acetylcholine [Ligand Id: 294] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL667 (Acetylcholine)
  • Acetylcholine-binding protein in Lymnaea stagnalis [ChEMBL: CHEMBL6084] [UniProtKB: P58154]
  • 5.35
1 CHEMBL667_lig_chart_1 Acetylcholine-binding protein Lymnaea stagnalis
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  • Acetylcholine receptor protein delta chain in Torpedo californica [ChEMBL: CHEMBL3916] [UniProtKB: P02718]
  • This target only has 0 pki data point
  • 0
2 CHEMBL667_lig_chart_2 Acetylcholine receptor protein delta chain Torpedo californica
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  • M1 receptor/Muscarinic acetylcholine receptor M1 in Human [ChEMBL: CHEMBL216] [GtoPdb: 13] [UniProtKB: P11229]
  • M1 receptor in Rat [GtoPdb: 13] [UniProtKB: P08482]
  • 5
3 CHEMBL667_lig_chart_3 Muscarinic acetylcholine receptor M1 HumanRat
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  • M2 receptor/Muscarinic acetylcholine receptor M2 in Human [ChEMBL: CHEMBL211] [GtoPdb: 14] [UniProtKB: P08172]
  • M2 receptor in Rat [GtoPdb: 14] [UniProtKB: P10980]
  • 6.4
4 CHEMBL667_lig_chart_4 Muscarinic acetylcholine receptor M2 HumanRat
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  • M3 receptor/Muscarinic acetylcholine receptor M3 in Human [ChEMBL: CHEMBL245] [GtoPdb: 15] [UniProtKB: P20309]
  • M3 receptor in Rat [GtoPdb: 15] [UniProtKB: P08483]
  • 5.6
5 CHEMBL667_lig_chart_5 Muscarinic acetylcholine receptor M3 HumanRat
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  • M4 receptor/Muscarinic acetylcholine receptor M4 in Human [ChEMBL: CHEMBL1821] [GtoPdb: 16] [UniProtKB: P08173]
  • 5.33
6 CHEMBL667_lig_chart_6 Muscarinic acetylcholine receptor M4 Human
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  • M5 receptor/Muscarinic acetylcholine receptor M5 in Human [ChEMBL: CHEMBL2035] [GtoPdb: 17] [UniProtKB: P08912]
  • 5.56
7 CHEMBL667_lig_chart_7 Muscarinic acetylcholine receptor M5 Human
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  • 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]
  • This target only has 1 pki data point
  • 7.37
8 CHEMBL667_lig_chart_8 Neuronal acetylcholine receptor Rat
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  • nicotinic acetylcholine receptor α2 subunit/nicotinic acetylcholine receptor β2 subunit/Neuronal acetylcholine receptor; alpha2/beta2 in Rat [ChEMBL: CHEMBL1907592] [GtoPdb: 463472] [UniProtKB: P12389P12390]
  • This target only has 1 pki data point
  • 7.96
9 CHEMBL667_lig_chart_9 Neuronal acetylcholine receptor; alpha2/beta2 Rat
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  • nicotinic acetylcholine receptor α3 subunit/nicotinic acetylcholine receptor β2 subunit/Neuronal acetylcholine receptor; alpha3/beta2 in Rat [ChEMBL: CHEMBL1907587] [GtoPdb: 464472] [UniProtKB: P04757P12390]
  • This target only has 1 pki data point
  • 7.39
10 CHEMBL667_lig_chart_10 Neuronal acetylcholine receptor; alpha3/beta2 Rat
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  • 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]
  • 6.21
11 CHEMBL667_lig_chart_11 Neuronal acetylcholine receptor; alpha3/beta4 HumanRat
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  • 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]
  • 7.48
12 CHEMBL667_lig_chart_12 Neuronal acetylcholine receptor; alpha4/beta2 HumanRat
