem (2024) 271: 116450-116450 [PMID:38701714] |
| 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 | 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 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 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 | 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 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 recombinant AchE | B | 7.49 | pIC50 | 32 | nM | IC50 | Eur J Med Chem (2021) 221: 113492-113492 [PMID:33984802] |
| 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 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 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 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 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 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 AChE (unknown origin) by Ellman's method | B | 7.6 | pIC50 | 25 | nM | IC50 | Bioorg Med Chem Lett (2022) 75: 128976-128976 [PMID:36067929] |
| ChEMBL | Inhibition of AChE (unknown origin) | B | 7.6 | pIC50 | 25 | nM | IC50 | Eur J Med Chem (2024) 273: 116523-116523 [PMID:38795518] |
| ChEMBL | Inhibition of human AChE | B | 7.6 | pIC50 | 25 | nM | IC50 | Eur J Med Chem (2023) 259: 115670-115670 [PMID:37515920] |
| 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 | Inhibition of human recombinant acetylcholinesterase | B | 7.64 | pIC50 | 23.1 | nM | IC50 | J Med Chem (2007) 50: 4882-4897 [PMID:17850125] |
| 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 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 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 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 | B | 7.64 | pIC50 | 22.91 | nM | IC50 | J Med Chem (2004) 47: 6490-6498 [PMID:15588084] |
| 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 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 | Inhibition of AChE (unknown origin) | B | 7.66 | pIC50 | 22 | nM | IC50 | Eur J Med Chem (2023) 259: 115670-115670 [PMID:37515920] |
| 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 | 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 AChE using acetylthiocholine iodide as substrate preincubated for 5 mins followed by substrate addition by DTNB reagent based Ellman's method | B | 7.68 | pIC50 | 21 | nM | IC50 | Eur J Med Chem (2022) 242: 114630-114630 [PMID:35987018] |
| 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 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 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 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 for 20 mins followed by substrate addition and measured after 10 mins by DTNB-reagent based Ellman's method | B | 7.74 | pIC50 | 18 | nM | IC50 | Eur J Med Chem (2024) 270: 116353-116353 [PMID:38579622] |
| 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 | 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 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 | 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 recombinant AChE expressed in HEK293 cells using acetylthiocholine iodide as substrate by Ellman's method | B | 7.77 | pIC50 | 17 | nM | IC50 | Eur J Med Chem (2024) 274: 116511-116511 [PMID:38820854] |
| ChEMBL | Inhibition of human serum recombinant AChE using acetylthiocholine iodide as a substrate incubated for 20 mins by DTNB reagent based Ellman's method | B | 7.77 | pIC50 | 17 | nM | IC50 | RSC Med Chem (2022) 13: 873-883 [PMID:35923722] |
| ChEMBL | Inhibition of human AChE by Ellman's spectrophotometric method | B | 7.77 | pIC50 | 17 | nM | IC50 | Eur J Med Chem (2022) 237: 114358-114358 [PMID:35462163] |
| ChEMBL | Inhibition of human recombinant AChE using acetylthiocholine iodide as substrate preincubated for 20 mins followed by substrate addition by DTNB reagent based Ellman's method | B | 7.77 | pIC50 | 17 | nM | IC50 | Eur J Med Chem (2023) 250: 115169-115169 [PMID:36753881] |
| 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 | 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 | 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 | 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 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 human AChE using acetylthiocholine iodide as substrate preincubated with enzyme for 20 mins followed by substrate addition and measured for 5 mins by Ellman's spectrophotometric method | B | 7.8 | pIC50 | 16 | nM | IC50 | Bioorg Med Chem (2023) 84: 117256-117256 [PMID:37003157] |
| 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 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 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 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 Assay: Acetylcholinesterase extracted from human erythrocytes (buffered aqueous solution, ≧500 units/mg, Sigma Aldrich) is diluted in a 20 mM HEPES buffer pH8, 0.1% Triton X-100, to obtain a standard solution with 2.5 units of enzyme activity/ml. 100 μL of a 0.3 mM 5,5-dithiobis(2-nitrobenzoic acid) (DTNB) solution in a pH 7.4 phosphate buffer are introduced into a 96-well plate, followed by 50 μL of compound to be tested in solution in DMSO and 50 μL of enzyme solution. After 5 min of preincubation, the reaction is initiated by injecting 50 μL of 10 mM acetylthiocholine iodide solution. Hydrolysis of the acetylthiocholine is followed by the formation of the anion 5-thio-2-nitrobenzoate, produced by the reaction of the DTNB with the thiocholine released by the enzymatic hydrolysis of the acetylthiocholine, by means of a microplate reader (TECAN Infinite M200, Lyon, France) at a wavelength of 412 nm per minute for 10 minutes. Donepezil is used as a reference product. | B | 7.96 | pIC50 | 11 | nM | IC50 | US-9663465-B2. Acetylcholinesterase inhibitors and promnesiant serotonin 5-HT4 receptor agonists, their methods of preparation and the pharmaceutical compositions containing the same (2017) |
