tacrine [Ligand Id: 6687] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL95 (Tacrina, Tacrinal, Tacrine)
  • nicotinic acetylcholine receptor ε subunit/Acetylcholine receptor protein epsilon chain in Human [ChEMBL: CHEMBL2484] [GtoPdb: 477] [UniProtKB: Q04844]
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  • Acetylcholinesterase in Torpedo californica [ChEMBL: CHEMBL4780] [UniProtKB: P04058]
  • Acetylcholinesterase in Electrophorus electricus [ChEMBL: CHEMBL4078] [UniProtKB: O42275]
  • acetylcholinesterase (Yt blood group)/Acetylcholinesterase in Human [ChEMBL: CHEMBL220] [GtoPdb: 2465] [UniProtKB: P22303]
  • Acetylcholinesterase in Bovine [ChEMBL: CHEMBL4768] [UniProtKB: P23795]
  • acetylcholinesterase (Yt blood group)/Acetylcholinesterase in Mouse [ChEMBL: CHEMBL3198] [GtoPdb: 2465] [UniProtKB: P21836]
  • acetylcholinesterase (Yt blood group)/Acetylcholinesterase in Rat [ChEMBL: CHEMBL3199] [GtoPdb: 2465] [UniProtKB: P37136]
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  • carboxylesterase 1/Acyl coenzyme A:cholesterol acyltransferase in Human [ChEMBL: CHEMBL2265] [GtoPdb: 2592] [UniProtKB: P23141]
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  • α1A-adrenoceptor/Alpha-1a adrenergic receptor in Rat [ChEMBL: CHEMBL319] [GtoPdb: 22] [UniProtKB: P43140]
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  • Alpha-ketoglutarate-dependent dioxygenase FTO in Human [ChEMBL: CHEMBL2331065] [UniProtKB: Q9C0B1]
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  • butyrylcholinesterase/Butyrylcholinesterase in Human [ChEMBL: CHEMBL1914] [GtoPdb: 2471] [UniProtKB: P06276]
  • Butyrylcholinesterase in Equus caballus [ChEMBL: CHEMBL5077] [UniProtKB: Q9N1N9]
  • butyrylcholinesterase/Butyrylcholinesterase in Mouse [ChEMBL: CHEMBL2528] [GtoPdb: 2471] [UniProtKB: Q03311]
  • Butyrylcholinesterase in Rat [ChEMBL: CHEMBL3403] [UniProtKB: Q9JKC1]
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  • CB1 receptor/Cannabinoid CB1 receptor in Human [ChEMBL: CHEMBL218] [GtoPdb: 56] [UniProtKB: P21554]
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  • CB2 receptor/Cannabinoid CB2 receptor in Human [ChEMBL: CHEMBL253] [GtoPdb: 57] [UniProtKB: P34972]
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  • choline O-acetyltransferase/Choline acetylase in Rat [ChEMBL: CHEMBL3945] [GtoPdb: 2480] [UniProtKB: P32738]
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  • cyclin dependent kinase 5/Cyclin-dependent kinase 5/CDK5 activator 1 in Human [ChEMBL: CHEMBL1907600] [GtoPdb: 1977] [UniProtKB: Q00535, Q15078]
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  • fatty acid binding protein 1/Fatty acid-binding protein, liver in Human [ChEMBL: CHEMBL5421] [GtoPdb: 2531] [UniProtKB: P07148]
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  • glycogen synthase kinase 3 beta/Glycogen synthase kinase-3 beta in Human [ChEMBL: CHEMBL262] [GtoPdb: 2030] [UniProtKB: P49841]
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  • M1 receptor/Muscarinic acetylcholine receptor M1 in Human [ChEMBL: CHEMBL216] [GtoPdb: 13] [UniProtKB: P11229]
  • M1 receptor/Muscarinic acetylcholine receptor M1 in Mouse [ChEMBL: CHEMBL3733] [GtoPdb: 13] [UniProtKB: P12657]
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  • M2 receptor/Muscarinic acetylcholine receptor M2 in Human [ChEMBL: CHEMBL211] [GtoPdb: 14] [UniProtKB: P08172]
  • Muscarinic acetylcholine receptor M2 in Pig [ChEMBL: CHEMBL4781] [UniProtKB: P06199]
  • M2 receptor/Muscarinic acetylcholine receptor M2 in Mouse [ChEMBL: CHEMBL3197] [GtoPdb: 14] [UniProtKB: Q9ERZ4]
  • M2 receptor/Muscarinic acetylcholine receptor M2 in Rat [ChEMBL: CHEMBL309] [GtoPdb: 14] [UniProtKB: P10980]
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  • nicotinic acetylcholine receptor α3 subunit/nicotinic acetylcholine receptor β4 subunit/nicotinic acetylcholine receptor α6 subunit/Nicotinic acetylcholine receptor alpha6/alpha3/beta4 in Rat [ChEMBL: CHEMBL3137276] [GtoPdb: 464, 474, 467] [UniProtKB: P04757, P12392, P43143]
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  • NET/Norepinephrine transporter in Human [ChEMBL: CHEMBL222] [GtoPdb: 926] [UniProtKB: P23975]
  • Norepinephrine transporter in Rat [ChEMBL: CHEMBL304] [UniProtKB: Q9WTR4]
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  • Organic cation transporter 1/Solute carrier family 22 member 1 in Human [ChEMBL: CHEMBL5685] [GtoPdb: 1019] [UniProtKB: O15245]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
nicotinic acetylcholine receptor ε subunit/Acetylcholine receptor protein epsilon chain in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2484] [GtoPdb: 477] [UniProtKB: Q04844]
ChEMBL Inhibition of AChE (unknown origin) by spectrophotometric analysis B 6.82 pKi 152.28 nM Ki Eur J Med Chem (2019) 180: 656-672 [PMID:31352246]
ChEMBL Inhibition of acetylcholinesterase B 7.36 pIC50 44 nM IC50 J Med Chem (2005) 48: 7496-7499 [PMID:16279811]
Acetylcholinesterase in Torpedo californica (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4780] [UniProtKB: P04058]
ChEMBL Inhibition of Torpedo californica AChE B 7.4 pKi 40 nM Ki J Med Chem (2008) 51: 3154-3170 [PMID:18479118]
ChEMBL Inhibition of Torpedo californica AChE using acetylthiocholine chloride as substrate peincubated for 15 mins followed by substrate addition measured after 5 mins by Ellman's method B 6.72 pIC50 190 nM IC50 Bioorg Med Chem Lett (2020) 30: 126880-126880 [PMID:31864798]
ChEMBL Inhibition of Torpedo californica eel AChE using acetylthiocholine/DTNB as substrate assessed as ROS-induced enzyme inactivation preincubated for 10 mins followed by substrate addition measured every 30 secs for 20 mins in presence of horseradish peroxidase and H2O2 B 6.74 pIC50 183 nM IC50 Medchemcomm (2011) 2: 406-412
ChEMBL Inhibition of Torpedo californica AChE by Ellman's method B 6.8 pIC50 157 nM IC50 J Med Chem (2007) 50: 5311-5323 [PMID:17902635]
ChEMBL Inhibition of Torpedo californica AChE using acetylthiocholine iodide as substrate preincubated for 5 mins followed by substrate addition measured at 1 min interval for 3 mins by Ellman's method B 7 pIC50 100 nM IC50 Bioorg Med Chem (2017) 25: 2387-2398 [PMID:28302511]
ChEMBL Inhibition of Torpedo californica eel AChE using acetylthiocholine/DTNB as substrate preincubated for 10 mins followed by substrate addition measured every 30 secs for 30 mins by Ellmans method B 7.28 pIC50 52.4 nM IC50 Medchemcomm (2011) 2: 406-412
ChEMBL Inhibitory activity against acetylcholinesterase (AChE) from Torpedo californica (Reversible type of inhibition) B 7.3 pIC50 50 nM IC50 Bioorg Med Chem Lett (2003) 13: 1825-1827 [PMID:12729674]
ChEMBL In vitro inhibition of Torpedo californica acetylcholinesterase. B 7.41 pIC50 39 nM IC50 J Med Chem (1999) 42: 730-741 [PMID:10052979]
ChEMBL Inhibition of Pacific electric ray AChE using acetylthiocholine iodide as substrate after 60 mins by Ellman's method B 7.54 pIC50 29 nM IC50 Bioorg Med Chem (2014) 22: 3341-3350 [PMID:24835788]
ChEMBL Inhibition of Torpedo californica AChE by spectrophotometry based Ellman's method B 7.54 pIC50 29 nM IC50 Bioorg Med Chem (2014) 22: 3838-3849 [PMID:25017625]
ChEMBL Inhibition of activity against Torpedo Ray acetylcholinesterase. B 8.09 pIC50 8.2 nM IC50 J Med Chem (2001) 44: 3203-3215 [PMID:11563919]
Acetylcholinesterase in Electrophorus electricus (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4078] [UniProtKB: O42275]
ChEMBL Binding affinity to electric eel AChE after 24 hrs by LC/MS-SIM analysis B 7.8 pKd 16 nM Kd J Med Chem (2018) 61: 9395-9409 [PMID:29873484]
ChEMBL Non-competitive inhibition of Electrophorus electricus AChE using acetylcholine as substrate by Lineweaver-Burk plot method B 6.47 pKi 340 nM Ki J Med Chem (2013) 56: 2038-2044 [PMID:23330848]
ChEMBL Inhibition of electric eel AChE using acetylthiocholine iodide as substrate preincubated for 15 mins followed by substrate addition measured after 5 mins by Ellman's method B 7.57 pKi 27 nM Ki Eur J Med Chem (2017) 138: 761-773 [PMID:28728108]
ChEMBL Inhibitory activity AChE from Electrophorus electricus using ATCh substrate and DTNB by spectrophotometry B 7.6 pKi 25 nM Ki J Med Chem (2005) 48: 8270-8288 [PMID:16366609]
ChEMBL Competitive inhibition of electric eel AChE assessed as enzyme-inhibitor complex using p-nitrophenyl acetate as substrate by Lineweaver-Burk plot analysis B 7.64 pKi 22.9 nM Ki Eur J Med Chem (2017) 138: 761-773 [PMID:28728108]
ChEMBL Inhibition of Electrophorus electricus AChE by Ellman's method B 7.69 pKi 20.2 nM Ki Bioorg Med Chem (2008) 16: 7759-7769 [PMID:18640842]
ChEMBL Tested for in vitro inhibition of acetylcholinesterase B 8 pKi 10 nM Ki Bioorg Med Chem Lett (1995) 5: 1131-1132
ChEMBL Inhibition of electric eel AChE by Ellman's method B 4.12 pIC50 76500 nM IC50 Bioorg Med Chem Lett (2021) 49: 128212-128212 [PMID:34153471]
ChEMBL Inhibition of electric eel AChE using acetylthiocholine iodide as substrate preincubated for 5 mins by Ellman method B 4.32 pIC50 47410 nM IC50 Bioorg Med Chem (2015) 23: 2445-2457 [PMID:25868744]
ChEMBL Inhibition of Electrophorus electricus AChE using acetylthiocholine iodide as substrate preincubated for 10 mins followed by substrate addition and measured after 10 mins by Ellman's method B 6.03 pIC50 930 nM IC50 Medchemcomm (2019) 10: 764-777 [PMID:31191867]
ChEMBL Inhibition of electric eel AChE using acetylcholine iodide as substrate preincubated for 20 mins by Ellman's method B 6.05 pIC50 900 nM IC50 Bioorg Med Chem Lett (2012) 22: 6498-6502 [PMID:22981331]
ChEMBL Inhibition of electric eel AChE using acetylthiocholine iodide as substrate preincubated for 10 mins prior to substrate addition by Ellman's method B 6.39 pIC50 410 nM IC50 Eur J Med Chem (2013) 68: 291-300 [PMID:23988412]
ChEMBL Non-competitive inhibition of Electrophorus electricus AChE using acetylcholine as substrate by Lineweaver-Burk plot method B 6.41 pIC50 386 nM IC50 J Med Chem (2013) 56: 2038-2044 [PMID:23330848]
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 6.43 pIC50 372 nM IC50 Eur J Med Chem (2016) 107: 219-232 [PMID:26588065]
ChEMBL Inhibition of electric eel AChE using acetylthiocholine iodide as substrate preincubated for 15 mins followed by substrate addition and measured for 5 mins by Ellmans method B 6.43 pIC50 371.5 nM IC50 Eur J Med Chem (2016) 124: 1026-1040 [PMID:27783974]
ChEMBL Inhibition of electric eel AChE using acetylthiocholine iodide as substrate preincubated for 10 mins followed by substrate addition measured for 6 mins by Ellman's method B 6.44 pIC50 365 nM IC50 Eur J Med Chem (2017) 139: 280-289 [PMID:28803044]
ChEMBL Inhibition of electric eel AChE using acetylthiocholine iodide as substrate preincubated for 5 mins followed by substrate addition measured for 1 min by Ellman's method B 6.45 pIC50 356 nM IC50 Eur J Med Chem (2017) 128: 237-246 [PMID:28189905]
ChEMBL Inhibition of electric eel AChE using acetylthiocholine iodide as substrate preincubated for 10 mins followed by substrate addition measured after 6 mins by Ellman's method B 6.46 pIC50 350 nM IC50 Eur J Med Chem (2019) 180: 656-672 [PMID:31352246]
ChEMBL Inhibition of electric eel AChE after 15 mins by DTNB reagent based assay B 6.5 pIC50 316 nM IC50 Medchemcomm (2018) 9: 149-159 [PMID:30108908]
ChEMBL Inhibition of electric eel AChE using acetylcholine as substrate by Ellman's method B 6.51 pIC50 311 nM IC50 Bioorg Med Chem (2012) 20: 3038-3048 [PMID:22472046]
ChEMBL Inhibition of electric eel AChE using acetylthiocholine chloride substrate as substrate preincubated for 15 mins by Ellman's method B 6.51 pIC50 311 nM IC50 Eur J Med Chem (2011) 46: 5885-5893 [PMID:22019228]
ChEMBL Inhibition of electric eel AChE after 15 mins by Ellman's method using acetylcholine as substrate B 6.51 pIC50 311 nM IC50 Bioorg Med Chem Lett (2010) 20: 6649-6652 [PMID:20880702]
ChEMBL Inhibition of Electrophorus electricus Acetylcholinesterase B 6.52 pIC50 300 nM IC50 J Med Chem (2007) 50: 5685-5695 [PMID:17944454]
ChEMBL Inhibition of electric eel AChE using acetylthiocholine iodide as substrate preincubated for 10 mins followed by substrate addition by Ellman's method B 6.55 pIC50 280 nM IC50 Eur J Med Chem (2015) 89: 296-303 [PMID:25462245]
ChEMBL Inhibition of electric eel AChE pre-incubated for 3 mins before acetylthiocholine substrate addition by Ellman's reagent based spectrophotometry B 6.55 pIC50 280 nM IC50 Eur J Med Chem (2015) 97: 181-189 [PMID:25969170]
ChEMBL Inhibition of electric eel AChE using acetylthiocholine iodide as substrate incubated for 6 mins prior to substrate addition measured after 60 to 180 secs by Ellman's method B 6.57 pIC50 269 nM IC50 Bioorg Med Chem Lett (2013) 23: 2636-2641 [PMID:23511019]
ChEMBL Inhibition of electric eel AChE using acetylthiocholine iodide as substrate preincubated for 6 mins prior to substrate addition measured at 60 to 180 seconds by Ellman's method B 6.57 pIC50 269 nM IC50 Eur J Med Chem (2013) 64: 540-553 [PMID:23685572]
ChEMBL Inhibition of electric eel AChE using acetylthiocholine iodide as substrate incubated for 6 mins by spectrophotometric method B 6.59 pIC50 260 nM IC50 Bioorg Med Chem (2014) 22: 6089-6104 [PMID:25282654]
ChEMBL Inhibition of electric eel AChE using acetylthiocholine iodide as substrate preincubated for 6 mins followed by substrate addition by Ellmans method B 6.59 pIC50 260 nM IC50 Eur J Med Chem (2013) 69: 632-646 [PMID:24095756]
ChEMBL Inhibition of electric eel acetylcholinesterase using acetylthiocholine iodide as substrate after 10 mins by Ellman's spectrophotometric method B 6.6 pIC50 250 nM IC50 Bioorg Med Chem Lett (2011) 21: 4097-4103 [PMID:21641207]
ChEMBL Inhibition of electric eel AChE using acetylthiocholine iodide as substrate preincubated for 15 mins followed by substrate addition by Ellman's method B 6.64 pIC50 230 nM IC50 Bioorg Med Chem Lett (2019) 29: 839-843 [PMID:30686752]
ChEMBL Inhibition of electric eel ACHE preincubated for 6 mins followed by addition of acetylcholine iodide as substrate by Ellman's method B 6.64 pIC50 230 nM IC50 Bioorg Med Chem (2016) 24: 4324-4338 [PMID:27460699]
ChEMBL Inhibition of electric eel AChE using acetylthiocholine iodide as substrate preincubated for 20 mins followed by substrate addition and measured after 5 mins by DTNB-reagent based Ellman's method B 6.64 pIC50 230 nM IC50 Eur J Med Chem (2022) 227: 113973-113973 [PMID:34752955]
ChEMBL Inhibition of Electrophorus electricus AChE using acetylthiocholine iodide as substrate preincubated for 15 mins followed by substrate addition and measured after 10 mins by Ellman's method B 6.64 pIC50 230 nM IC50 Medchemcomm (2018) 9: 1871-1881 [PMID:30568755]
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 6.65 pIC50 226 nM IC50 Eur J Med Chem (2017) 136: 36-51 [PMID:28478343]
ChEMBL Inhibition of electric eel AChE using acetylthiocholine iodide as substrate incubated for 10 mins by spectrophotometry based Ellman's method B 6.65 pIC50 223 nM IC50 Eur J Med Chem (2019) 167: 161-186 [PMID:30771604]
ChEMBL Inhibition of electric eel AChE B 6.65 pIC50 223 nM IC50 Bioorg Med Chem Lett (2020) 30: 127609-127609 [PMID:33039562]
ChEMBL inhibition of electric eel AChE by Ellman's method B 6.65 pIC50 222.7 nM IC50 Eur J Med Chem (2010) 45: 1415-1423 [PMID:20079560]
ChEMBL Inhibition of electric eel AChE using acetylthiocholine iodide as substrate incubated for 5 mins followed by substrate addition measured for 1 min by Ellman's method B 6.66 pIC50 221 nM IC50 Eur J Med Chem (2016) 123: 298-308 [PMID:27484515]
ChEMBL Inhibition of electric eel AChE by Ellman's assay B 6.66 pIC50 220 nM IC50 J Nat Prod (2006) 69: 1341-1346 [PMID:16989531]
ChEMBL Inhibition of electric eel AChE using acetylthiocholine chloride as substrate incubated for 15 mins prior to substrate addition by Ellman's method B 6.66 pIC50 219 nM IC50 Bioorg Med Chem (2013) 21: 7275-7282 [PMID:24148835]
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 6.66 pIC50 218 nM IC50 Eur J Med Chem (2016) 123: 282-297 [PMID:27484514]
ChEMBL Inhibition of electric eel AChE using acetylthiocholine chloride as substrate by spectrophotometer analysis B 6.67 pIC50 215 nM IC50 Bioorg Med Chem (2014) 22: 3213-3219 [PMID:24794747]
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 6.68 pIC50 210 nM IC50 Eur J Med Chem (2022) 242: 114630-114630 [PMID:35987018]
ChEMBL Inhibition of electric eel AChE using acetylthiocholine iodide as substrate by Ellman's method B 6.68 pIC50 207 nM IC50 Bioorg Med Chem Lett (2020) 30: 126927-126927 [PMID:31901382]
ChEMBL Inhibition of electric eel AChE using acetylthiocholine iodide as substrate incubated for 6 mins prior to substrate addition measured after 60 to 180 secs by Ellman's method B 6.69 pIC50 205 nM IC50 Medchemcomm (2014) 5: 609-616
ChEMBL Inhibition of electric eel AChE using ATC as substrate preincubated for 15 mins followed by substrate addition by UV-spectrophotometric analysis B 6.72 pIC50 192.6 nM IC50 Eur J Med Chem (2016) 122: 17-26 [PMID:27343850]
ChEMBL Inhibition of electric eel AChE by Ellman's method B 6.72 pIC50 192.6 nM IC50 Bioorg Med Chem (2011) 19: 763-770 [PMID:21211982]
ChEMBL Inhibition of electric eel AChE preincubated for 15 mins followed by substrate addition using acetylthiocholine iodide as substrate by Ellman's method B 6.72 pIC50 190 nM IC50 Eur J Med Chem (2021) 215: 113278-113278 [PMID:33662757]
ChEMBL Inhibition of electric eel AChE using acetylcholine iodide as substrate preincubated for 15 mins prior to substrate addition by Ellman's method B 6.72 pIC50 190 nM IC50 Bioorg Med Chem (2013) 21: 4559-4569 [PMID:23768661]
ChEMBL Inhibition of electric eel AChE using acetylcholine as substrate preincubated for 15 mins followed by substrate addition by Ellman's method B 6.72 pIC50 190 nM IC50 Eur J Med Chem (2016) 118: 178-192 [PMID:27128182]
ChEMBL Inhibition of electric eel AChE preincubated for 15 mins followed by addition of acetylcholine iodide as substrate by Ellman's assay B 6.72 pIC50 190 nM IC50 Medchemcomm (2015) 6: 1969-1977
ChEMBL Inhibition of electric eel AChE preincubated for 30 mins prior to horseradish peroxidase, H2O2 and DETAPAC addition measured for 20 mins under ROS condition by Muraoka and Miura method B 6.74 pIC50 183 nM IC50 Bioorg Med Chem (2013) 21: 3614-3623 [PMID:23535563]
ChEMBL Inhibition of electric eel AChE by Rappaport method B 6.74 pIC50 180 nM IC50 J Med Chem (2009) 52: 2724-2732 [PMID:19374444]
ChEMBL Inhibition of Electrophorus electricus AChE B 6.74 pIC50 180 nM IC50 J Med Chem (2006) 49: 7607-7610 [PMID:17181144]
ChEMBL Inhibition of Electrophorus electricus AChE by spectrophotometry B 6.74 pIC50 180 nM IC50 Bioorg Med Chem (2008) 16: 7759-7769 [PMID:18640842]
ChEMBL Inhibition of electric eel AChE B 6.76 pIC50 173 nM IC50 Bioorg Med Chem Lett (2010) 20: 3606-3609 [PMID:20472431]
ChEMBL Inhibition of Electrophorus electricus AChE by Ellman's method B 6.82 pIC50 150 nM IC50 Bioorg Med Chem (2007) 15: 6596-6607 [PMID:17681794]
ChEMBL Inhibition of electric eel AChE using acetylthiocholine chloride as substrate preincubated for 15 mins followed by substrate addition measured every minute by Ellman's method B 6.84 pIC50 143.5 nM IC50 Eur J Med Chem (2018) 144: 128-136 [PMID:29268129]
