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ChEMBL ligand: CHEMBL293950 (Dihydro-Beta-Erythroidine) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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nicotinic acetylcholine receptor α3 subunit/nicotinic acetylcholine receptor β4 subunit/Neuronal acetylcholine receptor; alpha3/beta4 in Rat (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL1907593] [GtoPdb: 464, 474] [UniProtKB: P04757, P12392] | ||||||||
ChEMBL | Displacement of [3H]epibatidine from rat alpha3beta4 nAChR transfected in HEK293 cells after 4 hrs by scintillation count analysis | B | 4 | pKi | 100000 | nM | Ki | ACS Med Chem Lett (2014) 5: 766-770 [PMID:25050162] |
ChEMBL | Activity at rat alpha3beta4 nicotinic receptor expressed in KXalpha-3-beta-4R2 cells assessed as nicotine-induced 86Rb+ efflux | B | 4 | pIC50 | 100000 | nM | IC50 | J Nat Prod (2006) 69: 1514-1516 [PMID:17067175] |
ChEMBL | Antagonist activity at rat alpha3beta4 nAChR transfected in HEK293 cells by FLIPR membrane potential blue (FMP) assay | B | 4 | pIC50 | 100000 | nM | IC50 | ACS Med Chem Lett (2014) 5: 766-770 [PMID:25050162] |
ChEMBL | Antagonist activity at rat alpha3beta4 nAChR | B | 4.64 | pIC50 | 23000 | nM | IC50 | J Med Chem (2014) 57: 8204-8223 [PMID:24901260] |
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]cytisine from alpha4/beta2 nAChR (unknown origin) | B | 7.01 | pKi | 98 | nM | Ki | J Med Chem (2013) 56: 9673-9682 [PMID:24187998] |
ChEMBL | Antagonist activity at (alpha4beta2)2beta2 nAChR (unknown origin) expressed in Xenopus oocytes assessed as inhibition of acetylcholine-induced current after 2 mins by two-electrode voltage clamp assay | B | 6.39 | pIC50 | 410 | nM | IC50 | Bioorg Med Chem (2013) 21: 2687-2694 [PMID:23561269] |
ChEMBL | Antagonist activity at (alpha4beta2)2alpha4 nAChR (unknown origin) expressed in Xenopus oocytes assessed as inhibition of acetylcholine-induced current after 2 mins by two-electrode voltage clamp assay | B | 7.7 | pIC50 | 20 | nM | IC50 | Bioorg Med Chem (2013) 21: 2687-2694 [PMID:23561269] |
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]epibatidine from rat alpha4beta2 nAChR transfected in HEK293 cells after 4 hrs by scintillation count analysis | B | 6.09 | pKi | 820 | nM | Ki | ACS Med Chem Lett (2014) 5: 766-770 [PMID:25050162] |
ChEMBL | Inhibition of rat membrane alpha4beta2 nAChR by [3H]cytisine binding assay | B | 6.85 | pKi | 140 | nM | Ki | ACS Med Chem Lett (2014) 5: 766-770 [PMID:25050162] |
ChEMBL | Antagonist activity at rat alpha4beta2 nAChR | B | 7.52 | pIC50 | 30 | nM | IC50 | J Med Chem (2014) 57: 8204-8223 [PMID:24901260] |
nicotinic acetylcholine receptor α4 subunit/nicotinic acetylcholine receptor β4 subunit/Neuronal acetylcholine receptor; alpha4/beta4 in Rat (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL1907595] [GtoPdb: 465, 474] [UniProtKB: P09483, P12392] | ||||||||
ChEMBL | Displacement of [3H]epibatidine from rat alpha4beta4 nAChR transfected in HEK293 cells after 4 hrs by scintillation count analysis | B | 4 | pKi | 100000 | nM | Ki | ACS Med Chem Lett (2014) 5: 766-770 [PMID:25050162] |
nicotinic acetylcholine receptor α4 subunit/Neuronal acetylcholine receptor protein alpha-4 subunit in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL307] [GtoPdb: 465] [UniProtKB: P09483] | ||||||||
ChEMBL | Blockade of Nicotinic acetylcholine receptor alpha4-beta2 | B | 8.44 | pIC50 | 3.66 | nM | IC50 | Bioorg Med Chem Lett (2004) 14: 1879-1887 [PMID:15050620] |
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 [3H]cytisine from alpha7 nAChR (unknown origin) | B | 4.98 | pKi | 10500 | nM | Ki | J Med Chem (2013) 56: 9673-9682 [PMID:24187998] |
nicotinic acetylcholine receptor β4 subunit/nicotinic acetylcholine receptor β2 subunit/Nicotinic acetylcholine receptor alpha-4/beta-2 in Mouse (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL3301382] [GtoPdb: 474, 472] [UniProtKB: Q8R493, Q9ERK7] | ||||||||
ChEMBL | Antagonist activity at mouse alpha4beta2 nAChR transfected in HEK293 cells by FLIPR membrane potential blue (FMP) assay | B | 5.92 | pIC50 | 1200 | nM | IC50 | ACS Med Chem Lett (2014) 5: 766-770 [PMID:25050162] |
nicotinic acetylcholine receptor β2 subunit/nicotinic acetylcholine receptor α5 subunit/nicotinic acetylcholine receptor α4 subunit/Nicotinic acetylcholine receptor alpha4/beta2/alpha5 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL3038461] [GtoPdb: 472, 466, 465] [UniProtKB: P17787, P30532, P43681] | ||||||||
ChEMBL | Antagonist activity at (alpha4beta2)2alpha5 nAChR (unknown origin) expressed in Xenopus oocytes assessed as inhibition of acetylcholine-induced current after 2 mins by two-electrode voltage clamp assay | B | 7.96 | pIC50 | 11 | nM | IC50 | Bioorg Med Chem (2013) 21: 2687-2694 [PMID:23561269] |
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]