[3H]epibatidine [Ligand Id: 3977] activity data from GtoPdb and ChEMBL
Click here for a description of the charts and data table
Please tell us if you are using this feature and what you think!
| ChEMBL ligand: CHEMBL6623 |
|---|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| 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 freshwater snail Lymnaea stagnalis AChBP assessed as [3H]EPI binding by radioligand binding assay | B | 9.52 | pKi | 0.3 | nM | Ki | J Agric Food Chem (2011) 59: 2825-2828 [PMID:21341671] |
| Acetylcholine receptor in Torpedo californica (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2096975] [UniProtKB: P02710, P02712, P02714, P02718] | ||||||||
| ChEMBL | Binding potency for nAChR subtype Alpha-1-beta-1-delta gamma(torpedo) | B | 8.57 | pKi | 2.7 | nM | Ki | J Med Chem (1997) 40: 4169-4194 [PMID:9435889] |
| ChEMBL | Functional potency for nAChR subtype Alpha-1-beta-1-delta gamma (torpedo) | B | 6.7 | pEC50 | 200 | nM | EC50 | J Med Chem (1997) 40: 4169-4194 [PMID:9435889] |
| 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 | Change in membrane potential in TE-671 cells expressing acetylcholine neuromuscular receptors | F | 10.28 | pEC50 | 0.05 | nM | EC50 | Bioorg Med Chem Lett (2005) 15: 1221-1224 [PMID:15686946] |
| nicotinic acetylcholine receptor α1 subunit/Acetylcholine receptor protein alpha chain in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4808] [GtoPdb: 462] [UniProtKB: P02708] | ||||||||
| ChEMBL | Inhibition of [3H]alpha-BGT binding to alpha1 nicotinic acetylcholine receptor in Homo sapiens (human) TE671 cells co-expressing gammaalpha1deltabeta1 nicotinic acetylcholine receptor subunits | B | 6.8 | pIC50 | 160 | nM | IC50 | J Agric Food Chem (2000) 48: 6016-6024 [PMID:11312774] |
| Acetylcholine receptor protein delta chain in Torpedo californica (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3916] [UniProtKB: P02718] | ||||||||
| ChEMBL | Agonist activity against Nicotinic acetylcholine receptor (nAchR) | F | 10 | pKi | 0.1 | nM | Ki | J Med Chem (1999) 42: 1481-1500 [PMID:10229619] |
| ChEMBL | Compound was evaluated for functional potencies and efficacies at human Nicotinic acetylcholine receptor subtype TE671 (muscle) | B | 6.7 | pEC50 | 200 | nM | EC50 | J Med Chem (1997) 40: 4169-4194 [PMID:9435889] |
| Acetylcholine receptor subunit beta-like 2 in Drosophila melanogaster (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2366470] [UniProtKB: P25162] | ||||||||
| ChEMBL | Binding affinity to Drosophila brain nicotinic acetylcholine receptor assessed as [3H]IMI binding by radioligand binding assay | B | 6.54 | pKi | 290 | nM | Ki | J Agric Food Chem (2011) 59: 2825-2828 [PMID:21341671] |
| ChEMBL | Inhibition of [3H]IMI binding to Drosophila melanogaster neuronal acetylcholine receptor | B | 6.37 | pIC50 | 430 | nM | IC50 | J Agric Food Chem (2000) 48: 6016-6024 [PMID:11312774] |
| 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 Chicken [GtoPdb: 464, 465, 463, 472, 473, 474, 466, 467, 469, 468, 470] | ||||||||
| GtoPdb | - | - | 10.46 | pKd | 0.04 | nM | Kd | |
| 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 | - | - | 9.64 | pKd | 0.23 | nM | Kd | |
| GtoPdb | - | - | 9.73 | pKd | 0.19 | nM | Kd | |
| GtoPdb | - | - | 10.38 | pKd | 0.04 | nM | Kd | |
| GtoPdb | - | - | 11 | pKd | 0.01 | nM | Kd | |
| GtoPdb | - | - | 11.15 | pKd | 0.01 | nM | Kd | |
| GtoPdb | - | - | 12.22 | pKd | 0 | nM | Kd | |
| 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] | ||||||||
| GtoPdb | - | - | 9.07 | pKd | 0.85 | nM | Kd | |
| GtoPdb | - | - | 9.52 | pKd | 0.3 | nM | Kd | |
| GtoPdb | - | - | 9.54 | pKd | 0.29 | nM | Kd | |
| GtoPdb | - | - | 10.08 | pKd | 0.08 | nM | Kd | |
| ChEMBL | Kapp value towards nicotinic acetylcholine receptor was obtained from three to four independent competition binding experiments using [3H]-NCEPB | B | 10.62 | pKd | 0.02 | nM | K app | J Med Chem (1997) 40: 2293-2295 [PMID:9240344] |
| GtoPdb | - | - | 10.85 | pKd | 0.01 | nM | Kd | |
| GtoPdb | - | - | 11 | pKd | 0.01 | nM | Kd | |
| ChEMBL | Binding affinity towards rat forebrain nicotinic acetylcholine receptor using [3H]EB as radioligand | B | 9.54 | pKi | 0.29 | nM | Ki | Bioorg Med Chem Lett (2004) 14: 1845-1848 [PMID:15050613] |
| ChEMBL | Binding affinity towards rat forebrain nicotinic acetylcholine receptor using [3H]EB as radioligand | B | 10.19 | pKi | 0.06 | nM | Ki | Bioorg Med Chem Lett (2004) 14: 1845-1848 [PMID:15050613] |
| ChEMBL | Compound was evaluated for its ability to displace [3H]-cytisine binding from high-affinity Nicotinic acetylcholine receptor in rat brain (principally the alpha4-beta2 nAChR subtype) | B | 10.37 | pKi | 0.04 | nM | Ki | J Med Chem (1998) 41: 407-412 [PMID:9484491] |
| ChEMBL | Binding affinity against Nicotinic Acetylcholine Receptor was determined by measuring the displacement of [3H]cytisine from a preparation of whole rat brain. | B | 10.37 | pKi | 0.04 | nM | Ki | J Med Chem (1996) 39: 817-825 [PMID:8632405] |
| ChEMBL | Displacement of [3H]epibatidine from rat forebrain nAChR after 4 hrs by liquid scintillation counting method | B | 10.39 | pKi | 0.04 | nM | Ki | J Nat Prod (2018) 81: 1029-1035 [PMID:29671588] |
| ChEMBL | Binding affinity against nicotinic acetylcholine receptor using [3H]epibatidine as radioligand in rat brain tissue | B | 10.47 | pKi | 0.03 | nM | Ki | Bioorg Med Chem Lett (2004) 14: 271-273 [PMID:14684341] |
| ChEMBL | Compound was evaluated for potency towards nicotinic acetylcholine receptor in rat P2 brain membranes using [3H]nicotine as a radioligand | B | 10.68 | pKi | 0.02 | nM | Ki | Bioorg Med Chem Lett (1997) 7: 2867-2870 |
