Co-Target(s) Information
| Target General Information | Top | ||||
|---|---|---|---|---|---|
| Target ID | T30082 | Target Info | |||
| Target Name | Acetylcholinesterase (AChE) | ||||
| Synonyms |
YT; N-ACHE; ARACHE
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| Target Type | Successful Target | ||||
| Gene Name | ACHE | ||||
| Biochemical Class | Carboxylic ester hydrolase | ||||
| UniProt ID | |||||
| Co-Targets of This Target | Top | |||||
|---|---|---|---|---|---|---|
| Co-Target Name | Cholinesterase (BCHE) | Successful Target | ||||
| UniProt ID | CHLE_HUMAN | |||||
| Gene Name | BCHE | |||||
| Synonyms |
Pseudocholinesterase; Choline esterase II; CHE1; Butyrylcholine esterase; Acylcholine acylhydrolase
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| Representative Drug(s) | Tacrine | Drug Info | IC50 = 0.0267 nM | Click to Show More | [1] | |
| 2 | Galantamine | Drug Info | IC50 = 0.38 ug.mL-1 | [2] | ||
| 3 | Eptastigmine | Drug Info | IC50 = 0.69 nM | [3] | ||
| 4 | Donepezil | Drug Info | IC50 = 14 nM | [5] | ||
| 5 | Rivastigmine | Drug Info | IC50 = 30 nM | [7] | ||
| 6 | Pyridostigmine | Drug Info | IC50 = 900 nM | [8] | ||
| Co-Target Name | Amyloid beta A4 protein (APP) | Successful Target | ||||
| UniProt ID | A4_HUMAN | |||||
| Gene Name | APP | |||||
| Synonyms |
Protease nexin-II; PreA4; PN-II; Cerebral vascular amyloid peptide; CVAP; Amyloid-beta precursor protein; Amyloid-beta A4 protein; Alzheimer disease amyloid protein; APPI; APP; AD1; ABPP; A4
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| Representative Drug(s) | Tacrine | Drug Info | IC50 = 12.21 nM | [4] | ||
| Co-Target Name | Opioid receptor sigma 1 (OPRS1) | Successful Target | ||||
| UniProt ID | SGMR1_HUMAN | |||||
| Gene Name | SIGMAR1 | |||||
| Synonyms |
hSigmaR1; Sigma1R; Sigma1-receptor; Sigma non-opioid intracellular receptor 1; Sigma 1-type opioid receptor; SRBP; SR31747-binding protein; SR31747 binding protein 1; SR-BP; SIG-1R; Opioid receptor, sigma 1, isoform 1; OPRS1 protein; Aging-associated gene 8 protein; AAG8
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| Representative Drug(s) | Donepezil | Drug Info | Ki = 14.6 nM | [6] | ||
| Co-Target Name | Cannabinoid receptor 1 (CB1) | Successful Target | ||||
| UniProt ID | CNR1_HUMAN | |||||
| Gene Name | CNR1 | |||||
| Synonyms |
Cannabinoid CB1 receptor; CNR; CB-R; CANN6
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| Representative Drug(s) | Tacrine | Drug Info | Ki ~ 1000 nM | [9] | ||
| Co-Target Name | Cannabinoid receptor 2 (CB2) | Successful Target | ||||
| UniProt ID | CNR2_HUMAN | |||||
| Gene Name | CNR2 | |||||
| Synonyms |
hCB2; Cannabinoid CB2 receptor; CX5; CB2B; CB2A; CB-2
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| Representative Drug(s) | Tacrine | Drug Info | Ki ~ 1000 nM | [9] | ||
| Co-Target Name | Serotonin transporter (SERT) | Successful Target | ||||
| UniProt ID | SC6A4_HUMAN | |||||
| Gene Name | SLC6A4 | |||||
| Synonyms |
Solute carrier family 6 member 4; HTT; 5HTT; 5HT transporter
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| Representative Drug(s) | Rivastigmine | Drug Info | IC50 ~ 1000 nM | [10] | ||
| Co-Target Name | Beta-secretase 1 (BACE1) | Clinical trial Target | ||||
| UniProt ID | BACE1_HUMAN | |||||
| Gene Name | BACE1 | |||||
| Synonyms |
Membrane-associated aspartic protease 2; Memapsin-2; KIAA1149; Beta-site amyloid precursor protein cleaving enzyme 1; Beta-site APP cleaving enzyme 1; BACE; Aspartyl protease 2; Asp 2; ASP2
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| Representative Drug(s) | Donepezil | Drug Info | IC50 = 169 nM | [11] | ||
| Co-Target Name | Histamine H3 receptor (H3R) | Clinical trial Target | ||||
| UniProt ID | HRH3_HUMAN | |||||
| Gene Name | HRH3 | |||||
| Synonyms |
Histamine receptor 3; HH3R; GPCR97; G-protein coupled receptor 97; G protein-coupled receptor 97