ChEMBL Inhibition of electric eel AChE using acetylthiocholine chloride as substrate incubated for 15 mins by Ellman's method B 6.85 pIC50 142 nM IC50 Bioorg Med Chem (2016) 24: 6031-6039 [PMID:27720328]
ChEMBL Inhibition of electric eel AChE B 6.85 pIC50 140 nM IC50 Eur J Med Chem (2019) 166: 381-389 [PMID:30739821]
ChEMBL Inhibition of Electrophorus electricus AChE using acetylthiocholine iodide as substrate by spectroscopic Ellmans method B 6.87 pIC50 136 nM IC50 Eur J Med Chem (2011) 46: 2193-2205 [PMID:21435752]
ChEMBL Inhibition of electric eel AchE using acetylthiocholine iodide as substrate by Ellman method B 6.87 pIC50 136 nM IC50 Bioorg Med Chem Lett (2015) 25: 830-833 [PMID:25597004]
ChEMBL Inhibition of Electrophorus electricus AChE using acetylthiocholine chloride as substrate after 15 mins incubation by Ellman's method B 6.89 pIC50 130 nM IC50 Bioorg Med Chem Lett (2012) 22: 2257-2261 [PMID:22341944]
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 6.89 pIC50 130 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 6.89 pIC50 130 nM IC50 Eur J Med Chem (2016) 119: 260-277 [PMID:27227482]
ChEMBL Inhibition of electric eel AChE by Ellman's method B 6.89 pIC50 130 nM IC50 J Med Chem (2009) 52: 2724-2732 [PMID:19374444]
ChEMBL Inhibition of electric eel AChE using ATC iodide substrate by Ellman's assay B 6.9 pIC50 126.7 nM IC50 Bioorg Med Chem (2015) 23: 5610-5618 [PMID:26242241]
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 6.9 pIC50 125 nM IC50 Eur J Med Chem (2022) 234: 114210-114210 [PMID:35303485]
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 6.95 pIC50 113 nM IC50 J Med Chem (2013) 56: 9089-9099 [PMID:24160297]
ChEMBL Inhibition of electric eel AChE using acetylthiocholine iodide as substrate preincubated for 6 mins before substrate addition by Ellman's method B 6.95 pIC50 112.1 nM IC50 Eur J Med Chem (2015) 93: 42-50 [PMID:25656088]
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 method B 6.95 pIC50 111 nM IC50 Bioorg Med Chem (2013) 21: 7406-7417 [PMID:24128814]
ChEMBL Inhibition of electric eel AChE using acetylthiocholine chloride as substrate after 15 mins by Ellman's method B 6.96 pIC50 110.2 nM IC50 Eur J Med Chem (2013) 62: 745-753 [PMID:23454517]
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 6.96 pIC50 110 nM IC50 Eur J Med Chem (2017) 139: 612-632 [PMID:28841514]
ChEMBL Inhibition of electric eel acetylcholinesterase using acetylthiocholine chloride as substrate preincubated for 15 mins followed by substrate addition by Ellman's method B 6.96 pIC50 110 nM IC50 Bioorg Med Chem (2014) 22: 1355-1361 [PMID:24461494]
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 6.96 pIC50 110 nM IC50 Bioorg Med Chem (2016) 24: 1528-1539 [PMID:26917219]
ChEMBL Inhibition of electric eel AchE using acetylthiocholine as substrate by Ellman's method B 6.96 pIC50 110 nM IC50 Bioorg Med Chem Lett (2019) 29: 2150-2152 [PMID:31281020]
ChEMBL Inhibition of electric eel AChE preincubated for 15 mins by Ellman's method B 6.96 pIC50 109 nM IC50 Eur J Med Chem (2014) 87: 429-439 [PMID:25282266]
ChEMBL Inhibition of electric eel AChE using acetylthiocholine chloride as substrate preincubated for 15 mins by Ellman's method B 6.96 pIC50 109 nM IC50 Bioorg Med Chem (2012) 20: 5884-5892 [PMID:22944335]
ChEMBL Inhibition of electric eel AChE using acetylthiocholine chloride as substrate preincubated for 15 mins by Ellman's method B 6.96 pIC50 109 nM IC50 Bioorg Med Chem Lett (2013) 23: 6737-6742 [PMID:24220172]
ChEMBL Inhibition of electric eel AChE using acetylthiocholine iodide as substrate preincubated for 15 mins followed by substrate addition by spectrophotometric analysis B 6.96 pIC50 109 nM IC50 Bioorg Med Chem (2017) 25: 2946-2955 [PMID:28454848]
ChEMBL Inhibition of electric eel acetylcholinesterase using acetylthiocholine as substrate incubated for 15 mins followed by substrate addition measured for 2 mins by Ellman's method B 6.97 pIC50 108 nM IC50 Eur J Med Chem (2013) 63: 299-312 [PMID:23501115]
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 6.97 pIC50 107 nM IC50 J Med Chem (2016) 59: 7683-7689 [PMID:27405689]
ChEMBL Inhibition of electric eel AChE by Ellman's method B 6.98 pIC50 105 nM IC50 Eur J Med Chem (2011) 46: 1572-1581 [PMID:21367493]
ChEMBL Inhibition of Electrophorus electricus AChE using acetylthiocholine chloride as substrate after 15 mins by Ellman's method B 6.98 pIC50 104 nM IC50 Eur J Med Chem (2011) 46: 4970-4979 [PMID:21871694]
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 6.98 pIC50 104 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 10 mins followed by substrate addition measured after 10 mins by Ellman's method B 6.99 pIC50 102 nM IC50 Eur J Med Chem (2017) 125: 853-864 [PMID:27744252]
ChEMBL Inhibition of electric eel AChE pre-incubated for 20 mins before acetylcholine iodide substrate addition by Ellman's assay B 7 pIC50 100 nM IC50 Bioorg Med Chem Lett (2015) 25: 807-810 [PMID:25597007]
ChEMBL Inhibition of electric eel AchE B 7 pIC50 100 nM IC50 Bioorg Med Chem Lett (2008) 18: 3790-3793 [PMID:18524585]
ChEMBL Inhibition of electric eel AChE using acetylthiocholine iodide as substrate incubated for 6 mins prior to substrate addition measured after 60 to 180 secs by Ellman method B 7.01 pIC50 97.3 nM IC50 Eur J Med Chem (2015) 95: 153-165 [PMID:25812965]
ChEMBL Inhibition of electric eel acetylcholinesterase using acetylcholine chloride as substrate preincubated for 15 mins before substrate addition by Ellman's method B 7.02 pIC50 96 nM IC50 Bioorg Med Chem (2012) 20: 2527-2534 [PMID:22444876]
ChEMBL Inhibition of electric eel AChE preincubated for 15 mins followed by addition of acetylthiocholine iodide as substrate measured after 30 mins by Ellman's microplate assay B 7.02 pIC50 95 nM IC50 Bioorg Med Chem (2016) 24: 3742-3751 [PMID:27328658]
ChEMBL Inhibition of electric eel AChE using acetylthiocholine as substrate preincubated for 20 mins followed by substrate addition measured every 2 mins for 20 mins by Ellman's method B 7.02 pIC50 94.69 nM IC50 Eur J Med Chem (2017) 139: 367-377 [PMID:28810188]
ChEMBL Inhibition of Electric eel AChE assessed as amount of thiocholine released using acetylthiocholine iodide as substrate after 6 mins by Ellman's method B 7.05 pIC50 90 nM IC50 J Nat Prod (2014) 77: 650-656 [PMID:24521095]
ChEMBL Inhibition of electric eel AChE using acetylthiocholine iodide as substrate after 10 mins by Ellman's method B 7.05 pIC50 89.91 nM IC50 Eur J Med Chem (2018) 145: 760-769 [PMID:29353726]
ChEMBL Inhibition of electric eel AChE using acetylthiocholine iodide as substrate preincubated for 15 mins followed by substrate addition by Ellman's method B 7.07 pIC50 86 nM IC50 Bioorg Med Chem (2018) 26: 3731-3762 [PMID:30017112]
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 7.07 pIC50 85.8 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 and measured every min for 10 mins by DTNB based Ellman's assay B 7.12 pIC50 76 nM IC50 Bioorg Med Chem (2024) 101: 117649-117649 [PMID:38401458]
ChEMBL Inhibition of electric eel AChE using acetylthiocholine iodide as substrate preincubated for 5 mins before substrate addition by Ellman's method B 7.12 pIC50 75 nM IC50 Bioorg Med Chem (2013) 21: 4928-4937 [PMID:23891231]
ChEMBL Inhibition of Electrophorus electricus AChE after 120 secs by Ellman spectroscopic method B 7.13 pIC50 74 nM IC50 Bioorg Med Chem (2010) 18: 7873-7877 [PMID:20943395]
ChEMBL Inhibition of Electrophorus electricus AChE by Ellman's method B 7.13 pIC50 74 nM IC50 J Med Chem (2007) 50: 5311-5323 [PMID:17902635]
ChEMBL Inhibition of electric eel AChE using acetylthiocholine chloride as substrate preincubated for 20 mins followed by substrate addition by Ellman's method B 7.13 pIC50 73.36 nM IC50 Eur J Med Chem (2016) 116: 200-209 [PMID:27061983]
ChEMBL Inhibition of electric eel AChE using acetylthiocholine iodide as substrate preincubated for 5 mins followed by DTNB addition for 5 mins and subsequent addition of substrate measured after 3 mins by Ellman's method B 7.15 pIC50 70.7 nM IC50 Eur J Med Chem (2018) 148: 238-254 [PMID:29466774]
ChEMBL Inhibition of electric eel AChE B 7.15 pIC50 70 nM IC50 Bioorg Med Chem (2023) 80: 117178-117178 [PMID:36706609]
ChEMBL Inhibition of electric eel AchE using acetylthiocholine as substrate measured for 6 mins by Ellman's method B 7.15 pIC50 70 nM IC50 J Nat Prod (2020) 83: 852-863 [PMID:32150413]
ChEMBL Inhibition of electric eel AChE using acetylthiocholine iodide as substrate pretreated followed by substrate addition and measured after 2 mins by Ellman's method B 7.16 pIC50 69.8 nM IC50 Bioorg Med Chem (2019) 27: 895-930 [PMID:30744931]
ChEMBL Inhibition of electric eel AChE using acetylthiocholine iodide as substrate after 5 mins by Ellman's method B 7.16 pIC50 69.8 nM IC50 Bioorg Med Chem Lett (2013) 23: 3162-3165 [PMID:23639542]
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 7.19 pIC50 65 nM IC50 Bioorg Med Chem (2014) 22: 2496-2507 [PMID:24657052]
ChEMBL Inhibition of electric eel acetylcholine esterase using acetylcholine chloride as substrate incubated for 5 mins prior to substrate addition measured every 3 mins by Ellman's assay B 7.19 pIC50 64.57 nM IC50 J Med Chem (2012) 55: 3588-3592 [PMID:22420827]
ChEMBL Inhibition of electric eel AChE using acetylthiocholine chloride substrate incubated for 5 mins before substrate addition measured at 3 min interval by Ellman method B 7.19 pIC50 64.57 nM IC50 Bioorg Med Chem (2012) 20: 6513-6522 [PMID:23000296]
ChEMBL Inhibition of Electrophorus electricus AChE using acetylthiocholine iodide as substrate incubated for 15 mins followed by substrate addition by Ellman's method B 7.21 pIC50 61 nM IC50 Eur J Med Chem (2016) 122: 326-338 [PMID:27376495]
ChEMBL Inhibition of Electrophorus electricus acetylcholinesterase using acetylthiocholineiodide as substrate measured at 30 secs intervals over 9 mins by Ellman's colorimetric assay B 7.24 pIC50 58 nM IC50 Bioorg Med Chem Lett (2015) 25: 5609-5612 [PMID:26510670]
ChEMBL Inhibition of electric eel AChE using acetylthiocholine as substrate preincubated for 10 mins prior to substrate addition measured every 30 seconds for 30 mins by Ellman's method B 7.28 pIC50 52.4 nM IC50 Bioorg Med Chem (2013) 21: 3614-3623 [PMID:23535563]
ChEMBL Inhibition of electric eel AChE using acetylthiocholine preincubated for 10 mins followed by addition of substrate and measured every 30 secs for 20 mins B 7.28 pIC50 52.4 nM IC50 Medchemcomm (2019) 10: 2052-2072 [PMID:32206241]
ChEMBL Inhibition of electric eel AChE using acetylthiocholine chloride as substrate peincubated for 15 mins followed by substrate addition measured at 1 min interval by Ellman's method B 7.29 pIC50 51.3 nM IC50 Bioorg Med Chem Lett (2020) 30: 126880-126880 [PMID:31864798]
ChEMBL Inhibition of Electrophorus electricus AChE pre-incubated for 5 mins before acetylthiocholine iodide substrate addition by Ellman's method B 7.3 pIC50 50 nM IC50 Bioorg Med Chem Lett (2015) 25: 3442-3446 [PMID:26212777]
ChEMBL Compound was assessed for in vitro inhibition of Acetylcholinesterase isolated from Electrophorus electricus B 7.3 pIC50 50 nM IC50 Bioorg Med Chem Lett (2000) 10: 637-639 [PMID:10762042]
ChEMBL Inhibition of Electrophorus electricus C2888 AChE using acetylthiocholine iodide as substrate by Ellman's spectroscopic method B 7.3 pIC50 50 nM IC50 J Nat Prod (2012) 75: 2012-2015 [PMID:23134335]
ChEMBL Inhibition of electric eel AChE using acetylthiocholine iodine as substrate for 20 mins by Ellman's method B 7.32 pIC50 48 nM IC50 Eur J Med Chem (2022) 242: 114701-114701 [PMID:36054949]
ChEMBL Inhibition of electric eel AChE using acetylthiocholine iodide as substrate preincubated for 15 mins followed by substrate addition measured after 20 mins by Ellman's method B 7.32 pIC50 48 nM IC50 Eur J Med Chem (2017) 125: 1200-1212 [PMID:27863370]
ChEMBL Inhibition of electric eel AChE by Ellman's method B 7.33 pIC50 46.5 nM IC50 Bioorg Med Chem (2011) 19: 1222-1235 [PMID:21232964]
ChEMBL Inhibition of electric eel AChE by Ellman's method B 7.33 pIC50 46.45 nM IC50 Bioorg Med Chem (2011) 19: 1222-1235 [PMID:21232964]
ChEMBL Inhibition of electric eel AChE by Ellman's method B 7.34 pIC50 45.71 nM IC50 J Med Chem (2010) 53: 2094-2103 [PMID:20158205]
ChEMBL Inhibition of electric eel AChE by colorimetric Ellman assay B 7.34 pIC50 45.71 nM IC50 J Med Chem (2012) 55: 5231-5242 [PMID:22624880]
ChEMBL Inhibition of Electric eel AChE B 7.35 pIC50 45.1 nM IC50 J Med Chem (2008) 51: 7666-7669 [PMID:19053746]
ChEMBL Inhibition of electric eel AchE by Ellman's assay B 7.35 pIC50 45.1 nM IC50 Bioorg Med Chem Lett (2008) 18: 2905-2909 [PMID:18406135]
ChEMBL Inhibition of electric eel AChE by modified Ellman's method B 7.35 pIC50 45.08 nM IC50 J Med Chem (2010) 53: 3611-3617 [PMID:20361801]
ChEMBL Inhibition of electric eel AChE by modified Ellman's method B 7.35 pIC50 45 nM IC50 J Med Chem (2010) 53: 3611-3617 [PMID:20361801]
ChEMBL Inhibition of Electrophorus electricus AChE pre-incubated for 10 mins before addition of acetylthiocholine iodide substrate and further incubated for 15 mins by Ellman's method B 7.35 pIC50 44.3 nM IC50 J Med Chem (2016) 59: 9967-9973 [PMID:27736061]
ChEMBL Inhibition of electric eel AChE by Ellman's method B 7.37 pIC50 42.95 nM IC50 Bioorg Med Chem (2010) 18: 1181-1193 [PMID:20061157]
ChEMBL Inhibition of electric eel AchE using acetylcholine as substrate preincubated for 15 mins followed by substrate addition measured for 5 mins by Ellman method B 7.4 pIC50 40 nM IC50 Eur J Med Chem (2014) 74: 491-501 [PMID:24502897]
ChEMBL In vitro inhibition of electric eel acetylcholinesterase B 7.41 pIC50 39 nM IC50 J Med Chem (2001) 44: 2707-2718 [PMID:11495583]
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 7.42 pIC50 38 nM IC50 Bioorg Med Chem (2016) 24: 2352-2359 [PMID:27083471]
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 7.5 pIC50 31.8 nM IC50 Eur J Med Chem (2020) 185: 111785-111785 [PMID:31669851]
ChEMBL Inhibition of Electrophorus electricus AChE using acetylthiocholine iodide as substrate pretreated for 10 mins followed by substrate addition measured after 15 mins by spectrophotometry based Ellman method B 7.52 pIC50 30 nM IC50 Eur J Med Chem (2017) 126: 576-589 [PMID:27918993]
ChEMBL Inhibition of electric eel AChE using acetylthiocholine iodide substrate by Ellman assay B 7.57 pIC50 27.2 nM IC50 J Med Chem (2015) 58: 6710-6715 [PMID:26278660]
ChEMBL Inhibitory activity AChE from Electrophorus electricus using ATCh substrate and DTNB by spectrophotometry B 7.57 pIC50 27 nM IC50 J Med Chem (2005) 48: 8270-8288 [PMID:16366609]
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 7.57 pIC50 27 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 electric eel AChE preincubated for 10 mins measured after 15 mins by Ellman's method B 7.57 pIC50 27 nM IC50 Eur J Med Chem (2011) 46: 4676-4681 [PMID:21715067]
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 (2012) 52: 251-262 [PMID:22503231]
ChEMBL Inhibition of Electrophorus electricus AChE using acetylthiocholine iodide as substrate preincubated for 10 mins before substrate addition by Ellman's method B 7.57 pIC50 27 nM IC50 Eur J Med Chem (2011) 46: 6119-6130 [PMID:22000936]
ChEMBL Inhibition of Electrophorus electricus acetylcholinesterase preincubated with compound for 10 mins using acetylcholine iodide as substrate after 15 mins by spectrophotometric analysis B 7.57 pIC50 27 nM IC50 Bioorg Med Chem Lett (2011) 21: 2384-2388 [PMID:21411323]
ChEMBL Inhibition of electric eel AChE after 15 mins by Ellman's method B 7.57 pIC50 27 nM IC50 Eur J Med Chem (2011) 46: 1-10 [PMID:21111515]
ChEMBL Inhibition of Electrophorus electricus AChE by Ellman's method B 7.57 pIC50 27 nM IC50 Bioorg Med Chem (2011) 19: 122-133 [PMID:21163662]
ChEMBL Inhibition of electric eel AChE by Ellman's method B 7.57 pIC50 27 nM IC50 J Med Chem (2010) 53: 5129-5143 [PMID:20575555]
ChEMBL Inhibition of electric eel AChE using acetylthiocholine iodide as substrate pretreated for 4.5 mins followed by substrate addition and measured after 2.5 mins by Ellman's method B 7.6 pIC50 25.12 nM IC50 Medchemcomm (2017) 8: 1346-1359 [PMID:30108847]
ChEMBL Inhibition of electric eel AChE B 7.62 pIC50 24.1 nM IC50 Bioorg Med Chem (2014) 22: 4867-4881 [PMID:25047936]
ChEMBL Inhibition of electric eel AChE B 7.62 pIC50 24.04 nM IC50 Bioorg Med Chem (2014) 22: 4867-4881 [PMID:25047936]
ChEMBL Inhibition of Electrophorus electricus AChE after 5 mins by Ellman's method B 7.62 pIC50 24 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 7.62 pIC50 24 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 7.62 pIC50 24 nM IC50 Bioorg Med Chem Lett (2016) 26: 4140-4145 [PMID:27445168]
ChEMBL Inhibition of Electrophorus electricus AChE pre-incubated for 5 mins before addition of acetylthiocholine iodide substrate by Ellman's assay B 7.62 pIC50 24 nM IC50 Bioorg Med Chem (2015) 23: 1629-1637 [PMID:25707322]
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 7.62 pIC50 24 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 7.64 pIC50 23 nM IC50 Eur J Med Chem (2020) 187: 111916-111916 [PMID:31812794]
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 7.64 pIC50 23 nM IC50 Eur J Med Chem (2021) 225: 113783-113783 [PMID:34461507]
ChEMBL Inhibition of Electric eel AChE using acetylthiocholine iodide as substrate preincubated for 5 mins followed by substrate addition measured after 5 mins by Ellman's method B 7.64 pIC50 23 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 7.64 pIC50 23 nM IC50 Eur J Med Chem (2021) 218: 113397-113397 [PMID:33838585]
ChEMBL Inhibition of electric eel AChE using acetylthiocholine iodide as substrate preincubated for 5 mins followed by substrate addition and measured after 1 min in presence of H2O2 by Ellman's method B 7.66 pIC50 21.63 nM IC50 Eur J Med Chem (2021) 212: 112997-112997 [PMID:33189440]
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 7.7 pIC50 20 nM IC50 Eur J Med Chem (2023) 249: 115135-115135 [PMID:36696766]
ChEMBL Inhibition of electric eel AChE by Ellman's method B 7.7 pIC50 20 nM IC50 Bioorg Med Chem Lett (2021) 49: 128316-128316 [PMID:34391893]
ChEMBL Inhibition of electric eel AChE preincubated for 5 mins by Ellman's method B 7.76 pIC50 17.38 nM IC50 Eur J Med Chem (2010) 45: 5602-5611 [PMID:20926161]
ChEMBL In vitro inhibitory activity against acetylcholinesterase (AChE) in Electrophorus electricus B 7.8 pIC50 16 nM IC50 Bioorg Med Chem Lett (2003) 13: 2389-2391 [PMID:12824041]
ChEMBL Inhibition of electric eel AChE by colorimetric Ellman assay B 7.81 pIC50 15.6 nM IC50 J Med Chem (2012) 55: 5231-5242 [PMID:22624880]
ChEMBL Inhibition of acetylcholinesterase (AChE) in electric eel (type V-S) by modified radiometric assay B 8.03 pIC50 9.33 nM IC50 Bioorg Med Chem Lett (1992) 2: 861-864
ChEMBL Inhibition of electric eel AChE using acetylthiocholine iodide as substrate by Ellman's method B 8.7 pIC50 2 nM IC50 Bioorg Med Chem Lett (2016) 26: 1624-1628 [PMID:26869193]
ChEMBL Inhibition of electric eel AChE by Ellman's method B 8.73 pIC50 1.87 nM IC50 Bioorg Med Chem Lett (2022) 77: 129037-129037 [PMID:36307033]
acetylcholinesterase (Yt blood group)/Acetylcholinesterase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL220] [GtoPdb: 2465] [UniProtKB: P22303]