| 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 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 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 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 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 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 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 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 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 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 AChE (unknown origin) | B | 8 | pIC50 | 10 | nM | IC50 | RSC Med Chem (2024) 15: 2037-2044 [PMID:38911155] |
| 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 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 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 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 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's assay | B | 8 | pIC50 | 10 | nM | IC50 | Eur J Med Chem (2019) 166: 90-107 [PMID:30685536] |
| ChEMBL | Inhibition of AChE (unknown origin) using acetylthiocholine iodide as substrate by Ellman's method | B | 8 | pIC50 | 10 | nM | IC50 | Eur J Med Chem (2024) 271: 116386-116386 [PMID:38614063] |
| 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 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 | Enzyme Assay: The potential of the compounds of the present invention to inhibit acetylcholinesterase and butyrylcholinesterase enzymes were tested according to the method of Ellman et.al. (i.e., Ellman, G. L., Courtney, K. D., Andres, V., and Featherstone, R. M., Biochem. Pharmacol., 1961, 7, 88-95).Human recombinant acetylcholinesterase and human recombinant butyrylcholinesterase were employed. Each reaction mixture contained the enzyme (either ACHE or BCHE) solution, DTNB and sample in Tris HCl buffer solution. The reactions were initiated by the addition of the substrate (either acetylthiocholine iodide or butyrylthiocholine iodide, respectively for ACHE and BCHE enzymes). The enzyme catalyzed formation of the yellow color was measured at 412 nm in terms of the calculation of enzyme activity concomitant to the presence of an inhibitor activity. | B | 8.1 | pIC50 | 8 | nM | IC50 | US-9586925-B2. 1-(dimethylamino)ethyl-substituted 6H-benzo[C]chromen-6-ones against senile dementia (2017) |
| 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 | 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 | Inhibition of AChE | B | 8.1 | pIC50 | 8 | nM | IC50 | Eur J Med Chem (2010) 45: 1167-1172 [PMID:20053484] |
| 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 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 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 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) 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 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 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 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 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 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) | B | 8.24 | pIC50 | 5.7 | nM | IC50 | Bioorg Med Chem (2013) 21: 676-683 [PMID:23273608] |
| 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 AChE (unknown origin) | B | 8.24 | pIC50 | 5.7 | nM | IC50 | Eur J Med Chem (2018) 147: 48-65 [PMID:29421570] |
| 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 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 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 AChE (unknown origin) incubated for 30 mins by Ellman's method | B | 8.4 | pIC50 | 4 | nM | IC50 | Eur J Med Chem (2022) 233: 114242-114242 [PMID:35276424] |
| ChEMBL | Inhibition of human erythrocyte AChE using acetylthiocholine iodide as substrate preincubated for 5 mins followed by substrate addition and measured every min for 10 mins by Ellman's method | B | 8.41 | pIC50 | 3.9 | nM | IC50 | RSC Med Chem (2024) 15: 963-980 [PMID:38516603] |
| 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] |
| ChEMBL | Inhibition of AChE in mouse cerebral cortex using acetylthiocholine iodide as substrate preincubated for 10 mins followed by substrate addition and measured for 180 secs by Ellman's spectrophotometric method | B | 8.27 | pIC50 | 5.4 | nM | IC50 | Eur J Med Chem (2022) 235: 114305-114305 [PMID:35339839] |
| 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] |
