lobeline [Ligand Id: 13498] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL122270 (.alpha.-lobeline, Alpha-Lobeline, Alpha-Lobeline HCl, Inflatine, Lobelina, (-)-Lobeline, Lobeline, Lobeline hydrochloride, Lobelinum, NSC-757421) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| Acetylcholine-binding protein in Lymnaea stagnalis (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6084] [UniProtKB: P58154] | ||||||||
| ChEMBL | Binding affinity to Lymnaea stagnalis AChBP after 300 seconds by SPR biosensor analysis | B | 6.2 | pKd | 630.96 | nM | Kd | Eur J Med Chem (2015) 102: 425-444 [PMID:26301559] |
| ChEMBL | Binding affinity to Lymnaea stagnalis AChBP after 300 seconds by SPR biosensor analysis | B | 6.2 | pKd | 630 | nM | Kd | Eur J Med Chem (2015) 102: 425-444 [PMID:26301559] |
| ChEMBL | Displacement of [3H]epibatidine from Lymnaea stagnalis acetylcholine binding protein expressed using baculoviral system after 1.5 hrs by scintillation counting | B | 6.2 | pKi | 630.96 | nM | Ki | Bioorg Med Chem Lett (2012) 22: 1448-1454 [PMID:22243960] |
| Acetylcholine receptor protein alpha chain in Torpedo californica (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3097] [UniProtKB: P02710] | ||||||||
| ChEMBL | Displacement of [3H]PCP from nAChR in Torpedo nobiliana electric organs membranes by scintillation counting method | B | 4.83 | pIC50 | 14900 | nM | IC50 | J Pestic Sci (1995) 20: 49-56 |
| ChEMBL | Displacement of [3H]PCP from nAChR in Torpedo nobiliana electric organs membranes in presence of 100 uM carbachol by scintillation counting method | B | 6 | pIC50 | 1010 | nM | IC50 | J Pestic Sci (1995) 20: 49-56 |
| DAT/Dopamine transporter in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL338] [GtoPdb: 927] [UniProtKB: P23977] | ||||||||
| ChEMBL | Inhibition of [3H]DA uptake at DAT in rat striatal synaptosomes | B | 4.55 | pKi | 28200 | nM | Ki | Bioorg Med Chem Lett (2006) 16: 5018-5021 [PMID:16905316] |
| ChEMBL | Inhibition of [3H]DA uptake at DAT in rat brain striatal synaptosomes by liquid scintillation spectrophotometry | B | 4.55 | pKi | 28200 | nM | Ki | Bioorg Med Chem (2010) 18: 640-649 [PMID:20036131] |
| H1 receptor/Histamine H1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL231] [GtoPdb: 262] [UniProtKB: P35367] | ||||||||
| ChEMBL | Antagonist activity at H1 receptor in human HeLa cells assessed as inhibition of histamine-induced Ca2+ release by using fura-2AM-based fluorescence assay | F | 4.35 | pIC50 | 44668.36 | nM | IC50 | J Med Chem (2012) 55: 7054-7060 [PMID:22793499] |
| H1 receptor/Histamine H1 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4701] [GtoPdb: 262] [UniProtKB: P31390] | ||||||||
| ChEMBL | Displacement of [3H]mepyramine from histamine H1 receptor in Sprague-Dawley rat brain membrane after 2 hr by scintillation counting | B | 4.95 | pIC50 | 11220.18 | nM | IC50 | J Med Chem (2012) 55: 7054-7060 [PMID:22793499] |
| nicotinic acetylcholine receptor α3 subunit/nicotinic acetylcholine receptor α4 subunit/nicotinic acetylcholine receptor α2 subunit/nicotinic acetylcholine receptor β2 subunit/nicotinic acetylcholine receptor β3 subunit/nicotinic acetylcholine receptor β4 subunit/nicotinic acetylcholine receptor α5 subunit/nicotinic acetylcholine receptor α6 subunit/nicotinic acetylcholine receptor α9 subunit/nicotinic acetylcholine receptor α7 subunit/nicotinic acetylcholine receptor α10 subunit in Human [GtoPdb: 464, 465, 463, 472, 473, 474, 466, 467, 469, 468, 470] [UniProtKB: P32297, P43681, Q15822, P17787, Q05901, P30926, P30532, Q15825, Q9UGM1, P36544, Q9GZZ6] | ||||||||
| GtoPdb | Binding affinity for α4β2 nAChR, mesuring [3H]epibatidine displacement | - | 8.3 | pKi | 5 | nM | Ki | Bioorg Med Chem Lett (2012) 22: 1448-54 [PMID:22243960] |
