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| ChEMBL ligand: CHEMBL395280 ((-)-huperzine a, Huperzine a, L-huperzine a, (-)-selagine, Selagine) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| Acetylcholinesterase in Torpedo californica (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4780] [UniProtKB: P04058] | ||||||||
| ChEMBL | Inhibition of Torpedo californica AChE | B | 6.76 | pKi | 175 | nM | Ki | J Med Chem (2008) 51: 3154-3170 [PMID:18479118] |
| ChEMBL | Inhibition of Torpedo californica AChE | B | 6.76 | pKi | 175 | nM | Ki | J Med Chem (2008) 51: 3154-3170 [PMID:18479118] |
| ChEMBL | Inhibition of Torpedo california AChE by Ellman's method | B | 7.94 | pIC50 | 11.4 | nM | IC50 | Bioorg Med Chem (2009) 17: 6937-6941 [PMID:19726199] |
| Acetylcholinesterase in Electrophorus electricus (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4078] [UniProtKB: O42275] | ||||||||
| ChEMBL | Inhibition of electric eel AChE using acetylthiocholine chloride as a substrate incubated for 20 mins followed by substrate addition and measured after 20 mins by Ellman's method | B | 4.96 | pIC50 | 11000 | nM | IC50 | J Nat Prod (2021) 84: 2374-2379 [PMID:34445873] |
| ChEMBL | Inhibition of Electric eel AChE using acetylcholine iodide as substrate by spectrophotometry based Ellman's method | B | 5.29 | pIC50 | 5170 | nM | IC50 | Bioorg Med Chem Lett (2020) 30: 126985-126985 [PMID:32008906] |
| ChEMBL | Inhibition of electric eel AChE using acetylthiocholine chloride as substrate after 15 mins by Ellman's method | B | 6.92 | pIC50 | 120 | nM | IC50 | J Nat Prod (2011) 74: 997-1002 [PMID:21510637] |
| acetylcholinesterase (Yt blood group)/Acetylcholinesterase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL220] [GtoPdb: 2465] [UniProtKB: P22303] | ||||||||
| ChEMBL | Binding affinity to CM5 sensor chip immobilized recombinant human AChE assessed as dissociation constant at 298.15 K by surface plasmon resonance assay | B | 7.77 | pKd | 17 | nM | Kd | J Med Chem (2021) 64: 1844-1855 [PMID:33570950] |
| GtoPdb | - | - | 7.77 | pKd | 17 | nM | Kd | J Med Chem (2021) 64: 1844-1855 [PMID:33570950] |
| ChEMBL | Inhibition of human AChE | B | 7.33 | pKi | 47 | nM | Ki | J Med Chem (2006) 49: 3421-3425 [PMID:16722663] |
| ChEMBL | Inhibition of AChE (unknown origin) using acetylthiocholine iodide as substrate by DTNB reagent based Ellman's method | B | 5.28 | pIC50 | 5280 | nM | IC50 | Bioorg Med Chem Lett (2022) 72: 128873-128873 [PMID:35779827] |
| ChEMBL | Inhibition of AChE (unknown origin) using acetylthiocholine iodide as substrate after 5 mins by spectrophotometric analysis | B | 5.37 | pIC50 | 4300 | nM | IC50 | J Nat Prod (2019) 82: 792-797 [PMID:30794407] |
| ChEMBL | Inhibition of AChE by Ellman's method | B | 5.77 | pIC50 | 1700 | nM | IC50 | J Nat Prod (2010) 73: 1858-1862 [PMID:20954721] |
| ChEMBL | Inhibition of human acetylcholinesterase after 30 mins by microplate reader-based Ellman's method | B | 6.22 | pIC50 | 600 | nM | IC50 | J Nat Prod (2015) 78: 3067-3070 [PMID:26618211] |
