xanomeline [Ligand Id: 57] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL21536 (Xanomeline)
  • M1 receptor/Muscarinic acetylcholine receptor M1 in Human [ChEMBL: CHEMBL216] [GtoPdb: 13] [UniProtKB: P11229]
  • M1 receptor/Muscarinic acetylcholine receptor M1 in Mouse [ChEMBL: CHEMBL3733] [GtoPdb: 13] [UniProtKB: P12657]
  • M1 receptor/Muscarinic acetylcholine receptor M1 in Rat [ChEMBL: CHEMBL276] [GtoPdb: 13] [UniProtKB: P08482]
  • 0
1 CHEMBL21536_lig_chart_1 Muscarinic acetylcholine receptor M1 HumanMouseRat
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  • M2 receptor/Muscarinic acetylcholine receptor M2 in Human [ChEMBL: CHEMBL211] [GtoPdb: 14] [UniProtKB: P08172]
  • M2 receptor/Muscarinic acetylcholine receptor M2 in Rat [ChEMBL: CHEMBL309] [GtoPdb: 14] [UniProtKB: P10980]
  • 0
2 CHEMBL21536_lig_chart_2 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/Muscarinic acetylcholine receptor M3 in Mouse [ChEMBL: CHEMBL5105] [GtoPdb: 15] [UniProtKB: Q9ERZ3]
  • 0
3 CHEMBL21536_lig_chart_3 Muscarinic acetylcholine receptor M3 HumanMouse
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  • M4 receptor/Muscarinic acetylcholine receptor M4 in Human [ChEMBL: CHEMBL1821] [GtoPdb: 16] [UniProtKB: P08173]
  • 7.4
4 CHEMBL21536_lig_chart_4 Muscarinic acetylcholine receptor M4 Human
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  • M5 receptor/Muscarinic acetylcholine receptor M5 in Human [ChEMBL: CHEMBL2035] [GtoPdb: 17] [UniProtKB: P08912]
  • 7.25
5 CHEMBL21536_lig_chart_5 Muscarinic acetylcholine receptor M5 Human
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  • 5-HT1A receptor in Human [GtoPdb: 1] [UniProtKB: P08908]
  • This target only has 1 pki data point
  • 7.2
6 CHEMBL21536_lig_chart_6 5-HT1A receptor Human
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  • 5-HT1B receptor in Human [GtoPdb: 2] [UniProtKB: P28222]
  • This target only has 1 pki data point
  • 7.3
7 CHEMBL21536_lig_chart_7 5-HT1B receptor Human
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  • 5-HT1D receptor in Human [GtoPdb: 3] [UniProtKB: P28221]
  • This target only has 1 pki data point
  • 8.2
8 CHEMBL21536_lig_chart_8 5-HT1D receptor Human
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  • 5-ht1e receptor in Human [GtoPdb: 4] [UniProtKB: P28566]
  • This target only has 1 pki data point
  • 5.6
9 CHEMBL21536_lig_chart_9 5-ht1e receptor Human
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  • 5-HT1F receptor in Human [GtoPdb: 5] [UniProtKB: P30939]
  • This target only has 1 pki data point
  • 6.5
10 CHEMBL21536_lig_chart_10 5-HT1F receptor Human
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  • 5-HT2A receptor in Human [GtoPdb: 6] [UniProtKB: P28223]
  • This target only has 1 pki data point
  • 6.9
11 CHEMBL21536_lig_chart_11 5-HT2A receptor Human
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  • 5-HT2B receptor in Human [GtoPdb: 7] [UniProtKB: P41595]
  • This target only has 1 pki data point
  • 7.7
12 CHEMBL21536_lig_chart_12 5-HT2B receptor Human
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  • 5-HT2C receptor in Human [GtoPdb: 8] [UniProtKB: P28335]
  • This target only has 1 pki data point
  • 7.4
13 CHEMBL21536_lig_chart_13 5-HT2C receptor Human
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  • 5-HT6 receptor in Human [GtoPdb: 11] [UniProtKB: P50406]
  • This target only has 1 pki data point
  • 5.9
14 CHEMBL21536_lig_chart_14 5-HT6 receptor Human
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  • 5-HT7 receptor in Human [GtoPdb: 12] [UniProtKB: P34969]
  • This target only has 1 pki data point
  • 6.9
15 CHEMBL21536_lig_chart_15 5-HT7 receptor Human
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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 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]
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 B 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 [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 [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 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]
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]
GtoPdb - - 7.4 pKi - - - Br J Pharmacol (1998) 125: 1413-20 [PMID:9884068];
Br J Pharmacol (1999) 126: 1620-4 [PMID:10323594]
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 B 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]
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]
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 B 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 B 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 B 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]
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 B 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 28:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, Cibrián-Uhalte E, Davies M, Dedman N, Karlsson A, Magariños MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]