ChEMBL Inhibition of AChE (unknown origin) by UV spectrophotometric analysis B 6.55 pKi 282.5 nM Ki Eur J Med Chem (2020) 205: 112666-112666 [PMID:32795767]
ChEMBL Inhibition of human recombinant AChE assessed as dissociation constant for enzyme-inhibitor complex by Lineweaver-Burk plot B 6.65 pKi 225 nM Ki J Med Chem (2014) 57: 7073-7084 [PMID:25089370]
ChEMBL Inhibitory activity of compound against acetylcholinesterase from human erythrocytes B 6.82 pKi 151 nM Ki J Med Chem (2003) 46: 954-966 [PMID:12620072]
ChEMBL Competitive inhibition constant for Acetylcholinesterase B 6.82 pKi 151 nM Ki J Med Chem (2005) 48: 24-27 [PMID:15633997]
ChEMBL Inhibition of human AChE B 6.86 pKi 137 nM Ki J Med Chem (2006) 49: 3421-3425 [PMID:16722663]
ChEMBL Binding affinity to AChE (unknown origin) assessed as inhibition constant B 6.96 pKi 109.75 nM Ki Eur J Med Chem (2022) 233: 114242-114242 [PMID:35276424]
ChEMBL Inhibition of human recombinant AChE assessed as dissociation constant for enzyme-inhibitor-substrate complex by Lineweaver-Burk plot B 7 pKi 101 nM Ki J Med Chem (2014) 57: 7073-7084 [PMID:25089370]
ChEMBL Inhibition of human recombinant AChE B 7.44 pKi 36 nM Ki Bioorg Med Chem Lett (2008) 18: 5213-5216 [PMID:18786825]
ChEMBL Inhibition of human recombinant AChE B 7.44 pKi 36 nM Ki J Med Chem (2008) 51: 3154-3170 [PMID:18479118]
ChEMBL Inhibition of human AChE assessed as acetylthiocholine hydrolysis B 7.45 pKi 35.7 nM Ki Bioorg Med Chem (2014) 22: 4784-4791 [PMID:25088549]
ChEMBL Inhibition of human recombinant AChE using acetylthiocholine as substrate B 7.49 pKi 32.12 nM Ki Bioorg Med Chem (2012) 20: 6739-6750 [PMID:23041347]
GtoPdb - - 7.5 pKi 30 nM Ki J Med Chem (2008) 51: 3154-70 [PMID:18479118]
ChEMBL Inhibition of AChE (unknown origin) B 7.64 pKi 22.99 nM Ki Eur J Med Chem (2020) 205: 112666-112666 [PMID:32795767]
ChEMBL Inhibition of AChE (unknown origin) using acetylcholine iodate as substrate preincubated for 10 mins followed by substrate addition by Lineweaver-Burk plot analysis B 8.12 pKi 7.64 nM Ki Bioorg Med Chem (2016) 24: 2318-2329 [PMID:27068142]
ChEMBL Inhibition of human recombinant AChE using S-acetylthiocholine as substrate by DTNB reagent based spectrophotometric analysis B 5.93 pIC50 1180 nM IC50 Bioorg Med Chem (2022) 73: 117030-117030 [PMID:36179486]
ChEMBL Inhibition of human recombinant AChE by Ellman's method B 5.99 pIC50 1030 nM IC50 J Med Chem (2007) 50: 5311-5323 [PMID:17902635]
ChEMBL Inhibition of human Acetylcholinesterase B 6.03 pIC50 926 nM IC50 J Med Chem (2007) 50: 5685-5695 [PMID:17944454]
ChEMBL Inhibition of human AChE by Ellmans test B 6.1 pIC50 800 nM IC50 J Med Chem (2010) 53: 6490-6505 [PMID:20684567]
ChEMBL Inhibition of human erythrocyte AChE using acetylthiocholine iodide as substrate preincubated for 10 mins followed by substrate addition by Ellman's method B 6.22 pIC50 600 nM IC50 Bioorg Med Chem (2017) 25: 5981-5994 [PMID:28986116]
ChEMBL Inhibition of human erythrocyte AChE using acetylthiocholine iodide as substrate incubated for 10 mins followed by substrate addition by Ellman's method B 6.22 pIC50 600 nM IC50 Bioorg Med Chem (2018) 26: 4716-4725 [PMID:30104121]
ChEMBL Inhibition of human erythrocyte acetylcholinesterase using acetylthiocholine iodide as substrate preincubated for 10 mins followed by substrate addition by Ellman's method B 6.22 pIC50 600 nM IC50 Bioorg Med Chem (2017) 25: 3997-4007 [PMID:28578994]
ChEMBL Inhibition of human erythrocyte acetylcholinesterase using acetylthiocholine chloride as substrate preincubated for 15 mins followed by substrate addition by Ellman's method B 6.27 pIC50 534 nM IC50 Bioorg Med Chem (2014) 22: 1355-1361 [PMID:24461494]
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 6.27 pIC50 534 nM IC50 J Med Chem (2013) 56: 9089-9099 [PMID:24160297]
ChEMBL Inhibition of recombinant human AChE using acetylthiocholine iodide as substrate preincubated for 5 mins before substrate addition by Ellman's method B 6.28 pIC50 520 nM IC50 Bioorg Med Chem (2013) 21: 4928-4937 [PMID:23891231]
ChEMBL Inhibition of acetylcholinesterase in human erythrocytes using acetylthiocholine iodide substrate by spectrophotometric Ellman's method B 6.3 pIC50 501 nM IC50 Bioorg Med Chem (2015) 23: 5610-5618 [PMID:26242241]
ChEMBL Inhibition of human recombinant AChE after 5 mins by Ellman method B 6.3 pIC50 500 nM IC50 J Med Chem (2014) 57: 8576-8589 [PMID:25259726]
ChEMBL Inhibition of human recombinant AChE pre-incubated for 5 mins before acetylthiocholine substrate addition by Ellman's method B 6.3 pIC50 500 nM IC50 J Med Chem (2014) 57: 7073-7084 [PMID:25089370]
ChEMBL Inhibition of human recombinant AChE after 5 mins using spectrophotometer by Ellman's method B 6.3 pIC50 500 nM IC50 Bioorg Med Chem Lett (2011) 21: 6563-6566 [PMID:21920739]
ChEMBL Inhibition of human SH-SY5Y cell lysate acetylcholinesterase using acetylthiocholine iodide as substrate preincubated for 5 mins followed by substrate addition by Ellman's method B 6.3 pIC50 500 nM IC50 Bioorg Med Chem (2019) 27: 895-930 [PMID:30744931]
ChEMBL Inhibition of human recombinant AChE after 5 mins B 6.3 pIC50 500 nM IC50 Bioorg Med Chem Lett (2010) 20: 6093-6095 [PMID:20817518]
ChEMBL Inhibition of human recombinant AchE using acetylthiocholine iodide as substrate by Ellman method B 6.32 pIC50 484 nM IC50 Bioorg Med Chem Lett (2015) 25: 830-833 [PMID:25597004]
ChEMBL Inhibition of recombinant human AChE using acetylthiocholine iodide as substrate by spectroscopic Ellmans method B 6.32 pIC50 484 nM IC50 Eur J Med Chem (2011) 46: 2193-2205 [PMID:21435752]
ChEMBL Inhibition of acetylcholinesterase (unknown origin) using acetylthiocholine iodide as substrate incubated for 30 mins by Ellman's coupled enzyme assay B 6.32 pIC50 480 nM IC50 Bioorg Med Chem (2020) 28: 115820-115820 [PMID:33120080]
ChEMBL Inhibition of human AChE using acetylthiocholine iodide as substrate incubated for 6 mins by spectrophotometric method B 6.33 pIC50 467 nM IC50 Bioorg Med Chem (2014) 22: 6089-6104 [PMID:25282654]
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 6.34 pIC50 459 nM IC50 Eur J Med Chem (2016) 123: 282-297 [PMID:27484514]
ChEMBL Inhibition of human erythrocyte ACHE preincubated for 6 mins followed by addition of acetylcholine iodide as substrate by Ellman's method B 6.35 pIC50 450 nM IC50 Bioorg Med Chem (2016) 24: 4324-4338 [PMID:27460699]
ChEMBL Inhibition of human erythrocyte AChE using acetylthiocholine iodide as substrate preincubated for 6 mins before substrate addition by Ellman's method B 6.36 pIC50 435.1 nM IC50 Eur J Med Chem (2015) 93: 42-50 [PMID:25656088]
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 6.37 pIC50 430 nM IC50 Eur J Med Chem (2018) 146: 287-298 [PMID:29407958]
ChEMBL Inhibition of human recombinant AChE B 6.37 pIC50 426.58 nM IC50 J Med Chem (2004) 47: 6490-6498 [PMID:15588084]
ChEMBL Inhibition of Acetylcholinesterase (unknown origin) using acetylthiocholine iodide as substrate by Ellman's spectrophotometric method B 6.37 pIC50 425.6 nM IC50 Bioorg Med Chem (2019) 27: 3979-3997 [PMID:31401008]
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 6.37 pIC50 424 nM IC50 Eur J Med Chem (2017) 141: 197-210 [PMID:29031067]
ChEMBL Inhibition of human recombinant AChE using ATCh as substrate preincubated for 20 mins followed by substrate addition and measured for 3 mins by Ellman method B 6.37 pIC50 424 nM IC50 Eur J Med Chem (2019) 168: 58-77 [PMID:30798053]
ChEMBL Inhibition of Acetylcholinesterase B 6.37 pIC50 424 nM IC50 J Med Chem (2005) 48: 24-27 [PMID:15633997]
ChEMBL Inhibition of recombinant human AChE using acetylthiocholine iodide as substrate preincubated for 20 mins followed by substrate addition by Ellman's method B 6.37 pIC50 424 nM IC50 J Med Chem (2016) 59: 114-131 [PMID:26632651]
ChEMBL Inhibitory concentration against human recombinant acetylcholinesterase B 6.37 pIC50 424 nM IC50 J Med Chem (2005) 48: 360-363 [PMID:15658850]
ChEMBL Inhibition of human recombinant AChE by Ellman's method B 6.37 pIC50 424 nM IC50 J Med Chem (2008) 51: 4381-4384 [PMID:18605718]
ChEMBL Inhibition of human recombinant AChE using acetylthiocholine iodide as substrate preincubated for 20 mins followed by substrate addition by Ellman's method B 6.37 pIC50 424 nM IC50 Eur J Med Chem (2014) 73: 141-152 [PMID:24389509]
ChEMBL Inhibition of human recombinant acetylcholinesterase B 6.37 pIC50 424 nM IC50 J Med Chem (2007) 50: 4882-4897 [PMID:17850125]
ChEMBL Inhibition of human serum recombinant AChE by Ellman's method B 6.37 pIC50 424 nM IC50 J Med Chem (2007) 50: 6446-6449 [PMID:18047264]
ChEMBL Inhibition of human AChE using acetylthiocholine iodide as substrate incubated for 6 mins prior to substrate addition measured after 60 to 180 secs by Ellman method B 6.38 pIC50 420.32 nM IC50 Eur J Med Chem (2015) 95: 153-165 [PMID:25812965]
ChEMBL Inhibition of human recombinant AChE using acetylthiocholine iodide as substrate by Ellman's method B 6.38 pIC50 420 nM IC50 Eur J Med Chem (2012) 52: 251-262 [PMID:22503231]
ChEMBL Inhibition of human AchE B 6.38 pIC50 420 nM IC50 J Med Chem (2008) 51: 347-372 [PMID:18181565]
ChEMBL Inhibition of AChE in human erythrocyte hemo-lyzates pre-incubated for 5 mins before addition of acetylthiocholine iodide substrate by Ellman's method B 6.38 pIC50 420 nM IC50 J Med Chem (2016) 59: 9967-9973 [PMID:27736061]
ChEMBL Inhibition of recombinant human AChE using acetylthiocholine iodide as substrate preincubated with compound for 20 mins followed by substrate addition and measured after 240 sec by spectrophotometer based Ellman's method B 6.38 pIC50 415 nM IC50 Bioorg Med Chem (2023) 91: 117419-117419 [PMID:37487339]
ChEMBL Inhibition of AChE (unknown origin) B 6.39 pIC50 412 nM IC50 Eur J Med Chem (2021) 226: 113874-113874 [PMID:34619465]
ChEMBL Inhibition of recombinant human AChE using acetylthiocholine iodide as substrate pre-incubated for 20 mins before substrate addition and measured for 180 secs by spectrophotometry based Ellman's method B 6.39 pIC50 412 nM IC50 Eur J Med Chem (2019) 167: 161-186 [PMID:30771604]
ChEMBL Inhibition of human erythrocyte AChE using acetylthiocholine chloride as substrate preincubated for 15 mins followed by substrate addition and measured at 1 min time interval by Ellman's method relative to control B 6.4 pIC50 400 nM IC50 Eur J Med Chem (2019) 167: 133-145 [PMID:30771601]
ChEMBL Inhibition of human recombinant AChE by Ellman's assay B 6.42 pIC50 383 nM IC50 Bioorg Med Chem Lett (2013) 23: 6254-6258 [PMID:24140444]
ChEMBL Inhibition of recombinant human AChE expressed in HEK293 cells using acetylthiocholine as substrate pretreated for 20 mins followed by substrate addition by Ellman's method B 6.43 pIC50 374 nM IC50 Eur J Med Chem (2018) 155: 839-846 [PMID:29958119]
ChEMBL Inhibition of human AChE B 6.46 pIC50 350 nM IC50 J Med Chem (2006) 49: 459-462 [PMID:16420031]
ChEMBL Inhibition of human AChE using acetylthiocholine iodide as substrate incubated for 10 mins prior to substrate addition measured after 15 mins by Ellman's method B 6.46 pIC50 350 nM IC50 Eur J Med Chem (2012) 54: 750-763 [PMID:22795665]
ChEMBL Inhibition of human erythrocytes AChE by Ellman's method B 6.46 pIC50 350 nM IC50 J Med Chem (2012) 55: 1303-1317 [PMID:22243648]
ChEMBL Inhibition of human AChE in erythrocyte B 6.46 pIC50 350 nM IC50 J Med Chem (2009) 52: 7249-7257 [PMID:19856923]
ChEMBL Inhibition of human erythrocyte AChE by Ellman's reaction B 6.46 pIC50 350 nM IC50 J Med Chem (2010) 53: 4927-4937 [PMID:20545360]
ChEMBL Inhibition of recombinant human AChE using acetylthiocholine iodide as substrate preincubated for 20 mins followed by substrate addition and measured for 5 mins by Ellman's assay B 6.46 pIC50 350 nM IC50 Medchemcomm (2017) 8: 1307-1317 [PMID:30108842]
ChEMBL Inhibition of human erythrocyte AChE using acetylthiocholine as substrate assessed as substrate hydrolysis preincubated for 20 mins followed by substrate addition measured after 30 mins by Ellman's assay B 6.48 pIC50 330 nM IC50 J Nat Prod (2015) 78: 3075-3079 [PMID:26583263]
ChEMBL DRUGMATRIX: Acetylcholinesterase enzyme inhibition (substrate: acetylthiocholine) B 6.48 pIC50 330 nM IC50 DrugMatrix in vitro pharmacology data
ChEMBL Inhibition of recombinant human AChE expressed in HEK293 cells using acetylthiocholine iodide as substrate preincubated for 15 mins followed by substrate addition by Ellman's method B 6.49 pIC50 320 nM IC50 J Med Chem (2020) 63: 9360-9390 [PMID:32706255]
ChEMBL Inhibition of human erythrocyte AChE using acetylthiocholine iodide as substrate preincubated for 5 mins followed by substrate addition measured at 2 mins time interval by Ellman's method B 6.49 pIC50 320 nM IC50 Eur J Med Chem (2018) 150: 292-306 [PMID:29533874]
ChEMBL Inhibition of human recombinant AChE using acetylthiocholine as substrate preincubated for 5 mins followed by substrate addition measured every 2 mins by Ellman's method B 6.49 pIC50 320 nM IC50 J Med Chem (2015) 58: 8985-9003 [PMID:26503905]
ChEMBL Inhibition of human recombinant AChE using acetylthiocholine iodide as substrate preincubated for 5 mins followed by substrate addition and measured over 2 mins by UV-Vis spectrophotometric analysis based Ellman's method B 6.49 pIC50 320 nM IC50 Eur J Med Chem (2019) 168: 491-514 [PMID:30851693]
ChEMBL Inhibition of human recombinant AChE assessed as reduction in cholinesterase activity using acetylthiocholine iodide as substrate by Ellman's method B 6.49 pIC50 320 nM IC50 Eur J Med Chem (2021) 219: 113434-113434 [PMID:33892271]
ChEMBL Inhibition of recombinant human AChE using acetylthiocholine as substrate by DTNB-reagent based Ellman's method B 6.49 pIC50 320 nM IC50 Bioorg Med Chem Lett (2021) 43: 128100-128100 [PMID:33984470]
ChEMBL Inhibition of human recombinant AChE using acetylthiocholine iodide as substrate preincubated for 20 mins prior substrate addition measured after 5 mins by spectrophotometry B 6.5 pIC50 317 nM IC50 J Med Chem (2012) 55: 661-669 [PMID:22185619]
ChEMBL Inhibition of AChE (unknown origin) B 6.52 pIC50 300 nM IC50 Bioorg Med Chem (2014) 22: 3806-3814 [PMID:24934993]
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 6.52 pIC50 300 nM IC50 Eur J Med Chem (2017) 130: 139-153 [PMID:28242549]
ChEMBL Inhibition of human recombinant AChE using acetylthiocholine iodide as substrate preincubated with enzyme for 20 mins prior to substrate addition by Ellman's method B 6.52 pIC50 300 nM IC50 Bioorg Med Chem Lett (2015) 25: 2804-2808 [PMID:26003339]
ChEMBL Inhibition of AChE (unknown origin) using acetylthiocholine iodide as substrate preincubated for 20 mins followed by substrate addition and measured every 30 secs for 1 hr by Ellman's assay B 6.52 pIC50 300 nM IC50 Bioorg Med Chem (2019) 27: 442-446 [PMID:30579802]
ChEMBL Inhibition of human erythrocyte AChE preincubated for 15 mins by Ellman's method B 6.55 pIC50 285 nM IC50 Eur J Med Chem (2014) 87: 429-439 [PMID:25282266]
ChEMBL Inhibition of human AChE using acetylthiocholine chloride as substrate preincubated for 15 mins by Ellman's method B 6.55 pIC50 285 nM IC50 Bioorg Med Chem Lett (2013) 23: 6737-6742 [PMID:24220172]
ChEMBL Inhibition of human erythrocytic AChE using acetylthiocholine chloride as substrate preincubated for 15 mins followed by substrate addition measured every 1 min by Ellman method B 6.55 pIC50 285 nM IC50 Bioorg Med Chem (2013) 21: 7406-7417 [PMID:24128814]
ChEMBL Compound was evaluated for the in vitro inhibition of the Acetylcholinesterase (AChE) from human erythrocytes, B 6.57 pIC50 270 nM IC50 J Med Chem (1994) 37: 2721-2734 [PMID:8064800]
ChEMBL Inhibition of AChE in human Erythrocyte incubated for 20 mins by Ellman reagent based spectrophotometry B 6.57 pIC50 270 nM IC50 J Nat Prod (2022) 85: 1486-1494 [PMID:35658485]
ChEMBL Inhibition of human erythrocyte AChE using S-acetylthiocholine iodide as substrate preincubated for 20 mins followed by substrate addition measured every 30 secs for 1 hr by Ellman's method B 6.57 pIC50 270 nM IC50 J Nat Prod (2017) 80: 1493-1504 [PMID:28445039]
ChEMBL Inhibition against Acetylcholinesterase (AChE) B 6.57 pIC50 269.77 nM IC50 J Med Chem (1996) 39: 380-387 [PMID:8558505]
ChEMBL Inhibition of human AchE using acetylthiocholine iodide as substrate incubated for 20 mins prior to substrate addition measured for 1 hr by Ellman's method B 6.57 pIC50 268 nM IC50 Bioorg Med Chem (2013) 21: 4218-4224 [PMID:23719283]
ChEMBL Concentration required to inhibit 50% of Acetylcholinesterase obtained from human erythrocytes was determined in vitro B 6.57 pIC50 267 nM IC50 J Med Chem (1995) 38: 1084-1089 [PMID:7707311]
ChEMBL Inhibitory concentration against human acetylcholinesterase B 6.57 pIC50 267 nM IC50 J Med Chem (2005) 48: 3564-3575 [PMID:15887964]
ChEMBL Compound was tested in vitro for inhibitory activity against Acetylcholinesterase B 6.6 pIC50 254 nM IC50 Bioorg Med Chem Lett (1997) 7: 2599-2602
ChEMBL Inhibitory activity against human erythrocyte acetylcholinesterase B 6.6 pIC50 251.19 nM IC50 J Med Chem (2004) 47: 4471-4482 [PMID:15317459]
ChEMBL Inhibition of human recombinant AChE expressed in HEK293 cells by photometry B 6.6 pIC50 251.19 nM IC50 J Med Chem (2010) 53: 1338-1346 [PMID:20047331]
ChEMBL Inhibitory concentration against acetylcholinesterase from human erythrocytes B 6.6 pIC50 251.19 nM IC50 J Med Chem (2003) 46: 954-966 [PMID:12620072]
ChEMBL Inhibition of human recombinant AChE using acetylthiocholine iodide as substrate preincubated for 20 mins by Ellman's method B 6.6 pIC50 250 nM IC50 Eur J Med Chem (2014) 78: 157-166 [PMID:24681980]
ChEMBL Inhibition of AChE (unknown origin) preincubated for 30 mins followed by substrate addition acetylthiocholineiodide measured after 40 mins by Ellman's method B 6.6 pIC50 250 nM IC50 Eur J Med Chem (2020) 200: 112415-112415 [PMID:32454229]
ChEMBL Inhibitory activity against human erythrocyte acetylcholinesterase B 6.6 pIC50 250 nM IC50 J Med Chem (2000) 43: 2007-2018 [PMID:10821713]
ChEMBL Inhibition of human serum recombinant AChE using acetylthiocholine iodide as substrate preincubated for 20 mins by Ellman's method B 6.6 pIC50 250 nM IC50 Eur J Med Chem (2011) 46: 4336-4343 [PMID:21798635]
ChEMBL Inhibition of human recombinant AchE using acetylthiocholine iodide as substrate incubated for 5 mins prior to substrate addition measured after 5 mins by Ellman method B 6.64 pIC50 230 nM IC50 J Med Chem (2014) 57: 3773-3785 [PMID:24738476]
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 6.64 pIC50 230 nM IC50 Eur J Med Chem (2018) 158: 781-800 [PMID:30245401]
ChEMBL Inhibition of recombinant human AChE using acetylthiocholine iodide as substrate preincubated for 20 mins followed by substrate addition by Ellman's method B 6.64 pIC50 230 nM IC50 J Med Chem (2021) 64: 4972-4990 [PMID:33829779]
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 6.64 pIC50 230 nM IC50 Eur J Med Chem (2017) 139: 773-791 [PMID:28863358]
ChEMBL Inhibition of AchE (unknown origin) B 6.64 pIC50 230 nM IC50 J Med Chem (2021) 64: 26-41 [PMID:33346659]
ChEMBL Inhibition of human AChE using acetylthiocholine iodide as substrate incubated for 20 mins followed by substrate addition measured after 2 mins by Ellman's method B 6.64 pIC50 230 nM IC50 ACS Med Chem Lett (2018) 9: 171-176 [PMID:29541355]