| ChEMBL | Inhibition of AChE (unknown origin) using acetylthiocholine iodide as substrate preincubated for 10 mins followed by substrate addition measured after 10 mins by Ellman's method | B | 6.4 | pIC50 | 400 | nM | IC50 | J Nat Prod (2018) 81: 2115-2119 [PMID:30183289] |
| ChEMBL | Inhibitory concentration against Acetylcholinesterase from human erythrocytes | B | 6.59 | pIC50 | 260 | nM | IC50 | J Med Chem (2005) 48: 1701-1704 [PMID:15771413] |
| ChEMBL | In vitro inhibitory concentration against acetylcholinesterase of human erythrocytes | B | 6.59 | pIC50 | 260 | nM | IC50 | J Med Chem (2001) 44: 4733-4736 [PMID:11741490] |
| ChEMBL | Inhibition of human erythrocyte AChE | B | 6.59 | pIC50 | 260 | nM | IC50 | J Med Chem (2006) 49: 6833-6840 [PMID:17154513] |
| ChEMBL | Inhibition of acetylcholinesterase isolated from Human erythrocytes. | B | 6.59 | pIC50 | 260 | nM | IC50 | J Med Chem (2000) 43: 4657-4666 [PMID:11101357] |
| ChEMBL | Inhibitory activity against acetylcholinesterase in human RBC | B | 6.82 | pIC50 | 150 | nM | IC50 | Bioorg Med Chem Lett (1996) 6: 737-742 |
| ChEMBL | Inhibition of AChE (unknown origin) using acetylthiocholine iodide as substrate after 8 mins by Ellman's spectrophotometric method | B | 6.9 | pIC50 | 125 | nM | IC50 | J Nat Prod (2013) 76: 1475-1484 [PMID:23941108] |
| ChEMBL | Ex vivo inhibition of human erythrocyte Acetylcholinesterase. | B | 7.33 | pIC50 | 47 | nM | IC50 | J Med Chem (2002) 45: 3684-3691 [PMID:12166941] |
| ChEMBL | Inhibitory concentration against human erythrocyte Acetylcholinesterase | B | 7.33 | pIC50 | 47 | nM | IC50 | J Med Chem (2005) 48: 986-994 [PMID:15715468] |
| ChEMBL | Anticholinesterase activity against human erythrocyte AChE | B | 7.33 | pIC50 | 47 | nM | IC50 | J Med Chem (2006) 49: 2174-2185 [PMID:16570913] |
| ChEMBL | Inhibition of AChE (unknown origin) | B | 7.35 | pIC50 | 45 | nM | IC50 | Bioorg Med Chem Lett (2013) 23: 1544-1547 [PMID:23395652] |
| ChEMBL | Inhibition of human AChE using acetylthiocholine iodide as substrate measured for 1 min by Ellman's method | B | 7.48 | pIC50 | 33 | nM | IC50 | J Nat Prod (2019) 82: 239-248 [PMID:30701972] |
| ChEMBL | DRUGMATRIX: Acetylcholinesterase enzyme inhibition (substrate: acetylthiocholine) | B | 7.54 | pIC50 | 29 | nM | IC50 | DrugMatrix in vitro pharmacology data |
| ChEMBL | Inhibition of human AChE by Ellman's method | B | 7.68 | pIC50 | 21 | nM | IC50 | Bioorg Med Chem (2009) 17: 6937-6941 [PMID:19726199] |
| ChEMBL | Inhibition of human AChE pre-incubated for 10 mins before acetylthiocholine iodide substrate addition | B | 7.92 | pIC50 | 12 | nM | IC50 | J Nat Prod (2012) 75: 1400-1404 [PMID:22775474] |
| ChEMBL | Inhibition of AChE-induced amyloid beta aggregation | B | 8.3 | pIC50 | 5 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 2687-2691 [PMID:21216144] |
| ChEMBL | In vitro inhibitory activity against Acetylcholinesterase (AChE). | B | 8.3 | pIC50 | 5 | nM | IC50 | Bioorg Med Chem Lett (1996) 6: 1927-1930 |
| ChEMBL | Inhibition of AChE (unknown origin) | B | 8.3 | pIC50 | 5 | nM | IC50 | Bioorg Med Chem Lett (2015) 25: 4848-4853 [PMID:26159481] |