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  • nicotinic acetylcholine receptor α4 subunit/nicotinic acetylcholine receptor β4 subunit/Neuronal acetylcholine receptor; alpha4/beta4 in Rat [ChEMBL: CHEMBL1907595] [GtoPdb: 465474] [UniProtKB: P09483P12392]
  • 7.24
13 CHEMBL667_lig_chart_13 Neuronal acetylcholine receptor; alpha4/beta4 Rat
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  • 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]
  • 5.03
14 CHEMBL667_lig_chart_14 Neuronal acetylcholine receptor protein alpha-7 subunit HumanRat
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  • Nicotinic acetylcholine receptor alpha8 subunit in Periplaneta americana [ChEMBL: CHEMBL2366437] [UniProtKB: H6TY12]
  • This target only has 0 pki data point
  • 0
15 CHEMBL667_lig_chart_15 Nicotinic acetylcholine receptor alpha8 subunit Periplaneta americana
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
Acetylcholine-binding protein in Lymnaea stagnalis (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6084] [UniProtKB: P58154]
ChEMBL Displacement of [3H]-epibatidine from histidine-tagged Lymnaea stagnalis AChBP expressed in Sf9 cells after 1.5 hrs by liquid scintillation counting B 5.2 pKi 6309.57 nM Ki Bioorg. Med. Chem. (2011) 19: 6107-6119 [PMID:21920761]
ChEMBL Displacement of [125I]alpha-bungarotoxin from Lymnaea stagnalis His-tagged AchBP B 5.5 pKi 3162.28 nM Ki J. Med. Chem. (2009) 52: 2372-2383 [PMID:19331415]
Acetylcholine receptor protein delta chain in Torpedo californica (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3916] [UniProtKB: P02718]
ChEMBL Compound was evaluated for functional potencies and efficacies at human Nicotinic acetylcholine receptor subtype TE671 (muscle) B 5.3 pEC50 5000 nM EC50 J. Med. Chem. (1997) 40: 4169-4194 [PMID:9435889]
M1 receptor/Muscarinic acetylcholine receptor M1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL216] [GtoPdb: 13] [UniProtKB: P11229]
ChEMBL Binding affinity to muscarinic M1 acetylcholine receptor (unknown origin) B 4.76 pKd 17378.01 nM Kd J. Med. Chem. (2015) 58: 560-576 [PMID:25478907]
ChEMBL Displacement of [3H]NMS from human muscarinic M1 acetylcholine receptor expressed in CHO cell membranes by radioligand binding assay B 4.76 pKd 17378.01 nM Kd J. Med. Chem. (2015) 58: 560-576 [PMID:25478907]
ChEMBL Displacement of [3H]N-methyl-scopolamine from human recombinant muscarinic M1 receptor expressed in CHO-FlpIn cells after 6 hrs by liquid scintillation counting method B 4.64 pKi 23000 nM Ki J Med Chem (2017) 60: 9239-9250 [PMID:29094937]
ChEMBL Displacement of [3H]N-methyl-scopolamine from human recombinant muscarinic M1 receptor expressed in CHO-FlpIn cells after 6 hrs by liquid scintillation counting method B 4.64 pKi 22908.68 nM Ki J Med Chem (2017) 60: 9239-9250 [PMID:29094937]
ChEMBL Displacement of [3H]NMS from human cloned muscarinic M1 receptor expressed in CHO cells B 4.87 pKi 13489.63 nM Ki Bioorg. Med. Chem. Lett. (2008) 18: 614-618 [PMID:18077164]
GtoPdb - - 4.9 pKi - - - Mol Pharmacol (1997) 52: 172-9 [PMID:9224827];
Mol Pharmacol (2013) 84: 425-37 [PMID:23798605]
ChEMBL Binding affinity to muscarinic M1 acetylcholine receptor (unknown origin) B 4.9 pKi 12589.25 nM Ki J. Med. Chem. (2015) 58: 560-576 [PMID:25478907]
ChEMBL Displacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M1 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting method B 5.24 pKi 5800 nM Ki J Med Chem (2017) 60: 9239-9250 [PMID:29094937]