| nicotinic acetylcholine receptor α3 subunit/nicotinic acetylcholine receptor α4 subunit/nicotinic acetylcholine receptor α2 subunit/nicotinic acetylcholine receptor β2 subunit/nicotinic acetylcholine receptor β3 subunit/nicotinic acetylcholine receptor β4 subunit/nicotinic acetylcholine receptor α5 subunit/nicotinic acetylcholine receptor α6 subunit/nicotinic acetylcholine receptor α9 subunit/nicotinic acetylcholine receptor α7 subunit/nicotinic acetylcholine receptor α10 subunit/Neuronal acetylcholine receptor in Rat (target type: PROTEIN COMPLEX GROUP) [ChEMBL: CHEMBL2094110] [GtoPdb: 464, 465, 463, 472, 473, 474, 466, 467, 469, 468, 470] [UniProtKB: P04757, P09483, P12389, P12390, P12391, P12392, P20420, P43143, P43144, Q05941, Q9JLB5] | ||||||||
| ChEMBL | Evaluated for its binding affinity towards Nicotinic acetylcholine receptor in rat brain homogenate | B | 8.4 | pKi | 4 | nM | Ki | J Med Chem (1999) 42: 3726-3731 [PMID:10479304] |
| ChEMBL | Binding affinity towards nicotinic acetylcholine receptor using [125I]alpha-bungarotoxin as radioligand in rat forebrain homogenates | B | 4.74 | pIC50 | 18100 | nM | IC50 | Bioorg Med Chem Lett (2003) 13: 3847-3851 [PMID:14552793] |
| ChEMBL | Binding affinity towards nicotinic acetylcholine receptor using [3H]-cytisine as radioligand in rat forebrain homogenates | B | 7.06 | pIC50 | 87 | nM | IC50 | Bioorg Med Chem Lett (2003) 13: 3847-3851 [PMID:14552793] |
| 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 expressed in HEK293 cells after 4 hrs by scintillation counting assay | B | 6.3 | pKi | 501.19 | nM | Ki | Eur J Med Chem (2015) 102: 425-444 [PMID:26301559] |
| ChEMBL | Displacement of [3H]epibatidine from rat alpha3beta4 nACHR expressed in HEK293 cells after 4 hrs by scintillation counting assay | B | 6.32 | pKi | 480 | nM | Ki | Eur J Med Chem (2015) 102: 425-444 [PMID:26301559] |
| 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 nAChR alpha4beta2 receptor expressed in human HEK293T cells by scintillation counting | B | 8.3 | pKi | 5.01 | nM | Ki | Bioorg Med Chem Lett (2012) 22: 1448-1454 [PMID:22243960] |
| ChEMBL | Binding affinity to alpha4beta2 (unknown origin) | B | 8.3 | pKi | 5.01 | nM | Ki | Eur J Med Chem (2015) 102: 425-444 [PMID:26301559] |
| GtoPdb | Binding affinity for α4β2 nAChR, mesuring [3H]epibatidine displacement | - | 8.3 | pKi | 5 | nM | Ki | Bioorg Med Chem Lett (2012) 22: 1448-54 [PMID:22243960] |
| ChEMBL | Binding affinity to alpha4beta2 (unknown origin) | B | 8.3 | pKi | 5 | nM | Ki | Eur J Med Chem (2015) 102: 425-444 [PMID:26301559] |
| ChEMBL | Displacement of [3H]-nicotine from alpha4beta2 nicotine acetylcholine receptor (unknown origin) | B | 8.4 | pKi | 4 | nM | Ki | Bioorg Med Chem (2015) 23: 4375-4389 [PMID:26142318] |
| 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 | Inhibition of 3 nM [3H]NIC binding to Nicotinic acetylcholine receptor alpha4-beta2 of rat striatal membranes | B | 7.4 | pKi | 40 | nM | Ki | J Med Chem (2005) 48: 5551-5560 [PMID:16107155] |
| ChEMBL | Inhibition of [3H]NIC binding to alpha-4-beta-2 nAChR in rat brain membrane | B | 8.4 | pKi | 4 | nM | Ki | Bioorg Med Chem Lett (2006) 16: 5018-5021 [PMID:16905316] |
| ChEMBL | Displacement of [3H]nicotine from alpha4beta2 nAChR in rat brain homogenate by liquid scintillation spectrophotometry | B | 8.4 | pKi | 4 | nM | Ki | Bioorg Med Chem (2010) 18: 640-649 [PMID:20036131] |
| ChEMBL | Displacement of [3H]epibatidine from rat alpha4beta2 nAChR expressed in HEK293 cells after 4 hrs by scintillation counting assay | B | 8.66 | pKi | 2.2 | nM | Ki | Eur J Med Chem (2015) 102: 425-444 [PMID:26301559] |
| ChEMBL | Displacement of [3H]epibatidine from rat alpha4beta2 nAChR expressed in HEK293 cells after 4 hrs by scintillation counting assay | B | 8.7 | pKi | 2 | nM | Ki | Eur J Med Chem (2015) 102: 425-444 [PMID:26301559] |