| ChEMBL | Inhibition of acetylcholinesterase (unknown origin) assessed as inhibition of acetylcholine hydrolysis after 30 mins by Ellmann's method | B | 9.27 | pIC50 | 0.54 | nM | IC50 | J Nat Prod (2014) 77: 2054-2059 [PMID:25222040] |
| Acetylcholinesterase in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4768] [UniProtKB: P23795] | ||||||||
| ChEMBL | Inhibitory constant against fetal bovine serum (FBS) acetylcholinesterase | B | 7.62 | pKi | 24 | nM | Ki | Bioorg Med Chem Lett (2002) 12: 1521-1523 [PMID:12031333] |
| ChEMBL | Dissociation constant for the inhibition of fetal bovine serum acetylcholinesterase was determined.. | B | 7.63 | pKi | 23.6 | nM | Ki | Bioorg Med Chem Lett (1996) 6: 259-262 |
| ChEMBL | Dissociation constant for the inhibition of fetal bovine serum acetylcholinesterase was determined.. | B | 8.23 | pKi | 5.9 | nM | Ki | Bioorg Med Chem Lett (1996) 6: 259-262 |
| ChEMBL | Binding affinity towards Acetylcholinesterase from fetal bovine serum | B | 8.23 | pKi | 5.9 | nM | Ki | Bioorg Med Chem Lett (2000) 10: 2467-2469 [PMID:11078202] |
| ChEMBL | Inhibition of bovine erythrocytes AChE using acetylthiocholine iodide as substrate incubated for 15 to 20 mins by Ellman's methods | B | 7 | pIC50 | 100 | nM | IC50 | J Nat Prod (2020) 83: 2831-2843 [PMID:32941036] |
| ChEMBL | Compound was evaluated for the inhibition of acetylcholinesterase of bovine erythrocytes | B | 7.13 | pIC50 | 74 | nM | IC50 | J Med Chem (2000) 43: 4657-4666 [PMID:11101357] |
| ChEMBL | In vitro inhibitory concentration against bovine acetylcholinesterase enzyme | B | 7.13 | pIC50 | 74 | nM | IC50 | J Med Chem (2001) 44: 4733-4736 [PMID:11741490] |
| ChEMBL | Inhibitory concentration against Acetylcholinesterase from bovine erythrocytes | B | 7.13 | pIC50 | 74 | nM | IC50 | J Med Chem (2005) 48: 1701-1704 [PMID:15771413] |
| ChEMBL | Inhibition of acetylcholinesterase (AChE)activity in bovine erythrocytes | B | 7.13 | pIC50 | 74 | nM | IC50 | J Med Chem (1999) 42: 3227-3242 [PMID:10464010] |
| ChEMBL | Inhibition of bovine AChE by Ellman's method | B | 7.13 | pIC50 | 74 | nM | IC50 | Bioorg Med Chem (2008) 16: 7450-7456 [PMID:18585045] |
| ChEMBL | Inhibition of bovine erythrocyte AChE | B | 7.13 | pIC50 | 74 | nM | IC50 | J Med Chem (2006) 49: 6833-6840 [PMID:17154513] |
| ChEMBL | Inhibition of bovine acetylcholinesterase | B | 7.28 | pIC50 | 53 | nM | IC50 | Bioorg Med Chem (2007) 15: 7803-7808 [PMID:17904850] |
| acetylcholinesterase (Yt blood group)/Acetylcholinesterase in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3198] [GtoPdb: 2465] [UniProtKB: P21836] | ||||||||
| ChEMBL | Inhibition of mouse AChE | B | 7.09 | pIC50 | 82 | nM | IC50 | J Med Chem (2013) 56: 7615-7624 [PMID:23984975] |
| acetylcholinesterase (Yt blood group)/Acetylcholinesterase in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3199] [GtoPdb: 2465] [UniProtKB: P37136] | ||||||||
| ChEMBL | Compound was tested for its ability to inhibit acetylcholinesterase (AChE) in rat brain; 0.024-0.040 uM | B | 7.62 | pKi | 24 | nM | Ki | Bioorg Med Chem Lett (2001) 11: 2627-2630 [PMID:11551765] |