ChEMBL Agonist activity at human muscarinic M1 receptor expressed in HEK293T cells co-expressing Galpha subunit and PLC-beta3 by split luciferase complementation assay B 6.87 pIC50 134.9 nM IC50 J Med Chem (2019) 62: 3009-3020 [PMID:30827105]
ChEMBL Agonist activity at human m1 muscarinic acetylcholine receptor expressed in HEK293 cells assessed as calcium mobilization by FLIPR assay F 4 pEC50 100000 nM EC50 Bioorg. Med. Chem. Lett. (2015) 25: 1546-1551 [PMID:25765911]
ChEMBL Agonist activity at human muscarinic M1 receptor Y381A mutant expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assay F 4.57 pEC50 27000 nM EC50 J. Med. Chem. (2010) 53: 6386-6397 [PMID:20684563]
ChEMBL Agonist activity at human muscarinic M1 receptor Y381A mutant expressed in BHK-21 cells assessed as calcium mobilization for 6 mins by Calcium4-based staining F 4.57 pEC50 27000 nM EC50 Bioorg. Med. Chem. Lett. (2012) 22: 5134-5140 [PMID:22677319]
ChEMBL Agonistic activity against M1 muscarinic receptor expressed in NIH 3T3 cells. F 4.7 pEC50 20000 nM EC50 J. Med. Chem. (2001) 44: 4563-4576 [PMID:11741475]
ChEMBL Agonist activity at Gq/11 coupled recombinant human muscarinic M1 AChR expressed in CHO-FlpIn cells assessed as IP-one accumulation after 40 mins by HTRF assay B 6.21 pEC50 620 nM EC50 J Med Chem (2017) 60: 9239-9250 [PMID:29094937]
ChEMBL Agonist activity at Gq/11 coupled recombinant human muscarinic M1 AChR expressed in CHO-FlpIn cells assessed as IP-one accumulation after 40 mins by HTRF assay B 6.21 pEC50 616.6 nM EC50 J Med Chem (2017) 60: 9239-9250 [PMID:29094937]
ChEMBL Partial agonist activity at human muscarinic M1 acetylcholine receptor expressed in CHO cells assessed as increase in IP1 accumulation incubated for 30 mins by FRET based HTRF assay B 6.43 pEC50 371.54 nM EC50 J. Med. Chem. (2015) 58: 560-576 [PMID:25478907]
ChEMBL Agonist activity at recombinant human muscarinic M1 receptor expressed in CHO cells assessed as upregulation in ERK1/2 phosphorylation after 5 mins by alphascreen assay B 7.33 pEC50 47 nM EC50 J Med Chem (2017) 60: 9239-9250 [PMID:29094937]
ChEMBL Agonist activity at recombinant human muscarinic M1 receptor expressed in CHO cells assessed as upregulation in ERK1/2 phosphorylation after 5 mins by alphascreen assay B 7.33 pEC50 46.77 nM EC50 J Med Chem (2017) 60: 9239-9250 [PMID:29094937]
ChEMBL Agonist activity at human muscarinic M1 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay B 7.59 pEC50 25.9 nM EC50 Bioorg. Med. Chem. Lett. (2015) 25: 4158-4163 [PMID:26299349]
ChEMBL Agonist activity at human M1 receptor expressed in CHO-K1 cells assessed as calcium mobilization for 6 mins by Calcium4-based staining F 8.96 pEC50 1.1 nM EC50 Bioorg. Med. Chem. Lett. (2012) 22: 5134-5140 [PMID:22677319]
ChEMBL Agonist activity at human muscarinic M1 receptor expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assay F 8.96 pEC50 1.1 nM EC50 J. Med. Chem. (2010) 53: 6386-6397 [PMID:20684563]
M1 receptor in Rat [GtoPdb: 13] [UniProtKB: P08482]
GtoPdb - - 5 pKi - - - J Pharmacol Exp Ther (2002) 303: 29-35 [PMID:12235229]
M2 receptor/Muscarinic acetylcholine receptor M2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL211] [GtoPdb: 14] [UniProtKB: P08172]
ChEMBL Displacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M2 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting method B 6.41 pKi 390 nM Ki J Med Chem (2017) 60: 9239-9250 [PMID:29094937]
ChEMBL Displacement of [3H]N-methyl-scopolamine from human recombinant muscarinic M2 receptor expressed in CHO-FlpIn cells after 6 hrs by liquid scintillation counting method B 6.42 pKi 380.19 nM Ki J Med Chem (2017) 60: 9239-9250 [PMID:29094937]
