xanomeline [Ligand Id: 57] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL21536 (LY-246708, LY246708, LY-246708 FREE BASE, Xanomeline) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| M1 receptor/Muscarinic acetylcholine receptor M1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL216] [GtoPdb: 13] [UniProtKB: P11229] | ||||||||
| ChEMBL | Displacement of [3H]NMS from human muscarinic M1 receptor expressed in CHO cells in ternary complex by EATCM analysis | B | 4.94 | pKd | 4.94 | - | logKd | J Med Chem (2010) 53: 2094-2103 [PMID:20158205] |
| ChEMBL | Displacement of [3H]NMS from human muscarinic M1 receptor expressed in CHO cells in binary complex by EATCM analysis | B | 7.4 | pKd | 7.4 | - | logKd | J Med Chem (2010) 53: 2094-2103 [PMID:20158205] |
| ChEMBL | Inhibition of [3H](R)-QNB binding to human M1 receptor Thr192Ala mutant expressed in A9 L cells | B | 5.4 | pKi | 3981.07 | nM | Ki | J Med Chem (2006) 49: 7518-7531 [PMID:17149881] |
| ChEMBL | Inhibition of [3H](R)-QNB to Muscarinic acetylcholine receptor M1 expressed in A9 L cells | B | 6.8 | pKi | 158.49 | nM | Ki | J Med Chem (2003) 46: 4273-4286 [PMID:13678406] |
| ChEMBL | Inhibition of [3H](R)-QNB binding to human M1 receptor expressed in A9 L cells | B | 6.8 | pKi | 158.49 | nM | Ki | J Med Chem (2006) 49: 7518-7531 [PMID:17149881] |
| ChEMBL | Binding affinity towards M1 muscarinic receptor expressed in A9 L cells by displacing [3H](R)-QNB radioligand. | B | 7.09 | pKi | 82 | nM | Ki | J Med Chem (2001) 44: 4563-4576 [PMID:11741475] |
| ChEMBL | Affinity towards human M1 receptor expressed in CHO cells using [3H]QNB as radioligand | B | 7.38 | pKi | 42 | nM | Ki | Bioorg Med Chem Lett (1999) 9: 1895-1900 [PMID:10450949] |
| GtoPdb | - | - | 7.9 | pKi | - | - | - |
Br J Pharmacol (1998) 125: 1413-20 [PMID:9884068]; Mol Pharmacol (1998) 53: 1120-30 [PMID:9614217]; Br J Pharmacol (1999) 126: 1620-4 [PMID:10323594]; Nat Chem Biol (2023) 19: 805-814 [PMID:36782010] |
| ChEMBL | Binding affinity to human cloned muscarinic M1 receptor expressed in CHO cells | B | 8.1 | pKi | 7.94 | nM | Ki | Bioorg Med Chem (2008) 16: 3049-3058 [PMID:18182302] |
| ChEMBL | Displacement of [3H]NMS from human M1 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assay | B | 8.1 | pKi | 7.94 | nM | Ki | J Med Chem (2014) 57: 9065-9077 [PMID:25275964] |
| ChEMBL | Displacement of [3H]NMS from human muscarinic M1 receptor expressed in CHO cells by wash-resistant binding method | B | 5.31 | pIC50 | 4897.79 | nM | IC50 | Bioorg Med Chem (2008) 16: 1376-1392 [PMID:17977730] |
| ChEMBL | Displacement of [3H]NMS from human muscarinic M1 receptor expressed in CHO cells at pH 6 by wash-resistant binding method | B | 5.62 | pIC50 | 2398.83 | nM | IC50 | Bioorg Med Chem (2008) 16: 1376-1392 [PMID:17977730] |
| ChEMBL | Displacement of [3H]NMS from human muscarinic M1 receptor expressed in CHO cells at pH 8 by wash-resistant binding method | B | 6.02 | pIC50 | 954.99 | nM | IC50 | Bioorg Med Chem (2008) 16: 1376-1392 [PMID:17977730] |