| ChEMBL | Inhibition of rat cortex AChE using acetylthiocholine iodide as substrate after 20 mins by by Ellman's method | B | 6.92 | pIC50 | 120 | nM | IC50 | Bioorg Med Chem (2018) 26: 3117-3125 [PMID:29729987] |
| ChEMBL | Inhibition of rat AChE | B | 6.94 | pIC50 | 114 | nM | IC50 | J Med Chem (2008) 51: 3154-3170 [PMID:18479118] |
| ChEMBL | Inhibition of rat AChE | B | 6.94 | pIC50 | 114 | nM | IC50 | J Med Chem (2008) 51: 3154-3170 [PMID:18479118] |
| ChEMBL | Inhibitory potency against acetylcholinesterase (AChE) of rat cortex homogenate with ethopropazine as BChE inhibitor | B | 6.94 | pIC50 | 114 | nM | IC50 | Bioorg Med Chem Lett (1999) 9: 2335-2338 [PMID:10476864] |
| ChEMBL | Inhibition of AChE in rat cortex homogenate using acetylthiocholine iodide as substrate after 20 mins by Ellman's method | B | 7.01 | pIC50 | 98 | nM | IC50 | Eur J Med Chem (2018) 143: 33-47 [PMID:29172081] |
| ChEMBL | Inhibitory activity against acetylcholinesterase in rat brain | B | 7.03 | pIC50 | 94 | nM | IC50 | Bioorg Med Chem Lett (1996) 6: 737-742 |
| ChEMBL | Inhibition of rat cortex homogenate acetylcholinesterase by spectrophotometric method | B | 7.09 | pIC50 | 82 | nM | IC50 | Bioorg Med Chem (2020) 28: 115820-115820 [PMID:33120080] |
| ChEMBL | Inhibition of rat cortex AChE using acetylthiocholine iodide as substrate measured after 20 mins by Ellman's method | B | 7.09 | pIC50 | 82 | nM | IC50 | J Med Chem (2016) 59: 8326-8344 [PMID:27552582] |
| ChEMBL | In vitro inhibitory activity against Acetylcholinesterase (AChE) using rat brain hippocampal crude homogenates. | B | 7.1 | pIC50 | 80 | nM | IC50 | Bioorg Med Chem Lett (1998) 8: 1661-1664 [PMID:9873409] |
| ChEMBL | Acetylcholinesterase inhibitory activity in rat striatal homogenates | B | 7.1 | pIC50 | 80 | nM | IC50 | J Med Chem (1995) 38: 3645-3651 [PMID:7658452] |
| ChEMBL | Inhibition of AChE in rat cortex at pH 5 | B | 7.14 | pIC50 | 72.4 | nM | IC50 | Bioorg Med Chem (2007) 15: 1394-1408 [PMID:17126020] |
| ChEMBL | Inhibitory concentration against acetylcholinesterase of rat cortex homogenate | B | 7.14 | pIC50 | 72.4 | nM | IC50 | J Med Chem (2005) 48: 655-657 [PMID:15689148] |
| ChEMBL | Compound was tested for its ability to inhibit the action of acetylcholinesterase isolated from rat brain cortex | B | 7.15 | pIC50 | 71.5 | nM | IC50 | J Med Chem (1991) 34: 3399-3402 [PMID:1766006] |
| ChEMBL | Inhibition of AChE in Sprague-Dawley rat cortices using acetylthiocholine iodide as substrate by Ellman's method | B | 7.19 | pIC50 | 65 | nM | IC50 | Bioorg Med Chem (2013) 21: 676-683 [PMID:23273608] |
| ChEMBL | In vitro inhibitory concentration against rat cortex acetylcholinesterase | B | 7.28 | pIC50 | 53 | nM | IC50 | Bioorg Med Chem Lett (2005) 15: 3834-3837 [PMID:15993600] |
| ChEMBL | Compound was tested for its ability to inhibit the action of acetylcholinesterase isolated from rat brain cortex | B | 7.35 | pIC50 | 44.5 | nM | IC50 | J Med Chem (1991) 34: 3399-3402 [PMID:1766006] |
| Butyrylcholinesterase in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3403] [UniProtKB: Q9JKC1] | ||||||||