| Monoamine oxidase B/Amine oxidase [flavin-containing] B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2039] [GtoPdb: 2490] [UniProtKB: P27338] | ||||||||
| ChEMBL | Inhibition of human recombinant MAO-B incubated for 30 mins by fluorescence based assay | B | 4.64 | pIC50 | 23000 | nM | IC50 | Eur J Med Chem (2022) 233: 114242-114242 [PMID:35276424] |
| 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/Amine oxidase [flavin-containing] 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] |
| Amyloid-beta precursor protein in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2487] [UniProtKB: P05067] | ||||||||
| ChEMBL | Inhibition of self mediated Amyloid beta (1 to 42) (unknown origin) aggregation measured every 5 mins by ThT fluorescence based assay | B | 4.06 | pIC50 | 87410 | nM | IC50 | Eur J Med Chem (2023) 262: 115880-115880 [PMID:37871406] |
| ABCB1/ATP-dependent translocase ABCB1 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] |
| 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 (7-Methoxycoumarin-4-acetyl-[Asn670, Leu671]-Amyloid beta/A4 precursor protein 770 fragments 667-676- (2, 4-dinitrophenyl) Lys-Arg-Arg amide trifluoroacetate salt as substrate incubated for 2 hrs by FRET-based analysis | B | 5.9 | pIC50 | 1247 | nM | IC50 | Eur J Med Chem (2024) 271: 116409-116409 [PMID:38663285] |
| 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 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 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 human BACE-1 measured after 2 hrs by FRET assay | B | 6.64 | pIC50 | 227 | nM | IC50 | Eur J Med Chem (2024) 271: 116450-116450 [PMID:38701714] |
| ChEMBL | Inhibition of BACE1 (unknown origin) | B | 6.77 | pIC50 | 169 | nM | IC50 | Eur J Med Chem (2017) 138: 738-747 [PMID:28728106] |
| ChEMBL | Inhibition of human recombinant BACE1 | B | 7.74 | pIC50 | 18 | nM | IC50 | Eur J Med Chem (2021) 221: 113492-113492 [PMID:33984802] |
| 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 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] |
| phosphodiesterase 5A/cGMP-specific 3`,5`-cyclic phosphodiesterase 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] |
| ChEMBL | Inhibition of PDE5A1 (unknown origin) using [3H]-cGMP substrate incubated for 15 mins by liquid scintillation counting method | B | 7.96 | pIC50 | 11 | nM | IC50 | Eur J Med Chem (2024) 271: 116386-116386 [PMID:38614063] |
| choline O-acetyltransferase/Choline O-acetyltransferase 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] |
| butyrylcholinesterase/Cholinesterase 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 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 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 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 recombinant BuChe using butyrylthiocholine iodide as substrate incubated for 10 mins by DTNB reagent based Ellman's method | B | 4.97 | pIC50 | 10660 | nM | IC50 | J Med Chem (2022) 65: 12292-12318 [PMID:36084304] |
| ChEMBL | Inhibition of BuChE (unknown origin) by Ellman's method | B | 4.97 | pIC50 | 10600 | nM | IC50 | RSC Med Chem (2024) 15: 207-222 [PMID:38283217] |
| 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 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 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 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 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 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 butyrylcholinesterase from human serum | B | 5.09 | pIC50 | 8200 | nM | IC50 | J Med Chem (2001) 44: 2707-2718 [PMID:11495583] |
| 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 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 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 serum BChE by Ellman's assay | B | 5.13 | pIC50 | 7420 | nM | IC50 | J Med Chem (2008) 51: 7308-7312 [PMID:18954037] |
| 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 method | B | 5.13 | pIC50 | 7420 | nM | IC50 | Eur J Med Chem (2009) 44: 1341-1348 [PMID:18396354] |
| 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 | 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 | Enzyme Assay: The potential of the compounds of the present invention to inhibit acetylcholinesterase and butyrylcholinesterase enzymes were tested according to the method of Ellman et.al. (i.e., Ellman, G. L., Courtney, K. D., Andres, V., and Featherstone, R. M., Biochem. Pharmacol., 1961, 7, 88-95).Human recombinant acetylcholinesterase and human recombinant butyrylcholinesterase were employed. Each reaction mixture contained the enzyme (either ACHE or BCHE) solution, DTNB and sample in Tris HCl buffer solution. The reactions were initiated by the addition of the substrate (either acetylthiocholine iodide or butyrylthiocholine iodide, respectively for ACHE and BCHE enzymes). The enzyme catalyzed formation of the yellow color was measured at 412 nm in terms of the calculation of enzyme activity concomitant to the presence of an inhibitor activity. | B | 5.15 | pIC50 | 7100 | nM | IC50 | US-9586925-B2. 1-(dimethylamino)ethyl-substituted 6H-benzo[C]chromen-6-ones against senile dementia (2017) |