| ChEMBL | Binding affinity towards nicotinic acetylcholine receptor using [125I]alpha-bungarotoxin as radioligand in rat forebrain homogenates | B | 8.43 | pIC50 | 3.7 | 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 | 9.1 | pIC50 | 0.8 | nM | IC50 | Bioorg Med Chem Lett (2003) 13: 3847-3851 [PMID:14552793] |
| ChEMBL | In vitro displacement of [3H]methylcarbamylcholine from nicotinic acetylcholine receptor in rat brain cortex | B | 9.52 | pIC50 | 0.3 | nM | IC50 | J Med Chem (1999) 42: 4970-4980 [PMID:10585207] |
| ChEMBL | Compound was evaluated for inhibitory activity towards nicotinic acetylcholine receptor in rat P2 brain membranes using [3H]nicotine as a radioligand | B | 10.39 | pIC50 | 0.04 | nM | IC50 | Bioorg Med Chem Lett (1997) 7: 2867-2870 |
| ChEMBL | Compound was evaluated for functional potencies and efficacies at rat Nicotinic acetylcholine receptor subtype PC12 (ganglionic) | B | 7 | pEC50 | 100 | nM | EC50 | J Med Chem (1997) 40: 4169-4194 [PMID:9435889] |
| nicotinic acetylcholine receptor α2 subunit/nicotinic acetylcholine receptor β2 subunit in Human [GtoPdb: 463, 472] [UniProtKB: Q15822, P17787] | ||||||||
| GtoPdb | - | - | 10.38 | pKd | 0.04 | nM | Kd | |
| nicotinic acetylcholine receptor α2 subunit/nicotinic acetylcholine receptor β2 subunit/Neuronal acetylcholine receptor; alpha2/beta2 in Rat (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL1907592] [GtoPdb: 463, 472] [UniProtKB: P12389, P12390] | ||||||||
| GtoPdb | - | - | 10.08 | pKd | 0.08 | nM | Kd | |
| ChEMBL | Tested for binding affinity against Nicotinic acetylcholine receptor alpha2-beta2 | B | 10.7 | pKd | 0.02 | nM | Kd | J Med Chem (2003) 46: 921-924 [PMID:12620069] |
| GtoPdb | - | - | 11 | pKd | 0.01 | nM | Kd | |
| ChEMBL | Binding affinity towards rat nicotinic acetylcholine receptor alpha2-beta2 expressed in HEK293 cells using [3H]EB as radioligand | B | 9.96 | pKi | 0.11 | nM | Ki | Bioorg Med Chem Lett (2004) 14: 1845-1848 [PMID:15050613] |
| ChEMBL | Binding affinity towards rat nicotinic acetylcholine receptor alpha2-beta2 expressed in HEK293 cells using [3H]EB as radioligand | B | 10.59 | pKi | 0.03 | nM | Ki | Bioorg Med Chem Lett (2004) 14: 1845-1848 [PMID:15050613] |
| ChEMBL | Tested for binding affinity against Nicotinic acetylcholine receptor alpha2-beta2 | B | 10.6 | pKi | 0.03 | nM | Ki | J Med Chem (2003) 46: 921-924 [PMID:12620069] |
| ChEMBL | Binding affinity towards nicotinic acetylcholine receptor alpha2-beta2 using [3H]epibatidine | B | 10.6 | pKi | 0.03 | nM | Ki | Bioorg Med Chem Lett (2004) 14: 1855-1859 [PMID:15050615] |
| ChEMBL | In vitro binding affinity towards rat Nicotinic acetylcholine receptor alpha2-beta2 using 0.5 nM [3H]epibatidine | B | 10.6 | pKi | 0.03 | nM | Ki | Bioorg Med Chem Lett (2005) 15: 4385-4388 [PMID:16039849] |
| ChEMBL | Displacement of [3H]epibatidine from rat alpha-2-beta-2 nACHR expressed in human HEK293 cells | B | 10.7 | pKi | 0.02 | nM | Ki | J Med Chem (2006) 49: 2673-2676 [PMID:16640326] |
| ChEMBL | Binding affinity towards rat alpha2-beta2 neuronal nAChR expressed in Xenopus oocytes using [3H]epibatidine as radioligand | B | 11 | pKi | 0.01 | nM | Ki | Bioorg Med Chem Lett (2004) 14: 1889-1896 [PMID:15050621] |
| nicotinic acetylcholine receptor β4 subunit/nicotinic acetylcholine receptor α2 subunit/Neuronal acetylcholine receptor; alpha2/beta4 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2109230] [GtoPdb: 474, 463] [UniProtKB: P30926, Q15822] | ||||||||
| GtoPdb | - | - | 10.38 | pKd | 0.04 | nM | Kd | |
| ChEMBL | Binding affinity against nicotinic acetylcholine receptor alpha2-beta4 using [3H]epibatidine as radioligand expressed in HEK293 cells or tsA cells | B | 10.04 | pKi | 0.09 | nM | Ki | Bioorg Med Chem Lett (2004) 14: 271-273 [PMID:14684341] |
| nicotinic acetylcholine receptor α2 subunit/nicotinic acetylcholine receptor β4 subunit/Neuronal acetylcholine receptor; alpha2/beta4 in Rat (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL1907590] [GtoPdb: 463, 474] [UniProtKB: P12389, P12392] | ||||||||
| GtoPdb | - | - | 10.08 | pKd | 0.08 | nM | Kd | |
| ChEMBL | Tested for binding affinity against Nicotinic acetylcholine receptor alpha2-beta4 | B | 10.1 | pKd | 0.08 | nM | Kd | J Med Chem (2003) 46: 921-924 [PMID:12620069] |
| GtoPdb | - | - | 11 | pKd | 0.01 | nM | Kd | |
| ChEMBL | In vitro binding affinity towards rat Nicotinic acetylcholine receptor alpha2-beta4 using 0.5 nM [3H]epibatidine | B | 10.02 | pKi | 0.1 | nM | Ki | Bioorg Med Chem Lett (2005) 15: 4385-4388 [PMID:16039849] |
| ChEMBL | Tested for binding affinity against Nicotinic acetylcholine receptor alpha2-beta4 | B | 10.02 | pKi | 0.1 | nM | Ki | J Med Chem (2003) 46: 921-924 [PMID:12620069] |
| ChEMBL | Binding affinity towards Nicotinic acetylcholine receptor alpha2-beta4 using [3H]epibatidine | B | 10.02 | pKi | 0.1 | nM | Ki | Bioorg Med Chem Lett (2004) 14: 1855-1859 [PMID:15050615] |
| ChEMBL | Displacement of [3H]epibatidine from rat alpha2beta4 nAChR expressed in HEK293 cells | B | 10.02 | pKi | 0.1 | nM | Ki | J Med Chem (2008) 51: 4751-4764 [PMID:18605717] |
| ChEMBL | Displacement of [3H]epibatidine from rat alpha2beta4 nicotinic receptor expressed in human HEK293 cells by liquid scintillation counting | B | 10.02 | pKi | 0.1 | nM | Ki | Bioorg Med Chem (2009) 17: 4367-4377 [PMID:19481945] |
| ChEMBL | Displacement of [3H]epibatidine from rat alpha-2-beta-4 nACHR expressed in human HEK293 cells | B | 10.05 | pKi | 0.09 | nM | Ki | J Med Chem (2006) 49: 2673-2676 [PMID:16640326] |
| ChEMBL | Binding affinity towards rat Nicotinic acetylcholine receptor alpha2-beta4 expressed in Xenopus oocytes using [3H]epibatidine as radioligand | B | 10.06 | pKi | 0.09 | nM | Ki | Bioorg Med Chem Lett (2004) 14: 1889-1896 [PMID:15050621] |
