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ChEMBL ligand: CHEMBL1162395 |
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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 | 9.4 | pKd | 0.4 | nM | Kd | Eur J Med Chem (2011) 46: 5625-5635 [PMID:21986237] |
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 | 6.01 | pKi | 970 | 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 | 6.01 | pKi | 970 | nM | Ki | Bioorg Med Chem Lett (2012) 22: 1179-1186 [PMID:22177081] |
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 | 7.72 | pKi | 19 | nM | Ki | Bioorg Med Chem Lett (2012) 22: 1179-1186 [PMID:22177081] |
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 | 1.16 | pKi | 1.16 | 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 | 7.15 | pKi | 70 | nM | Ki | Eur J Med Chem (2010) 45: 2433-2446 [PMID:20236734] |
ChEMBL | Displacement of [3H]-epibatidine from alpha4beta2 nAChR in rat cortical membranes after 2 hrs by liquid scintillation counting | B | 7.72 | pKi | 19 | nM | Ki | Eur J Med Chem (2011) 46: 5625-5635 [PMID:21986237] |
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 | 7.64 | pKd | 23 | nM | Kd | J Med Chem (2008) 51: 6293-6302 [PMID:18826295] |
ChEMBL | Agonist activity at human cloned wild-type alpha7 nAChR expressed in Xenopus laevis oocytes assessed as channel opening by voltage clamp electrophysiology | F | 5.52 | pEC50 | 3000 | nM | EC50 | J Med Chem (2008) 51: 6293-6302 [PMID:18826295] |
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 | 0.62 | pKi | 0.62 | 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 | 6.38 | pKi | 420 | nM | Ki | Eur J Med Chem (2011) 46: 5625-5635 [PMID:21986237] |
GtoPdb | Displacement of [3H]-methyllycaconitine from rat α7 nAChR in hippocampal membranes by liquid scintillation counting | - | 6.38 | pKi | 420 | nM | Ki | Eur J Med Chem (2011) 46: 5625-35 [PMID:21986237] |
ChEMBL | Displacement of [125I]-alpha-bungarotoxin from alpha7 nAChR in rat brain membrane after 3 hrs | B | 6.62 | pKi | 240 | nM | Ki | Eur J Med Chem (2010) 45: 2433-2446 [PMID:20236734] |
ChEMBL | Agonist activity at rat recombinant alpha7 nAChR expressed in GH4C1 cells by patch clamp technique | F | 5.8 | pEC50 | 1600 | nM | EC50 | Eur J Med Chem (2011) 46: 5625-5635 [PMID:21986237] |
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]