| ChEMBL | Displacement of [3H]NMS from human muscarinic M1 receptor expressed in CHO cells in continuous presence of radioligand | B | 7.09 | pIC50 | 81.28 | nM | IC50 | Bioorg Med Chem (2008) 16: 1376-1392 [PMID:17977730] |
| ChEMBL | Displacement of [3H]NMS from human muscarinic M1 receptor expressed in CHO cells at pH 8 in continuous presence of radioligand | B | 7.54 | pIC50 | 28.84 | nM | IC50 | Bioorg Med Chem (2008) 16: 1376-1392 [PMID:17977730] |
| ChEMBL | Displacement of [3H]NMS from human muscarinic M1 receptor expressed in CHO cells at pH 6 in continuous presence of radioligand | B | 7.74 | pIC50 | 18.2 | nM | IC50 | Bioorg Med Chem (2008) 16: 1376-1392 [PMID:17977730] |
| ChEMBL | Agonist activity at human M1 receptor expressed in HEK293T cells by BRET based beta-arrestin engagement assay | B | 4.79 | pEC50 | 16218.1 | nM | EC50 | J Med Chem (2014) 57: 9065-9077 [PMID:25275964] |
| ChEMBL | Agonistic activity against M1 muscarinic receptor expressed in NIH 3T3 cells | F | 5.59 | pEC50 | 2600 | nM | EC50 | J Med Chem (2001) 44: 4563-4576 [PMID:11741475] |
| ChEMBL | Agonist activity at human M1 receptor expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysis | F | 6.5 | pEC50 | 316.23 | nM | EC50 | J Med Chem (2006) 49: 7518-7531 [PMID:17149881] |
| ChEMBL | Effective concentration required for stimulation of phosphoinositol (PI) hydrolysis in the A9 L cell line transfected with the Muscarinic acetylcholine receptor M1. | F | 6.7 | pEC50 | 200 | nM | EC50 | J Med Chem (1998) 41: 379-392 [PMID:9464368] |
| ChEMBL | Agonist activity at human M1 receptor E170K mutant expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysis | F | 6.8 | pEC50 | 158.49 | nM | EC50 | J Med Chem (2006) 49: 7518-7531 [PMID:17149881] |
| ChEMBL | Agonist activity at human M1 receptor Q185E mutant expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysis | F | 6.8 | pEC50 | 158.49 | nM | EC50 | J Med Chem (2006) 49: 7518-7531 [PMID:17149881] |
| ChEMBL | Stimulation of phosphoinositol hydrolysis in the mouse fibroblast cell line A9L-M1 expressing Muscarinic acetylcholine receptor M1. | F | 6.87 | pEC50 | 134.5 | nM | EC50 | J Med Chem (1999) 42: 1999-2006 [PMID:10354408] |
| ChEMBL | Agonist activity at human muscarinic M1 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay | F | 7.17 | pEC50 | 67.3 | nM | EC50 | Bioorg Med Chem Lett (2015) 25: 4158-4163 [PMID:26299349] |
| ChEMBL | Agonistic activity against M1 muscarinic receptor expressed in A9 L cells. | F | 7.24 | pEC50 | 57 | nM | EC50 | J Med Chem (2001) 44: 4563-4576 [PMID:11741475] |
| ChEMBL | Agonist activity at human M1 receptor expressed in HEK293T cells by BRET based Gq protein engagement assay | B | 7.8 | pEC50 | 15.85 | nM | EC50 | J Med Chem (2014) 57: 9065-9077 [PMID:25275964] |
