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ChEMBL ligand: CHEMBL134713 (3-(2,4-Dimethoxybenzylidene)Anabaseine, Dimethoxybenzylidene anabaseine, Dmxb-a, Gts-21) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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Acetylcholine-binding protein in Lymnaea stagnalis (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6084] [UniProtKB: P58154] | ||||||||
ChEMBL | Displacement of [3H]-epibatidine from Lymnaea stagnalis N-terminal FLAG-tagged AChBP expressed in HEK293 cells after 2 hrs by liquid scintillation counting | B | 7.72 | pKd | 19 | nM | Kd | Eur J Med Chem (2011) 46: 5625-5635 [PMID:21986237] |
nicotinic acetylcholine receptor α1 subunit/nicotinic acetylcholine receptor γ subunit/nicotinic acetylcholine receptor β1 subunit/nicotinic acetylcholine receptor δ subunit/Acetylcholine receptor; alpha1/beta1/delta/gamma in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL1907588] [GtoPdb: 462, 475, 471, 476] [UniProtKB: P02708, P07510, P11230, Q07001] | ||||||||
ChEMBL | Displacement of [3H]-epibatidine from alpha1betagammadelta nAChR in human TE671 cellular membranes after 2 hrs by liquid scintillation counting | B | 5.41 | pKi | 3900 | nM | Ki | Eur J Med Chem (2011) 46: 5625-5635 [PMID:21986237] |
ChEMBL | Displacement of [3H]epibatidine from human alpha1/beta/gamma/delta nAchR expressed in TE-671 cell membrane | B | 5.41 | pKi | 3900 | nM | Ki | Bioorg Med Chem Lett (2012) 22: 1179-1186 [PMID:22177081] |
nicotinic acetylcholine receptor β4 subunit/nicotinic acetylcholine receptor α3 subunit/Neuronal acetylcholine receptor; alpha3/beta4 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL1907594] [GtoPdb: 474, 464] [UniProtKB: P30926, P32297] | ||||||||
ChEMBL | Displacement of [3H]-epibatidine from alpha3beta4 nAChR in human SH-SY5Y cellular membranes after 2 hrs by liquid scintillation counting | B | 5.6 | pKi | 2500 | nM | Ki | Eur J Med Chem (2011) 46: 5625-5635 [PMID:21986237] |
ChEMBL | Displacement of [3H]epibatidine from human alpha3beta4 nAchR expressed in SH-SY5Y cells | B | 5.6 | pKi | 2500 | nM | Ki | Bioorg Med Chem Lett (2012) 22: 1179-1186 [PMID:22177081] |
ChEMBL | Effective concentration against Nicotinic acetylcholine receptor alpha3-beta4 | B | 5 | pEC50 | >10000 | nM | EC50 | J Med Chem (2005) 48: 4705-4745 [PMID:16033252] |
nicotinic acetylcholine receptor β2 subunit/nicotinic acetylcholine receptor α4 subunit/Neuronal acetylcholine receptor; alpha4/beta2 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL1907589] [GtoPdb: 472, 465] [UniProtKB: P17787, P43681] | ||||||||
ChEMBL | Displacement of [3H]epibatidine from human alpha4beta2 nAchR expressed in SH-EP1 cells | B | 7.29 | pKi | 51 | nM | Ki | Bioorg Med Chem Lett (2012) 22: 1179-1186 [PMID:22177081] |
ChEMBL | Effective concentration against Nicotinic acetylcholine receptor alpha4-beta2 | B | 5 | pEC50 | >10000 | nM | EC50 | J Med Chem (2005) 48: 4705-4745 [PMID:16033252] |
nicotinic acetylcholine receptor α4 subunit/nicotinic acetylcholine receptor β2 subunit/Neuronal acetylcholine receptor; alpha4/beta2 in Rat (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL1907596] [GtoPdb: 465, 472] [UniProtKB: P09483, P12390] | ||||||||