ChEMBL Inhibition of AChE B 6.65 pIC50 223 nM IC50 Eur J Med Chem (2010) 45: 1167-1172 [PMID:20053484]
ChEMBL Inhibition of acetylcholinesterase (AChE) of human erythrocytes B 6.66 pIC50 218.78 nM IC50 J Med Chem (1998) 41: 4186-4189 [PMID:9784091]
ChEMBL Inhibition of human erythrocyte AChE B 6.69 pIC50 205 nM IC50 J Med Chem (2006) 49: 6833-6840 [PMID:17154513]
ChEMBL Inhibition of acetylcholinesterase isolated from Human erythrocytes. B 6.69 pIC50 205 nM IC50 J Med Chem (2000) 43: 4657-4666 [PMID:11101357]
ChEMBL Inhibition of human erythrocyte AChE B 6.7 pIC50 200 nM IC50 Eur J Med Chem (2014) 78: 455-467 [PMID:24704618]
ChEMBL Inhibition of AChE-induced amyloid beta aggregation B 6.7 pIC50 200 nM IC50 Bioorg Med Chem Lett (2011) 21: 2687-2691 [PMID:21216144]
ChEMBL Inhibitory concentration against acetylcholinesterase B 6.7 pIC50 200 nM IC50 Bioorg Med Chem Lett (2005) 15: 2711-2715 [PMID:15878275]
ChEMBL Inhibition of human AChE by Ellman's assay B 6.7 pIC50 200 nM IC50 J Nat Prod (2009) 72: 1151-1154 [PMID:19422203]
ChEMBL Inhibition of AChE by Ellman method B 6.7 pIC50 200 nM IC50 J Nat Prod (2007) 70: 1458-1461 [PMID:17822295]
ChEMBL Inhibition of AChE (unknown origin) B 6.7 pIC50 200 nM IC50 Bioorg Med Chem Lett (2015) 25: 4848-4853 [PMID:26159481]
ChEMBL Inhibition of human AChE using acetylthiocholine iodide as substrate preincubated for 20 mins followed by substrate addition and measured every 30 sec for 3 mins by DTNB-based UV analysis B 6.7 pIC50 199.53 nM IC50 RSC Med Chem (2022) 13: 944-954 [PMID:36092149]
ChEMBL Inhibition of human recombinant AChE expressed in HEK293 cells using acetylthiocholine iodide as substrate incubated for 10 mins by Ellman's method B 6.72 pIC50 190 nM IC50 Bioorg Med Chem (2021) 30: 115940-115940 [PMID:33340937]
ChEMBL Anticholinesterase activity against human erythrocyte AChE B 6.72 pIC50 190 nM IC50 J Med Chem (2006) 49: 2174-2185 [PMID:16570913]
ChEMBL Inhibition of AChE (unknown origin) B 6.72 pIC50 190 nM IC50 J Med Chem (2014) 57: 8167-8179 [PMID:25226236]
ChEMBL Inhibitory concentration against human erythrocyte Acetylcholinesterase B 6.72 pIC50 190 nM IC50 J Med Chem (2005) 48: 986-994 [PMID:15715468]
ChEMBL Ex vivo inhibition of human erythrocyte Acetylcholinesterase. B 6.72 pIC50 190 nM IC50 J Med Chem (2002) 45: 3684-3691 [PMID:12166941]
ChEMBL Inhibition of human erythrocytes AChE B 6.72 pIC50 190 nM IC50 Eur J Med Chem (2011) 46: 2170-2184 [PMID:21459491]
ChEMBL Inhibition of human plasma AChE B 6.72 pIC50 190 nM IC50 Eur J Med Chem (2011) 46: 2170-2184 [PMID:21459491]
ChEMBL Inhibition of human AChE using acetylthiocholine iodide as substrate preincubated for 20 mins followed by substrate addition and measured every 30 sec for 3 mins by DTNB-based UV analysis B 6.73 pIC50 188 nM IC50 RSC Med Chem (2022) 13: 944-954 [PMID:36092149]
ChEMBL Inhibitory concentration required against acetylcholinesterase activity B 6.74 pIC50 180 nM IC50 J Med Chem (2001) 44: 4011-4014 [PMID:11689088]
ChEMBL Inhibition of human acetylcholinesterase-I B 6.74 pIC50 180 nM IC50 J Med Chem (1992) 35: 1102-1108 [PMID:1552502]
ChEMBL In vitro acetyl cholinesterase (AChE-I) inhibitory activity, ability to reverse the cholinergic deficit characteristic of AD B 6.74 pIC50 180 nM IC50 J Med Chem (1992) 35: 3141-3147 [PMID:1507203]
ChEMBL Inhibition of human acetylcholinesterase using acetylthiocholine iodide as substrate incubated for 15 mins by Ellman's method B 6.75 pIC50 178 nM IC50 RSC Med Chem (2022) 13: 1644-1656 [PMID:36561075]
ChEMBL Inhibition of human AChE using acetylthiocholine iodide as substrate preincubated with enzyme for 1 min followed by substrate addition and measured after 10 mins by Ellman's method B 6.76 pIC50 171.9 nM IC50 Eur J Med Chem (2020) 207: 112751-112751 [PMID:32950908]
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 6.77 pIC50 170 nM IC50 Eur J Med Chem (2022) 242: 114630-114630 [PMID:35987018]
ChEMBL In vitro inhibition of Acetylcholinesterase from human erythrocytes B 6.77 pIC50 170 nM IC50 J Med Chem (1995) 38: 2802-2808 [PMID:7636841]
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 6.8 pIC50 160 nM IC50 Medchemcomm (2015) 6: 1930-1941
ChEMBL Inhibition of human AChE using acetylthiocholine iodide as substrate treated 5 mins before substrate addition measured up to 4 mins by Ellman's method B 6.8 pIC50 160 nM IC50 Bioorg Med Chem Lett (2013) 23: 4336-4341 [PMID:23791077]
ChEMBL Pseudo-irreversible inhibition of human AChE using acetylthiocholine iodide as substrate incubated for 20 mins followed by substrate addition by Ellman's method based UV analysis B 6.8 pIC50 158.49 nM IC50 J Med Chem (2023) 66: 6414-6435 [PMID:37127287]
ChEMBL Inhibition of human AChE B 6.8 pIC50 158.49 nM IC50 J Med Chem (2019) 62: 9078-9102 [PMID:31609608]
ChEMBL Pseudo-irreversible inhibition of human AChE using acetylthiocholine iodide as substrate incubated for 20 mins followed by substrate addition by Ellman's method based UV analysis B 6.82 pIC50 152 nM IC50 J Med Chem (2023) 66: 6414-6435 [PMID:37127287]
ChEMBL Inhibition of human erythrocyte AChE by Ellman's method B 6.82 pIC50 150 nM IC50 Bioorg Med Chem (2008) 16: 7759-7769 [PMID:18640842]
ChEMBL Inhibition of recombinant human AChE expressed in HEK293 cells using acetylthiocholine iodide as substrate preincubated for 5 mins before substrate addition measured after 10 mins by Ellman's method B 6.82 pIC50 150 nM IC50 Medchemcomm (2012) 3: 213-218
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 6.83 pIC50 148 nM IC50 Eur J Med Chem (2022) 244: 114806-114806 [PMID:36223681]
ChEMBL Inhibition of human serum AChE by Ellman's method B 6.83 pIC50 147 nM IC50 J Med Chem (2009) 52: 2724-2732 [PMID:19374444]
ChEMBL Inhibition of human erythrocyte AChE B 6.83 pIC50 147 nM IC50 J Med Chem (2006) 49: 7607-7610 [PMID:17181144]
ChEMBL In vitro inhibition of acetylcholinesterase isolated from human erythrocytes. B 6.84 pIC50 143 nM IC50 Bioorg Med Chem Lett (1991) 1: 411-414
ChEMBL Inhibition of AChE (unknown origin) after 10 min by Ellmans method B 6.85 pIC50 140 nM IC50 Med Chem Res (2012) 21: 1785-1795
ChEMBL Inhibition of human recombinant AChE after 5 mins by Ellman's method B 6.88 pIC50 131 nM IC50 Eur J Med Chem (2015) 92: 738-749 [PMID:25621991]
ChEMBL Inhibition of human recombinant AChE pre-incubated for 5 mins before addition of acetylthiocholine iodide substrate by Ellman's assay B 6.88 pIC50 131 nM IC50 Bioorg Med Chem (2015) 23: 1629-1637 [PMID:25707322]
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 6.88 pIC50 131 nM IC50 Eur J Med Chem (2016) 124: 63-81 [PMID:27560283]
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 6.88 pIC50 131 nM IC50 Eur J Med Chem (2020) 207: 112743-112743 [PMID:32882609]
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 6.88 pIC50 131 nM IC50 Eur J Med Chem (2020) 185: 111785-111785 [PMID:31669851]
ChEMBL Inhibition of recombinant human AChE expressed in HEK293 cells using acetylthiocholine iodide as substrate pretreated for 5 mins followed by substrate addition measured after 5 mins by spectrophotometry based Ellman method B 6.89 pIC50 130 nM IC50 Eur J Med Chem (2017) 126: 576-589 [PMID:27918993]
ChEMBL Inhibition of human AChE by Ellman's method B 6.89 pIC50 128 nM IC50 Bioorg Med Chem (2009) 17: 6937-6941 [PMID:19726199]
ChEMBL Inhibition of cerebral human recombinant AchE expressed in HEK293 cells using acetylthiocholine iodide as substrate preincubated for 10 mins measured after 15 mins of substrate addition by Ellman's method B 6.91 pIC50 122 nM IC50 J Med Chem (2011) 54: 8251-8270 [PMID:22023459]
ChEMBL Inhibition of human erythrocyte AChE using acetylthiocholine iodide as substrate preincubated for 5 mins followed by DTNB addition for 5 mins and subsequent addition of substrate measured after 3 mins by Ellman's method B 6.93 pIC50 116.8 nM IC50 Eur J Med Chem (2018) 148: 238-254 [PMID:29466774]
ChEMBL Inhibition of human AChE using acetylthiocholine iodide as substrate incubated for 20 mins followed by substrate addition by Ellman's method B 6.95 pIC50 111 nM IC50 J Med Chem (2021) 64: 9302-9320 [PMID:34152756]
ChEMBL Inhibition of human recombinant AChE after 20 mins using acetylthiocholine iodide as a substrate by Ellman's assay B 6.96 pIC50 110 nM IC50 J Med Chem (2011) 54: 2627-2645 [PMID:21417225]
ChEMBL Inhibition of human AChE using acetylthiocholine iodide as substrate incubated for 20 mins followed by substrate addition by Ellman's method B 6.96 pIC50 109.65 nM IC50 J Med Chem (2021) 64: 9302-9320 [PMID:34152756]
ChEMBL Inhibition of AChE in human erythrocytes by Ellman's method B 7 pIC50 100 nM IC50 J Med Chem (2010) 53: 5129-5143 [PMID:20575555]
ChEMBL Inhibition of acetylcholinesterase (unknown origin) B 7 pIC50 100 nM IC50 Bioorg Med Chem (2013) 21: 146-152 [PMID:23199476]
ChEMBL Inhibition of human recombinant AChE using acetylthiocholine as substrate preincubated for 5 mins followed by substrate addition by Ellman's method B 7 pIC50 99 nM IC50 Eur J Med Chem (2022) 231: 114152-114152 [PMID:35101650]
ChEMBL Inhibitory concentration against acetylcholinesterase (AChE) from human erythrocytes B 7.02 pIC50 95 nM IC50 J Med Chem (1999) 42: 730-741 [PMID:10052979]
ChEMBL In vitro inhibition of acetylcholinesterase from human erythrocytes B 7.02 pIC50 95 nM IC50 J Med Chem (2001) 44: 2707-2718 [PMID:11495583]
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 7.03 pIC50 93 nM IC50 RSC Med Chem (2022) 13: 873-883 [PMID:35923722]
ChEMBL Inhibitory concentration against Acetylcholinesterase activity B 7.05 pIC50 90 nM IC50 Bioorg Med Chem Lett (2005) 15: 353-356 [PMID:15603953]
ChEMBL Inhibition of human recombinant AChE B 7.08 pIC50 84 nM IC50 Bioorg Med Chem Lett (2020) 30: 127609-127609 [PMID:33039562]
ChEMBL Inhibition of human erythrocyte AChE using acetylthiocholine iodide as substrate preincubated for 10 mins followed by substrate addition by Ellman's method B 7.1 pIC50 79 nM IC50 Bioorg Med Chem (2016) 24: 1050-1062 [PMID:26827140]
ChEMBL Inhibition of AChE (unknown origin) by Ellman's method B 7.1 pIC50 79 nM IC50 Bioorg Med Chem Lett (2019) 29: 126754-126754 [PMID:31708262]
ChEMBL Inhibition of Acetylcholinesterase in human red blood cell B 7.11 pIC50 78 nM IC50 J Med Chem (1996) 39: 3014-3018 [PMID:8709135]
ChEMBL Inhibition of human AChE by Ellman's assay B 7.11 pIC50 77 nM IC50 Bioorg Med Chem Lett (2011) 21: 5881-5887 [PMID:21873056]
ChEMBL Inhibition of human AChE pre-incubated for 6 mins before ATCI substrate addition and measured after 12 mins by DTNB reagent dependent UV-Vis spectrophotometry based Ellman's method B 7.12 pIC50 76.5 nM IC50 Eur J Med Chem (2017) 140: 118-127 [PMID:28923380]
ChEMBL Inhibition acetylcholinesterase (AChE) enzyme. B 7.12 pIC50 76.03 nM IC50 J Med Chem (1997) 40: 4360-4371 [PMID:9435905]
ChEMBL Inhibitory activity against Acetylcholinesterase B 7.12 pIC50 76 nM IC50 J Med Chem (1996) 39: 5064-5071 [PMID:8978837]
ChEMBL Inhibition of Acetylcholinesterase in monkey red blood cell B 7.12 pIC50 75 nM IC50 J Med Chem (1996) 39: 3014-3018 [PMID:8709135]
ChEMBL Inhibition of human erythrocytes AChE by Ellman's method B 7.14 pIC50 72.38 nM IC50 Bioorg Med Chem Lett (2020) 30: 127659-127659 [PMID:33137375]
ChEMBL Inhibition of human AChE B 7.15 pIC50 71.61 nM IC50 Bioorg Med Chem (2014) 22: 4867-4881 [PMID:25047936]
ChEMBL Inhibition of human AChE B 7.15 pIC50 71.5 nM IC50 Bioorg Med Chem (2014) 22: 4867-4881 [PMID:25047936]
ChEMBL Inhibition of AChE (unknown origin) using acetylthiocholine iodide as substrate by Ellman's method B 7.26 pIC50 55 nM IC50 Eur J Med Chem (2019) 182: 111651-111651 [PMID:31479975]
ChEMBL In vitro inhibitory activity against acetylcholinesterase B 7.28 pIC50 52 nM IC50 J Med Chem (1992) 35: 584-589 [PMID:1738151]
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 7.3 pIC50 50 nM IC50 J Med Chem (2016) 59: 5823-5846 [PMID:27253679]
ChEMBL Inhibition of human erythrocytes BChE B 7.33 pIC50 47 nM IC50 Eur J Med Chem (2011) 46: 2170-2184 [PMID:21459491]
ChEMBL Inhibition of human plasma BChE B 7.33 pIC50 47 nM IC50 Eur J Med Chem (2011) 46: 2170-2184 [PMID:21459491]
ChEMBL Inhibition of AChE by Ellman's assay B 7.35 pIC50 45.1 nM IC50 J Med Chem (2008) 51: 713-716 [PMID:18232655]
ChEMBL Inhibition of AChE (unknown origin) B 7.36 pIC50 43.21 nM IC50 Eur J Med Chem (2020) 205: 112666-112666 [PMID:32795767]
ChEMBL In vitro inhibitory activity against human erythrocyte acetylcholinesterase B 7.47 pIC50 33.88 nM IC50 J Med Chem (2004) 47: 4471-4482 [PMID:15317459]
ChEMBL Inhibition of acetylcholinesterase (AChE) of human red blood cell (type XIII) by modified radiometric AChE assay B 7.47 pIC50 33.5 nM IC50 Bioorg Med Chem Lett (1992) 2: 861-864
ChEMBL Inhibition of AChE (unknown origin) using acetylthiocholine iodide as substrate incubated for 5 mins by Ellman's method B 7.49 pIC50 32 nM IC50 Eur J Med Chem (2022) 227: 113964-113964 [PMID:34743062]
ChEMBL Inhibition of human acetylcholinesterase B 7.52 pIC50 30 nM IC50 Bioorg Med Chem (2019) 27: 895-930 [PMID:30744931]
ChEMBL Inhibitory activity against acetylcholinesterase in human RBC B 7.52 pIC50 30 nM IC50 Bioorg Med Chem Lett (1996) 6: 737-742
ChEMBL Inhibition of human erythrocyte AChE using ATC iodide as substrate preincubated for 4.5 mins followed by substrate addition measured after 2.5 mins by Ellman's method B 7.7 pIC50 19.95 nM IC50 J Med Chem (2018) 61: 1646-1663 [PMID:29400965]
ChEMBL Inhibition of human erythrocyte AChE using ATC iodide as substrate preincubated for 4.5 mins followed by substrate addition measured after 2.5 mins by Ellman's method B 7.73 pIC50 18.5 nM IC50 J Med Chem (2018) 61: 1646-1663 [PMID:29400965]
ChEMBL Inhibition of recombinant human AChE using acetylthiocholine iodide as substrate preincubated for 20 mins followed by substrate addition and measured for 3 mins by spectrophotometry based Ellman's method B 7.9 pIC50 12.59 nM IC50 J Med Chem (2019) 62: 9078-9102 [PMID:31609608]
ChEMBL Inhibition of AChE (unknown origin) using acetylcholine iodate as substrate preincubated for 10 mins followed by substrate addition by Ellman's method B 8.12 pIC50 7.53 nM IC50 Bioorg Med Chem (2016) 24: 2318-2329 [PMID:27068142]
ChEMBL Inhibition of AChE by Ellman's method B 8.5 pIC50 3.16 nM IC50 Eur J Med Chem (2011) 46: 3250-3257 [PMID:21570751]
Acetylcholinesterase in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4768] [UniProtKB: P23795]
ChEMBL Inhibition of fetal Bovine serum AChE B 7.4 pKi 40 nM Ki J Med Chem (2003) 46: 1-4 [PMID:12502352]
ChEMBL Inhibition of acetylcholinesterase (AChE) of fetal bovine serum (FBS) B 7.4 pKi 40 nM Ki Bioorg Med Chem Lett (2001) 11: 1779-1782 [PMID:11425559]
ChEMBL Dissociation constant for inhibition of fetal bovine serum Acetylcholinesterase B 7.4 pKi 40 nM Ki J Med Chem (2005) 48: 1919-1929 [PMID:15771436]
ChEMBL Inhibition of bovine AChE by Elman's method B 6.15 pIC50 710 nM IC50 Bioorg Med Chem (2010) 18: 2173-2177 [PMID:20176490]
ChEMBL Inhibition of bovine erythrocyte acetylcholinesterase (AChE) B 6.26 pIC50 550 nM IC50 Bioorg Med Chem Lett (1996) 6: 77-80
ChEMBL Inhibition of bovine erythrocytes AChE by Ellman's method B 6.35 pIC50 446 nM IC50 J Med Chem (2007) 50: 5311-5323 [PMID:17902635]
ChEMBL Inhibition of bovine AChE B 6.35 pIC50 445 nM IC50 J Med Chem (2008) 51: 3154-3170 [PMID:18479118]
ChEMBL Inhibition of bovine erythrocytes AChE using acetylthiocholine iodide as substrate by Ellman's methods B 6.74 pIC50 180 nM IC50 Eur J Med Chem (2019) 166: 381-389 [PMID:30739821]
ChEMBL Inhibition of bovine erythrocyte AChE by Ellman's assay B 6.78 pIC50 167 nM IC50 J Med Chem (2008) 51: 3588-3598 [PMID:18517184]
ChEMBL Inhibition of AchE in bovine erythrocytes B 6.78 pIC50 167 nM IC50 J Med Chem (2005) 48: 7223-7233 [PMID:16279781]
ChEMBL Inhibition of bovine AChE by Ellman's method B 6.87 pIC50 134 nM IC50 Bioorg Med Chem (2008) 16: 7450-7456 [PMID:18585045]
ChEMBL Inhibition of acetylcholinesterase (AChE)activity in bovine erythrocytes B 6.89 pIC50 130 nM IC50 J Med Chem (1999) 42: 3227-3242 [PMID:10464010]
ChEMBL Inhibition of bovine erythrocyte AChE B 6.89 pIC50 130 nM IC50 J Med Chem (2006) 49: 6833-6840 [PMID:17154513]
ChEMBL Compound was evaluated for the inhibition of acetylcholinesterase of bovine erythrocytes B 6.89 pIC50 130 nM IC50 J Med Chem (2000) 43: 4657-4666 [PMID:11101357]
ChEMBL Inhibition of bovine erythrocytes AChE by Ellman's method B 6.96 pIC50 109 nM IC50 Bioorg Med Chem (2011) 19: 122-133 [PMID:21163662]
ChEMBL Inhibition of bovine erythrocyte AChE by Ellman's reaction B 7.4 pIC50 40 nM IC50 J Med Chem (2010) 53: 4927-4937 [PMID:20545360]
ChEMBL Inhibition of bovine erythrocyte AChE by Ellman's method B 7.4 pIC50 40 nM IC50 Eur J Med Chem (2010) 45: 6152-6158 [PMID:20926162]
ChEMBL Inhibition of AchE from bovine erythrocytes B 7.4 pIC50 40 nM IC50 J Med Chem (2006) 49: 459-462 [PMID:16420031]
ChEMBL Inhibition of AChE in bovine erythrocyte by Ellman method B 7.4 pIC50 40 nM IC50 J Med Chem (2009) 52: 7249-7257 [PMID:19856923]
ChEMBL Inhibition of AChE in bovine erythrocytes using acetylthiocholine as substrate by Ellman method B 7.4 pIC50 40 nM IC50 Eur J Med Chem (2011) 46: 2224-2235 [PMID:21420206]
ChEMBL Inhibition of bovine erythrocytes AChE by Ellman's method B 7.4 pIC50 40 nM IC50 J Med Chem (2012) 55: 1303-1317 [PMID:22243648]
ChEMBL Displacement of propidium iodide from AChE in bovine erythrocytes after 15 mins by fluorescence plate reader B 7.57 pIC50 27 nM IC50 J Med Chem (2010) 53: 5129-5143 [PMID:20575555]
acetylcholinesterase (Yt blood group)/Acetylcholinesterase in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3198] [GtoPdb: 2465] [UniProtKB: P21836]
ChEMBL Dissociation constant towards Acetylcholinesterase in mouse B 7.74 pKd 18 nM Kd J Med Chem (2004) 47: 3463-3482 [PMID:15214773]
ChEMBL Inhibition of mouse AChE using acetylthiocholine iodide as substrate incubated for 20 mins by Ellman's method B 6.7 pIC50 200 nM IC50 J Med Chem (2021) 64: 7483-7506 [PMID:34024109]
ChEMBL Inhibition of Acetylcholinesterase in mouse red blood cell B 6.84 pIC50 143 nM IC50 J Med Chem (1996) 39: 3014-3018 [PMID:8709135]
ChEMBL Inhibition of Swiss albino mouse RBC AChE after 30 mins by Ellman method B 6.89 pIC50 130 nM IC50 Bioorg Med Chem (2012) 20: 6313-6320 [PMID:23026084]
ChEMBL Inhibition of recombinant mouse AChE by Ellman method B 6.97 pIC50 106 nM IC50 J Med Chem (2014) 57: 8167-8179 [PMID:25226236]
ChEMBL Inhibition of mouse recombinant AChE using butyrylthiocholine iodide as substrate after 5 mins by Ellman's method B 6.97 pIC50 106 nM IC50 Bioorg Med Chem (2015) 23: 4442-4452 [PMID:26116179]
ChEMBL In vitro inhibitory concentration against acetylcholinesterase (AChE) obtained from mouse brain homogenate. B 7.09 pIC50 81 nM IC50 J Med Chem (1992) 35: 4542-4548 [PMID:1469686]
ChEMBL Inhibitory activity against acetylcholinesterase B 7.1 pIC50 80.3 nM IC50 J Med Chem (1995) 38: 4821-4829 [PMID:7490731]
ChEMBL Inhibition of AChE in Swiss Webster mouse cerebral homogenate using acetylthiocholine iodide as substrate preincubated for 10 mins followed substrate addition measured after 10 mins by Ellman's method B 7.46 pIC50 34.3 nM IC50 Bioorg Med Chem (2018) 26: 5566-5577 [PMID:30340901]