| 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 BuChE (unknown origin) using acetylthiocholine iodide as substrate incubated for 5 mins by Ellman's method | B | 5.19 | pIC50 | 6500 | nM | IC50 | Eur J Med Chem (2022) 227: 113964-113964 [PMID:34743062] |
| 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: 167-177 [PMID:24681981] |
| 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 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 BuChE using butyrylthiocholine iodide as substrate preincubated for 20 mins followed by substrate addition and measured after 10 mins by DTNB based Ellman's method | B | 5.29 | pIC50 | 5100 | nM | IC50 | Eur J Med Chem (2024) 270: 116353-116353 [PMID:38579622] |
| 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 recombinant BChE using acetylthiocholine iodide as substrate preincubated for 20 mins followed by substrate addition by DTNB reagent based Ellman's method | B | 5.32 | pIC50 | 4800 | nM | IC50 | Eur J Med Chem (2023) 250: 115169-115169 [PMID:36753881] |
| ChEMBL | Inhibition of human BChE using butyrylthiocholine iodide as substrate preincubated with enzyme for 20 mins followed by substrate addition and measured for 5 mins by Ellman's spectrophotometric method | B | 5.32 | pIC50 | 4800 | nM | IC50 | Bioorg Med Chem (2023) 84: 117256-117256 [PMID:37003157] |
| ChEMBL | Inhibition of human BuChE by Ellman's spectrophotometric method | B | 5.32 | pIC50 | 4800 | nM | IC50 | Eur J Med Chem (2022) 237: 114358-114358 [PMID:35462163] |
| ChEMBL | Inhibition of human serum recombinant BChE using butyrylthiocholine iodide as a substrate incubated for 20 mins by DTNB reagent based Ellman's method | B | 5.32 | pIC50 | 4800 | nM | IC50 | RSC Med Chem (2022) 13: 873-883 [PMID:35923722] |
| 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 BChE by Ellman's method | B | 5.34 | pIC50 | 4610 | nM | IC50 | Eur J Med Chem (2024) 274: 116511-116511 [PMID:38820854] |
| ChEMBL | Inhibition of BChE (unknown origin) by Ellman's method | B | 5.34 | pIC50 | 4530 | nM | IC50 | Bioorg Med Chem Lett (2022) 75: 128976-128976 [PMID:36067929] |
| 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 | Inhibition of BuchE (unknown origin) | B | 5.37 | pIC50 | 4260 | nM | IC50 | Bioorg Med Chem Lett (2022) 61: 128602-128602 [PMID:35124202] |
| ChEMBL | Anticholinesterase activity against human plasma BChE | B | 5.38 | pIC50 | 4150 | nM | IC50 | J Med Chem (2006) 49: 2174-2185 [PMID:16570913] |
| ChEMBL | Inhibition of BChE (unknown origin) | B | 5.38 | pIC50 | 4150 | nM | IC50 | Eur J Med Chem (2018) 156: 598-617 [PMID:30031971] |
| 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 | Inhibitory concentration against human plasma Butyrylcholinesterase | B | 5.38 | pIC50 | 4150 | nM | IC50 | J Med Chem (2005) 48: 986-994 [PMID:15715468] |
| 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 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 | 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 BChE (unknown origin) incubated for 30 mins by Ellman's method | B | 5.5 | pIC50 | 3130 | nM | IC50 | Eur J Med Chem (2022) 233: 114242-114242 [PMID:35276424] |
| 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 C-terminal 6His-tagged human recombinant BuChE (29 to 602 residues) using butyrylthiocholine iodide as substrate preincubated for 5 mins followed by substrate addition by Ellman's method | B | 5.59 | pIC50 | 2580 | nM | IC50 | Eur J Med Chem (2022) 231: 114152-114152 [PMID:35101650] |
| ChEMBL | Inhibition of human BuChE measured after 15 to 20 mins by DTNB reagent based Ellman's method | B | 5.59 | pIC50 | 2580 | nM | IC50 | Eur J Med Chem (2023) 262: 115880-115880 [PMID:37871406] |
| 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 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 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 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 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 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 human BuChE using butyrylthiocholine iodide as substrate preincubated for 5 mins followed by substrate addition by DTNB reagent based Ellman's method | B | 5.65 | pIC50 | 2240 | nM | IC50 | Eur J Med Chem (2022) 242: 114630-114630 [PMID:35987018] |
| 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 BChE using butyrylthiocholine iodide as substrate preincubated for 30 mins followed by substrate addition and measured after 30 mins by DTNB based Ellman's method | B | 5.85 | pIC50 | 1400 | nM | IC50 | Eur J Med Chem (2024) 271: 116450-116450 [PMID:38701714] |
| 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] |
| Cholinesterase in Equus caballus (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5763] [UniProtKB: P81908] | ||||||||
| ChEMBL | Binding affinity to equine BChE in phosphate buffer at pH 8 assessed as equilibrium dissociation constant by SPR analysis | B | 5.14 | pKd | 7200 | nM | Kd | Eur J Med Chem (2024) 270: 116353-116353 [PMID:38579622] |
| 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 horse serum BuChE using butyrylthiocholine iodide as substrate preincubated with enzyme for 20 mins followed by substrate addition and measured after 10 mins by Ellman's method | B | 4.45 | pIC50 | 35400 | nM | IC50 | Eur J Med Chem (2022) 238: 114503-114503 [PMID:35689855] |
