acetylcholine [Ligand Id: 294] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL667 (Acetylcholine) |
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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 | F | 6.43 | pEC50 | 371.54 | nM | EC50 | J Med Chem (2015) 58: 560-576 [PMID:25478907] |
| ChEMBL | Agonist activity at N-terminal FLAG tagged/C-terminal NanoLuc tagged human muscarinic M1 receptor expressed in HEK293T cells using furimazine as substrate assessed as receptor activation preincubated with substrate for 1 min followed by compound addition and measured for 6 mins 27 sec by NanoBRET assay | B | 6.72 | pEC50 | 190.55 | nM | EC50 | J Nat Prod (2023) 86: 869-881 [PMID:37042802] |
| 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 | F | 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 | F | 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 | F | 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 C-terminal NanoLuc tagged human muscarinic M2 receptor expressed in HEK293T cells using furimazine as substrate assessed as receptor activation preincubated with substrate for 1 min followed by compound addition and measured for 6 mins 27 sec by NanoBRET assay | B | 6.78 | pEC50 | 165.96 | nM | EC50 | J Nat Prod (2023) 86: 869-881 [PMID:37042802] |
| 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 | F | 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 | F | 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 | F | 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 | F | 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 C-terminal NanoLuc tagged human muscarinic M3 receptor expressed in HEK293T cells using furimazine as substrate assessed as receptor activation preincubated with substrate for 1 min followed by compound addition and measured for 6 mins 27 sec by NanoBRET assay | B | 6.3 | pEC50 | 501.19 | nM | EC50 | J Nat Prod (2023) 86: 869-881 [PMID:37042802] |
| 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 | F | 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 | Agonist activity at N-terminal FLAG tagged/C-terminal NanoLuc tagged human muscarinic M4 receptor expressed in HEK293T cells using furimazine as substrate assessed as receptor activation preincubated with substrate for 1 min followed by compound addition and measured for 6 mins 27 sec by NanoBRET assay | B | 6.87 | pEC50 | 134.9 | nM | EC50 | J Nat Prod (2023) 86: 869-881 [PMID:37042802] |
| 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 | F | 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 | F | 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 | F | 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 N-terminal FLAG tagged/C-terminal NanoLuc tagged human muscarinic M5 receptor expressed in HEK293T cells using furimazine as substrate assessed as receptor activation preincubated with substrate for 1 min followed by compound addition and measured for 6 mins 27 sec by NanoBRET assay | B | 6.83 | pEC50 | 147.91 | nM | EC50 | J Nat Prod (2023) 86: 869-881 [PMID:37042802] |
| ChEMBL | Agonist activity at human muscarinic M5 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay | F | 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: 464, 465, 463, 472, 473, 474, 466, 467, 469, 468, 470] [UniProtKB: P04757, P09483, P12389, P12390, P12391, P12392, P20420, P43143, P43144, Q05941, Q9JLB5] | ||||||||
| 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: 463, 472] [UniProtKB: P12389, P12390] | ||||||||
| 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: 464, 472] [UniProtKB: P04757, P12390] | ||||||||
| 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: 474, 464] [UniProtKB: P30926, P32297] | ||||||||
| 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: 464, 474] [UniProtKB: P04757, P12392] | ||||||||
| 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: 472, 465] [UniProtKB: P17787, P43681] | ||||||||
| 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: 465, 472] [UniProtKB: P09483, P12390] | ||||||||
| 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 | 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 | nM | Ki | J Med Chem (2013) 56: 940-951 [PMID:23256554] |
| 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 | nM | Ki | Eur J Med Chem (2015) 102: 425-444 [PMID:26301559] |
| ChEMBL | Displacement of [3H]-cytisine from Alpha4-beta2 Nicotinic acetylcholine receptor of rat brain homogenates | B | 8.12 | pKi | 7.6 | nM | Ki | J Med Chem (2005) 48: 5123-5130 [PMID:16078832] |
| ChEMBL | Functional potency measured as stimulation at rat Nicotinic acetylcholine receptor alpha4-beta2 expressed in Xenopus oocytes | F | 4.06 | pEC50 | 87000 | nM | EC50 | Bioorg Med Chem Lett (2004) 14: 1889-1896 [PMID:15050621] |
| ChEMBL | Agonist activity at rat alpha4beta2 expressed in Xenopus oocytes at -60 mV holding potential by electrophysiology method | B | 4.62 | pEC50 | 24000 | nM | EC50 | J Nat Prod (2018) 81: 1029-1035 [PMID:29671588] |
| nicotinic acetylcholine receptor α4 subunit/nicotinic acetylcholine receptor β4 subunit/Neuronal acetylcholine receptor; alpha4/beta4 in Rat (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL1907595] [GtoPdb: 465, 474] [UniProtKB: P09483, P12392] | ||||||||
