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 33:
Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]
