[125I]epibatidine [Ligand Id: 3976] 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
  • Acetylcholine-binding protein in Lymnaea stagnalis [ChEMBL: CHEMBL6084] [UniProtKB: P58154]
There should be some charts here, you may need to enable JavaScript!
There should be some charts here, you may need to enable JavaScript!
  • 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 [ChEMBL: CHEMBL1907588] [GtoPdb: 462475471476] [UniProtKB: P02708P07510P11230Q07001]
There should be some charts here, you may need to enable JavaScript!
  • nicotinic acetylcholine receptor α1 subunit/Acetylcholine receptor protein alpha chain in Human [ChEMBL: CHEMBL4808] [GtoPdb: 462] [UniProtKB: P02708]
There should be some charts here, you may need to enable JavaScript!
  • Acetylcholine receptor protein delta chain in Torpedo californica [ChEMBL: CHEMBL3916] [UniProtKB: P02718]
There should be some charts here, you may need to enable JavaScript!
  • Acetylcholine receptor subunit beta-like 2 in Drosophila melanogaster [ChEMBL: CHEMBL2366470] [UniProtKB: P25162]
There should be some charts here, you may need to enable JavaScript!
  • 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: 464465463472473474466467469468470] [UniProtKB: P32297P43681Q15822P17787Q05901P30926P30532Q15825Q9UGM1P36544Q9GZZ6]
  • 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 [ChEMBL: CHEMBL2094110] [GtoPdb: 464465463472473474466467469468470] [UniProtKB: P04757P09483P12389P12390P12391P12392P20420P43143P43144Q05941Q9JLB5]
There should be some charts here, you may need to enable JavaScript!
  • nicotinic acetylcholine receptor α2 subunit/nicotinic acetylcholine receptor β2 subunit in Human [GtoPdb: 463472] [UniProtKB: Q15822P17787]
  • nicotinic acetylcholine receptor α2 subunit/nicotinic acetylcholine receptor β2 subunit/Neuronal acetylcholine receptor; alpha2/beta2 in Rat [ChEMBL: CHEMBL1907592] [GtoPdb: 463472] [UniProtKB: P12389P12390]
There should be some charts here, you may need to enable JavaScript!
  • nicotinic acetylcholine receptor β4 subunit/nicotinic acetylcholine receptor α2 subunit/Neuronal acetylcholine receptor; alpha2/beta4 in Human [ChEMBL: CHEMBL2109230] [GtoPdb: 474463] [UniProtKB: P30926Q15822]
  • nicotinic acetylcholine receptor α2 subunit/nicotinic acetylcholine receptor β4 subunit/Neuronal acetylcholine receptor; alpha2/beta4 in Rat [ChEMBL: CHEMBL1907590] [GtoPdb: 463474] [UniProtKB: P12389P12392]
There should be some charts here, you may need to enable JavaScript!
  • nicotinic acetylcholine receptor β2 subunit/nicotinic acetylcholine receptor α3 subunit/Neuronal acetylcholine receptor; alpha3/beta2 in Human [ChEMBL: CHEMBL2109234] [GtoPdb: 472464] [UniProtKB: P17787P32297]
  • nicotinic acetylcholine receptor α3 subunit/nicotinic acetylcholine receptor β2 subunit/Neuronal acetylcholine receptor; alpha3/beta2 in Rat [ChEMBL: CHEMBL1907587] [GtoPdb: 464472] [UniProtKB: P04757P12390]
There should be some charts here, you may need to enable JavaScript!
  • nicotinic acetylcholine receptor β4 subunit/nicotinic acetylcholine receptor α3 subunit/Neuronal acetylcholine receptor; alpha3/beta4 in Human [ChEMBL: CHEMBL1907594] [GtoPdb: 474464] [UniProtKB: P30926P32297]
  • nicotinic acetylcholine receptor α3 subunit/nicotinic acetylcholine receptor β4 subunit/Neuronal acetylcholine receptor; alpha3/beta4 in Rat [ChEMBL: CHEMBL1907593] [GtoPdb: 464474] [UniProtKB: P04757P12392]
There should be some charts here, you may need to enable JavaScript!