| ChEMBL | Binding affinity towards rat Nicotinic acetylcholine receptor alpha4-beta4 expressed in HEK293 cells using [3H]EB as radioligand | B | 7.08 | pKi | 83 | nM | Ki | Bioorg Med Chem Lett (2004) 14: 1845-1848 [PMID:15050613] |
| ChEMBL | Displacement of [3H]epibatidine from rat recombinant alpha4beta4 nAChR expressed in HEK293 cells after 4 hrs by scintillation counting analysis | B | 7.24 | pKi | 58 | nM | Ki | J Med Chem (2013) 56: 940-951 [PMID:23256554] |
| ChEMBL | Displacement of [3H]epibatidine from rat alpha4beta4 nACHR expressed in HEK293 cells after 4 hrs by scintillation counting assay | B | 7.24 | pKi | 58 | nM | Ki | Eur J Med Chem (2015) 102: 425-444 [PMID:26301559] |
| ChEMBL | Displacement of [3H]epibatidine from rat recombinant alpha4beta4 nAChR expressed in HEK293 cells after 4 hrs by scintillation counting analysis | B | 7.24 | pKi | 57.54 | nM | Ki | J Med Chem (2013) 56: 940-951 [PMID:23256554] |
| ChEMBL | Displacement of [3H]epibatidine from rat alpha4beta4 nACHR expressed in HEK293 cells after 4 hrs by scintillation counting assay | B | 7.24 | pKi | 57.54 | nM | Ki | Eur J Med Chem (2015) 102: 425-444 [PMID:26301559] |
| ChEMBL | Functional potency measured as stimulation at rat Nicotinic acetylcholine receptor alpha4-beta4 expressed in Xenopus oocytes | F | 4.72 | pEC50 | 19000 | nM | EC50 | Bioorg Med Chem Lett (2004) 14: 1889-1896 [PMID:15050621] |
| nicotinic acetylcholine receptor α7 subunit/Neuronal acetylcholine receptor protein alpha-7 subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2492] [GtoPdb: 468] [UniProtKB: P36544] | ||||||||
| ChEMBL | Displacement of [3H]-MLA from human alpha7 nAChR expressed in human SH-SY5Y cells after 1.5 hrs by liquid scintillation counting | B | 5.1 | pKi | 7943.28 | nM | Ki | Bioorg Med Chem (2011) 19: 6107-6119 [PMID:21920761] |
| ChEMBL | Displacement of [3H]epibatidine from chimeric human alpha7-5-HT3A receptor expressed in HEK293 cells after 2 hrs by scintillation counter analysis | B | 6.3 | pKi | 501.19 | nM | Ki | Bioorg Med Chem (2012) 20: 5992-6002 [PMID:22959526] |
| ChEMBL | Agonist activity at human recombinant alpha7 nAChR expressed in Xenopus oocyte | F | 4.06 | pEC50 | 87000 | nM | EC50 | ACS Med Chem Lett (2010) 1: 422-426 [PMID:24900227] |
| ChEMBL | Agonist activity at human alpha-7 nAChR expressed in Xenopus oocytes by two-electrode voltage clamp technique | F | 4.08 | pEC50 | 83176.38 | nM | EC50 | J Med Chem (2008) 51: 7380-7395 [PMID:18989912] |
| ChEMBL | Agonist activity at human alpha-7 nAChR expressed in Xenopus oocytes by two-electrode voltage clamp technique | F | 4.08 | pEC50 | 83000 | nM | EC50 | J Med Chem (2008) 51: 7380-7395 [PMID:18989912] |
| ChEMBL | Agonist activity at human recombinant alpha7 nAChR expressed in Xenopus oocyte in presence of 6 uM (S)-ethyl 1-(2-cyanoethyl)pyrrolidine-2-carboxylate | F | 4.16 | pEC50 | 69000 | nM | EC50 | ACS Med Chem Lett (2010) 1: 422-426 [PMID:24900227] |
| ChEMBL | Antagonist activity at human alpha7nAChR co-expressed with human Ric3 in tsA201 cells by FMP assay | F | 5.4 | pEC50 | 4000 | nM | EC50 | J Med Chem (2007) 50: 4616-4629 [PMID:17722904] |
| ChEMBL | Antagonist activity at human alpha-7 nAChR in tsA201 cells coexpressed with Ric3 by FMP assay | F | 5.4 | pEC50 | 4000 | nM | EC50 | J Med Chem (2007) 50: 4616-4629 [PMID:17722904] |
| ChEMBL | Antagonist activity at human alpha7nAChR co-expressed with human Ric3 in tsA201 cells by FMP assay | F | 5.4 | pEC50 | 3981.07 | nM | EC50 | J Med Chem (2007) 50: 4616-4629 [PMID:17722904] |
| ChEMBL | Antagonist activity at human alpha-7 nAChR in tsA201 cells coexpressed with Ric3 by FMP assay | F | 5.4 | pEC50 | 3981.07 | nM | EC50 | J Med Chem (2007) 50: 4616-4629 [PMID:17722904] |
| nicotinic acetylcholine receptor α7 subunit/Neuronal acetylcholine receptor protein alpha-7 subunit in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4980] [GtoPdb: 468] [UniProtKB: Q05941] | ||||||||
| ChEMBL | Displacement of [125I]-alpha-bungarotoxin from alpha7 nAChR in rat hippocampus membranes | B | 4.6 | pKi | 25000 | nM | Ki | Bioorg Med Chem Lett (2013) 23: 6481-6485 [PMID:24128660] |
| ChEMBL | Displacement of [3H]alpha-bungaro-toxine from nicotinic alpha-7 receptor in rat brain | B | 5.45 | pKi | 3509 | nM | Ki | Bioorg Med Chem Lett (2008) 18: 2188-2193 [PMID:18262785] |
| ChEMBL | Agonist activity at rat alpha7 nAChR expressed in GH4C1 cells assessed as calcium influx measured every 1 sec for 1 min followed by every 30 secs for 10 mins by FLIPR assay | F | 5.51 | pEC50 | 3120 | nM | EC50 | J Med Chem (2012) 55: 4806-4823 [PMID:22468936] |
| Nicotinic acetylcholine receptor alpha8 subunit in Periplaneta americana (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2366437] [UniProtKB: H6TY12] | ||||||||
| ChEMBL | Agonist activity at Periplaneta americana (American cockroach) nAChR in terminal abdominal ganglion assessed as assessed as inward current by tight-seal whole cell patch clamp method | B | 4.94 | pEC50 | 11481.54 | nM | EC50 | J Pestic Sci (2006) 31: 35-40 |
ChEMBL data shown on this page come from version 34:
Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]