| nicotinic acetylcholine receptor β2 subunit/nicotinic acetylcholine receptor α3 subunit/Neuronal acetylcholine receptor; alpha3/beta2 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2109234] [GtoPdb: 472, 464] [UniProtKB: P17787, P32297] | ||||||||
| GtoPdb | - | - | 9.64 | pKd | 0.23 | nM | Kd | |
| ChEMBL | Dissociation constant against Nicotinic acetylcholine receptor alpha3-beta2 | B | 10.52 | pKd | 0.03 | nM | Kd | J Med Chem (2005) 48: 1721-1724 [PMID:15771418] |
| GtoPdb | - | - | 11.15 | pKd | 0.01 | nM | Kd | |
| ChEMBL | Inhibition of [3H]epibatidine binding to Nicotinic acetylcholine receptor alpha3-beta2 | B | 10.46 | pKi | 0.04 | nM | Ki | J Med Chem (2005) 48: 1721-1724 [PMID:15771418] |
| nicotinic acetylcholine receptor α3 subunit/nicotinic acetylcholine receptor β2 subunit/Neuronal acetylcholine receptor; alpha3/beta2 in Rat (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL1907587] [GtoPdb: 464, 472] [UniProtKB: P04757, P12390] | ||||||||
| GtoPdb | - | - | 9.54 | pKd | 0.29 | nM | Kd | |
| ChEMBL | Tested for binding affinity against Nicotinic acetylcholine receptor alpha3-beta2 | B | 10.52 | pKd | 0.03 | nM | Kd | J Med Chem (2003) 46: 921-924 [PMID:12620069] |
| GtoPdb | - | - | 10.85 | pKd | 0.01 | nM | Kd | |
| ChEMBL | Binding affinity towards rat Nicotinic acetylcholine receptor alpha3-beta2 expressed in HEK293 cells using [3H]EB as radioligand | B | 9.8 | pKi | 0.16 | nM | Ki | Bioorg Med Chem Lett (2004) 14: 1845-1848 [PMID:15050613] |
| ChEMBL | Displacement of [3H]epibatidine from rat alpha-3-beta-2 nACHR expressed in human HEK293 cells | B | 10.4 | pKi | 0.04 | nM | Ki | J Med Chem (2006) 49: 2673-2676 [PMID:16640326] |
| ChEMBL | Binding affinity towards Nicotinic acetylcholine receptor alpha3-beta2 using [3H]epibatidine | B | 10.46 | pKi | 0.04 | nM | Ki | Bioorg Med Chem Lett (2004) 14: 1855-1859 [PMID:15050615] |
| ChEMBL | In vitro binding affinity towards rat Nicotinic acetylcholine receptor alpha3-beta2 using 0.5 nM [3H]epibatidine | B | 10.46 | pKi | 0.04 | nM | Ki | Bioorg Med Chem Lett (2005) 15: 4385-4388 [PMID:16039849] |
| ChEMBL | Displacement of [3H]epibatidine from rat alpha3beta2 nicotinic receptor expressed in human HEK293 cells by liquid scintillation counting | B | 10.46 | pKi | 0.04 | nM | Ki | Bioorg Med Chem (2009) 17: 4367-4377 [PMID:19481945] |
| ChEMBL | Tested for binding affinity against Nicotinic acetylcholine receptor alpha3-beta2 | B | 10.46 | pKi | 0.04 | nM | Ki | J Med Chem (2003) 46: 921-924 [PMID:12620069] |
| ChEMBL | Displacement of [3H]epibatidine from rat alpha3beta2 nAChR expressed in HEK293 cells | B | 10.46 | pKi | 0.04 | nM | Ki | J Med Chem (2008) 51: 4751-4764 [PMID:18605717] |
| ChEMBL | Binding affinity towards rat Nicotinic acetylcholine receptor alpha3-beta2 expressed in HEK293 cells using [3H]EB as radioligand | B | 10.6 | pKi | 0.03 | nM | Ki | Bioorg Med Chem Lett (2004) 14: 1845-1848 [PMID:15050613] |
| ChEMBL | Binding affinity towards rat Nicotinic acetylcholine receptor alpha3-beta2 expressed in Xenopus oocytes using [3H]epibatidine as radioligand | B | 10.85 | pKi | 0.01 | nM | Ki | Bioorg Med Chem Lett (2004) 14: 1889-1896 [PMID:15050621] |
| 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 | Dissociation constant against Nicotinic acetylcholine receptor alpha3-beta4 | B | 9.52 | pKd | 0.3 | nM | Kd | J Med Chem (2005) 48: 1721-1724 [PMID:15771418] |
| GtoPdb | - | - | 9.64 | pKd | 0.23 | nM | Kd | |
| GtoPdb | - | - | 11.15 | pKd | 0.01 | nM | Kd | |
| ChEMBL | Binding affinity against nicotinic acetylcholine receptor alpha3-beta4 using [3H]epibatidine as radioligand expressed in HEK293 cells or tsA cells | B | 9.34 | pKi | 0.46 | nM | Ki | Bioorg Med Chem Lett (2004) 14: 271-273 [PMID:14684341] |
| ChEMBL | Binding affinity to human alpha3beta4 nAChR | B | 9.64 | pKi | 0.23 | nM | Ki | Bioorg Med Chem (2020) 28: 115820-115820 [PMID:33120080] |
| ChEMBL | Displacement of [3H]epibatidine from alpha3beta4 nAChR (unknown origin) expressed in HEK cell membranes after 4 hrs by liquid scintillation counting method | B | 9.66 | pKi | 0.22 | nM | Ki | J Nat Prod (2018) 81: 1029-1035 [PMID:29671588] |
| ChEMBL | Displacement of [3H]epibatidine from human recombinant alpha-3-beta-4 nAChR in HEK293 cells by SPA assay | B | 9.72 | pKi | 0.19 | nM | Ki | Bioorg Med Chem Lett (2006) 16: 5493-5497 [PMID:16934977] |
| ChEMBL | Displacement of [3H]epibatidine from human alpha3beta4 nAChR expressed in HEK293 cell membranes | B | 9.82 | pKi | 0.15 | nM | Ki | Eur J Med Chem (2018) 152: 401-416 [PMID:29751234] |
| ChEMBL | Agonist activity at alpha-3-beta-4 nAChR in KXalpha-3-beta-4R2 cells by rubidium efflux assay | F | 7.55 | pEC50 | 28.25 | nM | EC50 | J Med Chem (2004) 47: 6691-6701 [PMID:15615518] |
| ChEMBL | Agonist activity at human recombinant alpha3beta4 nAChR expressed in human IMR32 cells assessed as calcium dynamics by FLIPR assay | F | 7.57 | pEC50 | 27 | nM | EC50 | Bioorg Med Chem Lett (2009) 19: 1682-1685 [PMID:19232492] |
| ChEMBL | Agonistic potency against nicotinic acetylcholine receptor alpha3-beta4 | F | 7.72 | pEC50 | 19 | nM | EC50 | Bioorg Med Chem Lett (2004) 14: 271-273 [PMID:14684341] |
| ChEMBL | Agonist activity at recombinant human alpha-3-beta-4 nAChR expressed in HEK293 cells assessed as induction of calcium influx by FLIPR assay | F | 7.92 | pEC50 | 12.02 | nM | EC50 | J Med Chem (2007) 50: 5493-5508 [PMID:17929796] |
| ChEMBL | Agonist activity at recombinant human alpha-3-beta-4 nAChR expressed in HEK293 cells assessed as induction of calcium influx by FLIPR assay | F | 8 | pEC50 | 10 | nM | EC50 | J Med Chem (2007) 50: 5493-5508 [PMID:17929796] |