ChEMBL Displacement of [3H]N-methyl-scopolamine from human recombinant muscarinic M2 receptor expressed in CHO-FlpIn cells after 6 hrs by liquid scintillation counting method B 6.42 pKi 380 nM Ki J Med Chem (2017) 60: 9239-9250 [PMID:29094937]
GtoPdb - - 6.5 pKi - - - J Pharmacol Exp Ther (2002) 303: 29-35 [PMID:12235229];
Mol Pharmacol (1997) 52: 172-9 [PMID:9224827];
Mol Pharmacol (2013) 84: 425-37 [PMID:23798605]
ChEMBL Displacement of [3H]NMS from human cloned muscarinic M2 receptor expressed in CHO cells B 6.8 pKi 158.49 nM Ki Bioorg. Med. Chem. Lett. (2008) 18: 614-618 [PMID:18077164]
ChEMBL Agonist activity at recombinant human muscarinic M2 receptor expressed in HEK293 cells co-expressing beta-arrestin assessed as increase in beta-arrestin recruitment after 24 hrs by Bright-Glo luminescence assay B 5.72 pEC50 1905.46 nM EC50 J Med Chem (2017) 60: 9239-9250 [PMID:29094937]
ChEMBL Agonist activity at recombinant human muscarinic M2 receptor expressed in HEK293 cells co-expressing beta-arrestin assessed as increase in beta-arrestin recruitment after 24 hrs by Bright-Glo luminescence assay B 5.72 pEC50 1900 nM EC50 J Med Chem (2017) 60: 9239-9250 [PMID:29094937]
ChEMBL Agonist activity at Gi/o protein-coupled recombinant human muscarinic M2 receptor expressed in CHO-FlpIn cells preincubated for 60 mins followed by [35S]GTPgammaS addition measured after 30 mins by liquid scintillation counting method B 6.29 pEC50 512.86 nM EC50 J Med Chem (2017) 60: 9239-9250 [PMID:29094937]
ChEMBL Agonist activity at Gi/o protein-coupled recombinant human muscarinic M2 receptor expressed in CHO-FlpIn cells preincubated for 60 mins followed by [35S]GTPgammaS addition measured after 30 mins by liquid scintillation counting method B 6.29 pEC50 510 nM EC50 J Med Chem (2017) 60: 9239-9250 [PMID:29094937]
ChEMBL Agonist activity at human muscarinic M2 receptor expressed in CHO-K1 cells assessed as calcium mobilization for 6 mins by Calcium4-based staining F 6.66 pEC50 220 nM EC50 Bioorg. Med. Chem. Lett. (2012) 22: 5134-5140 [PMID:22677319]
ChEMBL Agonist activity at human muscarinic M2 receptor expressed in CHO-K1 cells coexpressing Galpha16 subunit assessed as increase of acetylcholine-induced calcium flux by FLIPR assay F 6.66 pEC50 220 nM EC50 J. Med. Chem. (2010) 53: 6386-6397 [PMID:20684563]
ChEMBL Agonist activity at human recombinant muscarinic M2 receptor co-expressed with Galphaqi5-HA in African green monkey COS7 cells assessed as IP accumulation after 2 hrs in presence of myo-[3H]inositol by liquid scintillation counting method B 7.25 pEC50 56 nM EC50 J Med Chem (2017) 60: 9239-9250 [PMID:29094937]
ChEMBL Agonist activity at recombinant human muscarinic M2 receptor expressed in HEK293 cells assessed as inhibition of forskolin-mediated cAMP accumulation after 10 mins by FRET assay B 7.31 pEC50 49 nM EC50 J Med Chem (2017) 60: 9239-9250 [PMID:29094937]
ChEMBL Agonist activity at recombinant human muscarinic M2 receptor expressed in HEK293 cells assessed as inhibition of forskolin-mediated cAMP accumulation after 10 mins by FRET assay B 7.31 pEC50 48.98 nM EC50 J Med Chem (2017) 60: 9239-9250 [PMID:29094937]
ChEMBL Agonist activity at recombinant human muscarinic M2 receptor expressed in CHO cells assessed as upregulation in ERK1/2 phosphorylation after 5 mins by alphascreen assay B 7.89 pEC50 13 nM EC50 J Med Chem (2017) 60: 9239-9250 [PMID:29094937]