ChEMBL Inhibition of mouse brain AChE B 7.47 pIC50 34 nM IC50 RSC Med Chem (2021) 12: 2001-2015 [PMID:35028560]
ChEMBL Inhibition of AChE in Swiss mouse brain using acetylthiocholine iodide as substrate incubated for 10 mins followed by substrate addition and measured after 10 mins B 7.52 pIC50 30 nM IC50 Medchemcomm (2019) 10: 2089-2101 [PMID:32904099]
acetylcholinesterase (Yt blood group)/Acetylcholinesterase in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3199] [GtoPdb: 2465] [UniProtKB: P37136]
ChEMBL Inhibition of rat brain Acetylcholinesterase using acetylthiocholine as substrate in presence of BChE inhibitor ethopropazine B 6.22 pIC50 600 nM IC50 J Med Chem (2020) 63: 11420-11435 [PMID:32539387]
ChEMBL Inhibitory concentration against Acetylcholinesterase in rat brain B 6.23 pIC50 590 nM IC50 J Med Chem (2004) 47: 3463-3482 [PMID:15214773]
ChEMBL Inhibition of rat brain Acetylcholinesterase using acetylthiocholine as substrate in presence of BChE inhibitor ethopropazine by spectrophotometric method B 6.23 pIC50 590 nM IC50 Bioorg Med Chem (2019) 27: 895-930 [PMID:30744931]
ChEMBL Concentration that causes 50% inhibition of Acetylcholinesterase (AChE) using rat cortex homogenate and ethopropazine B 6.48 pIC50 333 nM IC50 J Med Chem (2002) 45: 2277-2282 [PMID:12014965]
ChEMBL Inhibitory activity against acetylcholinesterase in rat striatal preparation B 6.49 pIC50 320 nM IC50 J Med Chem (1996) 39: 570-581 [PMID:8558529]
ChEMBL In vitro inhibition against acetylcholinesterase in rat striata. B 6.5 pIC50 319 nM IC50 J Med Chem (1989) 32: 1805-1813 [PMID:2754707]
ChEMBL In vitro inhibitory activity against acetylcholinesterase using rat striatal preparations B 6.51 pIC50 310 nM IC50 J Med Chem (1988) 31: 1278-1279 [PMID:3385720]
ChEMBL Inhibition of acetylcholinesterase (AChE) B 6.57 pIC50 270.9 nM IC50 J Med Chem (1994) 37: 2292-2299 [PMID:8057278]
ChEMBL Inhibition of AChE in Sprague-Dawley rat cortices using acetylthiocholine iodide as substrate by Ellman's method B 6.6 pIC50 249 nM IC50 Bioorg Med Chem (2013) 21: 676-683 [PMID:23273608]
ChEMBL Inhibition of rat cortex AChE using acetylthiocholine iodide as substrate by Ellman's method B 6.63 pIC50 237 nM IC50 Eur J Med Chem (2021) 226: 113827-113827 [PMID:34530383]
ChEMBL Inhibition of AChE in rat cortex using acetylthiocholine iodide as substrate preincubated with enzyme for 10 mins prior to substrate addition by Ellman's colorimetric method B 6.64 pIC50 230 nM IC50 Bioorg Med Chem (2013) 21: 1064-1073 [PMID:23380475]
ChEMBL Inhibition of acetylcholinesterase B 6.64 pIC50 230 nM IC50 Bioorg Med Chem Lett (1992) 2: 865-870
ChEMBL Inhibition of rat cortex AChE B 6.65 pIC50 223 nM IC50 J Med Chem (2008) 51: 3588-3598 [PMID:18517184]
ChEMBL Inhibitory concentration against rat cortex Acetylcholinesterase B 6.65 pIC50 223 nM IC50 Bioorg Med Chem Lett (2004) 14: 4639-4642 [PMID:15324879]
ChEMBL Inhibition of rat brain AChE B 6.65 pIC50 223 nM IC50 J Med Chem (2006) 49: 5491-5500 [PMID:16942022]
ChEMBL Inhibitory potency against acetylcholinesterase (AChE) of rat cortex homogenate with ethopropazine as BChE inhibitor B 6.65 pIC50 223 nM IC50 Bioorg Med Chem Lett (1999) 9: 2335-2338 [PMID:10476864]
ChEMBL Inhibition of rat brain acetylcholine esterase in presence of acetylcholine substrate by chemiluminescent assay B 6.7 pIC50 200 nM IC50 Eur J Med Chem (2008) 43: 657-661 [PMID:17624631]
ChEMBL Inhibitory activity against acetylcholinesterase in rat brain B 6.7 pIC50 200 nM IC50 Bioorg Med Chem Lett (1996) 6: 737-742
ChEMBL Compound was tested in vitro for inhibitory activity against Acetylcholinesterase in rat cortex B 6.7 pIC50 200 nM IC50 Bioorg Med Chem Lett (1997) 7: 2599-2602
ChEMBL Inhibition of Sprague-Dawley rat acetylcholinesterase using acetylthiocholine iodide as substrate measured at 30 secs for 5 mins by Ellman's method B 6.77 pIC50 170 nM IC50 Bioorg Med Chem Lett (2020) 30: 127498-127498 [PMID:32818604]
ChEMBL Inhibitory activity against rat brain total Acetylcholinesterase (AChE) was determined using Ellman's method B 6.8 pIC50 160 nM IC50 J Med Chem (2003) 46: 1144-1152 [PMID:12646025]
ChEMBL Inhibition of rat cortex acetylcholinesterase using acetylthiocholine iodide as substrate incubated for 20 mins by Ellman's method B 6.88 pIC50 131 nM IC50 Bioorg Med Chem (2019) 27: 895-930 [PMID:30744931]
ChEMBL Inhibition of rat cortex AChE using acetylthiocholine iodide as substrate after 20 mins by by Ellman's method B 6.89 pIC50 130 nM IC50 Bioorg Med Chem (2018) 26: 3117-3125 [PMID:29729987]
ChEMBL Inhibition of Wistar rat brain AChE using acetylthiochloline iodide as substrate after 30 mins by Ellman's method B 6.94 pIC50 114.32 nM IC50 Eur J Med Chem (2016) 121: 758-772 [PMID:27392529]
ChEMBL Inhibition against acetylcholinesterase (AChE) B 6.96 pIC50 110 nM IC50 J Med Chem (1994) 37: 689-695 [PMID:8126709]
ChEMBL Inhibition of rat cortex homogenate acetylcholinesterase by spectrophotometric method B 7.03 pIC50 93 nM IC50 Bioorg Med Chem (2020) 28: 115820-115820 [PMID:33120080]
ChEMBL Inhibition of AChE from rat cortex by Ellman assay B 7.06 pIC50 88 nM IC50 Eur J Med Chem (2010) 45: 526-535 [PMID:19954865]
ChEMBL Inhibitory concentration in vitro and ex vivo for anti-AChE activity in rat brain B 7.09 pIC50 80.6 nM IC50 Bioorg Med Chem Lett (1992) 2: 871-876
ChEMBL In vitro inhibition of acetylcholinesterase, isolated from rat brain. B 7.11 pIC50 78 nM IC50 J Med Chem (1997) 40: 3516-3523 [PMID:9357518]
ChEMBL In vitro inhibitory effect on rat Acetylcholinesterase B 7.2 pIC50 63 nM IC50 J Med Chem (1995) 38: 2969-2973 [PMID:7636858]
ChEMBL Inhibition of Acetylcholinesterase in rat red blood cell B 7.34 pIC50 46 nM IC50 J Med Chem (1996) 39: 3014-3018 [PMID:8709135]
carboxylesterase 1/Acyl coenzyme A:cholesterol acyltransferase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2265] [GtoPdb: 2592] [UniProtKB: P23141]
ChEMBL Inhibition of human carboxylesterase 1 using o-nitrophenylacetate as substrate by spectrophotometry analysis B 4 pIC50 >100000 nM IC50 Bioorg Med Chem (2016) 24: 1050-1062 [PMID:26827140]
α1A-adrenoceptor/Alpha-1a adrenergic receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL319] [GtoPdb: 22] [UniProtKB: P43140]
ChEMBL DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin) B 5.95 pKi 1113 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin) B 5.56 pIC50 2749 nM IC50 DrugMatrix in vitro pharmacology data
Alpha-ketoglutarate-dependent dioxygenase FTO in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2331065] [UniProtKB: Q9C0B1]
ChEMBL Inhibition of FTO (unknown origin) demethylation activity using m6A7-Broccoli RNA as substrate incubated for 3 mins under shaking condition and measured after 2 hrs by fluorescence based analysis B 5.77 pIC50 1710 nM IC50 J Med Chem (2021) 64: 16974-17003 [PMID:34792334]
Amyloid-beta A4 protein in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2487] [UniProtKB: P05067]
ChEMBL Inhibition of self-mediated amyloid beta (1 to 42) (unknown origin) aggregation after 24 hrs by thioflavin T fluorescence assay B 7.91 pIC50 12.21 nM IC50 Eur J Med Chem (2016) 116: 200-209 [PMID:27061983]
butyrylcholinesterase/Butyrylcholinesterase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1914] [GtoPdb: 2471] [UniProtKB: P06276]
GtoPdb - - 7.2 pKi 70 nM Ki J Med Chem (2008) 51: 3154-70 [PMID:18479118]
ChEMBL Inhibition of human recombinant BChE using acetylthiocholine as substrate B 8.06 pKi 8.72 nM Ki Bioorg Med Chem (2012) 20: 6739-6750 [PMID:23041347]
ChEMBL Inhibition of human BChE assessed as acetylthiocholine hydrolysis B 8.06 pKi 8.7 nM Ki Bioorg Med Chem (2014) 22: 4784-4791 [PMID:25088549]
ChEMBL Inhibition of human BuChE B 8.15 pKi 7 nM Ki J Med Chem (2006) 49: 3421-3425 [PMID:16722663]
ChEMBL Inhibition of human recombinant BChE B 8.15 pKi 7 nM Ki Bioorg Med Chem Lett (2008) 18: 5213-5216 [PMID:18786825]
ChEMBL Inhibition of human recombinant BuChE B 8.15 pKi 7 nM Ki J Med Chem (2008) 51: 3154-3170 [PMID:18479118]
ChEMBL Inhibition of human serum BChE using butyrylthiocholine iodide as substrate preincubated with compound for 20 mins followed by substrate addition and measured after 240 sec by spectrophotometer based Ellman's method B 4.46 pIC50 35000 nM IC50 Bioorg Med Chem (2023) 91: 117419-117419 [PMID:37487339]
ChEMBL Inhibition of Butyrylcholinesterase (BChE) of human erythrocytes [-log IC50 (uM)] B 6.44 pIC50 363.08 nM IC50 J Med Chem (1998) 41: 4186-4189 [PMID:9784091]
ChEMBL Inhibition of human BChE using butyrylthiocholine iodide as substrate preincubated for 20 mins followed by substrate addition and measured for 3 mins by spectrophotometry based Ellman's method B 6.8 pIC50 158.49 nM IC50 J Med Chem (2019) 62: 9078-9102 [PMID:31609608]
ChEMBL Inhibition of human Cholinesterase B 7.02 pIC50 95 nM IC50 Bioorg Med Chem (2019) 27: 895-930 [PMID:30744931]
ChEMBL Concentration that causes 50% inhibition of Butyrylcholinesterase (BChE) using human serum and BW284c51 B 7.05 pIC50 89 nM IC50 J Med Chem (2002) 45: 2277-2282 [PMID:12014965]
ChEMBL Inhibition of human plasmatic BuChE using butyrylthiocholine iodide as substrate preincubated for 5 mins followed by substrate addition measured at 2 mins time interval by Ellman's method B 7.06 pIC50 88.1 nM IC50 Eur J Med Chem (2018) 150: 292-306 [PMID:29533874]
ChEMBL Inhibition of human BuChE using butyrylthiocholine iodide as substrate peincubated for 5 mins followed by substrate addition by DTNB-reagent based Ellman's method B 7.07 pIC50 85 nM IC50 Eur J Med Chem (2021) 210: 113059-113059 [PMID:33310288]
ChEMBL Inhibition of human plasma BuChE using butyrylthiocholine as substrate preincubated for 5 mins followed by substrate addition by Ellman's method B 7.09 pIC50 82 nM IC50 Eur J Med Chem (2022) 231: 114152-114152 [PMID:35101650]
ChEMBL Inhibition of human plasmatic BuChE assessed as reduction in cholinesterase activity by Ellman's method B 7.1 pIC50 80 nM IC50 Eur J Med Chem (2021) 219: 113434-113434 [PMID:33892271]
ChEMBL Inhibition of recombinant human BuChE using butyrylthiocholine as substrate by Ellman's method B 7.1 pIC50 80 nM IC50 Bioorg Med Chem Lett (2021) 43: 128100-128100 [PMID:33984470]
ChEMBL Inhibition of human plasmatic BChE using butyrylthiocholine as substrate preincubated for 5 mins followed by substrate addition measured every 2 mins by Ellman's method B 7.1 pIC50 80 nM IC50 J Med Chem (2015) 58: 8985-9003 [PMID:26503905]
ChEMBL Inhibition of human recombinant BChE using butyrylthiocholine iodide as substrate preincubated for 5 mins followed by substrate addition and measured over 2 mins by UV-Vis spectrophotometric analysis based Ellman's method B 7.1 pIC50 80 nM IC50 Eur J Med Chem (2019) 168: 491-514 [PMID:30851693]
ChEMBL Inhibition of human recombinant serum BuchE using butyrylthiocholine iodide as substrate by Ellman method B 7.14 pIC50 73 nM IC50 Bioorg Med Chem Lett (2015) 25: 830-833 [PMID:25597004]
ChEMBL Inhibition of recombinant human serum BChE using butyrylthiocholine iodide as substrate by spectroscopic Ellmans method B 7.14 pIC50 73 nM IC50 Eur J Med Chem (2011) 46: 2193-2205 [PMID:21435752]
ChEMBL Inhibition of human erythrocyte BuChE using S-butyrylthiocholine iodide as substrate preincubated for 20 mins followed by substrate addition and measured every 30 secs for 1 hr by Ellman's method B 7.15 pIC50 70 nM IC50 J Nat Prod (2019) 82: 3221-3226 [PMID:31736307]
ChEMBL Inhibition of BChE (unknown origin) incubated for 10 mins by Ellman's method B 7.18 pIC50 66 nM IC50 Bioorg Med Chem Lett (2019) 29: 126754-126754 [PMID:31708262]
ChEMBL Inhibition of human serum BuChE by Ellman's method B 7.24 pIC50 58 nM IC50 J Med Chem (2007) 50: 5311-5323 [PMID:17902635]
ChEMBL Inhibition of human recombinant BuChE by Ellman's assay B 7.24 pIC50 58 nM IC50 Bioorg Med Chem Lett (2013) 23: 6254-6258 [PMID:24140444]
ChEMBL Inhibition of human BChE using butyrylthiocholine iodide as substrate incubated for 20 mins followed by substrate addition by Ellman's method B 7.27 pIC50 54 nM IC50 J Med Chem (2021) 64: 9302-9320 [PMID:34152756]
ChEMBL Inhibitory concentration against butyrylcholinesterase from human serum B 7.27 pIC50 53.7 nM IC50 J Med Chem (2003) 46: 954-966 [PMID:12620072]
ChEMBL Inhibition of human BChE using butyrylthiocholineiodide as substrate preincubated for 20 mins followed by substrate addition and measured every 30 sec for 3 mins by DTNB-based UV analysis B 7.3 pIC50 50.12 nM IC50 RSC Med Chem (2022) 13: 944-954 [PMID:36092149]
ChEMBL Pseudo-irreversible inhibition of human BChE using butyrylthiocholine iodide as substrate incubated for 20 mins followed by substrate addition by Ellman's method based UV analysis B 7.3 pIC50 50.12 nM IC50 J Med Chem (2023) 66: 6414-6435 [PMID:37127287]
ChEMBL Inhibition of human BuChE using butyrylthiocholine iodide as substrate incubated for 10 mins followed by substrate addition by DTNB-reagent based Ellman's colorimetric assay B 7.3 pIC50 50.1 nM IC50 Eur J Med Chem (2022) 239: 114510-114510 [PMID:35728508]
ChEMBL Inhibition of BuChE (unknown origin) preincubated for 30 mins followed by substrate addition acetylthiocholineiodide measured after 40 mins by Ellman's method B 7.3 pIC50 50 nM IC50 Eur J Med Chem (2020) 200: 112415-112415 [PMID:32454229]
ChEMBL Inhibition of BuChE in human serum using butyrylthiocholine iodide as substrate measured every 30s for 5 mins by Ellman's spectrophotometric method B 7.3 pIC50 50 nM IC50 Eur J Med Chem (2014) 75: 21-30 [PMID:24508831]
ChEMBL Inhibition of human BChE using butyrylthiocholineiodide as substrate incubated for 10 mins by Ellman's method B 7.3 pIC50 50 nM IC50 Bioorg Med Chem (2021) 30: 115940-115940 [PMID:33340937]
ChEMBL Inhibition of human serum recombinant BChE using butyrylthiocholine iodide as substrate preincubated for 20 mins by Ellman's method B 7.3 pIC50 50 nM IC50 Eur J Med Chem (2011) 46: 4336-4343 [PMID:21798635]
ChEMBL Anticholinesterase activity against human plasma BChE B 7.33 pIC50 47 nM IC50 J Med Chem (2006) 49: 2174-2185 [PMID:16570913]
ChEMBL Ex vivo inhibition of human plasma Butyrylcholinesterase. B 7.33 pIC50 47 nM IC50 J Med Chem (2002) 45: 3684-3691 [PMID:12166941]
ChEMBL Inhibitory concentration against human plasma Butyrylcholinesterase B 7.33 pIC50 47 nM IC50 J Med Chem (2005) 48: 986-994 [PMID:15715468]
ChEMBL Inhibition of human BChE using butyrylthiocholineiodide as substrate preincubated for 20 mins followed by substrate addition and measured every 30 sec for 3 mins by DTNB-based UV analysis B 7.33 pIC50 46.8 nM IC50 RSC Med Chem (2022) 13: 944-954 [PMID:36092149]
ChEMBL Inhibition of human serum BChE using butyrylthiocholine iodide as substrate preincubated for 20 mins followed by substrate addition measured for 3 mins by Ellman's method B 7.34 pIC50 46 nM IC50 Eur J Med Chem (2017) 141: 197-210 [PMID:29031067]
ChEMBL Inhibition of human serum BuChE using butyrylthiocholine iodide as substrate by Ellman's method B 7.34 pIC50 46 nM IC50 Eur J Med Chem (2012) 52: 251-262 [PMID:22503231]
ChEMBL Inhibition of human serum BChE using butyrylthiocholine iodide as substrate preincubated for 20 mins followed by substrate addition measured after 5 mins by Ellman's method B 7.34 pIC50 46 nM IC50 Eur J Med Chem (2014) 73: 141-152 [PMID:24389509]
ChEMBL Inhibition of Butyrylcholinesterase B 7.34 pIC50 45.8 nM IC50 J Med Chem (2005) 48: 24-27 [PMID:15633997]
ChEMBL Inhibitory concentration against human recombinant butyrylcholinesterase B 7.34 pIC50 45.8 nM IC50 J Med Chem (2005) 48: 360-363 [PMID:15658850]
ChEMBL Inhibition of human serum BChE using butyrylthiocholine iodide as substrate preincubated for 20 mins followed by substrate addition by Ellman's method B 7.34 pIC50 45.8 nM IC50 J Med Chem (2021) 64: 4972-4990 [PMID:33829779]
ChEMBL Inhibition of human recombinant butyrylcholinesterase B 7.34 pIC50 45.8 nM IC50 J Med Chem (2007) 50: 4882-4897 [PMID:17850125]
ChEMBL Inhibition of human serum BChE using butyrylthiocholine iodide as substrate preincubated for 20 mins followed by substrate addition by Ellman's method B 7.34 pIC50 45.8 nM IC50 J Med Chem (2016) 59: 114-131 [PMID:26632651]
ChEMBL Inhibition of human serum BChE by Ellman's method B 7.34 pIC50 45.8 nM IC50 J Med Chem (2008) 51: 4381-4384 [PMID:18605718]
ChEMBL Inhibition of human serum recombinant BChE by Ellman's method B 7.34 pIC50 45.8 nM IC50 J Med Chem (2007) 50: 6446-6449 [PMID:18047264]
ChEMBL Inhibition of human recombinant BChE B 7.34 pIC50 45.71 nM IC50 J Med Chem (2004) 47: 6490-6498 [PMID:15588084]
ChEMBL Inhibition of human BuChE at 10 uM B 7.35 pIC50 45 nM IC50 Bioorg Med Chem Lett (2020) 30: 127609-127609 [PMID:33039562]
ChEMBL Pseudo-irreversible inhibition of human BChE using butyrylthiocholine iodide as substrate incubated for 20 mins followed by substrate addition by Ellman's method based UV analysis B 7.35 pIC50 45 nM IC50 J Med Chem (2023) 66: 6414-6435 [PMID:37127287]
ChEMBL Inhibition of recombinant human serum BChE using butyrylthiocholine as substrate pretreated for 20 mins followed by substrate addition by Ellman's method B 7.35 pIC50 44.2 nM IC50 Eur J Med Chem (2018) 155: 839-846 [PMID:29958119]
ChEMBL Inhibition of human serum BuChe by Ellman's method B 7.35 pIC50 44.2 nM IC50 Eur J Med Chem (2019) 181: 111550-111550 [PMID:31376562]
ChEMBL Inhibition of human BuchE B 7.36 pIC50 44 nM IC50 Bioorg Med Chem Lett (2020) 30: 127075-127075 [PMID:32165042]
ChEMBL Inhibition of human serum BChE B 7.36 pIC50 43.9 nM IC50 J Med Chem (2006) 49: 6833-6840 [PMID:17154513]
ChEMBL Inhibition of butyrylcholinesterase (BChE) in human serum B 7.36 pIC50 43.9 nM IC50 J Med Chem (2000) 43: 4657-4666 [PMID:11101357]
ChEMBL Inhibition of butyrylcholinesterase (BChE) activity in human serum B 7.36 pIC50 43.9 nM IC50 J Med Chem (1999) 42: 3227-3242 [PMID:10464010]
ChEMBL Inhibition of human BChE using butyrylthiocholine iodide as substrate incubated for 20 mins followed by substrate addition by Ellman's method B 7.37 pIC50 42.66 nM IC50 J Med Chem (2021) 64: 9302-9320 [PMID:34152756]
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 7.39 pIC50 41 nM IC50 Eur J Med Chem (2016) 123: 282-297 [PMID:27484514]
ChEMBL Inhibition of human BuChE in serum B 7.4 pIC50 40 nM IC50 J Med Chem (2009) 52: 7249-7257 [PMID:19856923]
ChEMBL Inhibition of human serum BChE by Ellman's reaction B 7.4 pIC50 40 nM IC50 J Med Chem (2010) 53: 4927-4937 [PMID:20545360]
ChEMBL Inhibition of human serum BChE by Ellman's method B 7.4 pIC50 40 nM IC50 J Med Chem (2012) 55: 1303-1317 [PMID:22243648]
ChEMBL Inhibition of human BuChE using butyrylthiocholine iodide as substrate incubated for 10 mins prior to substrate addition measured after 15 mins by Ellman's method B 7.4 pIC50 40 nM IC50 Eur J Med Chem (2012) 54: 750-763 [PMID:22795665]
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 7.4 pIC50 40 nM IC50 Bioorg Med Chem Lett (2013) 23: 4336-4341 [PMID:23791077]
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 7.4 pIC50 40 nM IC50 Eur J Med Chem (2017) 139: 773-791 [PMID:28863358]
ChEMBL Inhibition of human BuChE B 7.4 pIC50 40 nM IC50 J Med Chem (2006) 49: 459-462 [PMID:16420031]
ChEMBL Inhibition of human serum BChE using butyrylthiocholine iodide as substrate pre-incubated for 20 mins before substrate addition and measured for 180 secs by spectrophotometry based Ellman's method B 7.4 pIC50 40 nM IC50 Eur J Med Chem (2019) 167: 161-186 [PMID:30771604]