| nicotinic acetylcholine receptor α4 subunit/nicotinic acetylcholine receptor β4 subunit in Human [GtoPdb: 465, 474] [UniProtKB: P43681, P30926] | ||||||||
| GtoPdb | Binding affinity for α4β2 nAChR, mesuring [3H]epibatidine displacement | - | 8.3 | pKi | 5 | nM | Ki | Bioorg Med Chem Lett (2012) 22: 1448-54 [PMID:22243960] |
| 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 expressed in HEK293 cells after 4 hrs by scintillation counting assay | B | 6.9 | pKi | 125.89 | nM | Ki | Eur J Med Chem (2015) 102: 425-444 [PMID:26301559] |
| ChEMBL | Displacement of [3H]epibatidine from rat alpha4beta4 nACHR expressed in HEK293 cells after 4 hrs by scintillation counting assay | B | 6.92 | pKi | 120 | nM | Ki | Eur J Med Chem (2015) 102: 425-444 [PMID:26301559] |
| 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]MLA from nAChR alpha7 receptor in human SH-SY5Y cells by scintillation counting | B | 5.1 | pKi | 7943.28 | nM | Ki | Bioorg Med Chem Lett (2012) 22: 1448-1454 [PMID:22243960] |
| 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 [3H]-methyllycaconitine from alpha7 nicotine acetylcholine receptor in rat brain membranes | B | 5.18 | pKi | 6600 | nM | Ki | Bioorg Med Chem (2015) 23: 4375-4389 [PMID:26142318] |
| ChEMBL | Inhibition of 3 nM [3H]-MLA binding to Nicotinic acetylcholine receptor alpha7 of rat brain membranes | B | 5.2 | pKi | 6260 | nM | Ki | J Med Chem (2005) 48: 5551-5560 [PMID:16107155] |
| ChEMBL | Inhibition of [3H]MLA binding to alpha-7 nAChR in rat brain membrane | B | 5.2 | pKi | 6260 | nM | Ki | Bioorg Med Chem Lett (2006) 16: 5018-5021 [PMID:16905316] |
| Nicotinic acetylcholine receptor alpha 5 subunit in Musca domestica (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2366408] [UniProtKB: A9XFY4] | ||||||||
| ChEMBL | Displacement of [3H]alpha-bungarotoxin from nAChR in Musca domestica (house fly) head membrane after 60 min by scintillation counting | B | 4.89 | pKi | 12800 | nM | Ki | J Pestic Sci (1992) 17: 231-236 |
| 5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223] | ||||||||
| ChEMBL | Displacement of [125I]DOI from human 5HT2A receptor expressed in HEK293 cell membranes | B | 5.13 | pKi | 7400 | nM | Ki | J Med Chem (2018) 61: 9121-9131 [PMID:30240563] |
| SERT/Serotonin transporter in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL313] [GtoPdb: 928] [UniProtKB: P31652] | ||||||||
| ChEMBL | Inhibition of [3H]5-HT uptake at SERT in rat hippocampal synaptosomes | B | 4.33 | pKi | 46800 | nM | Ki | Bioorg Med Chem Lett (2006) 16: 5018-5021 [PMID:16905316] |
| ChEMBL | Inhibition of [3H]5HT uptake at SERT in rat brain hippocampal synaptosomes by liquid scintillation spectrophotometry | B | 4.33 | pKi | 46800 | nM | Ki | Bioorg Med Chem (2010) 18: 640-649 [PMID:20036131] |
| Soluble acetylcholine receptor in Aplysia californica (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1944497] [UniProtKB: Q8WSF8] | ||||||||
| ChEMBL | Displacement of [3H]epibatidine from Aplysia californica acetylcholine binding protein expressed using baculoviral system after 1.5 hrs by scintillation counting | B | 8.6 | pKi | 2.51 | nM | Ki | Bioorg Med Chem Lett (2012) 22: 1448-1454 [PMID:22243960] |
| Vesicular monoamine transporter 2/Synaptic vesicular amine transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1893] [GtoPdb: 1012] [UniProtKB: Q05940] | ||||||||
| ChEMBL | Displacement of [3H]DHTB from human VMAT2 expressed in HEK293 cell membranes incubated for 90 mins by microbeta scintillation counting method | B | 5 | pKi | >10000 | nM | Ki | J Med Chem (2018) 61: 9121-9131 [PMID:30240563] |
| ChEMBL | Binding affinity to VMAT2 receptor | B | 5.56 | pKi | 2760 | nM | Ki | Bioorg Med Chem (2010) 18: 640-649 [PMID:20036131] |