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| Representative Drug(s) | Donepezil | Drug Info | IC50 = 350 nM | [12] | ||
| Co-Target Name | Acetylcholine receptor protein epsilon chain (CHRNE) | Co-Target | ||||
| UniProt ID | ACHE_HUMAN | |||||
| Gene Name | CHRNE | |||||
| Synonyms |
Acetylcholine receptor subunit epsilon
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| Representative Drug(s) | Galantamine | Drug Info | IC50 = 0.767 ug.mL-1 | Click to Show More | [13] | |
| 2 | Tacrine | Drug Info | IC50 = 44 nM | [14] | ||
| Co-Target Name | Solute carrier family 22 member 2 (SLC22A2) | Co-Target | ||||
| UniProt ID | S22A2_HUMAN | |||||
| Gene Name | SLC22A2 | |||||
| Synonyms |
Organic cation transporter 2; hOCT2
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| Representative Drug(s) | Tacrine | Drug Info | IC50 = 680 nM | [15] | ||
| References | Top | ||||
|---|---|---|---|---|---|
| REF 1 | Synthesis, biological activity and HPLC validation of 1,2,3,4-tetrahydroacridine derivatives as acetylcholinesterase inhibitors. Eur J Med Chem. 2011 Aug;46(8):3250-7. | ||||
| REF 2 | New septanoside and 20-hydroxyecdysone septanoside derivative from Atriplex portulacoides roots with preliminary biological activities. Bioorg Med Chem Lett. 2015 Apr 15;25(8):1665-70. | ||||
| REF 3 | Synthesis and preliminary structure-activity relationships of 1-[(3-fluoro-4-pyridinyl)amino]-3-methyl-1H-indol-5-yl methyl carbamate (P10358), a novel acetylcholinesterase inhibitor. Bioorg Med Chem Lett. 1997 Jan 21;7(2):157-62. | ||||
| REF 4 | Design, synthesis and evaluation of novel tacrine-multialkoxybenzene hybrids as multi-targeted compounds against Alzheimer's disease. Eur J Med Chem. 2016 Jun 30;116:200-9. | ||||
| REF 5 | Anti-cholinesterase hybrids as multi-target-directed ligands against Alzheimer's disease (1998-2018). Bioorg Med Chem. 2019 Mar 15;27(6):895-930. | ||||
| REF 6 | Synthesis and biological evaluation of 2-(5-methyl-4-phenyl-2-oxopyrrolidin-1-yl)-acetamide stereoisomers as novel positive allosteric modulators of sigma-1 receptor. Bioorg Med Chem. 2013 May 15;21(10):2764-71. | ||||
| REF 7 | Discovery, biological evaluation, and crystal structure of a novel nanomolar selective butyrylcholinesterase inhibitor. J Med Chem. 2014 Oct 9;57(19):8167-79. | ||||
| REF 8 | Long-acting anticholinesterases for myasthenia gravis: synthesis and activities of quaternary phenylcarbamates of neostigmine, pyridostigmine and physostigmine. Bioorg Med Chem. 2010 Jul 1;18(13):4687-93. | ||||
| REF 9 | Design, synthesis, biological properties, and molecular modeling investigations of novel tacrine derivatives with a combination of acetylcholineste... J Med Chem. 2010 Feb 11;53(3):1338-46. | ||||
| REF 10 | Multi-target-directed ligands to combat neurodegenerative diseases. J Med Chem. 2008 Feb 14;51(3):347-72. | ||||
| REF 11 | Multipotent AChE and BACE-1 inhibitors for the treatment of Alzheimer's disease: Design, synthesis and bio-analysis of 7-amino-1,4-dihydro-2H-isoquilin-3-one derivates. Eur J Med Chem. 2017 Sep 29;138:738-47. | ||||
| REF 12 | Lead identification of acetylcholinesterase inhibitors-histamine H3 receptor antagonists from molecular modeling. Bioorg Med Chem. 2008 Mar 15;16(6):2968-73. | ||||
| REF 13 | Triazole derivatives as inhibitors of Alzheimer's disease: Current developments and structure-activity relationships. Eur J Med Chem. 2019 Oct 15;180:656-672. | ||||
| REF 14 | Random chemistry as a new tool for the generation of small compound libraries: development of a new acetylcholinesterase inhibitor. J Med Chem. 2005 Nov 17;48(23):7496-9. | ||||
| REF 15 | Profiling of a prescription drug library for potential renal drug-drug interactions mediated by the organic cation transporter 2. J Med Chem. 2011 Jul 14;54(13):4548-58. | ||||
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