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 7.4 pIC50 40 nM IC50 Medchemcomm (2015) 6: 1930-1941
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 7.4 pIC50 40 nM IC50 Eur J Med Chem (2018) 158: 781-800 [PMID:30245401]
ChEMBL Inhibition of human serum BuChE using butyrylthiocholine iodide as substrate preincubated for 20 mins followed by substrate addition and measured for 5 mins by Ellman's assay B 7.4 pIC50 40 nM IC50 Medchemcomm (2017) 8: 1307-1317 [PMID:30108842]
ChEMBL Inhibition of human BuChE using butyrylthiocholine iodide as substrate incubated for 20 mins followed by substrate addition measured after 2 mins by Ellman's method B 7.4 pIC50 40 nM IC50 ACS Med Chem Lett (2018) 9: 171-176 [PMID:29541355]
ChEMBL Inhibition of human BuChE using butyrylthiocholine iodide as substrate preincubated with enzyme for 1 min followed by substrate addition and measured after 10 mins by Ellman's method B 7.4 pIC50 39.6 nM IC50 Eur J Med Chem (2020) 207: 112751-112751 [PMID:32950908]
ChEMBL Inhibition of human serum BChE by Ellman's method B 7.44 pIC50 36 nM IC50 J Med Chem (2009) 52: 2724-2732 [PMID:19374444]
ChEMBL Inhibition of human serum BuChE B 7.44 pIC50 36 nM IC50 J Med Chem (2006) 49: 7607-7610 [PMID:17181144]
ChEMBL Inhibition of human serum BuChE using butyrylthiocholine iodide as substrate by Ellman's methods B 7.44 pIC50 36 nM IC50 Eur J Med Chem (2019) 166: 381-389 [PMID:30739821]
ChEMBL Inhibition of BuChE (unknown origin) B 7.44 pIC50 36 nM IC50 Eur J Med Chem (2019) 166: 381-389 [PMID:30739821]
ChEMBL Inhibition of human serum BuchE using butyrylthiocholine iodide as substrate preincubated for 10 mins measured after 15 mins of substrate addition by Ellman's method B 7.44 pIC50 36 nM IC50 J Med Chem (2011) 54: 8251-8270 [PMID:22023459]
ChEMBL Inhibition of human serum BuChE by Ellman's method B 7.44 pIC50 36 nM IC50 Bioorg Med Chem (2008) 16: 7759-7769 [PMID:18640842]
ChEMBL Inhibition of recombinant human BChE using butyrylthiocholine iodide as substrate preincubated for 15 mins followed by substrate addition by Ellman's method B 7.45 pIC50 35.2 nM IC50 J Med Chem (2020) 63: 9360-9390 [PMID:32706255]
ChEMBL Inhibition of human serum BCHE using butyrylthiocholine iodide as substrate preincubated for 5 mins followed by DTNB addition for 5 mins and subsequent addition of substrate measured after 3 mins by Ellman's method B 7.46 pIC50 34.4 nM IC50 Eur J Med Chem (2018) 148: 238-254 [PMID:29466774]
ChEMBL Inhibition of human BuChE by spectrophotometric based Ellman's method B 7.47 pIC50 34 nM IC50 Eur J Med Chem (2020) 207: 112743-112743 [PMID:32882609]
ChEMBL Inhibition of human BuchE using butyrylthiocholine as substrate preincubated for 5 mins followed by substrate addition and measured after 5 mins by Ellman's method B 7.47 pIC50 34 nM IC50 Eur J Med Chem (2021) 218: 113397-113397 [PMID:33838585]
ChEMBL Inhibition of human BChE using butyrylthiocholine iodide as substrate preincubated followed by substrate addition by Ellman's method B 7.47 pIC50 34 nM IC50 Bioorg Med Chem (2016) 24: 1050-1062 [PMID:26827140]
ChEMBL Inhibition of BuChE in human plasma using BTC as substrate preincubated with enzyme for 5 mins followed by substrate addition for 5 mins by Ellman's method B 7.47 pIC50 33.6 nM IC50 Eur J Med Chem (2021) 225: 113792-113792 [PMID:34530376]
ChEMBL Inhibition of human serum BChE using BTCh as substrate preincubated for 20 mins followed by substrate addition and measured for 3 mins by Ellman's method B 7.47 pIC50 33.5 nM IC50 Eur J Med Chem (2019) 168: 58-77 [PMID:30798053]
ChEMBL Inhibition of human BChE using acetylthiocholine iodide or butyrylthiocholine iodide as substrate preincubated for 5 mins followed by substrate addition by Ellman's method B 7.52 pIC50 30.11 nM IC50 J Med Chem (2022) 65: 11365-11387 [PMID:35969197]
ChEMBL Inhibition of human BChE by Ellman's method B 7.52 pIC50 30 nM IC50 Bioorg Med Chem (2007) 15: 6596-6607 [PMID:17681794]
ChEMBL Inhibition of human serum BCHE preincubated for 6 mins followed by addition of S-butyrylcholine iodide as substrate by Ellman's method B 7.52 pIC50 30 nM IC50 Bioorg Med Chem (2016) 24: 4324-4338 [PMID:27460699]
ChEMBL Inhibition of human recombinant 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 7.52 pIC50 30 nM IC50 Eur J Med Chem (2023) 249: 115135-115135 [PMID:36696766]
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 7.54 pIC50 29 nM IC50 Eur J Med Chem (2022) 242: 114630-114630 [PMID:35987018]
ChEMBL Inhibitory concentration against butyrylcholinesterase B 7.57 pIC50 27 nM IC50 J Med Chem (2005) 48: 3564-3575 [PMID:15887964]
ChEMBL Inhibition of human BuChE using S-butyrylthiocholine iodide as substrate incubated for 6 mins prior to substrate addition measured after 60 to 180 secs by Ellman method B 7.6 pIC50 25.33 nM IC50 Eur J Med Chem (2015) 95: 153-165 [PMID:25812965]
ChEMBL Inhibition of BuChE in human erythrocyte hemo-lyzates pre-incubated for 5 mins before addition of butyrylthiocholine iodide substrate by Ellman's method B 7.6 pIC50 25 nM IC50 J Med Chem (2016) 59: 9967-9973 [PMID:27736061]
ChEMBL In vitro inhibition of Butyrylcholinesterase from human plasma. B 7.6 pIC50 25 nM IC50 J Med Chem (1997) 40: 3516-3523 [PMID:9357518]
ChEMBL Inhibition of human serum BChE using butyrylthiocholine iodide as substrate preincubated for 20 mins prior substrate addition measured after 5 mins by spectrophotometry B 7.61 pIC50 24.5 nM IC50 J Med Chem (2012) 55: 661-669 [PMID:22185619]
ChEMBL Inhibition of human serum BChE by Ellman's assay B 7.62 pIC50 24 nM IC50 J Med Chem (2008) 51: 3588-3598 [PMID:18517184]
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 7.62 pIC50 24 nM IC50 RSC Med Chem (2022) 13: 873-883 [PMID:35923722]
ChEMBL Inhibition of human serum BChE B 7.62 pIC50 24 nM IC50 J Med Chem (2005) 48: 7223-7233 [PMID:16279781]
ChEMBL Inhibition of human serum BuChE using S-butyrylthiocholine iodide as substrate preincubated for 6 mins before substrate addition by Ellman's method B 7.63 pIC50 23.2 nM IC50 Eur J Med Chem (2015) 93: 42-50 [PMID:25656088]
ChEMBL Inhibition of human BChE using butyrylthiocholine iodide as substrate preincubated for 5 mins followed by substrate addition and measured for 1 min by Ellman's assay B 7.63 pIC50 23.2 nM IC50 Eur J Med Chem (2018) 156: 598-617 [PMID:30031971]
ChEMBL The compound was evaluated for the inhibition human of Butyrylcholinesterase I B 7.64 pIC50 23 nM IC50 J Med Chem (1992) 35: 1102-1108 [PMID:1552502]
ChEMBL Inhibition of human BuChE pre-incubated for 5 mins before butylthiocholine substrate addition by Ellman's method B 7.64 pIC50 23 nM IC50 J Med Chem (2014) 57: 7073-7084 [PMID:25089370]
ChEMBL Inhibition of human recombinant BuChe using butyrylthiocholine as substrate preincubated for 5 mins followed by substrate addition measured for 1 min by Ellman's method B 7.64 pIC50 23 nM IC50 Bioorg Med Chem (2017) 25: 633-645 [PMID:27908752]
ChEMBL Inhibition of human BChE after 20 mins using butyrylthiocholine iodide as a substrate by Ellman's assay B 7.64 pIC50 23 nM IC50 J Med Chem (2011) 54: 2627-2645 [PMID:21417225]
ChEMBL Inhibition of human plasmatic BChE after 5 mins by Ellman method B 7.64 pIC50 23 nM IC50 J Med Chem (2014) 57: 8576-8589 [PMID:25259726]
ChEMBL In vitro Butyrylcholinesterase inhibitory activity to determine its ability to reverse the cholinergic deficit characteristic of AD B 7.64 pIC50 23 nM IC50 J Med Chem (1992) 35: 3141-3147 [PMID:1507203]
ChEMBL Inhibition of human plasmatic BChE after 5 mins using spectrophotometer by Ellman's method B 7.64 pIC50 23 nM IC50 Bioorg Med Chem Lett (2011) 21: 6563-6566 [PMID:21920739]
ChEMBL Inhibition of human plasmatic BChE after 5 mins B 7.64 pIC50 23 nM IC50 Bioorg Med Chem Lett (2010) 20: 6093-6095 [PMID:20817518]
ChEMBL Inhibition of human plasma BuChE using S-butyrylthiocholine iodide as substrate after 30 mins by Ellman's method B 7.64 pIC50 22.73 nM IC50 Eur J Med Chem (2016) 121: 758-772 [PMID:27392529]
ChEMBL Inhibition of butyrylcholinesterase from human serum B 7.68 pIC50 21 nM IC50 J Med Chem (2001) 44: 2707-2718 [PMID:11495583]
ChEMBL Inhibitory concentration against Butyrylcholinesterase (BuChE) from human serum B 7.68 pIC50 21 nM IC50 J Med Chem (1999) 42: 730-741 [PMID:10052979]
ChEMBL Inhibition of human serum BuChE using butyrylthiocholine chloride as substrate preincubated for 15 mins followed by substrate addition and measured at 1 min time interval by Ellman's method relative to control B 7.7 pIC50 20 nM IC50 Eur J Med Chem (2019) 167: 133-145 [PMID:30771601]
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 7.7 pIC50 20 nM IC50 Eur J Med Chem (2017) 130: 139-153 [PMID:28242549]
ChEMBL Inhibition of butyrylcholinesterase (unknown origin) B 7.7 pIC50 20 nM IC50 Bioorg Med Chem (2013) 21: 146-152 [PMID:23199476]
ChEMBL Inhibition of human BuChE using butyrylthiocholine iodide as substrate incubated for 20 mins prior to substrate addition measured for 1 hr by Ellman's method B 7.72 pIC50 19 nM IC50 Bioorg Med Chem (2013) 21: 4218-4224 [PMID:23719283]
ChEMBL Inhibition of human BuChE using butyrylthiocholine iodide as substrate preincubated for 5 mins followed by substrate addition measured for 1 min by Ellman's method B 7.85 pIC50 14 nM IC50 Eur J Med Chem (2017) 128: 237-246 [PMID:28189905]
ChEMBL Inhibition of human BChE B 7.9 pIC50 12.59 nM IC50 J Med Chem (2019) 62: 9078-9102 [PMID:31609608]
ChEMBL Inhibition of BChE B 7.92 pIC50 12 nM IC50 Bioorg Med Chem Lett (2011) 21: 2687-2691 [PMID:21216144]
ChEMBL Inhibition of human recombinant BChE using butyrylthiocholine iodide as substrate after 5 mins by Ellman's method B 7.92 pIC50 12 nM IC50 Bioorg Med Chem (2015) 23: 4442-4452 [PMID:26116179]
ChEMBL Inhibition of human recombinant BChE using butyrylthiocholine iodide as substrate incubated for 5 mins followed by substrate addition measured for 1 min by Ellman's method B 7.92 pIC50 12 nM IC50 Eur J Med Chem (2016) 123: 298-308 [PMID:27484515]
ChEMBL Inhibition of recombinant human BChE by Ellman method B 7.92 pIC50 12 nM IC50 J Med Chem (2014) 57: 8167-8179 [PMID:25226236]
ChEMBL Inhibition of human BChE pre-incubated for 6 mins before ATCI substrate addition and measured after 12 mins by DTNB reagent dependent UV-Vis spectrophotometry based Ellman's method B 7.97 pIC50 10.8 nM IC50 Eur J Med Chem (2017) 140: 118-127 [PMID:28923380]
ChEMBL Inhibitory concentration against Butyrylcholinesterase activity B 8 pIC50 10 nM IC50 Bioorg Med Chem Lett (2005) 15: 353-356 [PMID:15603953]
ChEMBL Inhibition of human BChE using BTC iodide as substrate preincubated for 4.5 mins followed by substrate addition measured after 2.5 mins by Ellman's method B 8 pIC50 10 nM IC50 J Med Chem (2018) 61: 1646-1663 [PMID:29400965]
ChEMBL Inhibition of human BChE using BTC iodide as substrate preincubated for 4.5 mins followed by substrate addition measured after 2.5 mins by Ellman's method B 8.04 pIC50 9.1 nM IC50 J Med Chem (2018) 61: 1646-1663 [PMID:29400965]
ChEMBL Inhibition of BuchE (unknown origin) B 8.1 pIC50 8 nM IC50 Bioorg Med Chem Lett (2022) 61: 128602-128602 [PMID:35124202]
ChEMBL Concentration required to inhibit 50% of Butyrylcholinesterase obtained from human serum was determined in vitro B 8.22 pIC50 6 nM IC50 J Med Chem (1995) 38: 1084-1089 [PMID:7707311]
ChEMBL In vitro inhibition of Butyrylcholinesterase from human erythrocytes B 8.22 pIC50 6 nM IC50 J Med Chem (1995) 38: 2802-2808 [PMID:7636841]
ChEMBL Inhibition of BuChE (unknown origin) using acetylthiocholine iodide as substrate incubated for 5 mins by Ellman's method B 8.23 pIC50 5.9 nM IC50 Eur J Med Chem (2022) 227: 113964-113964 [PMID:34743062]
ChEMBL Inhibition of BuChE by Ellman's assay B 8.29 pIC50 5.1 nM IC50 J Med Chem (2008) 51: 713-716 [PMID:18232655]
ChEMBL Inhibition of human BChE using butyrylthiocholine iodide as substrate measured for 3 mins by Ellman's method B 8.52 pIC50 3 nM IC50 Eur J Med Chem (2022) 243: 114729-114729 [PMID:36084535]
ChEMBL In vitro inhibitory activity against Butyrylcholinesterase (BChE) in human serum B 9.05 pIC50 0.9 nM IC50 Bioorg Med Chem Lett (2003) 13: 2389-2391 [PMID:12824041]
ChEMBL Inhibition of BChE by Ellman's method B 10.57 pIC50 0.03 nM IC50 Eur J Med Chem (2011) 46: 3250-3257 [PMID:21570751]
Butyrylcholinesterase in Equus caballus (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5077] [UniProtKB: Q9N1N9]
ChEMBL Inhibition of Equine Butyrylcholinesterase B 8.15 pKi 7 nM Ki J Med Chem (2003) 46: 1-4 [PMID:12502352]
ChEMBL Inhibition of equine (Eq) Butyrylcholinesterase B 8.15 pKi 7 nM Ki Bioorg Med Chem Lett (2001) 11: 1779-1782 [PMID:11425559]
ChEMBL Dissociation constant for inhibition of equine Butyrylcholinesterase (BuChE) B 8.15 pKi 7 nM Ki J Med Chem (2005) 48: 1919-1929 [PMID:15771436]
ChEMBL Inhibition of equine BChE after 15 mins by Ellman's method using acetylcholine as substrate B 7.39 pIC50 41 nM IC50 Bioorg Med Chem Lett (2010) 20: 6649-6652 [PMID:20880702]
ChEMBL Inhibition of equine BChE by Ellman's method B 7.57 pIC50 27.08 nM IC50 Bioorg Med Chem (2011) 19: 763-770 [PMID:21211982]
ChEMBL Inhibition of equine BChE preincubated for 15 mins by Ellman's method B 7.82 pIC50 15.2 nM IC50 Eur J Med Chem (2014) 87: 429-439 [PMID:25282266]
ChEMBL Inhibition of BuChE from horse serum B 8 pIC50 10 nM IC50 J Med Chem (2006) 49: 459-462 [PMID:16420031]
ChEMBL Compound was evaluated for the in vitro inhibition of the Butyrylcholinesterase from horse serum B 8.22 pIC50 6 nM IC50 J Med Chem (1994) 37: 2721-2734 [PMID:8064800]
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 8.28 pIC50 5.2 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 equine serum BChE using butyrylthiocholine iodide as substrate after 15 mins by Ellman's method B 8.28 pIC50 5.2 nM IC50 Eur J Med Chem (2012) 52: 251-262 [PMID:22503231]
ChEMBL Inhibition of (BChE) Butyrylcholinesterase of horse serum B 8.29 pIC50 5.17 nM IC50 Bioorg Med Chem Lett (1992) 2: 861-864
ChEMBL Inhibition of equine BChE by Ellman's assay B 8.29 pIC50 5.1 nM IC50 Bioorg Med Chem Lett (2008) 18: 2905-2909 [PMID:18406135]
ChEMBL Inhibition of BuChE from equine serum B 8.29 pIC50 5.1 nM IC50 J Med Chem (2008) 51: 7666-7669 [PMID:19053746]
butyrylcholinesterase/Butyrylcholinesterase in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2528] [GtoPdb: 2471] [UniProtKB: Q03311]
ChEMBL Inhibition of BuChE in Swiss Webster mouse whole blood serum using butyrylthiocholine iodide as substrate preincubated for 10 mins followed substrate addition measured after 10 mins by Ellman's method B 7.2 pIC50 62.5 nM IC50 Bioorg Med Chem (2018) 26: 5566-5577 [PMID:30340901]
ChEMBL Inhibition of mouse serum BuChE B 7.21 pIC50 62 nM IC50 RSC Med Chem (2021) 12: 2001-2015 [PMID:35028560]
ChEMBL Inhibition of BuChE in Swiss mouse serum using butyrylthiocholine iodide as substrate incubated for 10 mins followed by substrate addition and measured after 10 mins B 7.22 pIC50 60 nM IC50 Medchemcomm (2019) 10: 2089-2101 [PMID:32904099]
Butyrylcholinesterase in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3403] [UniProtKB: Q9JKC1]
ChEMBL Inhibitory concentration against rat brain butyrylcholinesterase (BuChE) was determined using Ellman's method B 6.62 pIC50 240 nM IC50 J Med Chem (2003) 46: 1144-1152 [PMID:12646025]
ChEMBL Inhibition of rat serum BChE using butyrylthiocholine iodide as substrate by Ellman's method B 6.83 pIC50 147 nM IC50 Eur J Med Chem (2021) 226: 113827-113827 [PMID:34530383]
ChEMBL Inhibition of rat serum BuChE B 7.04 pIC50 92 nM IC50 J Med Chem (2006) 49: 5491-5500 [PMID:16942022]
ChEMBL Inhibitory potency against rat serum Butyrylcholinesterase with BW284c51 as AChE inhibitor B 7.04 pIC50 92 nM IC50 Bioorg Med Chem Lett (1999) 9: 2335-2338 [PMID:10476864]
ChEMBL Inhibitory concentration against rat serum Butyrylcholinesterase B 7.04 pIC50 92 nM IC50 Bioorg Med Chem Lett (2004) 14: 4639-4642 [PMID:15324879]
ChEMBL Inhibition of rat serum BChE B 7.04 pIC50 92 nM IC50 J Med Chem (2008) 51: 3588-3598 [PMID:18517184]
ChEMBL Inhibition of rat serum BChE using butyrylthiocholine iodide as substrate after 20 mins by by Ellman's method B 7.1 pIC50 80 nM IC50 Bioorg Med Chem (2018) 26: 3117-3125 [PMID:29729987]
ChEMBL Inhibition of rat cortex homogenate BuChE by spectrophotometric method B 7.13 pIC50 74 nM IC50 Bioorg Med Chem (2020) 28: 115820-115820 [PMID:33120080]
ChEMBL Butyrylcholinesterase B 7.14 pIC50 73 nM IC50 J Med Chem (1995) 38: 4821-4829 [PMID:7490731]
ChEMBL In vitro inhibitory concentration against Butyrylcholinesterase obtained from rat plasma B 7.14 pIC50 73 nM IC50 J Med Chem (1992) 35: 4542-4548 [PMID:1469686]
ChEMBL Inhibitory concentration was determined in in vitro for Butyrylcholinesterase in rat plasma B 7.14 pIC50 73 nM IC50 Bioorg Med Chem Lett (1992) 2: 871-876
ChEMBL Compound was tested in vitro for inhibitory activity against Butyrylcholinesterase B 7.26 pIC50 54.7 nM IC50 Bioorg Med Chem Lett (1997) 7: 2599-2602
ChEMBL Inhibition of rat serum butyrylcholinesterase using butyrylthiocholine as substrate in presence of AChE inhibitor BW284C51 by spectrophotometric method B 7.36 pIC50 44 nM IC50 Bioorg Med Chem (2019) 27: 895-930 [PMID:30744931]
ChEMBL Inhibition of rat plasma butyrylcholine esterase in presence of butyrylcholine substrate by chemiluminescent assay B 8.05 pIC50 9 nM IC50 Eur J Med Chem (2008) 43: 657-661 [PMID:17624631]
CB1 receptor/Cannabinoid CB1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL218] [GtoPdb: 56] [UniProtKB: P21554]
ChEMBL Displacement of [3H]CP-55940 from human CB1 receptor expressed in CHO cells B 6 pKi >1000 nM Ki J Med Chem (2010) 53: 1338-1346 [PMID:20047331]
CB2 receptor/Cannabinoid CB2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL253] [GtoPdb: 57] [UniProtKB: P34972]
ChEMBL Displacement of [3H]CP-55940 from human CB2 receptor expressed in CHO cells B 6 pKi >1000 nM Ki J Med Chem (2010) 53: 1338-1346 [PMID:20047331]
choline O-acetyltransferase/Choline acetylase in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3945] [GtoPdb: 2480] [UniProtKB: P32738]
ChEMBL Inhibition constant determined against Acetylcholinesterase (AChE) receptor. B 9.82 pKi 0.15 nM Ki J Med Chem (1998) 41: 4186-4189 [PMID:9784091]
Cholinesterase in Equus caballus (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5763] [UniProtKB: P81908]
ChEMBL Competitive inhibition of equine serum BuChE assessed as enzyme-inhibitor complex using p-nitrophenyl butyrate as substrate by Lineweaver-Burk plot analysis B 7.76 pKi 17.2 nM Ki Eur J Med Chem (2017) 138: 761-773 [PMID:28728108]
ChEMBL Inhibition of equine serum BuChE assessed as dissociation constant for enzyme-inhibitor complex using butyrylthiocholine iodide as substrate measured for 125 secs by Ellman's method B 7.77 pKi 17 nM Ki Eur J Med Chem (2019) 181: 111550-111550 [PMID:31376562]
ChEMBL Inhibition of equine serum BuChE by Ellman's method B 4.97 pIC50 10800 nM IC50 Bioorg Med Chem Lett (2021) 49: 128212-128212 [PMID:34153471]
ChEMBL Inhibition of horse serum BChE using butyrylthiocholine iodide as substrate preincubated for 5 mins by Ellman method B 5.09 pIC50 8130 nM IC50 Bioorg Med Chem (2015) 23: 2445-2457 [PMID:25868744]