| ChEMBL | Agonist activity at human M1 receptor expressed in HEK293T cells by BRET based Gq protein activation assay | B | 7.88 | pEC50 | 13.18 | nM | EC50 | J Med Chem (2014) 57: 9065-9077 [PMID:25275964] |
| ChEMBL | Effective concentration was evaluated against Muscarinic acetylcholine receptor M1 expressed in A9 L cells | B | 8 | pEC50 | 10 | nM | EC50 | J Med Chem (2003) 46: 4273-4286 [PMID:13678406] |
| 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 | 8.8 | pEC50 | 1.6 | nM | EC50 | J Med Chem (2010) 53: 6386-6397 [PMID:20684563] |
| M1 receptor/Muscarinic acetylcholine receptor M1 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3733] [GtoPdb: 13] [UniProtKB: P12657] | ||||||||
| ChEMBL | Tested against Muscarinic acetylcholine receptor M1 expressed in A9 L cell line | B | 5.24 | pEC50 | 5700 | nM | EC50 | J Med Chem (1997) 40: 1230-1246 [PMID:9111297] |
| M1 receptor/Muscarinic acetylcholine receptor M1 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL276] [GtoPdb: 13] [UniProtKB: P08482] | ||||||||
| ChEMBL | In vitro binding affinity towards Muscarinic acetylcholine receptor M1 by the displacement of [3H]oxotremorine-M in rat brain membranes | B | 8 | pIC50 | 10 | nM | IC50 | Bioorg Med Chem Lett (1994) 4: 2205-2210 |
| ChEMBL | Displacement of [3H]oxotremorine-M (Oxo-M) from rat hippocampus muscarinic acetylcholine receptor M1 | B | 8.01 | pIC50 | 9.7 | nM | IC50 | J Med Chem (1992) 35: 4011-4019 [PMID:1433209] |
| ChEMBL | Displacement of [3H]pirenzepine (Pz) from rat hippocampus muscarinic acetylcholine receptor M1 | B | 8.15 | pIC50 | 7 | nM | IC50 | J Med Chem (1992) 35: 4011-4019 [PMID:1433209] |
| ChEMBL | In vitro binding affinity towards Muscarinic acetylcholine receptor M1 by the displacement of [3H]pirenzepine in rat cerebral cortical membranes | B | 8.15 | pIC50 | 7 | nM | IC50 | Bioorg Med Chem Lett (1994) 4: 2205-2210 |
| ChEMBL | Displacement of [3H]-Pz (pirenzepine) from the muscarinic receptor M1 of the rat hippocampus | B | 8.15 | pIC50 | 7 | nM | IC50 | Bioorg Med Chem Lett (1992) 2: 809-814 |
| ChEMBL | Binding activity against muscarinic acetylcholine receptor M1 in rat brain, using [3H]-Pz as the radioligand. | B | 8.3 | pIC50 | 5 | nM | IC50 | J Med Chem (1995) 38: 3469-3481 [PMID:7658434] |
| ChEMBL | Binding affinity for muscarinic acetylcholine receptor M1 using [3H]pirenzepine (Pz) radioligand in rat hippocampus membranes. | B | 8.3 | pIC50 | 5 | nM | IC50 | J Med Chem (1998) 41: 379-392 [PMID:9464368] |
| ChEMBL | Binding activity against muscarinic acetylcholine receptor M1 in rat brain, using [3H]OXO-M as the radioligand. | B | 8.7 | pIC50 | 2 | nM | IC50 | J Med Chem (1995) 38: 3469-3481 [PMID:7658434] |
| ChEMBL | Binding affinity for muscarinic acetylcholine receptor M1 using [3H]oxotremorine-M (Oxo-M) radioligand in rat hippocampus membranes | B | 8.7 | pIC50 | 2 | nM | IC50 | J Med Chem (1998) 41: 379-392 [PMID:9464368] |