| ChEMBL | Displacement of [3H](+)-syn-Ethyl 1-(2-(2,4-Dioxo-1,2-dihydroquinazolin-3(4H)-yl)ethyl)-4-(4-fluorophenyl)piperidine-3-carboxylate from human VMAT2 expressed in HEK293 cell membranes incubated for 60 mins by scintillation counting method | B | 5.71 | pKi | 1950 | nM | Ki | J Med Chem (2018) 61: 9121-9131 [PMID:30240563] |
| ChEMBL | Displacement of [3H]reserpine from human VMAT2 expressed in HEK293 cell membranes incubated for 60 mins by scintillation counting method | B | 5.74 | pKi | 1840 | nM | Ki | J Med Chem (2018) 61: 9121-9131 [PMID:30240563] |
| ChEMBL | Inhibition of human VMAT2 expressed in HEK293 cell membranes assessed as reduction in [3H[-5HT uptake pre-incubated for 10 mins before [3H[-5HT addition and measured after 6 mins | B | 5.38 | pIC50 | 4200 | nM | IC50 | J Med Chem (2018) 61: 9121-9131 [PMID:30240563] |
| Vesicular monoamine transporter 2/Synaptic vesicular amine transporter in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4295886] [GtoPdb: 1012] [UniProtKB: Q8BRU6] | ||||||||
| ChEMBL | Inhibition of VMAT2 in C57Bl/6J mouse striatal membranes assessed as reduction in [3H[-5HT uptake pre-incubated for 10 mins before [3H[-5HT addition and measured after 8 mins | B | 6.42 | pIC50 | 381 | nM | IC50 | J Med Chem (2018) 61: 9121-9131 [PMID:30240563] |
| Vesicular monoamine transporter 2/Synaptic vesicular amine transporter in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4828] [GtoPdb: 1012] [UniProtKB: Q01827] | ||||||||
| ChEMBL | Inhibition constant against [3H]methyllycaconitine binding to vesicular monoamine transporter-2 of rat brain membranes | B | 5.2 | pKi | 6260 | nM | Ki | Bioorg Med Chem Lett (2005) 15: 4463-4466 [PMID:16112864] |
| ChEMBL | Displacement of [3H]MTBZ from VMAT2 in rat whole brain vesicles by liquid scintillation spectrophotometry | B | 5.26 | pKi | 5460 | nM | Ki | Bioorg Med Chem (2010) 18: 640-649 [PMID:20036131] |
| ChEMBL | Inhibition of [3H]DTBZ binding to VMAT2 in rat synaptic vesicle membrane | B | 5.56 | pKi | 2760 | nM | Ki | Bioorg Med Chem Lett (2006) 16: 5018-5021 [PMID:16905316] |
| ChEMBL | Displacement of [3H]dihydrotetrabenazine from vesicular monoamine transporter-2 in rat brain synaptosome | B | 5.56 | pKi | 2760 | nM | Ki | Bioorg Med Chem Lett (2008) 18: 6509-6512 [PMID:18976906] |
| ChEMBL | Displacement of [3H]DTBZ from VMAT2 dihydrotetrabenazine binding site in rat brain synaptic vesicle by scintillation counting | B | 5.56 | pKi | 2760 | nM | Ki | J Med Chem (2009) 52: 7878-7882 [PMID:19691331] |
| ChEMBL | Inhibition of [3H]DTBZ binding to VMAT2 in rat synaptic vesicle membranes | B | 5.56 | pKi | 2760 | nM | Ki | Medchemcomm (2013) 4: 564-568 [PMID:23527317] |
| ChEMBL | Inhibition constant against [3H]dihydrotetrabenazine binding to vesicular monoamine transporter-2 of rat synaptic vesicle membranes | B | 5.56 | pKi | 2760 | nM | Ki | Bioorg Med Chem Lett (2005) 15: 4463-4466 [PMID:16112864] |
| ChEMBL | Inhibition of 5 nM [3H]DTBZ binding to Vesicular Monoamine Transporter (VAMT2) of rat vesicle membranes | B | 5.56 | pKi | 2760 | nM | Ki | J Med Chem (2005) 48: 5551-5560 [PMID:16107155] |
| ChEMBL | Inhibition of [3H]DA uptake at VMAT2 in rat striatal synaptic vesicles | B | 6.33 | pKi | 470 | nM | Ki | Medchemcomm (2013) 4: 564-568 [PMID:23527317] |
| ChEMBL | Inhibition of [3H]dopamine uptake at VMAT2 in rat brain synaptic vesicle by liquid scintillation spectroscopy | B | 6.33 | pKi | 470 | nM | Ki | J Med Chem (2009) 52: 7878-7882 [PMID:19691331] |
| ChEMBL | Inhibition constant against [3H]nicotine binding to vesicular monoamine transporter-2 of rat brain membranes | B | 8.4 | pKi | 4 | nM | Ki | Bioorg Med Chem Lett (2005) 15: 4463-4466 [PMID:16112864] |
ChEMBL data shown on this page come from version 34:
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]