ChEMBL Agonist activity at recombinant human muscarinic M2 receptor expressed in CHO cells assessed as upregulation in ERK1/2 phosphorylation after 5 mins by alphascreen assay B 7.9 pEC50 12.59 nM EC50 J Med Chem (2017) 60: 9239-9250 [PMID:29094937]
ChEMBL Agonist activity at human muscarinic M2 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay B 8.15 pEC50 7 nM EC50 Bioorg. Med. Chem. Lett. (2015) 25: 4158-4163 [PMID:26299349]
M2 receptor in Rat [GtoPdb: 14] [UniProtKB: P10980]
GtoPdb - - 6.4 pKi - - - J Pharmacol Exp Ther (1998) 284: 500-7 [PMID:9454790]
M3 receptor/Muscarinic acetylcholine receptor M3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL245] [GtoPdb: 15] [UniProtKB: P20309]
ChEMBL Displacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells B 5.15 pKi 7079.46 nM Ki Bioorg. Med. Chem. Lett. (2008) 18: 614-618 [PMID:18077164]
ChEMBL Displacement of [3H]N-methyl-scopolamine from human recombinant muscarinic M3 receptor expressed in CHO-FlpIn cells after 6 hrs by liquid scintillation counting method B 5.17 pKi 6800 nM Ki J Med Chem (2017) 60: 9239-9250 [PMID:29094937]
ChEMBL Displacement of [3H]N-methyl-scopolamine from human recombinant muscarinic M3 receptor expressed in CHO-FlpIn cells after 6 hrs by liquid scintillation counting method B 5.17 pKi 6760.83 nM Ki J Med Chem (2017) 60: 9239-9250 [PMID:29094937]
ChEMBL Displacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting method B 5.33 pKi 4700 nM Ki J Med Chem (2017) 60: 9239-9250 [PMID:29094937]
GtoPdb - - 5.4 pKi - - - J Pharmacol Exp Ther (2002) 303: 29-35 [PMID:12235229];
Mol Pharmacol (1997) 52: 172-9 [PMID:9224827];
Mol Pharmacol (2013) 84: 425-37 [PMID:23798605]
ChEMBL Agonist activity at Gq/11 coupled recombinant human muscarinic M3 AChR expressed in CHO-FlpIn cells assessed as IP-one accumulation after 40 mins by HTRF assay B 6.62 pEC50 240 nM EC50 J Med Chem (2017) 60: 9239-9250 [PMID:29094937]
ChEMBL Agonist activity at Gq/11 coupled recombinant human muscarinic M3 AChR expressed in CHO-FlpIn cells assessed as IP-one accumulation after 40 mins by HTRF assay B 6.62 pEC50 239.88 nM EC50 J Med Chem (2017) 60: 9239-9250 [PMID:29094937]
ChEMBL Agonist activity at human muscarinic M3 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay B 6.69 pEC50 205 nM EC50 Bioorg. Med. Chem. Lett. (2015) 25: 4158-4163 [PMID:26299349]
ChEMBL Agonist activity at recombinant human muscarinic M3 receptor expressed in CHO cells assessed as upregulation in ERK1/2 phosphorylation after 5 mins by alphascreen assay B 7.64 pEC50 23 nM EC50 J Med Chem (2017) 60: 9239-9250 [PMID:29094937]
ChEMBL Agonist activity at recombinant human muscarinic M3 receptor expressed in CHO cells assessed as upregulation in ERK1/2 phosphorylation after 5 mins by alphascreen assay B 7.64 pEC50 22.91 nM EC50 J Med Chem (2017) 60: 9239-9250 [PMID:29094937]
ChEMBL Agonist activity at human muscarinic M3 receptor expressed in BHK-21 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assay F 8.49 pEC50 3.2 nM EC50 J. Med. Chem. (2010) 53: 6386-6397 [PMID:20684563]
ChEMBL Agonist activity at human muscarinic M3 receptor expressed in BHK-21 cells assessed as calcium mobilization for 6 mins by Calcium4-based staining F 8.49 pEC50 3.2 nM EC50 Bioorg. Med. Chem. Lett. (2012) 22: 5134-5140 [PMID:22677319]
M3 receptor in Rat [GtoPdb: 15] [UniProtKB: P08483]
GtoPdb - - 5.6 pKi - - - J Pharmacol Exp Ther (2002) 303: 29-35 [PMID:12235229]