| ChEMBL | Compound was evaluated for functional potencies and efficacies at human Nicotinic acetylcholine receptor subtype IMR-32 (ganglionic) | B | 8.15 | pEC50 | 7 | nM | EC50 | J Med Chem (1997) 40: 4169-4194 [PMID:9435889] |
| 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 | Tested for binding affinity against Nicotinic acetylcholine receptor alpha3-beta4 | B | 9.52 | pKd | 0.3 | nM | Kd | J Med Chem (2003) 46: 921-924 [PMID:12620069] |
| GtoPdb | - | - | 9.54 | pKd | 0.29 | nM | Kd | |
| GtoPdb | - | - | 10.85 | pKd | 0.01 | nM | Kd | |
| ChEMBL | Binding affinity towards rat Nicotinic acetylcholine receptor alpha3-beta4 expressed in HEK293 cells using [3H]EB as radioligand | B | 9.08 | pKi | 0.83 | nM | Ki | Bioorg Med Chem Lett (2004) 14: 1845-1848 [PMID:15050613] |
| ChEMBL | Displacement of [3H]epibatidine from rat alpha3beta4 nicotinic receptor expressed in human HEK293 cells by liquid scintillation counting | B | 9.24 | pKi | 0.57 | nM | Ki | Bioorg Med Chem (2009) 17: 4367-4377 [PMID:19481945] |
| ChEMBL | Displacement of [3H]epibatidine from rat alpha3beta4 nACHR expressed in human HEK293 cells | B | 9.24 | pKi | 0.57 | nM | Ki | J Med Chem (2006) 49: 2673-2676 [PMID:16640326] |
| ChEMBL | Inhibition of [3H]epibatidine binding to rat Nicotinic acetylcholine receptor alpha3-beta4 | B | 9.24 | pKi | 0.57 | nM | Ki | J Med Chem (2005) 48: 1721-1724 [PMID:15771418] |
| ChEMBL | In vitro binding affinity towards rat Nicotinic acetylcholine receptor alpha3-beta4 using 0.5 nM [3H]epibatidine | B | 9.24 | pKi | 0.57 | nM | Ki | Bioorg Med Chem Lett (2005) 15: 4385-4388 [PMID:16039849] |
| ChEMBL | Displacement of [3H]epibatidine from rat alpha3beta4 nAChR expressed in HEK293 cells | B | 9.24 | pKi | 0.57 | nM | Ki | J Med Chem (2008) 51: 4751-4764 [PMID:18605717] |
| ChEMBL | Tested for binding affinity against Nicotinic acetylcholine receptor alpha3-beta4 | B | 9.25 | pKi | 0.56 | nM | Ki | J Med Chem (2003) 46: 921-924 [PMID:12620069] |
| ChEMBL | Binding affinity towards Nicotinic acetylcholine receptor alpha3-beta4 using [3H]epibatidine | B | 9.25 | pKi | 0.56 | nM | Ki | Bioorg Med Chem Lett (2004) 14: 1855-1859 [PMID:15050615] |
| ChEMBL | Binding affinity towards rat Nicotinic acetylcholine receptor alpha3-beta4 expressed in HEK293 cells using [3H]EB as radioligand | B | 9.32 | pKi | 0.48 | nM | Ki | Bioorg Med Chem Lett (2004) 14: 1845-1848 [PMID:15050613] |
| ChEMBL | Displacement of [3H]epibatidine from Alpha3 Beta4 Nicotinic acetylcholine receptor of rat brain homogenates | B | 9.42 | pKi | 0.38 | nM | Ki | J Med Chem (2005) 48: 5123-5130 [PMID:16078832] |
| ChEMBL | Binding affinity towards rat Nicotinic acetylcholine receptor alpha3-beta4 expressed in Xenopus oocytes using [3H]epibatidine as radioligand | B | 9.52 | pKi | 0.3 | nM | Ki | Bioorg Med Chem Lett (2004) 14: 1889-1896 [PMID:15050621] |
| ChEMBL | Displacement of [3H]epibatidine from rat alpha3beta4 nAChR expressed in HEK292 cells after 3 hrs | B | 9.82 | pKi | 0.15 | nM | Ki | J Med Chem (2010) 53: 8187-8191 [PMID:20979364] |
| ChEMBL | Binding affinity at rat brain Nicotinic acetylcholine receptor alpha3-beta4 | B | 10.11 | pKi | 0.08 | nM | Ki | J Med Chem (2002) 45: 3235-3245 [PMID:12109907] |
| ChEMBL | Effective concentration against alpha3-beta4 nicotinic acetylcholine receptor (nAChR) expressed in IMR32 cell | B | 6.15 | pEC50 | 700 | nM | EC50 | J Med Chem (2005) 48: 5123-5130 [PMID:16078832] |
| ChEMBL | Functional potency measured as stimulation at rat Nicotinic acetylcholine receptor alpha3-beta4 expressed in Xenopus oocytes | F | 6.89 | pEC50 | 128 | nM | EC50 | Bioorg Med Chem Lett (2004) 14: 1889-1896 [PMID:15050621] |
| ChEMBL | Agonist activity at rat alpha3beta4 nAChR by cell-based rubidium flux assay | B | 7.39 | pEC50 | 41 | nM | EC50 | J Nat Prod (2018) 81: 1029-1035 [PMID:29671588] |
| ChEMBL | Agonist activity at rat alpha3beta4 nAChR expressed in HEK292 cells assessed as increase of calcium influx by FLIPR assay | F | 7.8 | pEC50 | 16 | nM | EC50 | J Med Chem (2010) 53: 8187-8191 [PMID:20979364] |
| ChEMBL | Activation potency at Nicotinic acetylcholine receptor alpha3beta4, expressed as concentration required to achieve a half maximal activation | B | 7.85 | pEC50 | 14 | nM | EC50 | J Med Chem (2002) 45: 3235-3245 [PMID:12109907] |
| ChEMBL | Effective concentration in KXalpha-3-beta-4R2 cells expressing rat nicotinic acetylcholine receptor alpha3-beta4 subunits | F | 10.43 | pEC50 | 0.04 | nM | EC50 | Bioorg Med Chem Lett (2005) 15: 1221-1224 [PMID:15686946] |
| 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] | ||||||||
| GtoPdb | - | - | 9.73 | pKd | 0.19 | nM | Kd | |
| GtoPdb | - | - | 11 | pKd | 0.01 | nM | Kd | |
| ChEMBL | Inhibition of alpha4beta2 nicotinic acetylcholine receptor (unknown origin) | B | 10.15 | pKi | 0.07 | nM | Ki | Med Chem Res (2005) 14: 241-259 |
| ChEMBL | Displacement of [3H]cytisine from human alpha4beta2 nAChR expressed in human K177 cell membrane incubated for 75 mins by liquid scintillation spectroscopy | B | 10.22 | pKi | 0.06 | nM | Ki | Bioorg Med Chem (2020) 28: 115820-115820 [PMID:33120080] |
| ChEMBL | Displacement of [3H]epibatidine from human recombinant alpha4beta2 nAChR in HEK293 cells by SPA assay | B | 10.25 | pKi | 0.06 | nM | Ki | Bioorg Med Chem Lett (2006) 16: 5493-5497 [PMID:16934977] |
| ChEMBL | Displacement of [3H]cytisine from human alpha4beta2 nAChR expressed in human K177 cell membrane incubated for 75 mins by liquid scintillation spectroscopy | B | 10.3 | pKi | 0.05 | nM | Ki | Bioorg Med Chem (2020) 28: 115820-115820 [PMID:33120080] |