ChEMBL | Displacement of [3H]cytisine from alpha4beta2 nAChR in rat brain membrane after 3 hrs | B | 0.6 | pKi | 0.6 | uM | pKi | Eur J Med Chem (2010) 45: 2433-2446 [PMID:20236734] |
ChEMBL | Displacement of [3H]cytisine from alpha4beta2 nAChR in rat brain membrane after 3 hrs | B | 6.6 | pKi | 250 | nM | Ki | Eur J Med Chem (2010) 45: 2433-2446 [PMID:20236734] |
ChEMBL | Inhibition of [3H]cytisine binding to nicotinic acetylcholine receptor alpha4-beta2 from rat cerebral cortex | B | 7.08 | pKi | 84 | nM | Ki | J Med Chem (2005) 48: 2678-2686 [PMID:15801858] |
ChEMBL | Displacement of [3H]-epibatidine from alpha4beta2 nAChR in rat cortical membranes after 2 hrs by liquid scintillation counting | B | 7.29 | pKi | 51 | nM | Ki | Eur J Med Chem (2011) 46: 5625-5635 [PMID:21986237] |
nicotinic acetylcholine receptor β4 subunit/nicotinic acetylcholine receptor α4 subunit/Neuronal acetylcholine receptor; alpha4/beta4 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL1907591] [GtoPdb: 474, 465] [UniProtKB: P30926, P43681] | ||||||||
ChEMBL | Effective concentration against Nicotinic acetylcholine receptor alpha4-beta4 | B | 5 | pEC50 | >10000 | nM | EC50 | J Med Chem (2005) 48: 4705-4745 [PMID:16033252] |
nicotinic acetylcholine receptor α7 subunit/Neuronal acetylcholine receptor protein alpha-7 subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2492] [GtoPdb: 468] [UniProtKB: P36544] | ||||||||
ChEMBL | Displacement of [125I]alpha-bungarotoxin from alpha7 nAChR | B | 6.8 | pKd | 158 | nM | Kd | J Med Chem (2008) 51: 6293-6302 [PMID:18826295] |
ChEMBL | Partial agonist activity at human alpha7 nAChR expressed in Xenopus laevis oocytes incubated for 90 secs followed by washout period for 5 mins by electrophysiological method | B | 5.22 | pEC50 | 6000 | nM | EC50 | Eur J Med Chem (2018) 160: 37-48 [PMID:30317024] |
ChEMBL | Agonist activity at human recombinant alpha7 nAChR expressed in rat GH3 cells by calcium influx assay | F | 5.7 | pEC50 | 1995.26 | nM | EC50 | Bioorg Med Chem Lett (2009) 19: 1287-1291 [PMID:19208472] |
nicotinic acetylcholine receptor α7 subunit/Neuronal acetylcholine receptor protein alpha-7 subunit in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4980] [GtoPdb: 468] [UniProtKB: Q05941] | ||||||||
ChEMBL | Displacement of [125I]-alpha-bungarotoxin from alpha7 nAChR in rat brain membrane after 3 hrs | B | 0.89 | pKi | 0.89 | uM | pKi | Eur J Med Chem (2010) 45: 2433-2446 [PMID:20236734] |
ChEMBL | Displacement of [3H]-methyllycaconitine from alpha7 nAChR in rat hippocampal membranes after 2 hrs by liquid scintillation counting | B | 5.89 | pKi | 1300 | nM | Ki | Eur J Med Chem (2011) 46: 5625-5635 [PMID:21986237] |
ChEMBL | Inhibition of [125I]alpha-bungarotoxin binding to rat nicotinic acetylcholine receptor alpha7 | B | 6.66 | pKi | 220 | nM | Ki | J Med Chem (2005) 48: 2678-2686 [PMID:15801858] |
GtoPdb | Inhibition of [125I]alpha-bungarotoxin binding to rat α nAChR | - | 6.66 | pKi | 220 | nM | Ki | J Med Chem (2005) 48: 2678-86 [PMID:15801858] |
ChEMBL | Displacement of [125I]-alpha-bungarotoxin from alpha7 nAChR in rat brain membrane after 3 hrs | B | 6.89 | pKi | 130 | nM | Ki | Eur J Med Chem (2010) 45: 2433-2446 [PMID:20236734] |
ChEMBL data shown on this page come from version 33:
Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]