  • nicotinic acetylcholine receptor β2 subunit/nicotinic acetylcholine receptor α4 subunit/Neuronal acetylcholine receptor; alpha4/beta2 in Human [ChEMBL: CHEMBL1907589] [GtoPdb: 472465] [UniProtKB: P17787P43681]
  • nicotinic acetylcholine receptor α4 subunit/nicotinic acetylcholine receptor β2 subunit/Neuronal acetylcholine receptor; alpha4/beta2 in Rat [ChEMBL: CHEMBL1907596] [GtoPdb: 465472] [UniProtKB: P09483P12390]
There should be some charts here, you may need to enable JavaScript!
  • nicotinic acetylcholine receptor β4 subunit/nicotinic acetylcholine receptor α4 subunit/Neuronal acetylcholine receptor; alpha4/beta4 in Human [ChEMBL: CHEMBL1907591] [GtoPdb: 474465] [UniProtKB: P30926P43681]
  • nicotinic acetylcholine receptor α4 subunit/nicotinic acetylcholine receptor β4 subunit/Neuronal acetylcholine receptor; alpha4/beta4 in Rat [ChEMBL: CHEMBL1907595] [GtoPdb: 465474] [UniProtKB: P09483P12392]
There should be some charts here, you may need to enable JavaScript!
  • nicotinic acetylcholine receptor α2 subunit in Human [GtoPdb: 463] [UniProtKB: Q15822]
  • nicotinic acetylcholine receptor α2 subunit/Neuronal acetylcholine receptor protein alpha-2 subunit in Rat [ChEMBL: CHEMBL2584] [GtoPdb: 463] [UniProtKB: P12389]
There should be some charts here, you may need to enable JavaScript!
  • nicotinic acetylcholine receptor α4 subunit in Human [GtoPdb: 465] [UniProtKB: P43681]
  • nicotinic acetylcholine receptor α4 subunit/Neuronal acetylcholine receptor protein alpha-4 subunit in Mouse [ChEMBL: CHEMBL4457] [GtoPdb: 465] [UniProtKB: O70174]
  • nicotinic acetylcholine receptor α4 subunit in Rat [GtoPdb: 465] [UniProtKB: P09483]
There should be some charts here, you may need to enable JavaScript!
  • nicotinic acetylcholine receptor α7 subunit/Neuronal acetylcholine receptor protein alpha-7 subunit in Human [ChEMBL: CHEMBL2492] [GtoPdb: 468] [UniProtKB: P36544]
  • nicotinic acetylcholine receptor α7 subunit/Neuronal acetylcholine receptor protein alpha-7 subunit in Rat [ChEMBL: CHEMBL4980] [GtoPdb: 468] [UniProtKB: Q05941]
There should be some charts here, you may need to enable JavaScript!
  • nicotinic acetylcholine receptor α3 subunit/Neuronal acetylcholine receptor subunit alpha-3 in Human [ChEMBL: CHEMBL3068] [GtoPdb: 464] [UniProtKB: P32297]
  • nicotinic acetylcholine receptor α3 subunit in Rat [GtoPdb: 464] [UniProtKB: P04757]
There should be some charts here, you may need to enable JavaScript!
  • Neuronal acetylcholine receptor subunit alpha-4 in Chicken [ChEMBL: CHEMBL5569] [UniProtKB: P09482]
There should be some charts here, you may need to enable JavaScript!
  • nicotinic acetylcholine receptor β4 subunit/Neuronal acetylcholine receptor subunit beta-4 in Rat [ChEMBL: CHEMBL2658] [GtoPdb: 474] [UniProtKB: P12392]
There should be some charts here, you may need to enable JavaScript!
  • Soluble acetylcholine receptor in Aplysia californica [ChEMBL: CHEMBL1944497] [UniProtKB: Q8WSF8]
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: P02710P02712P02714P02718]
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: 462475471476] [UniProtKB: P02708P07510P11230Q07001]
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 Human [GtoPdb: 464465463472473474466467469468470] [UniProtKB: P32297P43681Q15822P17787Q05901P30926P30532Q15825Q9UGM1P36544Q9GZZ6]
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
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: 464465463472473474466467469468470] [UniProtKB: P04757P09483P12389P12390P12391P12392P20420P43143P43144Q05941Q9JLB5]
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 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 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 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: 463472] [UniProtKB: Q15822P17787]
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: 463472] [UniProtKB: P12389P12390]
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: 474463] [UniProtKB: P30926Q15822]
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: 463474] [UniProtKB: P12389P12392]
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: 472464] [UniProtKB: P17787P32297]
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: 464472] [UniProtKB: P04757P12390]
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: 474464] [UniProtKB: P30926P32297]
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 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 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: 464474] [UniProtKB: P04757P12392]
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