| ChEMBL | Binding affinity at heteropentameric Nicotinic acetylcholine receptor alpha4-beta2 subtype using [3H]bungarotoxin as radioligand | B | 10.3 | pKi | 0.05 | nM | Ki | J Med Chem (1999) 42: 3066-3074 [PMID:10447950] |
| ChEMBL | Binding affinity against nicotinic acetylcholine receptor alpha4-beta2 using [3H]epibatidine as radioligand expressed in HEK293 cells or tsA cells | B | 10.34 | pKi | 0.05 | nM | Ki | Bioorg Med Chem Lett (2004) 14: 271-273 [PMID:14684341] |
| ChEMBL | Binding affinity to alpha4 beta-2 receptor subtype from mouse fibroblast M10 cells was measured using [3 H]nicotine | B | 10.46 | pKi | 0.04 | nM | Ki | Bioorg Med Chem Lett (2003) 13: 525-527 [PMID:12565964] |
| ChEMBL | Displacement of [3H]epibatidine from alpha4beta2 nAChR (unknown origin) expressed in HEK cell membranes after 4 hrs by liquid scintillation counting method | B | 10.48 | pKi | 0.03 | nM | Ki | J Nat Prod (2018) 81: 1029-1035 [PMID:29671588] |
| ChEMBL | Potency to displace [3H]nicotine binding to Nicotinic acetylcholine receptor alpha4-beta2 immuno-isolated from M10 cells | B | 11 | pKi | 0.01 | nM | Ki | J Med Chem (2002) 45: 2832-2840 [PMID:12061885] |
| ChEMBL | Inhibition of alpha-4-beta-2 nAChR | B | 8.97 | pIC50 | 1.06 | nM | IC50 | Bioorg Med Chem Lett (2007) 17: 6245-6249 [PMID:17889526] |
| ChEMBL | Agonist activity at human recombinant alpha4beta2 nAChR expressed in human IMR32 cells assessed as calcium dynamics by FLIPR assay | F | 6.92 | pEC50 | 120 | nM | EC50 | Bioorg Med Chem Lett (2009) 19: 1682-1685 [PMID:19232492] |
| ChEMBL | Agonist activity at recombinant human alpha-4-beta-2 nAChR expressed in HEK293 cells assessed as induction of calcium influx by FLIPR assay | F | 7.27 | pEC50 | 53.7 | nM | EC50 | J Med Chem (2007) 50: 5493-5508 [PMID:17929796] |
| ChEMBL | Agonist activity at recombinant human alpha-4-beta-2 nAChR expressed in HEK293 cells assessed as induction of calcium influx by FLIPR assay | F | 7.3 | pEC50 | 50 | nM | EC50 | J Med Chem (2007) 50: 5493-5508 [PMID:17929796] |
| ChEMBL | Agonist activity at alpha-4-beta-2 in IMR-32cells assessed as calcium influx by FLIPR assay | F | 7.56 | pEC50 | 27.54 | nM | EC50 | J Med Chem (2007) 50: 3627-3644 [PMID:17585748] |
| ChEMBL | Agonist activity at alpha-4-beta-2 in IMR-32cells assessed as calcium influx by FLIPR assay | F | 7.57 | pEC50 | 27 | nM | EC50 | J Med Chem (2007) 50: 3627-3644 [PMID:17585748] |
| ChEMBL | Agonist activity at human alpha4beta2 nAChR by cell-based rubidium flux assay | B | 7.6 | pEC50 | 25 | nM | EC50 | J Nat Prod (2018) 81: 1029-1035 [PMID:29671588] |
| ChEMBL | Compound was evaluated for functional potencies and efficacies at human Nicotinic acetylcholine receptor alpha4-beta2 | B | 7.77 | pEC50 | 17 | nM | EC50 | J Med Chem (1997) 40: 4169-4194 [PMID:9435889] |
| ChEMBL | Agonist activity at alpha4beta 2 nAChR | F | 10.7 | pEC50 | 0.02 | nM | EC50 | J Med Chem (2012) 55: 4605-4618 [PMID:22591063] |
| 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] | ||||||||
| GtoPdb | - | - | 9.07 | pKd | 0.85 | nM | Kd | |
| GtoPdb | - | - | 9.52 | pKd | 0.3 | nM | Kd | |
| ChEMBL | Tested for binding affinity against Nicotinic acetylcholine receptor alpha4-beta2 | B | 10.4 | pKd | 0.04 | nM | Kd | J Med Chem (2003) 46: 921-924 [PMID:12620069] |
| ChEMBL | Dissociation constant against Nicotinic acetylcholine receptor alpha4-beta2 | B | 10.4 | pKd | 0.04 | nM | Kd | J Med Chem (2005) 48: 1721-1724 [PMID:15771418] |
| ChEMBL | Cholinergic interactions was measured as displaced [3H]cystine from Nicotinic acetylcholine receptor alpha4-beta2 in rat brain membranes | B | 7.38 | pKi | 42 | nM | Ki | J Med Chem (1998) 41: 674-681 [PMID:9513595] |
| ChEMBL | Inhibition of [3H]nicotine binding to Nicotinic acetylcholine receptor alpha4-beta2 from rat membranes | B | 8.12 | pKi | 7.6 | nM | Ki | Bioorg Med Chem Lett (2004) 14: 1889-1896 [PMID:15050621] |
| ChEMBL | Inhibition of [3H]cytisine binding to Nicotinic acetylcholine receptor alpha4-beta2 of rat cortical membranes | B | 9.05 | pKi | 0.9 | nM | Ki | Bioorg Med Chem Lett (2004) 14: 5713-5713 |
| ChEMBL | Inhibition of [3H]nicotine binding to Nicotinic acetylcholine receptor alpha4-beta2 of rat cortical membranes | B | 9.59 | pKi | 0.26 | nM | Ki | Bioorg Med Chem Lett (2004) 14: 5713-5713 |
| ChEMBL | Binding affinity towards alpha4-beta2 nicotinic receptor was determined in rat brain membrane using [3H]cytisine as radioligand | B | 9.74 | pKi | 0.18 | nM | Ki | Bioorg Med Chem Lett (2003) 13: 1001-1004 [PMID:12643898] |
| ChEMBL | Binding affinity towards rat Nicotinic acetylcholine receptor alpha4-beta2 expressed in HEK293 cells using [3H]EB as radioligand | B | 9.82 | pKi | 0.15 | nM | Ki | Bioorg Med Chem Lett (2004) 14: 1845-1848 [PMID:15050613] |
| ChEMBL | in vitro binding affinity by inhibiting [3H]cytisine binding in rat brain tissue at Nicotinic acetylcholine receptor alpha4-beta2 | B | 9.85 | pKi | 0.14 | nM | Ki | J Med Chem (2002) 45: 3041-3047 [PMID:12086489] |
| ChEMBL | In vitro binding affinity by inhibiting [3H]cytisine binding in rat brain tissue at Nicotinic acetylcholine receptor alpha4-beta2 | B | 10.1 | pKi | 0.08 | nM | Ki | J Med Chem (2002) 45: 3041-3047 [PMID:12086489] |
| ChEMBL | Displacement of [3H]-cytisine from Alpha4-beta2 Nicotinic acetylcholine receptor of rat brain homogenates | B | 10.14 | pKi | 0.07 | nM | Ki | J Med Chem (2005) 48: 5123-5130 [PMID:16078832] |
| ChEMBL | Binding potency for Nicotinic acetylcholine receptor alpha4-beta2 (rat brain) | B | 10.15 | pKi | 0.07 | nM | Ki | J Med Chem (1997) 40: 4169-4194 [PMID:9435889] |