| M2 receptor/Muscarinic acetylcholine receptor M2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL211] [GtoPdb: 14] [UniProtKB: P08172] | ||||||||
| ChEMBL | Displacement of [3H]UR-AP060 from human muscarinic acetylcholine receptor M2 expressed in CHOK9 cell homogenate after 3 hrs by liquid scintillation counting assay | B | 5.35 | pKi | 4466.84 | nM | Ki | J Med Chem (2017) 60: 3314-3334 [PMID:28388054] |
| ChEMBL | Displacement of 4-(2-((1E,3E)-5-((E)-3,3-Dimethyl-1-(6-oxo-6-((2-(4-(4-(1-(2-oxo-2-(11-oxo-10,11-dihydro-5H-dibenzo[b,e][1,4]diazepin-5-yl)ethyl)piperidin-4-yl)butyl)piperazin-1-yl)ethyl)amino)hexyl)indolin-2-ylidene)penta-1,3-dien-1-yl)-3,3-dimethyl-3H-indol-1-ium-1-yl)butane-1-sulfonate Tris(hydrotrifluoroacetate fluorescent tracer from human muscarinic M2 receptor expressed in CHO-K9 cells measured after 60 mins by Hoechst H33342 dye based confocal plate reader assay | B | 6.14 | pKi | 724.44 | nM | Ki | J Med Chem (2020) 63: 4133-4154 [PMID:32233403] |
| ChEMBL | Displacement of 4-(2-((1E,3E)-5-((E)-3,3-Dimethyl-1-(6-oxo-6-((2-(4-(4-(1-(2-oxo-2-(11-oxo-10,11-dihydro-5H-dibenzo[b,e][1,4]diazepin-5-yl)ethyl)piperidin-4-yl)butyl)piperazin-1-yl)ethyl)amino)hexyl)-5-sulfoindolin-2-ylidene)penta-1,3-dien-1-yl)-3,3-dimethyl-3H-indol-1-ium-1-yl)butane-1-sulfonate Bis(hydrotrifluoroacetate) fluorescent tracer from human muscarinic M2 receptor expressed in CHO-K9 cells measured after 60 mins by Hoechst H33342 dye based confocal plate reader assay | B | 6.42 | pKi | 380.19 | nM | Ki | J Med Chem (2020) 63: 4133-4154 [PMID:32233403] |
| ChEMBL | Displacement of 4-(2-((1E,3E)-5-((E)-3,3-Dimethyl-1-(6-oxo-6-((2-(3-(1-(4-(1-(2-oxo-2-(11-oxo-10,11-dihydro-5H-dibenzo[b,e][1,4]diazepin-5-yl)ethyl)piperidin-4-yl)butyl)-1H-imidazol-4-yl)propanamido)ethyl)-amino)hexyl)-5-sulfoindolin-2-ylidene)penta-1,3-dien-1-yl)-3,3-dimethyl-3H-indol-1-ium-1-yl)butane-1-sulfonateHydrotrifluoroacetate fluorescent tracer from human muscarinic M2 receptor expressed in CHO-K9 cells measured after 60 mins by Hoechst H33342 dye based confocal plate reader assay | B | 6.49 | pKi | 323.59 | nM | Ki | J Med Chem (2020) 63: 4133-4154 [PMID:32233403] |
| ChEMBL | Displacement of 4-(2-((1E,3E)-5-((E)-1-(6-((3,5-Bis((2-(3-(1-(4-(1-(2-oxo-2-(11-oxo-10,11-dihydro-5H-dibenzo[b,e][1,4]diazepin-5-yl)ethyl)piperidin-4-yl)butyl)-1H-imidazol-4-yl)propanamido)ethyl)carbamoyl)benzyl)amino)-6-oxohexyl)-3,3-dimethyl-5-sulfoindolin-2-ylidene)penta-1,3-dien-1-yl)-3,3-dimethyl-3H-indol-1-ium-1-yl)butane-1-sulfonate Tris(hydrotrifluoroacetate) fluorescent tracer from human muscarinic M2 receptor expressed in CHO-K9 cells measured after 60 mins by Hoechst H33342 dye based confocal plate reader assay | B | 6.56 | pKi | 275.42 | nM | Ki | J Med Chem (2020) 63: 4133-4154 [PMID:32233403] |
| ChEMBL | Displacement of [3H]UNSW-MK259 from human muscarinic acetylcholine receptor M2 expressed in CHOK9 cells after 3 hrs by liquid scintillation counting assay | B | 6.57 | pKi | 269.15 | nM | Ki | J Med Chem (2017) 60: 3314-3334 [PMID:28388054] |