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 5.75 pIC50 1770 nM IC50 Eur J Med Chem (2016) 107: 219-232 [PMID:26588065]
ChEMBL Inhibition of equine serum BChE pre-incubated for 5 mins before butyrylthiocholineiodide substrate addition by Ellman's method B 6.09 pIC50 820 nM IC50 Bioorg Med Chem Lett (2015) 25: 3442-3446 [PMID:26212777]
ChEMBL Inhibition of equine serum BuChE using butylthiocholine iodide as substrate preincubated for 10 mins followed by substrate addition by Ellman's method B 6.46 pIC50 350 nM IC50 Eur J Med Chem (2015) 89: 296-303 [PMID:25462245]
ChEMBL Inhibition of equine serum BuChE pre-incubated for 3 mins before butyrylthiocholine substrate addition by Ellman's reagent based spectrophotometry B 6.46 pIC50 350 nM IC50 Eur J Med Chem (2015) 97: 181-189 [PMID:25969170]
ChEMBL Inhibition of equine serum BuchE using butyrylthiocholine as substrate by Ellman's method B 6.67 pIC50 216 nM IC50 Bioorg Med Chem Lett (2019) 29: 2150-2152 [PMID:31281020]
ChEMBL Inhibition of equine BuchE using butyrylthiocholine as substrate by Ellman's method B 6.96 pIC50 110 nM IC50 Bioorg Med Chem Lett (2020) 30: 127075-127075 [PMID:32165042]
ChEMBL Inhibition of horse serum BuChE using butyrylthiocholine iodide as substrate preincubated for 20 mins by Ellman's method B 7 pIC50 100 nM IC50 Bioorg Med Chem Lett (2012) 22: 6498-6502 [PMID:22981331]
ChEMBL Inhibition of equine serum BuChE 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 7.03 pIC50 93 nM IC50 Eur J Med Chem (2022) 244: 114806-114806 [PMID:36223681]
ChEMBL Inhibition of horse serum BChE after 15 mins by DTNB reagent based assay B 7.18 pIC50 66 nM IC50 Medchemcomm (2018) 9: 149-159 [PMID:30108908]
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 7.24 pIC50 57 nM IC50 Eur J Med Chem (2022) 242: 114630-114630 [PMID:35987018]
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 7.25 pIC50 56 nM IC50 Eur J Med Chem (2017) 136: 36-51 [PMID:28478343]
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 7.27 pIC50 54 nM IC50 Eur J Med Chem (2016) 119: 260-277 [PMID:27227482]
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 7.27 pIC50 54 nM IC50 Bioorg Med Chem (2016) 24: 2777-2788 [PMID:27157006]
ChEMBL Inhibition of equine serum BuChE using S-butyrylthiocholine iodide as substrate incubated for 6 mins prior to substrate addition measured after 60 to 180 secs by Ellman's method B 7.27 pIC50 54 nM IC50 Bioorg Med Chem Lett (2013) 23: 2636-2641 [PMID:23511019]
ChEMBL Inhibition of horse BuChE using S-butyrylcholine iodide as substrate incubated for 6 mins prior to substrate addition measured after 60 to 180 secs by Ellman's method B 7.28 pIC50 52 nM IC50 Medchemcomm (2014) 5: 609-616
ChEMBL Inhibition of equine serum BChE using S-butyrylthiocholine chloride as substrate incubated for 6 mins by spectrophotometric method B 7.3 pIC50 50.5 nM IC50 Bioorg Med Chem (2014) 22: 6089-6104 [PMID:25282654]
ChEMBL Inhibition of equine serum BChE B 7.3 pIC50 50 nM IC50 Bioorg Med Chem (2023) 80: 117178-117178 [PMID:36706609]
ChEMBL Inhibition of equine serum BuChE using S-butyrylcholinesterase iodide as substrate preincubated for 6 mins followed by substrate addition by Ellmans method B 7.3 pIC50 50 nM IC50 Eur J Med Chem (2013) 69: 632-646 [PMID:24095756]
ChEMBL Inhibition of equine serum BuChE using butyrylthiocholine iodide as substrate preincubated for 5 mins followed by substrate addition measured at 1 min interval for 3 mins by Ellmans method B 7.3 pIC50 50 nM IC50 Bioorg Med Chem (2017) 25: 2387-2398 [PMID:28302511]
ChEMBL Inhibition of equine BCHE preincubated for 6 mins followed by addition of S-butyrylcholine iodide as substrate by Ellman's method B 7.3 pIC50 50 nM IC50 Bioorg Med Chem (2016) 24: 4324-4338 [PMID:27460699]
ChEMBL Inhibition of equine serum BChE using butylthiocholine chloride as substrate incubated for 15 mins prior to substrate addition by Ellman's method B 7.33 pIC50 47 nM IC50 Bioorg Med Chem (2013) 21: 7275-7282 [PMID:24148835]
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 7.34 pIC50 46 nM IC50 Eur J Med Chem (2016) 123: 282-297 [PMID:27484514]
ChEMBL Inhibition of equine serum BChE using S-butyrylthiocholine iodide as substrate preincubated for 6 mins prior to substrate addition measured at 60 to 180 seconds by Ellman's method B 7.38 pIC50 42 nM IC50 Eur J Med Chem (2013) 64: 540-553 [PMID:23685572]
ChEMBL Inhibition of equine serum BuChE using butyrylthiocholine chloride as substrate preincubated for 15 mins by Ellman's method B 7.39 pIC50 41 nM IC50 Eur J Med Chem (2011) 46: 5885-5893 [PMID:22019228]
ChEMBL Inhibition of equine serum BuChE using butyrylcholine as substrate by Ellman's method B 7.39 pIC50 41 nM IC50 Bioorg Med Chem (2012) 20: 3038-3048 [PMID:22472046]
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 7.4 pIC50 40 nM IC50 Eur J Med Chem (2022) 227: 113973-113973 [PMID:34752955]
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 7.4 pIC50 40 nM IC50 Eur J Med Chem (2019) 177: 198-211 [PMID:31136894]
ChEMBL Inhibition of horse serum BuChE pre-incubated for 20 mins before butylthicoline iodide substrate addition by Ellman's assay B 7.4 pIC50 40 nM IC50 Bioorg Med Chem Lett (2015) 25: 807-810 [PMID:25597007]
ChEMBL Inhibition of horse serum BuChE by Ellman's method B 7.4 pIC50 40 nM IC50 J Nat Prod (2006) 69: 1341-1346 [PMID:16989531]
ChEMBL Inhibition of horse serum BChE using BTC as substrate preincubated for 15 mins followed by substrate addition by UV-spectrophotometric analysis B 7.43 pIC50 37.08 nM IC50 Eur J Med Chem (2016) 122: 17-26 [PMID:27343850]
ChEMBL Inhibition of equine serum BChE using butyrylthiocholine chloride as substrate by spectrophotometer analysis B 7.43 pIC50 37 nM IC50 Bioorg Med Chem (2014) 22: 3213-3219 [PMID:24794747]
ChEMBL Inhibition of equine serum BuChE using S-butyrylthiocholine iodide as substrate preincubated for 6 mins before substrate addition by Ellman's method B 7.45 pIC50 35.2 nM IC50 Eur J Med Chem (2015) 93: 42-50 [PMID:25656088]
ChEMBL Inhibition of horse serum butyrylcholinesterase using butylthiocholine as substrate incubated for 15 mins followed by substrate addition measured for 2 mins by Ellman's method B 7.48 pIC50 33.4 nM IC50 Eur J Med Chem (2013) 63: 299-312 [PMID:23501115]
ChEMBL Inhibition of equine serum BChE using butyrylthiocholine iodide as substrate preincubated for 10 mins prior to substrate addition by Ellman's method B 7.49 pIC50 32 nM IC50 Eur J Med Chem (2013) 68: 291-300 [PMID:23988412]
ChEMBL Inhibition of equine serum BuChE B 7.52 pIC50 30 nM IC50 Bioorg Med Chem Lett (2020) 30: 127609-127609 [PMID:33039562]
ChEMBL inhibition of equine serum BuChE by Ellman's method B 7.52 pIC50 29.98 nM IC50 Eur J Med Chem (2010) 45: 1415-1423 [PMID:20079560]
ChEMBL Inhibition of equine serum butyrylcholinesterase using butyrylthiocholine iodide as substrate preincubated for 10 mins followed by substrate addition by Ellman's method B 7.54 pIC50 29 nM IC50 Bioorg Med Chem (2017) 25: 3997-4007 [PMID:28578994]
ChEMBL Inhibition of equine serum BChE using butylthiocholine iodide as substrate incubated for 10 mins followed by substrate addition by Ellman's method B 7.54 pIC50 29 nM IC50 Bioorg Med Chem (2018) 26: 4716-4725 [PMID:30104121]
ChEMBL Inhibition of equine serum BChE using butyrylthiocholine iodide as substrate preincubated for 10 mins followed by substrate addition by Ellman's method B 7.54 pIC50 29 nM IC50 Bioorg Med Chem (2017) 25: 5981-5994 [PMID:28986116]
ChEMBL Inhibition of equine serum BuChE using butyrylthiocholine chloride as substrate preincubated for 15 mins followed by substrate addition measured every minute by Ellman's method B 7.61 pIC50 24.27 nM IC50 Eur J Med Chem (2018) 144: 128-136 [PMID:29268129]
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 7.64 pIC50 23 nM IC50 Eur J Med Chem (2022) 234: 114210-114210 [PMID:35303485]
ChEMBL Inhibition of horse serum BChE using butyrylthiocholine chloride as substrate after 15 mins by Ellman's method B 7.67 pIC50 21.6 nM IC50 Eur J Med Chem (2013) 62: 745-753 [PMID:23454517]
ChEMBL Inhibition of equine BuChE by Ellman's method B 7.68 pIC50 21 nM IC50 Bioorg Med Chem Lett (2011) 21: 5881-5887 [PMID:21873056]
ChEMBL Inhibition of equine serum BChE after 15 mins incubation by spectrophotometry based Ellman's method B 7.68 pIC50 21 nM IC50 Bioorg Med Chem Lett (2012) 22: 2257-2261 [PMID:22341944]
ChEMBL Inhibition of equine serum BChE using acetylthiocholine chloride as substrate after 15 mins by Ellman's method B 7.68 pIC50 21 nM IC50 Eur J Med Chem (2011) 46: 4970-4979 [PMID:21871694]
ChEMBL Inhibition of horse serum BuChE using S-butyrylthiocholine iodide as substrate incubated for 6 mins prior to substrate addition measured after 60 to 180 secs by Ellman method B 7.69 pIC50 20.19 nM IC50 Eur J Med Chem (2015) 95: 153-165 [PMID:25812965]
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 7.7 pIC50 20 nM IC50 Bioorg Med Chem (2016) 24: 1528-1539 [PMID:26917219]
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 7.7 pIC50 20 nM IC50 Eur J Med Chem (2023) 249: 115135-115135 [PMID:36696766]
ChEMBL Inhibition of horse serum BuChE using butylthiocholine chloride as substrate preincubated for 15 mins followed by substrate addition measured every 1 min by Ellman method B 7.72 pIC50 19.2 nM IC50 Bioorg Med Chem (2013) 21: 7406-7417 [PMID:24128814]
ChEMBL Inhibition of equine serum BuChE B 7.72 pIC50 19 nM IC50 Bioorg Med Chem Lett (2010) 20: 3606-3609 [PMID:20472431]
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 7.77 pIC50 17 nM IC50 Eur J Med Chem (2017) 125: 853-864 [PMID:27744252]
ChEMBL Inhibition of equine serum BuChE using acetylthiocholine iodide as substrate preincubated for 15 mins followed by substrate addition by spectrophotometric analysis B 7.8 pIC50 16 nM IC50 Bioorg Med Chem (2017) 25: 2946-2955 [PMID:28454848]
ChEMBL Inhibition of equine serum BuChE using butyrylthiocholine chloride as substrate preincubated for 15 mins by Ellman's method B 7.8 pIC50 15.8 nM IC50 Bioorg Med Chem (2012) 20: 5884-5892 [PMID:22944335]
ChEMBL Inhibition of equine serum BuChE using butylthiocholine chloride as substrate preincubated for 15 mins by Ellman's method B 7.8 pIC50 15.8 nM IC50 Bioorg Med Chem Lett (2013) 23: 6737-6742 [PMID:24220172]
ChEMBL Inhibition of horse serum BChE using acetylthiocholine iodide or butyrylthiocholine iodide as substrate preincubated for 5 mins followed by substrate addition by Ellman's method B 7.82 pIC50 15.22 nM IC50 J Med Chem (2022) 65: 11365-11387 [PMID:35969197]
ChEMBL Inhibition of equine serum BuChE by Ellman's method B 7.82 pIC50 15 nM IC50 Bioorg Med Chem (2023) 88-89: 117333-117333 [PMID:37236021]
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 7.82 pIC50 15 nM IC50 Eur J Med Chem (2023) 261: 115832-115832 [PMID:37837674]
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 7.82 pIC50 15 nM IC50 Eur J Med Chem (2021) 225: 113783-113783 [PMID:34461507]
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 7.82 pIC50 15 nM IC50 Eur J Med Chem (2020) 187: 111916-111916 [PMID:31812794]
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 7.82 pIC50 15 nM IC50 J Med Chem (2013) 56: 9089-9099 [PMID:24160297]
ChEMBL Inhibition of equine serum butyrylcholinesterase using butyrylthiocholine chloride as substrate preincubated for 15 mins followed by substrate addition by Ellman's method B 7.82 pIC50 15 nM IC50 Bioorg Med Chem (2014) 22: 1355-1361 [PMID:24461494]
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 7.82 pIC50 15 nM IC50 Eur J Med Chem (2021) 218: 113397-113397 [PMID:33838585]
ChEMBL Inhibition of equine serum BuChE using acetylthiocholine iodide as substrate after 8 mins by Ellman's method B 7.82 pIC50 14.98 nM IC50 Eur J Med Chem (2018) 145: 760-769 [PMID:29353726]
ChEMBL Inhibition of equine serum BuChE using butylthiocholine chloride as substrate preincubated for 20 mins followed by substrate addition by Ellman's method B 7.84 pIC50 14.45 nM IC50 Eur J Med Chem (2016) 116: 200-209 [PMID:27061983]
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 7.85 pIC50 14 nM IC50 J Med Chem (2016) 59: 7683-7689 [PMID:27405689]
ChEMBL Inhibition of equine serum BChE using butyrylthiocholine as substrate preincubated for 20 mins followed by substrate addition measured every 2 mins for 20 mins by Ellman's method B 7.85 pIC50 14 nM IC50 Eur J Med Chem (2017) 139: 367-377 [PMID:28810188]
ChEMBL Inhibition of equine serum butyrylcholinesterase using butyrylthiocholine chloride as substrate preincubated for 15 mins before substrate addition by Ellman's method B 7.85 pIC50 14 nM IC50 Bioorg Med Chem (2012) 20: 2527-2534 [PMID:22444876]
ChEMBL Inhibition of equine serum BuChE using butyl thiocholine iodine as substrate for 20 mins by Ellman's method B 7.89 pIC50 13 nM IC50 Eur J Med Chem (2022) 242: 114701-114701 [PMID:36054949]
ChEMBL Inhibition of equine serum BuChE using butyrylthiocholine iodide as substrate preincubated for 10 mins followed by substrate addition measured for 6 mins by Ellman's method B 7.89 pIC50 13 nM IC50 Eur J Med Chem (2017) 139: 280-289 [PMID:28803044]
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 7.89 pIC50 13 nM IC50 Bioorg Med Chem Lett (2012) 22: 4462-4466 [PMID:22633691]
ChEMBL Inhibition of equine serum BuChE by Ellman's method B 7.89 pIC50 12.8 nM IC50 Bioorg Med Chem Lett (2022) 77: 129037-129037 [PMID:36307033]
ChEMBL Inhibition of equine serum BChE by Ellman's method B 7.96 pIC50 11 nM IC50 Eur J Med Chem (2011) 46: 1572-1581 [PMID:21367493]
ChEMBL Inhibition of equine serum BChE using butyrylthiocholine iodide as substrate after 5 mins by Ellman's method B 7.97 pIC50 10.6 nM IC50 Bioorg Med Chem Lett (2013) 23: 3162-3165 [PMID:23639542]
ChEMBL Inhibition of equine serum BuChE using butyrylthiocholine iodide as substrate pretreated followed by substrate addition and measured after 2 mins by Ellman's method B 7.97 pIC50 10.6 nM IC50 Bioorg Med Chem (2019) 27: 895-930 [PMID:30744931]
ChEMBL Inhibition of horse serum BuChE using butyrylthiocholine as substrate by UV spectroscopic analysis B 8 pIC50 10 nM IC50 Eur J Med Chem (2014) 81: 350-358 [PMID:24858540]
ChEMBL Inhibition of equine serum BChE preincubated for 15 mins followed by addition of S-butyrylthiocholine iodide as substrate measured after 30 mins by Ellman's microplate assay B 8 pIC50 10 nM IC50 Bioorg Med Chem (2016) 24: 3742-3751 [PMID:27328658]
ChEMBL Inhibition of horse serum BChE by Ellman's method B 8 pIC50 10 nM IC50 J Med Chem (2012) 55: 1303-1317 [PMID:22243648]
ChEMBL Inhibition of BuChE in horse serum by Ellman method B 8 pIC50 10 nM IC50 J Med Chem (2009) 52: 7249-7257 [PMID:19856923]
ChEMBL Inhibition of equine serum BChE by Ellman's method B 8 pIC50 10 nM IC50 Bioorg Med Chem (2010) 18: 2173-2177 [PMID:20176490]
ChEMBL Inhibition of equine serum BuChE using butyrylthiocholine iodide as substrate preincubated for 15 mins followed by substrate addition measured after 20 mins by Ellman's method B 8 pIC50 10 nM IC50 Eur J Med Chem (2017) 125: 1200-1212 [PMID:27863370]
ChEMBL Inhibition of horse serum BChE by Ellman's reaction B 8 pIC50 10 nM IC50 J Med Chem (2010) 53: 4927-4937 [PMID:20545360]
ChEMBL Inhibition of equine serum BuChE by Ellman's method B 8 pIC50 10 nM IC50 Eur J Med Chem (2010) 45: 6152-6158 [PMID:20926162]
ChEMBL Inhibition of BuChE in horse serum using butyrylthiocholine as substrate by Ellman method B 8 pIC50 10 nM IC50 Eur J Med Chem (2011) 46: 2224-2235 [PMID:21420206]
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 8 pIC50 10 nM IC50 J Med Chem (2016) 59: 5823-5846 [PMID:27253679]
ChEMBL Inhibition of equine serum BuchE B 8 pIC50 10 nM IC50 Bioorg Med Chem Lett (2008) 18: 3790-3793 [PMID:18524585]
ChEMBL Inhibition of horse serum BChE using acetylthiocholine iodide as substrate preincubated for 5 mins before substrate addition by Ellman's method B 8.01 pIC50 9.8 nM IC50 Bioorg Med Chem (2013) 21: 4928-4937 [PMID:23891231]
ChEMBL Inhibition of equine serum BChE using (S)-butyrylthiocholine iodide as substrate measured for 6 mins by Ellman's method B 8.1 pIC50 8 nM IC50 J Nat Prod (2020) 83: 852-863 [PMID:32150413]
ChEMBL Inhibition of equine serum BCHE using butyrylthiocholine iodide as substrate preincubated for 5 mins followed by DTNB addition for 5 mins and subsequent addition of substrate measured after 3 mins by Ellman's method B 8.14 pIC50 7.2 nM IC50 Eur J Med Chem (2018) 148: 238-254 [PMID:29466774]
ChEMBL Inhibition of horse serum BChE by Ellman's method B 8.16 pIC50 6.95 nM IC50 Bioorg Med Chem (2010) 18: 1181-1193 [PMID:20061157]
ChEMBL Inhibition of horse serum BChE using butyrylthiocholine iodide as substrate preincubated for 35 mins followed by enzyme addition measured after 3 mins by Ellman's method B 8.16 pIC50 6.95 nM IC50 Eur J Med Chem (2014) 81: 158-175 [PMID:24836068]
ChEMBL Inhibition of equine serum BChE by Ellman's method B 8.19 pIC50 6.4 nM IC50 Bioorg Med Chem (2011) 19: 1222-1235 [PMID:21232964]
ChEMBL Inhibition of equine serum BChE by Ellman's method B 8.19 pIC50 6.38 nM IC50 Bioorg Med Chem (2011) 19: 1222-1235 [PMID:21232964]
ChEMBL Inhibition of equine serum BuChE using butyrylthiocholine iodide as substrate incubated for 10 mins followed by substrate addition by DTNB-reagent based Ellman's colorimetric assay B 8.28 pIC50 5.22 nM IC50 Eur J Med Chem (2022) 239: 114510-114510 [PMID:35728508]
ChEMBL Inhibition of horse serum butyrylcholinesterase preincubated with compound for 10 mins using butrylcholine iodide as substrate after 15 mins by spectrophotometric analysis B 8.28 pIC50 5.2 nM IC50 Bioorg Med Chem Lett (2011) 21: 2384-2388 [PMID:21411323]
ChEMBL Inhibition of equine serum BuChE using butyrylthiocholine iodide as substrate preincubated for 10 mins before substrate addition by Ellman's method B 8.28 pIC50 5.2 nM IC50 Eur J Med Chem (2011) 46: 6119-6130 [PMID:22000936]
ChEMBL Inhibition of horse serum BuChE by Ellman's method B 8.28 pIC50 5.2 nM IC50 Bioorg Med Chem (2011) 19: 122-133 [PMID:21163662]
ChEMBL Inhibition of horse serum BChE after 15 mins by Ellman's method B 8.28 pIC50 5.2 nM IC50 Eur J Med Chem (2011) 46: 1-10 [PMID:21111515]
ChEMBL Inhibition of Equus caballus BChE preincubated for 10 mins measured after 15 mins by Ellman's method B 8.28 pIC50 5.2 nM IC50 Eur J Med Chem (2011) 46: 4676-4681 [PMID:21715067]
ChEMBL Inhibition of equine serum BuChE by Ellman's method B 8.28 pIC50 5.2 nM IC50 J Med Chem (2010) 53: 5129-5143 [PMID:20575555]
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 8.28 pIC50 5.2 nM IC50 Bioorg Med Chem (2024) 101: 117649-117649 [PMID:38401458]
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 8.28 pIC50 5.2 nM IC50 Bioorg Med Chem (2016) 24: 2352-2359 [PMID:27083471]
ChEMBL Inhibition of BChE from equine serum by Ellman's method B 8.29 pIC50 5.13 nM IC50 J Med Chem (2010) 53: 2094-2103 [PMID:20158205]
ChEMBL Inhibition of horse AChE by colorimetric Ellman assay B 8.29 pIC50 5.13 nM IC50 J Med Chem (2012) 55: 5231-5242 [PMID:22624880]
ChEMBL Inhibition of horse serum BuChE pre-incubated for 10 mins before addition of butyrylthiocholine iodide substrate and further incubated for 15 mins by Ellman's method B 8.29 pIC50 5.07 nM IC50 J Med Chem (2016) 59: 9967-9973 [PMID:27736061]