| ChEMBL | Binding affinity towards rat Nicotinic acetylcholine receptor alpha4-beta2 expressed in HEK293 cells using [3H]EB as radioligand | B | 10.2 | pKi | 0.06 | nM | Ki | Bioorg Med Chem Lett (2004) 14: 1845-1848 [PMID:15050613] |
| ChEMBL | Binding affinity towards Nicotinic acetylcholine receptor alpha4-beta2 using [3H]epibatidine | B | 10.21 | pKi | 0.06 | nM | Ki | Bioorg Med Chem Lett (2004) 14: 1855-1859 [PMID:15050615] |
| ChEMBL | In vitro binding affinity towards rat Nicotinic acetylcholine receptor alpha4-beta2 using 0.5 nM [3H]epibatidine | B | 10.21 | pKi | 0.06 | nM | Ki | Bioorg Med Chem Lett (2005) 15: 4385-4388 [PMID:16039849] |
| ChEMBL | Displacement of [3H]epibatidine from rat alpha4beta2 nicotinic receptor expressed in human HEK293 cells by liquid scintillation counting | B | 10.21 | pKi | 0.06 | nM | Ki | Bioorg Med Chem (2009) 17: 4367-4377 [PMID:19481945] |
| ChEMBL | Displacement of [3H]epibatidine from rat alpha4beta2 nAChR expressed in HEK293 cells | B | 10.21 | pKi | 0.06 | nM | Ki | J Med Chem (2008) 51: 4751-4764 [PMID:18605717] |
| ChEMBL | Inhibition of [3H]epibatidine binding to rat Nicotinic acetylcholine receptor alpha4-beta2 | B | 10.21 | pKi | 0.06 | nM | Ki | J Med Chem (2005) 48: 1721-1724 [PMID:15771418] |
| ChEMBL | Tested for binding affinity against Nicotinic acetylcholine receptor alpha4-beta2 | B | 10.21 | pKi | 0.06 | nM | Ki | J Med Chem (2003) 46: 921-924 [PMID:12620069] |
| ChEMBL | Displacement of [3H]epibatidine from rat alpha4beta2 nAChR expressed in HEK292 cells after 3 hrs | B | 10.22 | pKi | 0.06 | nM | Ki | J Med Chem (2010) 53: 8187-8191 [PMID:20979364] |
| ChEMBL | Displacement of [3H]epibatidine from rat forebrain alpha4beta2 nACHR | B | 10.22 | pKi | 0.06 | nM | Ki | J Med Chem (2006) 49: 2673-2676 [PMID:16640326] |
| ChEMBL | Displacement of [3H]epibatidine from rat alpha-4-beta-2 nACHR expressed in human HEK293 cells | B | 10.22 | pKi | 0.06 | nM | Ki | J Med Chem (2006) 49: 2673-2676 [PMID:16640326] |
| ChEMBL | Displacement of [3H]epibatidine from alpha4beta2 nAChR in rat cortex membranes | B | 10.3 | pKi | 0.05 | nM | Ki | Eur J Med Chem (2018) 152: 401-416 [PMID:29751234] |
| ChEMBL | Affinity at alpha4-beta2 nACh receptors in rat brain (minus cerebellum) homogenates. | B | 10.3 | pKi | 0.05 | nM | Ki | Bioorg Med Chem Lett (2003) 13: 733-735 [PMID:12639569] |
| ChEMBL | Displacement of [3H]epibatidine from nAChR alpha4beta2 receptor on rat cortical membrane homogenate by beta-counting | B | 10.3 | pKi | 0.05 | nM | Ki | Bioorg Med Chem Lett (2012) 22: 829-832 [PMID:22222032] |
| ChEMBL | Displacement of [3H]cytisine from alpha4beta2 nAChR in rat brain membrane | B | 10.33 | pKi | 0.05 | nM | Ki | Bioorg Med Chem Lett (2009) 19: 1682-1685 [PMID:19232492] |
| ChEMBL | Displacement of [3H]cytisine from alpha-4-beta-2 in rat cerebral cortical membrane | B | 10.33 | pKi | 0.05 | nM | Ki | J Med Chem (2007) 50: 3627-3644 [PMID:17585748] |
| ChEMBL | Displacement of [3H]cytisine from alpha4beta2 nicotinic acetylcholine receptor in rat brain minus cerebellum membrane | B | 10.33 | pKi | 0.05 | nM | Ki | J Med Chem (2009) 52: 4126-4141 [PMID:19552432] |
| ChEMBL | Displacement of [3H]cytisine from alpha-4-beta-2 in rat cerebral cortical membrane | B | 10.33 | pKi | 0.05 | nM | Ki | J Med Chem (2007) 50: 3627-3644 [PMID:17585748] |
| ChEMBL | Inhibition of [3H]cytisine binding to Nicotinic acetylcholine receptor alpha4-beta2 of rat cortical membranes | B | 10.4 | pKi | 0.04 | nM | Ki | Bioorg Med Chem Lett (2004) 14: 5713-5713 |
| ChEMBL | Displacement of (+/-)-[3H]epibatidine from alpha4beta2 nAChR in rat cortical membrane | B | 10.46 | pKi | 0.04 | nM | Ki | Bioorg Med Chem (2010) 18: 4498-4508 [PMID:20478710] |
| ChEMBL | Displacement of [3H]nicotine from alpha4beta2 nAChR in rat cortical membrane | B | 10.46 | pKi | 0.04 | nM | Ki | Bioorg Med Chem Lett (2008) 18: 4651-4654 [PMID:18644719] |
| ChEMBL | Binding affinity towards rat Nicotinic acetylcholine receptor alpha4-beta2 expressed in Xenopus oocytes using [3H]epibatidine as radioligand | B | 10.52 | pKi | 0.03 | nM | Ki | Bioorg Med Chem Lett (2004) 14: 1889-1896 [PMID:15050621] |
| ChEMBL | Inhibition of [3H]epibatidine binding to Nicotinic acetylcholine receptor alpha4-beta2 in rat cerebral cortex | B | 10.59 | pKi | 0.03 | nM | Ki | J Med Chem (2005) 48: 1221-1228 [PMID:15715488] |
| ChEMBL | Inhibition of [3H]epibatidine binding to Nicotinic acetylcholine receptor alpha4-beta2 from rat membranes | F | 10.59 | pKi | 0.03 | nM | Ki | Bioorg Med Chem Lett (2004) 14: 1889-1896 [PMID:15050621] |
| ChEMBL | Displacement of [3H]epibatidine from alpha-4-beta-2 nAChR in rat cerebral cortex | B | 10.59 | pKi | 0.03 | nM | Ki | Bioorg Med Chem (2008) 16: 746-754 [PMID:17964169] |
| ChEMBL | Binding affinity at rat brain Nicotinic acetylcholine receptor alpha4-beta2 | B | 10.68 | pKi | 0.02 | nM | Ki | J Med Chem (2002) 45: 3235-3245 [PMID:12109907] |
| ChEMBL | Inhibition of [3H]nicotine binding to Nicotinic acetylcholine receptor alpha4-beta2 of rat cortical membranes | B | 10.7 | pKi | 0.02 | nM | Ki | Bioorg Med Chem Lett (2004) 14: 5713-5713 |
| ChEMBL | In vitro inhibition of 5-(125I)A-85380 binding to nicotinic acetylcholine receptor (nAChR) of rat brain | B | 11 | pKi | 0.01 | nM | Ki | J Med Chem (2002) 45: 2841-2849 [PMID:12061886] |
| ChEMBL | Functional potency for Nicotinic acetylcholine receptor alpha4-beta2 (rat brain) | B | 7.77 | pEC50 | 17 | nM | EC50 | J Med Chem (1997) 40: 4169-4194 [PMID:9435889] |
| ChEMBL | Compound was evaluated for functional potencies and efficacies at rat Nicotinic acetylcholine receptor alpha4-beta2 | B | 7.8 | pEC50 | 16 | nM | EC50 | J Med Chem (1997) 40: 4169-4194 [PMID:9435889] |