| ChEMBL | Inhibition of rat cortex homogenate BuChE by spectrophotometric method | B | 4.13 | pIC50 | 74430 | nM | IC50 | Bioorg Med Chem (2020) 28: 115820-115820 [PMID:33120080] |
| ChEMBL | Inhibition of BuChE in rat serum | B | 4.15 | pIC50 | 70200 | nM | IC50 | Bioorg Med Chem (2007) 15: 1394-1408 [PMID:17126020] |
| ChEMBL | In vitro inhibitory concentration against butyrylcholinesterase was determined using rat serum homogenate | B | 4.25 | pIC50 | 56200 | nM | IC50 | Bioorg Med Chem Lett (2005) 15: 3834-3837 [PMID:15993600] |
| ChEMBL | Inhibition of rat serum BChE using butyrylthiocholine iodide as substrate after 20 mins by by Ellman's method | B | 4.44 | pIC50 | 36400 | nM | IC50 | Bioorg Med Chem (2018) 26: 3117-3125 [PMID:29729987] |
| ChEMBL | Inhibition of BuChE in rat serum using butyrylthiocholine iodide as substrate after 20 mins by Ellman's method | B | 4.44 | pIC50 | 36400 | nM | IC50 | Eur J Med Chem (2018) 143: 33-47 [PMID:29172081] |
| butyrylcholinesterase/Cholinesterase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1914] [GtoPdb: 2471] [UniProtKB: P06276] | ||||||||
| ChEMBL | Inhibition of human BuChE | B | 6 | pKi | >1000 | nM | Ki | J Med Chem (2006) 49: 3421-3425 [PMID:16722663] |
| ChEMBL | Inhibition of BuChE (unknown origin) using butyrylthiocholine iodide as substrate by DTNB reagent based Ellman's method | B | 2 | pIC50 | >10000000 | nM | IC50 | Bioorg Med Chem Lett (2022) 72: 128873-128873 [PMID:35779827] |
| ChEMBL | Inhibition of butyrylcholinesterase (BChE) activity in human serum | B | 4 | pIC50 | >100000 | nM | IC50 | J Med Chem (1999) 42: 3227-3242 [PMID:10464010] |
| ChEMBL | Inhibition of human BuChE using butyrylthiocholine iodide as substrate measured for 1 min by Ellman's method | B | 4 | pIC50 | >100000 | nM | IC50 | J Nat Prod (2019) 82: 239-248 [PMID:30701972] |
| ChEMBL | Inhibitory concentration against human plasma Butyrylcholinesterase | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2005) 48: 986-994 [PMID:15715468] |
| ChEMBL | Ex vivo inhibition of human plasma Butyrylcholinesterase. | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2002) 45: 3684-3691 [PMID:12166941] |
| ChEMBL | Anticholinesterase activity against human plasma BChE | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2006) 49: 2174-2185 [PMID:16570913] |
| ChEMBL | Inhibition of human serum BChE | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2006) 49: 6833-6840 [PMID:17154513] |
| ChEMBL | Inhibitory concentration against Butyrylcholinesterase from human erythrocytes | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2005) 48: 1701-1704 [PMID:15771413] |
| ChEMBL | Inhibition of butyrylcholinesterase (BChE) in human serum | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2000) 43: 4657-4666 [PMID:11101357] |
| ChEMBL | In vitro inhibitory concentration against BChE of human serum | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2001) 44: 4733-4736 [PMID:11741490] |
| ChEMBL | Inhibition of BChE | B | 7 | pIC50 | 100 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 2687-2691 [PMID:21216144] |
ChEMBL data shown on this page come from version 36:
Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]