| ChEMBL | Displacement of 4-(2-((1E,3E)-5-((E)-3,3-Dimethyl-1-(6-oxo-6-((2-(4-(4-(1-(2-oxo-2-(11-oxo-10,11-dihydro-5H-dibenzo[b,e][1,4]diazepin-5-yl)ethyl)piperidin-4-yl)butyl)piperazin-1-yl)ethyl)amino)hexyl)-5-sulfoindolin-2-ylidene)penta-1,3-dien-1-yl)-3,3-dimethyl-3H-indol-1-ium-1-yl)butane-1-sulfonate Bis(hydrotrifluoroacetate) fluorescent tracer from human muscarinic M2 receptor expressed in CHO-K9 cells by FACSCalibur flow cytometry | B | 6.67 | pKi | 213.8 | nM | Ki | J Med Chem (2020) 63: 4133-4154 [PMID:32233403] |
| ChEMBL | Displacement of [3H]-NMS from human muscarinic M2 receptor expressed in CHO-K9 cells measured after 60 mins by Hoechst H33342 dye based confocal plate reader assay | B | 6.7 | pKi | 199.53 | nM | Ki | J Med Chem (2020) 63: 4133-4154 [PMID:32233403] |
| ChEMBL | Displacement of [3H]-AFDX-384 from human muscarinic M2 receptor expressed in CHO-K1 cells | B | 6.92 | pKi | 120 | nM | Ki | J Med Chem (2010) 53: 6386-6397 [PMID:20684563] |
| ChEMBL | Inhibition of [3H](R)-QNB binding to human M2 receptor expressed in A9 L cells | B | 7.3 | pKi | 50.12 | nM | Ki | J Med Chem (2006) 49: 7518-7531 [PMID:17149881] |
| ChEMBL | Compound was tested for binding inhibition of [3H](R)-QNB to Muscarinic acetylcholine receptor M2 expressed in A9 L cells | B | 7.3 | pKi | 50.12 | nM | Ki | J Med Chem (2003) 46: 4273-4286 [PMID:13678406] |
| GtoPdb | - | - | 7.4 | pKi | - | - | - |
Br J Pharmacol (1998) 125: 1413-20 [PMID:9884068]; Br J Pharmacol (1999) 126: 1620-4 [PMID:10323594]; Nat Chem Biol (2023) 19: 805-814 [PMID:36782010] |
| ChEMBL | Binding affinity to human cloned muscarinic M2 receptor expressed in CHO cells | B | 7.93 | pKi | 11.75 | nM | Ki | Bioorg Med Chem (2008) 16: 3049-3058 [PMID:18182302] |
| ChEMBL | Displacement of [3H]NMS from human M2 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assay | B | 8.09 | pKi | 8.13 | nM | Ki | J Med Chem (2014) 57: 9065-9077 [PMID:25275964] |
| ChEMBL | Displacement of [3H]NMS from human muscarinic acetylcholine receptor M2 expressed in CHO cells after 60 mins by scintillation counting assay | B | 6.5 | pIC50 | 316.23 | nM | IC50 | J Med Chem (2017) 60: 3314-3334 [PMID:28388054] |
| ChEMBL | Inhibitory activity was evaluated against Muscarinic acetylcholine receptor M2 expressed in A9 L cells | B | 7.9 | pIC50 | 12.59 | nM | IC50 | J Med Chem (2003) 46: 4273-4286 [PMID:13678406] |
| ChEMBL | Compound was tested for its potency towards Muscarinic acetylcholine receptor M2 by inhibiting forskolin induced c-AMP formation in CHO-M2 cells | F | 6.4 | pEC50 | 398 | nM | EC50 | J Med Chem (1999) 42: 1999-2006 [PMID:10354408] |
| ChEMBL | Agonist activity at human muscarinic M2 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay | F | 6.92 | pEC50 | 121 | nM | EC50 | Bioorg Med Chem Lett (2015) 25: 4158-4163 [PMID:26299349] |