| ChEMBL | Functional potency measured as stimulation at rat Nicotinic acetylcholine receptor alpha4-beta2 expressed in Xenopus oocytes | F | 7.85 | pEC50 | 14 | nM | EC50 | Bioorg Med Chem Lett (2004) 14: 1889-1896 [PMID:15050621] |
| ChEMBL | In vitro binding affinity by inhibiting [3H]dopamine release in rat brain tissue at Nicotinic acetylcholine receptor alpha4-beta2 | F | 9.4 | pEC50 | 0.4 | nM | EC50 | J Med Chem (2002) 45: 3041-3047 [PMID:12086489] |
| ChEMBL | In vitro binding affinity by inhibiting [3H]dopamine release in rat brain tissue at Nicotinic acetylcholine receptor alpha4-beta2 | F | 9.7 | pEC50 | 0.2 | nM | EC50 | J Med Chem (2002) 45: 3041-3047 [PMID:12086489] |
| 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] | ||||||||
| GtoPdb | - | - | 9.73 | pKd | 0.19 | nM | Kd | |
| GtoPdb | - | - | 11 | pKd | 0.01 | nM | Kd | |
| ChEMBL | Binding affinity against nicotinic acetylcholine receptor alpha4-beta4 using [3H]epibatidine as radioligand expressed in HEK293 cells or tsA cells | B | 10.14 | pKi | 0.07 | nM | Ki | Bioorg Med Chem Lett (2004) 14: 271-273 [PMID:14684341] |
| 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] | ||||||||
| GtoPdb | - | - | 9.07 | pKd | 0.85 | nM | Kd | |
| GtoPdb | - | - | 9.52 | pKd | 0.3 | nM | Kd | |
| ChEMBL | Tested for binding affinity against Nicotinic acetylcholine receptor alpha4-beta4 | B | 10.05 | pKd | 0.09 | nM | Kd | J Med Chem (2003) 46: 921-924 [PMID:12620069] |
| ChEMBL | Binding affinity towards rat Nicotinic acetylcholine receptor alpha4-beta4 expressed in HEK293 cells using [3H]EB as radioligand | B | 9.8 | pKi | 0.16 | nM | Ki | Bioorg Med Chem Lett (2004) 14: 1845-1848 [PMID:15050613] |
| ChEMBL | In vitro binding affinity towards rat Nicotinic acetylcholine receptor alpha4-beta4 using 0.5 nM [3H]epibatidine | B | 9.8 | pKi | 0.16 | nM | Ki | Bioorg Med Chem Lett (2005) 15: 4385-4388 [PMID:16039849] |
| ChEMBL | Displacement of [3H]epibatidine from rat alpha-4-beta-4 nACHR expressed in human HEK293 cells | B | 9.8 | pKi | 0.16 | nM | Ki | J Med Chem (2006) 49: 2673-2676 [PMID:16640326] |
| ChEMBL | Displacement of [3H]epibatidine from rat alpha4beta4 nAChR expressed in HEK293 cells | B | 9.8 | pKi | 0.16 | nM | Ki | J Med Chem (2008) 51: 4751-4764 [PMID:18605717] |
| ChEMBL | Displacement of [3H]epibatidine from rat alpha4beta4 nicotinic receptor expressed in human HEK293 cells by liquid scintillation counting | B | 9.8 | pKi | 0.16 | nM | Ki | Bioorg Med Chem (2009) 17: 4367-4377 [PMID:19481945] |
| ChEMBL | Tested for binding affinity against Nicotinic acetylcholine receptor alpha4-beta4 | B | 9.8 | pKi | 0.16 | nM | Ki | J Med Chem (2003) 46: 921-924 [PMID:12620069] |
| ChEMBL | Binding affinity towards Nicotinic acetylcholine receptor alpha4-beta4 using [3H]epibatidine | B | 9.8 | pKi | 0.16 | nM | Ki | Bioorg Med Chem Lett (2004) 14: 1855-1859 [PMID:15050615] |
| ChEMBL | Binding affinity towards rat Nicotinic acetylcholine receptor alpha4-beta4 expressed in HEK293 cells using [3H]EB as radioligand | B | 9.82 | pKi | 0.15 | nM | Ki | Bioorg Med Chem Lett (2004) 14: 1845-1848 [PMID:15050613] |
| ChEMBL | Binding affinity towards rat Nicotinic acetylcholine receptor alpha4-beta4 expressed in Xenopus oocytes using [3H]epibatidine as radioligand | B | 10.07 | pKi | 0.09 | nM | Ki | Bioorg Med Chem Lett (2004) 14: 1889-1896 [PMID:15050621] |
| nicotinic acetylcholine receptor α2 subunit in Human [GtoPdb: 463] [UniProtKB: Q15822] | ||||||||
| GtoPdb | - | - | 10.38 | pKd | 0.04 | nM | Kd | |
| nicotinic acetylcholine receptor α2 subunit/Neuronal acetylcholine receptor protein alpha-2 subunit in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2584] [GtoPdb: 463] [UniProtKB: P12389] | ||||||||
| GtoPdb | - | - | 10.08 | pKd | 0.08 | nM | Kd | |
| GtoPdb | - | - | 11 | pKd | 0.01 | nM | Kd | |
| ChEMBL | Displacement of [3H]epibatidine from rat alpha2beta2 nAChR expressed in HEK293 cells | B | 10.6 | pKi | 0.03 | nM | Ki | J Med Chem (2008) 51: 4751-4764 [PMID:18605717] |
| ChEMBL | Displacement of [3H]epibatidine from rat alpha2beta2 nicotinic receptor expressed in human HEK293 cells by liquid scintillation counting | B | 10.6 | pKi | 0.03 | nM | Ki | Bioorg Med Chem (2009) 17: 4367-4377 [PMID:19481945] |
| nicotinic acetylcholine receptor α4 subunit in Human [GtoPdb: 465] [UniProtKB: P43681] | ||||||||
| GtoPdb | - | - | 9.73 | pKd | 0.19 | nM | Kd | |
| GtoPdb | - | - | 11 | pKd | 0.01 | nM | Kd | |
| nicotinic acetylcholine receptor α4 subunit/Neuronal acetylcholine receptor protein alpha-4 subunit in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4457] [GtoPdb: 465] [UniProtKB: O70174] | ||||||||
| ChEMBL | Inhibition of [3H]nicotine binding to alpha4 nicotinic acetylcholine receptor in Mus musculus (mouse) M10 cells co-expressing beta2 nicotinic acetylcholine receptor subunits | B | 10.43 | pIC50 | 0.04 | nM | IC50 | J Agric Food Chem (2000) 48: 6016-6024 [PMID:11312774] |
| nicotinic acetylcholine receptor α4 subunit in Rat [GtoPdb: 465] [UniProtKB: P09483] | ||||||||
| GtoPdb | - | - | 9.07 | pKd | 0.85 | nM | Kd | |
| GtoPdb | - | - | 9.52 | pKd | 0.3 | nM | Kd | |
| 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]epibatidine from chimeric human alpha7-5-HT3A receptor expressed in HEK293 cells after 2 hrs by scintillation counter analysis | B | 8.2 | pKd | 6.31 | nM | Kd | Bioorg Med Chem (2012) 20: 5992-6002 [PMID:22959526] |
| ChEMBL | Dissociation constant for nicotinic acetylcholine receptor alpha 7 from human neuroblastoma SH-SY5Y cells; n=3 | B | 8.97 | pKd | 1.06 | nM | Kd | Bioorg Med Chem Lett (2005) 15: 877-881 [PMID:15686879] |
| GtoPdb | - | - | 12.22 | pKd | 0 | nM | Kd | |