M4 receptor/Muscarinic acetylcholine receptor M4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1821] [GtoPdb: 16] [UniProtKB: P08173]
ChEMBL Displacement of [3H]NMS from human cloned muscarinic M4 receptor expressed in CHO cells B 5.07 pKi 8511.38 nM Ki Bioorg. Med. Chem. Lett. (2008) 18: 614-618 [PMID:18077164]
GtoPdb - - 5.6 pKi - - - Mol Pharmacol (1997) 52: 172-9 [PMID:9224827];
Mol Pharmacol (2013) 84: 425-37 [PMID:23798605]
ChEMBL Positive allosteric modulatory activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as as increase in acteylcholine-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol/acetylcholine by Glosensor cAMP reagent/plate reader based luminescence assay B 7.24 pEC50 57 nM EC50 ACS Med Chem Lett (2019) 10: 941-948 [PMID:31223452]
ChEMBL Agonist activity at human muscarinic M4 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay B 7.31 pEC50 48.8 nM EC50 Bioorg. Med. Chem. Lett. (2015) 25: 4158-4163 [PMID:26299349]
ChEMBL Agonist activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as decrease in isoproterenol-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol by Glosensor cAMP reagent/plate reader based luminescence assay B 7.37 pEC50 43 nM EC50 ACS Med Chem Lett (2019) 10: 941-948 [PMID:31223452]
ChEMBL Agonist activity at human muscarinic M4 receptor expressed in BHK-21 cells coexpressing Galpha16 subunit assessed as increase of acetylcholine-induced calcium flux by FLIPR assay F 8 pEC50 10 nM EC50 J. Med. Chem. (2010) 53: 6386-6397 [PMID:20684563]
ChEMBL Agonist activity at muscarinic human M4 receptor expressed in BHK-21 cells assessed as calcium mobilization for 6 mins by Calcium4-based staining F 8 pEC50 10 nM EC50 Bioorg. Med. Chem. Lett. (2012) 22: 5134-5140 [PMID:22677319]
M5 receptor/Muscarinic acetylcholine receptor M5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2035] [GtoPdb: 17] [UniProtKB: P08912]
ChEMBL Displacement of [3H]NMS from human cloned muscarinic M5 receptor expressed in CHO cells B 5.01 pKi 9772.37 nM Ki Bioorg. Med. Chem. Lett. (2008) 18: 614-618 [PMID:18077164]
GtoPdb - - 6.1 pKi - - - J Pharmacol Exp Ther (2002) 303: 29-35 [PMID:12235229]
ChEMBL Agonistic activity against muscarinic acetylcholine receptor M5 expressed in NIH 3T3 cells. F 6.2 pEC50 630 nM EC50 J. Med. Chem. (2001) 44: 4563-4576 [PMID:11741475]
ChEMBL Agonist activity at human muscarinic M5 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay B 7.72 pEC50 19.1 nM EC50 Bioorg. Med. Chem. Lett. (2015) 25: 4158-4163 [PMID:26299349]
ChEMBL Agonist activity at human muscarinic M5 receptor expressed in BHK-21 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assay F 8.92 pEC50 1.2 nM EC50 J. Med. Chem. (2010) 53: 6386-6397 [PMID:20684563]
ChEMBL Agonist activity at human muscarinic M5 receptor expressed in BHK-21 cells assessed as calcium mobilization for 6 mins by Calcium4-based staining F 8.92 pEC50 1.2 nM EC50 Bioorg. Med. Chem. Lett. (2012) 22: 5134-5140 [PMID:22677319]
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]
ChEMBL Binding affinity towards rat forebrain nicotinic acetylcholine receptor using [3H]EB as radioligand B 7.37 pKi 43 nM Ki Bioorg. Med. Chem. Lett. (2004) 14: 1845-1848 [PMID:15050613]
ChEMBL Compound was evaluated for functional potencies and efficacies at rat Nicotinic acetylcholine receptor subtype PC12 (ganglionic) B 4.4 pEC50 40000 nM EC50 J. Med. Chem. (1997) 40: 4169-4194 [PMID:9435889]
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]