| M2 receptor/Muscarinic acetylcholine receptor M2 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL309] [GtoPdb: 14] [UniProtKB: P10980] | ||||||||
| ChEMBL | In vitro Muscarinic acetylcholine receptor M2 binding was evaluated in rat brain membranes by using [3H]- Oxo-M | B | 7.8 | pIC50 | 16 | nM | IC50 | J Med Chem (1999) 42: 1999-2006 [PMID:10354408] |
| M3 receptor/Muscarinic acetylcholine receptor M3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL245] [GtoPdb: 15] [UniProtKB: P20309] | ||||||||
| ChEMBL | Compound was tested for binding inhibition of [3H](R)-QNB to Muscarinic acetylcholine receptor M3 expressed in A9 L cells | B | 7.1 | pKi | 79.43 | nM | Ki | J Med Chem (2003) 46: 4273-4286 [PMID:13678406] |
| ChEMBL | Inhibition of [3H](R)-QNB binding to human M3 receptor expressed in A9 L cells | B | 7.1 | pKi | 79.43 | nM | Ki | J Med Chem (2006) 49: 7518-7531 [PMID:17149881] |
| GtoPdb | - | - | 7.4 | pKi | - | - | - |
Br J Pharmacol (1998) 125: 1413-20 [PMID:9884068]; Br J Pharmacol (1999) 126: 1620-4 [PMID:10323594]; Nat Chem Biol (2023) 19: 805-814 [PMID:36782010] |
| ChEMBL | Displacement of [3H]-4-DAMP from human muscarinic M3 receptor expressed in BHK-21 cells | B | 7.89 | pKi | 13 | nM | Ki | J Med Chem (2010) 53: 6386-6397 [PMID:20684563] |
| ChEMBL | Displacement of [3H]NMS from human M3 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assay | B | 8.11 | pKi | 7.76 | nM | Ki | J Med Chem (2014) 57: 9065-9077 [PMID:25275964] |
| ChEMBL | Agonist activity at human M3 receptor expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysis | F | 4.6 | pEC50 | 25118.86 | nM | EC50 | J Med Chem (2006) 49: 7518-7531 [PMID:17149881] |
| 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 | 6.92 | pEC50 | 120 | nM | EC50 | J Med Chem (2010) 53: 6386-6397 [PMID:20684563] |
| M3 receptor/Muscarinic acetylcholine receptor M3 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5105] [GtoPdb: 15] [UniProtKB: Q9ERZ3] | ||||||||
| ChEMBL | Tested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell line | F | 4.96 | pEC50 | 11000 | nM | EC50 | J Med Chem (1997) 40: 1230-1246 [PMID:9111297] |
| M4 receptor/Muscarinic acetylcholine receptor M4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1821] [GtoPdb: 16] [UniProtKB: P08173] | ||||||||
| ChEMBL | Displacement of [3H]-4-DAMP from human muscarinic M4 receptor expressed in BHK-21 cells | B | 7.14 | pKi | 72 | nM | Ki | J Med Chem (2010) 53: 6386-6397 [PMID:20684563] |
| ChEMBL | Compound was tested for binding inhibition of [3H](R)-QNB to Muscarinic acetylcholine receptor M4 expressed in A9 L cells | B | 7.4 | pKi | 39.81 | nM | Ki | J Med Chem (2003) 46: 4273-4286 [PMID:13678406] |
| ChEMBL | Inhibition of [3H](R)-QNB binding to human M4 receptor expressed in A9 L cells | B | 7.4 | pKi | 39.81 | nM | Ki | J Med Chem (2006) 49: 7518-7531 [PMID:17149881] |