| ChEMBL | Binding affinity at homopentameric Nicotinic acetylcholine receptor alpha-7 subtype using [3H]S-(-)-nicotine as radioligand | B | 7.6 | pKi | 25 | nM | Ki | J Med Chem (1999) 42: 3066-3074 [PMID:10447950] |
| ChEMBL | Binding affinity to alpha-7 receptor subtype from human neuroblastoma SH-SY5Y cells was measured using [125I]-alpha-bungarotoxin as radioligand | B | 7.99 | pKi | 10.2 | nM | Ki | Bioorg Med Chem Lett (2003) 13: 525-527 [PMID:12565964] |
| ChEMBL | Binding affinity for nicotinic acetylcholine receptor alpha 7 from human neuroblastoma SH-SY5Y cells; n=3 | B | 8 | pKi | 10 | nM | Ki | Bioorg Med Chem Lett (2005) 15: 877-881 [PMID:15686879] |
| ChEMBL | Displacement of [3H]epibatidine from alpha7 nAChR (unknown origin) expressed in HEK cell membranes after 4 hrs by liquid scintillation counting method | B | 8.57 | pKi | 2.7 | nM | Ki | J Nat Prod (2018) 81: 1029-1035 [PMID:29671588] |
| ChEMBL | Displacement of [125I]alpha-bungarotoxin from human alpha7 nAChR expressed in K28 cell membrane | B | 8.66 | pKi | 2.2 | nM | Ki | Bioorg Med Chem (2020) 28: 115820-115820 [PMID:33120080] |
| ChEMBL | Inhibition of [3H]alpha-BGT binding to alpha7 nicotinic acetylcholine receptor in Homo sapiens (human) SH-SY5Y cells | B | 7.51 | pIC50 | 31 | nM | IC50 | J Agric Food Chem (2000) 48: 6016-6024 [PMID:11312774] |
| ChEMBL | Compound was evaluated for functional potencies and efficacies at human Nicotinic acetylcholine receptor alpha7 | B | 5.46 | pEC50 | 3500 | nM | EC50 | J Med Chem (1997) 40: 4169-4194 [PMID:9435889] |
| 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 | Inhibition of [125I]-iodo-MLA binding to Nicotinic acetylcholine receptor alpha-7 in rat cerebral cortex | B | 6.7 | pKi | 198 | nM | Ki | J Med Chem (2005) 48: 1221-1228 [PMID:15715488] |
| ChEMBL | Inhibition of [125I]- iodo-MLA binding at the Nicotinic acetylcholine receptor alpha-7 (nAChR) in male rat cerebral cortex | B | 6.7 | pKi | 198 | nM | Ki | J Med Chem (2002) 45: 4755-4761 [PMID:12361403] |
| ChEMBL | Displacement of [125I]iodoMLA from alpha-7 nAChR in rat cerebral cortex | B | 6.7 | pKi | 198 | nM | Ki | Bioorg Med Chem (2008) 16: 746-754 [PMID:17964169] |
| ChEMBL | Binding affinity at rat brain Nicotinic acetylcholine receptor alpha7 | B | 7 | pKi | 101 | nM | Ki | J Med Chem (2002) 45: 3235-3245 [PMID:12109907] |
| ChEMBL | Binding potency for Nicotinic acetylcholine receptor alpha-7 (rat brain) | B | 7.68 | pKi | 21 | nM | Ki | J Med Chem (1997) 40: 4169-4194 [PMID:9435889] |
| ChEMBL | Displacement of [125I]alpha-Bungarotoxin from alpha7 nAChR in rat cortical membrane | B | 7.99 | pKi | 10.2 | nM | Ki | Bioorg Med Chem (2010) 18: 4498-4508 [PMID:20478710] |
| ChEMBL | Displacement of [3H]epibatidine from alpha7 nAChR in rat brain membranes after 2 hrs | B | 8.38 | pKi | 4.2 | nM | Ki | J Med Chem (2010) 53: 8187-8191 [PMID:20979364] |
| ChEMBL | Binding affinity to subtype Nicotinic acetylcholine receptor alpha-7 using [125I]-alpha-BTX as radioligand in rat brain | B | 8.4 | pKi | 4 | nM | Ki | J Med Chem (2002) 45: 1064-1072 [PMID:11855986] |
| ChEMBL | Displacement of [3H]A585539 from alpha7 nicotinic acetylcholine receptor in rat brain minus cerebellum membrane | B | 8.57 | pKi | 2.7 | nM | Ki | J Med Chem (2009) 52: 4126-4141 [PMID:19552432] |
| ChEMBL | Displacement of [3H]585539 from alpha7 nAChR in rat brain | B | 8.57 | pKi | 2.7 | nM | Ki | Bioorg Med Chem Lett (2010) 20: 104-107 [PMID:19954975] |
| ChEMBL | Functional potency for Nicotinic acetylcholine receptor alpha-7 (rat brain) | B | 5.89 | pEC50 | 1300 | nM | EC50 | J Med Chem (1997) 40: 4169-4194 [PMID:9435889] |
| nicotinic acetylcholine receptor α3 subunit/Neuronal acetylcholine receptor subunit alpha-3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3068] [GtoPdb: 464] [UniProtKB: P32297] | ||||||||
| GtoPdb | - | - | 9.64 | pKd | 0.23 | nM | Kd | |
| GtoPdb | - | - | 11.15 | pKd | 0.01 | nM | Kd | |
| ChEMBL | Functional activation of human sympathetic ganglionic type nAChRs in IMR-32 cells containing alpha-3 subtype | F | 8.15 | pEC50 | 7 | nM | EC50 | J Med Chem (1998) 41: 407-412 [PMID:9484491] |
| nicotinic acetylcholine receptor α3 subunit in Rat [GtoPdb: 464] [UniProtKB: P04757] | ||||||||
| GtoPdb | - | - | 9.54 | pKd | 0.29 | nM | Kd | |
| GtoPdb | - | - | 10.85 | pKd | 0.01 | nM | Kd | |
| Neuronal acetylcholine receptor subunit alpha-4 in Chicken (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5569] [UniProtKB: P09482] | ||||||||
| ChEMBL | Binding affinity to recombinant Gallus gallus (chicken) alpha4beta2 nicotinic acetylcholine receptor assessed as [3H]NIC binding by radioligand binding assay | B | 11 | pKi | 0.01 | nM | Ki | J Agric Food Chem (2011) 59: 2825-2828 [PMID:21341671] |
| nicotinic acetylcholine receptor β4 subunit/Neuronal acetylcholine receptor subunit beta-4 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2658] [GtoPdb: 474] [UniProtKB: P12392] | ||||||||
| ChEMBL | Binding affinity to Nicotinic acetylcholine receptor alpha3-beta4 using +/-[3H]epibatidine as radioligand in pig adrenal gland | B | 10.66 | pKi | 0.02 | nM | Ki | J Med Chem (2002) 45: 1064-1072 [PMID:11855986] |
| Soluble acetylcholine receptor in Aplysia californica (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1944497] [UniProtKB: Q8WSF8] | ||||||||
| ChEMBL | Binding affinity to salt water mollusc Aplysia californica AChBP Y55W mutant assessed as [3H]acetamiprid binding by radioligand binding assay | B | 9 | pKi | 1 | nM | Ki | J Agric Food Chem (2011) 59: 2825-2828 [PMID:21341671] |
| nicotinic acetylcholine receptor α8 subunit (avian) in Human [GtoPdb: 752] | ||||||||
| GtoPdb | - | - | 9.7 | pKd | 0.2 | nM | Kd | |
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]