ChEMBL Inhibition of equine serum BChE using butyrylthiocholine iodide as substrate preincubated for 5 mins followed by substrate addition and measured after 2 mins by DTNB-reagent based Ellman's method B 8.3 pIC50 5 nM IC50 J Med Chem (2021) 64: 6856-6876 [PMID:33973470]
ChEMBL Inhibition of horse serum BChE B 8.3 pIC50 5 nM IC50 Eur J Med Chem (2017) 138: 774-806 [PMID:28734245]
ChEMBL Inhibition of equine serum BChE by modified Ellman's method B 8.3 pIC50 5 nM IC50 J Med Chem (2010) 53: 3611-3617 [PMID:20361801]
ChEMBL Inhibition of equine serum BChE by modified Ellman's method B 8.3 pIC50 4.97 nM IC50 J Med Chem (2010) 53: 3611-3617 [PMID:20361801]
ChEMBL Inhibition of horse serum BChE preincubated for 5 mins by Ellman's method B 8.31 pIC50 4.9 nM IC50 Eur J Med Chem (2010) 45: 5602-5611 [PMID:20926161]
ChEMBL Inhibition of equine serum BChE using ATC iodide substrate by Ellman's assay B 8.33 pIC50 4.7 nM IC50 Bioorg Med Chem (2015) 23: 5610-5618 [PMID:26242241]
ChEMBL Inhibition of BChE in equine serum using butyrylthiocholine iodide substrate by Ellman assay B 8.36 pIC50 4.4 nM IC50 J Med Chem (2015) 58: 6710-6715 [PMID:26278660]
ChEMBL Inhibition of equine serum BuChE using S-butyrylthiocholine as substrate at by DTNB reagent based spectrophotometric analysis B 8.4 pIC50 4 nM IC50 Bioorg Med Chem (2022) 73: 117030-117030 [PMID:36179486]
ChEMBL Inhibition of horse serum BChE by spectrophotometry based Ellman's method B 8.4 pIC50 4 nM IC50 Bioorg Med Chem (2014) 22: 3838-3849 [PMID:25017625]
ChEMBL Inhibition of BChE in horse serum using butyrylthiocholine iodide as substrate after 120 mins by Ellman's method B 8.4 pIC50 4 nM IC50 Bioorg Med Chem (2014) 22: 3341-3350 [PMID:24835788]
ChEMBL Inhibition of horse serum butyrylcholine esterase in presence of acetylcholine substrate by chemiluminescent assay B 8.4 pIC50 4 nM IC50 Eur J Med Chem (2008) 43: 657-661 [PMID:17624631]
ChEMBL Inhibition of equine serum BuChE by Ellman's method B 8.4 pIC50 4 nM IC50 Bioorg Med Chem Lett (2021) 49: 128316-128316 [PMID:34391893]
ChEMBL Inhibition of equine serum butyrylcholine esterase using butyrylcholine chloride as substrate incubated for 5 mins prior to substrate addition measured every 3 mins by Ellman's assay B 8.42 pIC50 3.8 nM IC50 J Med Chem (2012) 55: 3588-3592 [PMID:22420827]
ChEMBL Inhibition of equine serum BuChE using butyrylthiocholine chloride substrate incubated for 5 mins before substrate addition measured at 3 min interval by Ellman method B 8.42 pIC50 3.8 nM IC50 Bioorg Med Chem (2012) 20: 6513-6522 [PMID:23000296]
ChEMBL Inhibition of equine serum BChE B 8.43 pIC50 3.7 nM IC50 Bioorg Med Chem (2014) 22: 4867-4881 [PMID:25047936]
ChEMBL Inhibition of equine serum BChE B 8.44 pIC50 3.66 nM IC50 Bioorg Med Chem (2014) 22: 4867-4881 [PMID:25047936]
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 8.48 pIC50 3.3 nM IC50 Bioorg Med Chem (2014) 22: 2496-2507 [PMID:24657052]
ChEMBL Inhibition of horse AChE by colorimetric Ellman assay B 8.49 pIC50 3.2 nM IC50 J Med Chem (2012) 55: 5231-5242 [PMID:22624880]
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 8.49 pIC50 3.2 nM IC50 Eur J Med Chem (2018) 145: 165-190 [PMID:29324339]
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 spectrophotometric method B 8.49 pIC50 3.2 nM IC50 J Med Chem (2017) 60: 5909-5926 [PMID:28613859]
ChEMBL Inhibition of equine serum BChE using butyrylthiocholine iodide as substrate pretreated for 4.5 mins followed by substrate addition and measured after 2.5 mins by Ellman's method B 8.57 pIC50 2.69 nM IC50 Medchemcomm (2017) 8: 1346-1359 [PMID:30108847]
ChEMBL Inhibition of equine BuChE using butyrylthiocholine iodide as substrate preincubated for 5 mins before substrate addition measured for 10 mins by Ellman's method B 8.61 pIC50 2.43 nM IC50 Medchemcomm (2012) 3: 627-634
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 8.7 pIC50 2 nM IC50 Eur J Med Chem (2017) 125: 676-695 [PMID:27721153]
ChEMBL Inhibition of equine serum BuChE preincubated for 5 mins followed by butyrylthiocholine iodide substrate addition measured after 5 mins by Ellman's method B 8.7 pIC50 2 nM IC50 Eur J Med Chem (2016) 124: 63-81 [PMID:27560283]
ChEMBL Inhibition of equine serum BuChE after 5 mins by Ellman's method B 8.7 pIC50 2 nM IC50 Eur J Med Chem (2015) 92: 738-749 [PMID:25621991]
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 8.7 pIC50 2 nM IC50 Eur J Med Chem (2021) 225: 113792-113792 [PMID:34530376]
ChEMBL Inhibition of BuChE in horse serum pre-incubated for 5 mins before addition of butyrylthiocholine iodide substrate by Ellman's assay B 8.7 pIC50 2 nM IC50 Bioorg Med Chem (2015) 23: 1629-1637 [PMID:25707322]
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 8.7 pIC50 2 nM IC50 Bioorg Med Chem Lett (2016) 26: 4140-4145 [PMID:27445168]
ChEMBL Inhibition of equine serum BuChE using butyrylthiocholine iodide as substrate preincubated for 5 mins followed by substrate addition and measured every min for 10 mins by Ellman's method B 8.72 pIC50 1.9 nM IC50 RSC Med Chem (2024) 15: 963-980 [PMID:38516603]
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 8.82 pIC50 1.53 nM IC50 Eur J Med Chem (2020) 185: 111785-111785 [PMID:31669851]
ChEMBL Inhibition of equine serum BuChE using butyrylthiocholine iodide as substrate incubated for 15 mins followed by substrate addition by Ellman's method B 8.92 pIC50 1.2 nM IC50 Eur J Med Chem (2016) 122: 326-338 [PMID:27376495]
ChEMBL Inhibition of horse serum BuChE using butyrylthiocholine as substrate pretreated for 10 mins followed by substrate addition measured after 15 mins by spectrophotometry based Ellman method B 10.3 pIC50 0.05 nM IC50 Eur J Med Chem (2017) 126: 576-589 [PMID:27918993]
cyclin dependent kinase 5/Cyclin-dependent kinase 5/CDK5 activator 1 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL1907600] [GtoPdb: 1977] [UniProtKB: Q00535, Q15078]
ChEMBL Inhibition of human recombinant CDK5/p25 using histone H1 as substrate in presence of [gamma-33P]ATP incubated for 30 mins by liquid scintillation counting assay B 5 pIC50 >10000 nM IC50 Eur J Med Chem (2019) 168: 58-77 [PMID:30798053]
CYP2D6/Cytochrome P450 2D6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL289] [GtoPdb: 1329] [UniProtKB: P10635]
ChEMBL DRUGMATRIX: CYP450, 2D6 enzyme inhibition (substrate: 3-Cyano-7-ethoxycoumarin) B 6.52 pIC50 300 nM IC50 DrugMatrix in vitro pharmacology data
DAT/Dopamine transporter in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL338] [GtoPdb: 927] [UniProtKB: P23977]
ChEMBL Inhibition of the reuptake of dopamine in rat corpora striata. F 4.66 pIC50 22000 nM IC50 J Med Chem (1989) 32: 1805-1813 [PMID:2754707]
fatty acid binding protein 1/Fatty acid-binding protein, liver in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5421] [GtoPdb: 2531] [UniProtKB: P07148]
ChEMBL Binding affinity to recombinant human N-terminal His6 and Avi-tagged FABP1 expressed in Escherichia coli NEB cells by surface plasmon resonance method B 3.05 pKd 900000 nM Kd J Med Chem (2016) 59: 8094-8102 [PMID:27500412]
fatty acid binding protein 6/Gastrotropin in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4523235] [GtoPdb: 2536] [UniProtKB: P51161]
ChEMBL Binding affinity to recombinant human N-terminal His6 and Avi-tagged FABP6 expressed in Escherichia coli NEB cells by surface plasmon resonance method B 3.7 pKd 200000 nM Kd J Med Chem (2016) 59: 8094-8102 [PMID:27500412]
GluN1/GluN2A/Glutamate NMDA receptor; GRIN1/GRIN2A in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL1907604] [GtoPdb: 455, 456] [UniProtKB: Q05586, Q12879]
ChEMBL Inhibition of human GluN1a/GluN2A receptor expressed in HEK293 cells assessed as relative inhibition of glycine/glutamate-induced current measured at +40 mV holding potential by whole-cell patch clamp method B 4.07 pIC50 84600 nM IC50 Eur J Med Chem (2021) 219: 113434-113434 [PMID:33892271]
ChEMBL Inhibition of human GluN1a/GluN2A receptor expressed in HEK293 cells assessed as inhibition of glycine/glutamate-induced current measured at -60 mV holding potential by whole-cell patch clamp method B 5.04 pIC50 9100 nM IC50 Eur J Med Chem (2021) 219: 113434-113434 [PMID:33892271]
ChEMBL Inhibition of dexamethasone-induced human NR1-1a/NR2A receptor-mediated excitotoxicity in (S)-glutamate/glycine-stimulated mouse L12-G10 cells assessed as LDH release after 30 mins B 5.31 pIC50 4900 nM IC50 J Med Chem (2010) 53: 3611-3617 [PMID:20361801]
ChEMBL Inhibition of human NR1-1a/NR2A expressed in mouse L12-G10 cells assessed as inhibition of glutamate-induced excitotoxicity incubated for 16 hrs by LDH release assay B 5.31 pIC50 4900 nM IC50 J Med Chem (2015) 58: 6710-6715 [PMID:26278660]
GluN1/GluN2B/Glutamate NMDA receptor; GRIN1/GRIN2B in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL1907603] [GtoPdb: 455, 457] [UniProtKB: Q05586, Q13224]
ChEMBL Inhibition of dexamethasone-induced human NR1-1a/NR2B receptor-mediated excitotoxicity in (S)-glutamate/glycine-stimulated mouse L13-E6 cells assessed as LDH release after 30 mins B 4.36 pIC50 44000 nM IC50 J Med Chem (2010) 53: 3611-3617 [PMID:20361801]
ChEMBL Inhibition of human NR1-1a/NR2B expressed in mouse L13-E6 cells assessed as inhibition of glutamate-induced excitotoxicity incubated for 16 hrs by LDH release assay B 4.36 pIC50 44000 nM IC50 J Med Chem (2015) 58: 6710-6715 [PMID:26278660]
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 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]
ChEMBL Inhibition of recombinant human N-terminal His6-tagged GSK-3beta H350L mutant expressed in baculovirus infected Sf21 cells using GSM as substrate incubated for 30 mins in presence of ATP by kinase-glo luminescence assay B 6 pIC50 >1000 nM IC50 Eur J Med Chem (2020) 207: 112751-112751 [PMID:32950908]
Kv11.1/HERG in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809]
ChEMBL Inhibition of hERG expressed in CHO-K1 cells assessed as reduction in thallium influx incubated for 30 minutes by FLIPR B 4.84 pIC50 14312 nM IC50 Eur J Med Chem (2021) 226: 113827-113827 [PMID:34530383]
Histamine N-methyltransferase in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3241] [UniProtKB: Q01984]
ChEMBL Inhibition of rat kidney Histamine N-Methyltransferase (HMT) activity determined by the formation of N-methyl-histamine B 6.96 pIC50 110 nM IC50 J Med Chem (2002) 45: 1128-1141 [PMID:11855993]
Monoamine oxidase A in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3254] [UniProtKB: P21398]
ChEMBL Inhibition of recombinant bovine mitochondrial MAO-A using benzylamine or serotonin as substrate incubated for 60 mins by fluorimetry assay B 7.33 pIC50 47 nM IC50 Eur J Med Chem (2022) 227: 113964-113964 [PMID:34743062]
Monoamine oxidase A in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3358] [UniProtKB: P21396]
ChEMBL Inhibition Assay: The inhibitory activity of monoamine oxidases A and B was assessed by the Fowler and Tipton radiometric method (Biochem Pharmacol 1981, 30, 3329) using a purification of rat liver mitochondria as the source of enzymes. The inhibitory activity of MAO-B was compared to 25 ul of [14C]-phenylethylamine (PEA), 20 uM of activity, 2.5 mCi/mmol. The inhibitory activity of MAO-A was compared to 25 ul of [14C]-(5-hydroxytriptamine) (5-HT), 100 uM of activity, 0.5 mCi/mmol. Inhibition curves were performed in triplicate by incubating at least nine inhibitor concentrations for 30 min. A triplicate sample without inhibitor was always present so as to be aware of 100% of the MAO activity. The reaction took place with the addition of the substrate in a final volume of 225 ul of 50 mM phosphate buffer, pH 7.4, containing 20 ul of rat liver mitochondria at a concentration of 5 mg/ml. The reaction was carried out under continuous stirring at 37 C. for 4 minutes. B 4.39 pIC50 40300 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 mitochondrial MAO-A in rat liver homogenates using [14C]-(5-hydroxy-triptamine) as substrate preincubated for 30 mins by liquid scintillation counting B 7.4 pIC50 40 nM IC50 Eur J Med Chem (2012) 52: 251-262 [PMID:22503231]
Monoamine oxidase B in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2993] [GtoPdb: 2490] [UniProtKB: P19643]
ChEMBL Inhibition of mitochondrial MAO-B in rat liver homogenates using [14C]-phenylethylamine as substrate preincubated for 30 mins by liquid scintillation counting B 7 pIC50 >100 nM IC50 Eur J Med Chem (2012) 52: 251-262 [PMID:22503231]
M1 receptor/Muscarinic acetylcholine receptor M1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL216] [GtoPdb: 13] [UniProtKB: P11229]
ChEMBL Displacement of [3H]NMS from human muscarinic M1 receptor expressed in CHO cells in ternary complex by EATCM analysis B 5.18 pKd 5.18 - logKd J Med Chem (2010) 53: 2094-2103 [PMID:20158205]
ChEMBL Displacement of [3H]NMS from human muscarinic M1 receptor expressed in CHO cells in binary complex by EATCM analysis B 5.86 pKd 5.86 - logKd J Med Chem (2010) 53: 2094-2103 [PMID:20158205]
ChEMBL Antagonist activity at human M1 mAChR expressed in CHO cells assessed as inhibition of oxotremorine M-stimulated calcium influx preincubated for 10 mins followed by oxotremorine M addition by Fluo-4 NW dye based fluorescence assay F 4.89 pIC50 13000 nM IC50 Eur J Med Chem (2018) 150: 292-306 [PMID:29533874]
M1 receptor/Muscarinic acetylcholine receptor M1 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3733] [GtoPdb: 13] [UniProtKB: P12657]
ChEMBL Binding affinity against mouse Muscarinic acetylcholine receptor M1 using cerebral cortex and [3H]pirenzepine B 5.7 pIC50 2000 nM IC50 J Med Chem (1992) 35: 3141-3147 [PMID:1507203]
ChEMBL Compound was evaluated for the competitive inhibition of [3H]pirenzepine binding to Muscarinic acetylcholine receptor M1 of mouse cerebral cortex B 5.7 pIC50 2000 nM IC50 J Med Chem (1992) 35: 1102-1108 [PMID:1552502]
GtoPdb - - 5.7 pIC50 2000 nM IC50 J Med Chem (1992) 35: 1102-8 [PMID:1552502]
M2 receptor/Muscarinic acetylcholine receptor M2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL211] [GtoPdb: 14] [UniProtKB: P08172]
ChEMBL Binding affinity against mouse Muscarinic acetylcholine receptor M2 using heart tissue and [3H]N-methylscopolamine F 5.24 pKi 5800 nM Ki J Med Chem (1992) 35: 3141-3147 [PMID:1507203]
Muscarinic acetylcholine receptor M2 in Pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4781] [UniProtKB: P06199]
ChEMBL Inhibition of [3H]NMS dissociation from porcine muscarinic M2 receptor B 5.2 pEC50 6309.57 nM EC50 J Med Chem (2007) 50: 5685-5695 [PMID:17944454]
ChEMBL Inhibition of [3H]NMS dissociation from porcine muscarinic M2 receptor B 5.2 pEC50 6300 nM EC50 J Med Chem (2007) 50: 5685-5695 [PMID:17944454]
M2 receptor/Muscarinic acetylcholine receptor M2 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3197] [GtoPdb: 14] [UniProtKB: Q9ERZ4]
ChEMBL Ability to displace [3H]oxotremorine ([3H]-OXO-M) from mouse cerebral cortex B 6.66 pKi 220 nM Ki J Med Chem (1992) 35: 3141-3147 [PMID:1507203]
ChEMBL Compound was evaluated for the competitive inhibition of [3H]methylscopolamine binding to Muscarinic acetylcholine receptor M2 of mouse cerebral cortex B 5.68 pIC50 2100 nM IC50 J Med Chem (1992) 35: 1102-1108 [PMID:1552502]
GtoPdb - - 5.68 pIC50 2100 nM IC50 J Med Chem (1992) 35: 1102-8 [PMID:1552502]
M2 receptor/Muscarinic acetylcholine receptor M2 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL309] [GtoPdb: 14] [UniProtKB: P10980]
ChEMBL Binding affinity against mouse M2 muscarinic receptor using heart tissue and [3H]N-methylscopolamine B 5.68 pIC50 2100 nM IC50 J Med Chem (1992) 35: 3141-3147 [PMID:1507203]
nicotinic acetylcholine receptor α3 subunit/nicotinic acetylcholine receptor β4 subunit/nicotinic acetylcholine receptor α6 subunit/Nicotinic acetylcholine receptor alpha6/alpha3/beta4 in Rat (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL3137276] [GtoPdb: 464, 474, 467] [UniProtKB: P04757, P12392, P43143]
ChEMBL Inhibition of human GluN1a/GluN2B receptor expressed in HEK293 cells assessed as inhibition of glycine/glutamate-induced current measured at -60 mV holding potential by whole-cell patch clamp method B 4.71 pIC50 19700 nM IC50 Eur J Med Chem (2021) 219: 113434-113434 [PMID:33892271]
NET/Norepinephrine transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL222] [GtoPdb: 926] [UniProtKB: P23975]
ChEMBL DRUGMATRIX: Norepinephrine Transporter radioligand binding (ligand: [125I] RTI-55) B 6.29 pKi 513 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL Inhibitory activity against norepinephrine (NE) uptake in rat whole brain synaptosome preparation F 4.96 pIC50 11000 nM IC50 J Med Chem (1996) 39: 570-581 [PMID:8558529]
ChEMBL DRUGMATRIX: Norepinephrine Transporter radioligand binding (ligand: [125I] RTI-55) B 6.29 pIC50 517 nM IC50 DrugMatrix in vitro pharmacology data
Norepinephrine transporter in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL304] [UniProtKB: Q9WTR4]
ChEMBL Inhibition of norepinephrine reuptake in rat whole brains minus cerebellar F 4.96 pIC50 11000 nM IC50 J Med Chem (1989) 32: 1805-1813 [PMID:2754707]
ChEMBL Inhibition of neuronal uptake of Noradrenaline in rat brain homogenate F 5.1 pIC50 7900 nM IC50 J Med Chem (1997) 40: 3516-3523 [PMID:9357518]
Plasmodium falciparum (target type: ORGANISM) [ChEMBL: CHEMBL364]
ChEMBL Antimalarial activity against chloroquine-sensitive ring-stage Plasmodium falciparum 3D7 assessed as parasite viability after 72 hrs by malstat assay F 4.9 pIC50 12500 nM IC50 Bioorg Med Chem (2016) 24: 3636-3642 [PMID:27316542]
SERT/Serotonin transporter in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL313] [GtoPdb: 928] [UniProtKB: P31652]
ChEMBL Inhibition of serotonin reuptake in rat whole brains without cerebellum F 4.72 pIC50 19000 nM IC50 J Med Chem (1989) 32: 1805-1813 [PMID:2754707]
ChEMBL Inhibition of neuronal uptake of 5 - Hydroxytryptamine in rat brain homogenate F 5.12 pIC50 7600 nM IC50 J Med Chem (1997) 40: 3516-3523 [PMID:9357518]
Organic cation transporter 1/Solute carrier family 22 member 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5685] [GtoPdb: 1019] [UniProtKB: O15245]
ChEMBL Inhibition of human OCT1 expressed in HEK293 cells assessed as decrease in uptake of ASP+ after 2 mins by fluorescence assay B 4.66 pIC50 21720 nM IC50 J Med Chem (2017) 60: 2685-2696 [PMID:28230985]
Son of sevenless homolog 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4524041] [UniProtKB: Q07890]
ChEMBL Binding affinity to biotinylated SOS2 (unknown origin) by surface plasmon resonance analysis B 3.26 pKd 550000 nM Kd J Med Chem (2024) 67: 774-781 [PMID:38156904]
Cav2.1/Cav3.1/Cav1.4/Cav3.2/Cav2.2/Cav1.3/Cav1.1/Cav1.2/Cav2.3/Cav3.3/Voltage-gated calcium channel in Human (target type: PROTEIN COMPLEX GROUP) [ChEMBL: CHEMBL2363032] [GtoPdb: 532, 535, 531, 536, 533, 530, 528, 529, 534, 537] [UniProtKB: O00305, O00555, O43497, O60359, O60840, O95180, P54284, P54289, P62955, Q00975, Q01668, Q02641, Q06432, Q08289, Q13698, Q13936, Q15878, Q7Z3S7, Q8IZS8, Q8WXS5, Q9BXT2, Q9NY47, Q9P0X4, Q9UBN1, Q9UF02, Q9Y698]
ChEMBL Inhibition of VGCC (unknown origin) B 4.77 pIC50 17000 nM IC50 Eur J Med Chem (2019) 166: 381-389 [PMID:30739821]

ChEMBL data shown on this page come from version 34:

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]