[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 |
|---|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
| 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 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]