ChEMBL Binding affinity towards rat nicotinic acetylcholine receptor alpha2-beta2 expressed in HEK293 cells using [3H]EB as radioligand B 7.96 pKi 11 nM Ki Bioorg. Med. Chem. Lett. (2004) 14: 1845-1848 [PMID:15050613]
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]
ChEMBL Binding affinity towards rat Nicotinic acetylcholine receptor alpha3-beta2 expressed in HEK293 cells using [3H]EB as radioligand B 7.39 pKi 41 nM Ki Bioorg. Med. Chem. Lett. (2004) 14: 1845-1848 [PMID:15050613]
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 Compound was evaluated for functional potencies and efficacies at human Nicotinic acetylcholine receptor subtype IMR-32 (ganglionic) B 4.52 pEC50 30000 nM EC50 J. Med. Chem. (1997) 40: 4169-4194 [PMID:9435889]
ChEMBL Agonist activity at alpha3beta4 nAChR expressed in HEK293 cells by FLIPR membrane potential assay F 4.7 pEC50 19952.62 nM EC50 Bioorg. Med. Chem. Lett. (2009) 19: 87-91 [PMID:19027295]
ChEMBL Agonist activity at alpha3beta4 nAChR expressed in HEK293 cells by FLIPR membrane potential assay F 4.72 pEC50 19000 nM EC50 Bioorg. Med. Chem. Lett. (2009) 19: 87-91 [PMID:19027295]
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 Displacement of [3H]epibatidine from Alpha3 Beta4 Nicotinic acetylcholine receptor of rat brain homogenates B 6.06 pKi 881 nM Ki J. Med. Chem. (2005) 48: 5123-5130 [PMID:16078832]
ChEMBL Binding affinity towards rat Nicotinic acetylcholine receptor alpha3-beta4 expressed in HEK293 cells using [3H]EB as radioligand B 6.09 pKi 820 nM Ki Bioorg. Med. Chem. Lett. (2004) 14: 1845-1848 [PMID:15050613]
ChEMBL Displacement of [3H]epibatidine from rat alpha3beta4 nACHR expressed in HEK293 cells after 4 hrs by scintillation counting assay B 6.21 pKi 620 nM Ki Eur. J. Med. Chem. (2015) 102: 425-444 [PMID:26301559]
ChEMBL Displacement of [3H]epibatidine from rat alpha3beta4 nAChR expressed in HEK292 cells after 3 hrs B 6.21 pKi 620 nM Ki J. Med. Chem. (2010) 53: 8187-8191 [PMID:20979364]
ChEMBL Displacement of [3H]epibatidine from rat recombinant alpha3beta4 nAChR expressed in HEK293 cells after 4 hrs by scintillation counting analysis B 6.21 pKi 620 nM Ki J. Med. Chem. (2013) 56: 940-951 [PMID:23256554]
ChEMBL Displacement of [3H]epibatidine from rat recombinant alpha3beta4 nAChR expressed in HEK293 cells after 4 hrs by scintillation counting analysis B 6.21 pKi 616.6 nM Ki J. Med. Chem. (2013) 56: 940-951 [PMID:23256554]
ChEMBL Displacement of [3H]epibatidine from rat alpha3beta4 nACHR expressed in HEK293 cells after 4 hrs by scintillation counting assay B 6.21 pKi 616.6 nM Ki Eur. J. Med. Chem. (2015) 102: 425-444 [PMID:26301559]
ChEMBL Agonist activity at rat alpha-3-beta-4 nAChR expressed in HEK293 cells by FMP assay F 5.05 pEC50 8900 nM EC50 J. Med. Chem. (2008) 51: 7380-7395 [PMID:18989912]
ChEMBL Antagonist activity at rat alpha3beta4 nAChR expressed in HEK293 cells by FMP assay F 5.06 pEC50 8700 nM EC50 J. Med. Chem. (2007) 50: 4616-4629 [PMID:17722904]
ChEMBL Antagonist activity at rat alpha3beta4 nAChR expressed in HEK293 cells by FMP assay F 5.1 pEC50 7943.28 nM EC50 J. Med. Chem. (2007) 50: 4616-4629 [PMID:17722904]
ChEMBL Agonist activity at rat alpha-3-beta-4 nAChR expressed in HEK293 cells by FMP assay F 5.1 pEC50 7943.28 nM EC50 J. Med. Chem. (2008) 51: 7380-7395 [PMID:18989912]
nicotinic acetylcholine receptor β2 subunit/nicotinic acetylcholine receptor α4 subunit/Neuronal acetylcholine receptor; alpha4/beta2 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL1907589] [GtoPdb: 472465] [UniProtKB: P17787P43681]