| GtoPdb | - | - | 7.7 | pKi | - | - | - |
Br J Pharmacol (1998) 125: 1413-20 [PMID:9884068]; Br J Pharmacol (1999) 126: 1620-4 [PMID:10323594]; Nat Chem Biol (2023) 19: 805-814 [PMID:36782010]; ACS Chem Neurosci (2022) 13: 1206-1218 [PMID:35380782] |
| ChEMBL | Displacement of [3H]NMS from human M4 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assay | B | 7.95 | pKi | 11.22 | nM | Ki | J Med Chem (2014) 57: 9065-9077 [PMID:25275964] |
| ChEMBL | Inhibitory activity was evaluated against Muscarinic acetylcholine receptor M4 expressed in A9 L cells | B | 7.6 | pIC50 | 25.12 | nM | IC50 | J Med Chem (2003) 46: 4273-4286 [PMID:13678406] |
| ChEMBL | Activity at human M4 receptor assessed as inhibition of forskolin-stimulated cAMP accumulation | F | 7.6 | pIC50 | 25.12 | nM | IC50 | J Med Chem (2006) 49: 7518-7531 [PMID:17149881] |
| ChEMBL | Agonist activity at human M4 receptor expressed in HEK293T cells by BRET based Gq protein engagement assay | B | 5.2 | pEC50 | 6309.57 | nM | EC50 | J Med Chem (2014) 57: 9065-9077 [PMID:25275964] |
| ChEMBL | Agonist activity at human muscarinic M4 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay | F | 6.64 | pEC50 | 229 | nM | EC50 | Bioorg Med Chem Lett (2015) 25: 4158-4163 [PMID:26299349] |
| ChEMBL | Agonist activity at human M4 receptor expressed in HEK293T cells by BRET based beta-arrestin engagement assay | B | 6.73 | pEC50 | 186.21 | nM | EC50 | J Med Chem (2014) 57: 9065-9077 [PMID:25275964] |
| 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 | 7.74 | pEC50 | 18 | nM | EC50 | ACS Med Chem Lett (2019) 10: 941-948 [PMID:31223452] |
| ChEMBL | Agonist activity at human M4 receptor expressed in HEK293T cells by BRET based Gq protein activation assay | B | 7.79 | pEC50 | 16.22 | nM | EC50 | J Med Chem (2014) 57: 9065-9077 [PMID:25275964] |
| 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 | 8.21 | pEC50 | 6.2 | nM | EC50 | J Med Chem (2010) 53: 6386-6397 [PMID:20684563] |
| 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 | 8.22 | pEC50 | 6 | nM | EC50 | ACS Med Chem Lett (2019) 10: 941-948 [PMID:31223452] |
| M5 receptor/Muscarinic acetylcholine receptor M5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2035] [GtoPdb: 17] [UniProtKB: P08912] | ||||||||
| ChEMBL | Compound was tested for binding inhibition of [3H](R)-QNB to Muscarinic acetylcholine receptor M5 expressed in A9 L cells | B | 5.8 | pKi | 1584.89 | nM | Ki | J Med Chem (2003) 46: 4273-4286 [PMID:13678406] |
| ChEMBL | Inhibition of [3H](R)-QNB binding to human M5 receptor expressed in A9 L cells | B | 5.8 | pKi | 1584.89 | nM | Ki | J Med Chem (2006) 49: 7518-7531 [PMID:17149881] |
| ChEMBL | Displacement of [3H]-4-DAMP from human muscarinic M5 receptor expressed in BHK-21 cells | B | 7.1 | pKi | 80 | nM | Ki | J Med Chem (2010) 53: 6386-6397 [PMID:20684563] |
| GtoPdb | - | - | 7.4 | pKi | - | - | - |