| 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 for 20 mins followed by substrate addition and measured after 20 mins by DTNB reagent based Ellman's method | B | 5.01 | pIC50 | 9830 | nM | IC50 | Eur J Med Chem (2023) 257: 115502-115502 [PMID:37224761] |
| 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 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 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 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 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 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 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 and measured after 5 mins by DTNB-reagent based Ellman's method | B | 5.13 | pIC50 | 7390 | nM | IC50 | Eur J Med Chem (2022) 227: 113973-113973 [PMID:34752955] |
| 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 using S-butyrylthiocholine iodide as substrate pre-incubated for 30 mins followed by substrate addition and measured after 5 mins by DTNB reagent based Ellman's method | B | 5.14 | pIC50 | 7290 | nM | IC50 | Eur J Med Chem (2024) 264: 116013-116013 [PMID:38052155] |
| 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 serum BchE using S-butyryl thiocholine iodide as substrate incubated for 10 mins followed by substrate addition measured at 0 to 180 secs by Ellman's method | B | 5.19 | pIC50 | 6410 | nM | IC50 | Eur J Med Chem (2022) 234: 114210-114210 [PMID:35303485] |
| 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 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 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 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 | B | 5.29 | pIC50 | 5130 | nM | IC50 | Bioorg Med Chem (2023) 80: 117178-117178 [PMID:36706609] |
| 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 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 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 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 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 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 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 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 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 BuChE using butyrylthiocholine as substrate preincubated for 10 mins followed by substrate addition by spectrophotometric based Ellman's method | B | 5.33 | pIC50 | 4700 | nM | IC50 | Bioorg Med Chem (2022) 71: 116952-116952 [PMID:35930852] |
| 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 butyrylthiocholine iodide as substrate preincubated with enzyme for 20 mins followed by substrate addition and measured for 10 mins by Ellman's method | B | 5.35 | pIC50 | 4500 | nM | IC50 | Eur J Med Chem (2024) 266: 116131-116131 [PMID:38215587] |
| 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 BuChE using ATCI and BTCI as substrate preincubated for 5 mins followed by substrate addition and measured after 3 mins by DTNB-reagent based Ellman's method | B | 5.37 | pIC50 | 4260 | nM | IC50 | Bioorg Med Chem (2023) 78: 117146-117146 [PMID:36580744] |
| ChEMBL | Inhibition of equine serum BuChE using butyrylthiocholine iodide as substrate preincubated for 5 mins followed by substrate addition by DTNB reagent based Ellman's method | B | 5.37 | pIC50 | 4220 | nM | IC50 | Eur J Med Chem (2022) 242: 114630-114630 [PMID:35987018] |
| 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 with enzyme for 20 mins followed by substrate addition and measured after 20 mins by Ellman's method | B | 5.45 | pIC50 | 3550 | nM | IC50 | Eur J Med Chem (2022) 229: 114095-114095 [PMID:34995924] |
| ChEMBL | Inhibition of equine serum BuChE using butylthiocholine iodine as substrate preincubated for 20 mins followed by substrate addition and measured after 20 mins by DTNB reagent based Ellman's method | B | 5.45 | pIC50 | 3550 | nM | IC50 | Eur J Med Chem (2022) 242: 114689-114689 [PMID:36007469] |
| 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 butyrylthiocholine chloride as substrate by Ellman's method | B | 5.51 | pIC50 | 3100 | nM | IC50 | Eur J Med Chem (2023) 251: 115253-115253 [PMID:36921526] |
| 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 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 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 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 BChE using butyrylthiocholine iodide as substrate preincubated for 20 mins followed by substrate addition and measured after 5 mins by Ellman's method | B | 5.56 | pIC50 | 2750 | nM | IC50 | Eur J Med Chem (2023) 259: 115695-115695 [PMID:37567058] |
| 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 BuChE using butyrylthiocholine iodide as substrate preincubated for 20 mins followed by substrate addition and measured after 10 mins by DTNB based Ellman's method | B | 5.64 | pIC50 | 2300 | nM | IC50 | Eur J Med Chem (2024) 270: 116353-116353 [PMID:38579622] |