ChEMBL Agonist activity at human alpha4beta2 nAChR in (alpha4)3(beta2)2 stoichiometry form B 4 pEC50 100000 nM EC50 J. Med. Chem. (2015) 58: 6665-6677 [PMID:26225816]
ChEMBL Agonist activity at human alpha4beta2 nAChR low affinity form expressed in rat GH4C1 cells assessed as induction of peak current amplitude at holding potential of -70 mV by whole-cell patch clamp assay B 4 pEC50 100000 nM EC50 J. Med. Chem. (2015) 58: 6665-6677 [PMID:26225816]
ChEMBL Agonist activity at alpha4beta2 nAChR low sensitivity form F 4 pEC50 100000 nM EC50 J. Med. Chem. (2012) 55: 9929-9945 [PMID:23025891]
ChEMBL Agonist activity at human alpha-4-beta-2 nAChR expressed in Xenopus oocytes by two-electrode voltage clamp technique F 4.15 pEC50 70794.58 nM EC50 J. Med. Chem. (2008) 51: 7380-7395 [PMID:18989912]
ChEMBL Agonist activity at human alpha-4-beta-2 nAChR expressed in Xenopus oocytes by two-electrode voltage clamp technique F 4.15 pEC50 70000 nM EC50 J. Med. Chem. (2008) 51: 7380-7395 [PMID:18989912]
ChEMBL Partial agonist activity at human 2:3 alpha4beta2 nAChR expressed in Xenopus laevis oocytes after 1 min by two electrode voltage clamp technique B 5.8 pEC50 1600 nM EC50 J. Med. Chem. (2013) 56: 940-951 [PMID:23256554]
ChEMBL Agonist activity at human alpha4beta2 nAChR in (alpha4)2(beta2)3 stoichiometry form B 6 pEC50 1000 nM EC50 J. Med. Chem. (2015) 58: 6665-6677 [PMID:26225816]
ChEMBL Agonist activity at alpha4beta2 nAChR high sensitivity form F 6 pEC50 1000 nM EC50 J. Med. Chem. (2012) 55: 9929-9945 [PMID:23025891]
ChEMBL Agonist activity at human alpha4beta2 nAChR high affinity form expressed in rat GH4C1 cells assessed as induction of peak current amplitude at holding potential of -70 mV by whole-cell patch clamp assay B 6.4 pEC50 400 nM EC50 J. Med. Chem. (2015) 58: 6665-6677 [PMID:26225816]
ChEMBL Activation of alpha4beta2* nAChR low affinity site (unknown origin) expressed in xenopus oocytes by electrophysiology method B 7.14 pEC50 73 nM EC50 J. Med. Chem. (2014) 57: 8204-8223 [PMID:24901260]
ChEMBL Activation of alpha4beta2* nAChR high affinity site (unknown origin) expressed in xenopus oocytes by electrophysiology method B 8.77 pEC50 1.7 nM EC50 J. Med. Chem. (2014) 57: 8204-8223 [PMID:24901260]
nicotinic acetylcholine receptor α4 subunit/nicotinic acetylcholine receptor β2 subunit/Neuronal acetylcholine receptor; alpha4/beta2 in Rat (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL1907596] [GtoPdb: 465472] [UniProtKB: P09483P12390]
ChEMBL Binding affinity towards rat Nicotinic acetylcholine receptor alpha4-beta2 expressed in HEK293 cells using [3H]EB as radioligand B 7.35 pKi 45 nM Ki Bioorg. Med. Chem. Lett. (2004) 14: 1845-1848 [PMID:15050613]
ChEMBL Displacement of [3H]cystisine from nicotinic alpha-4-beta-2 receptor in rat brain B 7.41 pKi 39 nM Ki Bioorg. Med. Chem. Lett. (2008) 18: 2188-2193 [PMID:18262785]
ChEMBL Displacement of [3H]epibatidine from rat alpha4beta2 nAChR expressed in HEK292 cells after 3 hrs B 7.42 pKi 37.7 nM Ki J. Med. Chem. (2010) 53: 8187-8191 [PMID:20979364]
ChEMBL Displacement of [3H]epibatidine from rat alpha4beta2 nAChR expressed in HEK293 cells after 4 hrs by scintillation counting assay B 7.48 pKi 33.11 nM Ki Eur. J. Med. Chem. (2015) 102: 425-444 [PMID:26301559]
ChEMBL Displacement of [3H]epibatidine from rat recombinant alpha4beta2 nAChR expressed in HEK293 cells after 4 hrs by scintillation counting analysis B 7.48 pKi 33.11 nM Ki J. Med. Chem. (2013) 56: 940-951 [PMID:23256554]
ChEMBL