Br J Pharmacol (1998) 125: 1413-20 [PMID:9884068]; Br J Pharmacol (1999) 126: 1620-4 [PMID:10323594]; J Pharmacol Exp Ther (2005) 315: 313-9 [PMID:16002459]; Nat Chem Biol (2023) 19: 805-814 [PMID:36782010] |
| ChEMBL | Binding affinity to human cloned muscarinic M5 receptor expressed in CHO cells | B | 7.82 | pKi | 15.14 | nM | Ki | Bioorg Med Chem (2008) 16: 3049-3058 [PMID:18182302] |
| ChEMBL | Displacement of [3H]NMS from human M5 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assay | B | 8.03 | pKi | 9.33 | nM | Ki | J Med Chem (2014) 57: 9065-9077 [PMID:25275964] |
| ChEMBL | Agonist activity at human M5 receptor expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysis | F | 4.9 | pEC50 | 12589.25 | nM | EC50 | J Med Chem (2006) 49: 7518-7531 [PMID:17149881] |
| ChEMBL | Effective concentration was evaluated against Muscarinic acetylcholine receptor M5 expressed in A9 L cells | B | 5.6 | pEC50 | 2511.89 | nM | EC50 | J Med Chem (2003) 46: 4273-4286 [PMID:13678406] |
| ChEMBL | Agonist activity at human muscarinic M5 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay | F | 6.85 | pEC50 | 142 | 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 | 6.85 | pEC50 | 140 | nM | EC50 | J Med Chem (2010) 53: 6386-6397 [PMID:20684563] |
| 5-HT1A receptor in Human [GtoPdb: 1] [UniProtKB: P08908] | ||||||||
| GtoPdb | - | - | 7.2 | pKi | - | - | - | Br J Pharmacol (1998) 125: 1413-20 [PMID:9884068] |
| 5-HT1B receptor in Human [GtoPdb: 2] [UniProtKB: P28222] | ||||||||
| GtoPdb | - | - | 7.3 | pKi | - | - | - | Br J Pharmacol (1998) 125: 1413-20 [PMID:9884068] |
| 5-HT1D receptor in Human [GtoPdb: 3] [UniProtKB: P28221] | ||||||||
| GtoPdb | - | - | 8.2 | pKi | - | - | - | Br J Pharmacol (1998) 125: 1413-20 [PMID:9884068] |
| 5-ht1e receptor in Human [GtoPdb: 4] [UniProtKB: P28566] | ||||||||
| GtoPdb | - | - | 5.6 | pKi | - | - | - | Br J Pharmacol (1998) 125: 1413-20 [PMID:9884068] |
| 5-HT1F receptor in Human [GtoPdb: 5] [UniProtKB: P30939] | ||||||||
| GtoPdb | - | - | 6.5 | pKi | - | - | - | Br J Pharmacol (1998) 125: 1413-20 [PMID:9884068] |
| 5-HT2A receptor in Human [GtoPdb: 6] [UniProtKB: P28223] | ||||||||
| GtoPdb | - | - | 6.9 | pKi | - | - | - | Br J Pharmacol (1998) 125: 1413-20 [PMID:9884068] |
| 5-HT2B receptor in Human [GtoPdb: 7] [UniProtKB: P41595] | ||||||||
| GtoPdb | - | - | 7.7 | pKi | - | - | - | Br J Pharmacol (1998) 125: 1413-20 [PMID:9884068] |
| 5-HT2C receptor in Human [GtoPdb: 8] [UniProtKB: P28335] | ||||||||
| GtoPdb | - | - | 7.4 | pKi | - | - | - | Br J Pharmacol (1998) 125: 1413-20 [PMID:9884068] |
| 5-HT6 receptor in Human [GtoPdb: 11] [UniProtKB: P50406] | ||||||||
| GtoPdb | - | - | 5.9 | pKi | - | - | - | Br J Pharmacol (1998) 125: 1413-20 [PMID:9884068] |
| 5-HT7 receptor in Human [GtoPdb: 12] [UniProtKB: P34969] | ||||||||
| GtoPdb | - | - | 6.9 | pKi | - | - | - | Br J Pharmacol (1998) 125: 1413-20 [PMID:9884068] |
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]