| 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 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 horse serum BChE assessed as residual enzyme activity using butyrylthiocholine iodide as substrate by Ellman's colorimetric assay | B | 5.65 | pIC50 | 2250 | nM | IC50 | Bioorg Med Chem (2024) 110: 117829-117829 [PMID:39002183] |
| 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 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 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 equine BuChE by Ellman's method | B | 5.69 | pIC50 | 2057 | nM | IC50 | Eur J Med Chem (2021) 215: 113278-113278 [PMID:33662757] |
| ChEMBL | Inhibition of equine serum BuChE preincubated for 5 mins followed by substrate addition and measured after 5 mins using S-butyrylthiocholine iodide as substrate by Ellman's method | B | 5.7 | pIC50 | 1980 | nM | IC50 | Eur J Med Chem (2021) 215: 113278-113278 [PMID:33662757] |
| 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 serum BChE using butyrylthiocholine iodide as substrate preincubated for 20 mins followed by substrate addition by DTNB reagent based Ellman's method | B | 5.72 | pIC50 | 1900 | nM | IC50 | Eur J Med Chem (2023) 250: 115169-115169 [PMID:36753881] |
| 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 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 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 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 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 horse serum BuChE using butyrylthiocholine iodide as substrate preincubated for 5 mins followed by substrate addition and measured after 5 mins by DTNB-reagent based Ellman's method | B | 5.74 | pIC50 | 1830 | nM | IC50 | Eur J Med Chem (2023) 249: 115135-115135 [PMID:36696766] |
| 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 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 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 equine serum BuChE using butyrylthiocholine iodide as substrate preincubated for 5 mins followed by substrate addition and measured after 5 mins by DTNB reagent based Ellman's method | B | 5.74 | pIC50 | 1830 | nM | IC50 | Eur J Med Chem (2023) 261: 115832-115832 [PMID:37837674] |
| ChEMBL | Inhibition of equine serum BuChE by Ellman's method | B | 5.74 | pIC50 | 1830 | nM | IC50 | Bioorg Med Chem (2023) 88-89: 117333-117333 [PMID:37236021] |
| 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 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 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 equine serum BChE using butyrylthiocholine as substrate by Ellman's method | B | 5.78 | pIC50 | 1670 | nM | IC50 | Eur J Med Chem (2024) 276: 116592-116592 [PMID:39013357] |
| 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 10 mins followed by substrate addition and measured every min for 10 mins by DTNB based Ellman's assay | B | 5.9 | pIC50 | 1260 | nM | IC50 | Bioorg Med Chem (2024) 101: 117649-117649 [PMID:38401458] |
| ChEMBL | Inhibition of equine serum BuChE using butyrylthiocholine iodide as substrate preincubated with enzyme for 10 mins followed by substrate addition and measured every 1 min for 20 mins by spectrophotometric analysis | B | 6.03 | pIC50 | 941 | nM | IC50 | Eur J Med Chem (2023) 259: 115670-115670 [PMID:37515920] |
| 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 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 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 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 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 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 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] |
| butyrylcholinesterase/Cholinesterase 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] |
| 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] |
| 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] |
| carboxylesterase 1/Liver carboxylesterase 1 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] |
| microtubule affinity regulating kinase 4/MAP/microtubule affinity-regulating kinase 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5754] [GtoPdb: 2100] [UniProtKB: Q96L34] | ||||||||
| ChEMBL | Inhibition of human MARK4 expressed in Escherichia coli preincubated for 1 hr followed by ATP addition and measured after 30 mins by colorimetric assay | B | 5.28 | pIC50 | 5300 | nM | IC50 | RSC Med Chem (2024) 15: 1942-1958 [PMID:38911173] |
| sigma non-opioid intracellular receptor 1/Sigma non-opioid intracellular receptor 1 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] |
| Sigma non-opioid intracellular receptor 1 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] |
| ChEMBL | Displacement of [3H]-(+)-pentazocine from sigma1 receptor in guinea pig brain membrane measured after 120 mins by scintillation counting method | B | 7.84 | pKi | 14.6 | nM | Ki | J Med Chem (2022) 65: 12292-12318 [PMID:36084304] |
| Kv11.1/Voltage-gated inwardly rectifying potassium channel KCNH2 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] |
ChEMBL data shown on this page come from version 36:
Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
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]