pirenzepine [Ligand Id: 328] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL9967 (ACI-91, Gastri p, Gastrozepin, Pirenzepina, Pirenzepine) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| Muscarinic acetylcholine receptor DM1 in Drosophila melanogaster (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2366467] [UniProtKB: P16395] | ||||||||
| ChEMBL | Displacement of [3H]QNB from Drosophila melanogaster mAChR by scintillation counting | B | 6.37 | pKi | 430 | nM | Ki | J Agric Food Chem (2007) 55: 2276-2281 [PMID:17319687] |
| ChEMBL | Displacement of [3H]AF-DX 384 from Drosophila melanogaster mAChR by scintillation counting | B | 6.41 | pKi | 390 | nM | Ki | J Agric Food Chem (2007) 55: 2276-2281 [PMID:17319687] |
| M1 receptor/Muscarinic acetylcholine receptor M1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL216] [GtoPdb: 13] [UniProtKB: P11229] | ||||||||
| ChEMBL | Apparent dissociation constant for human muscarinic receptor M1 from FRET based binding assay | B | 7.7 | pKd | 20 | nM | Kd | J Med Chem (2004) 47: 4300-4315 [PMID:15294002] |
| ChEMBL | Displacement of radiolabeled pirenzepine from human muscarinic M1 receptor | B | 7.6 | pKi | 25 | nM | Ki | J Med Chem (2008) 51: 7094-7098 [PMID:18983139] |
| ChEMBL | Displacement of [3H]pirenzepine from human recombinant Muscarinic acetylcholine receptor M1 expressed in CHO cells after 60 mins by scintillation counting | B | 7.62 | pKi | 24 | nM | Ki | J Med Chem (2017) 60: 349-361 [PMID:27997171] |
| ChEMBL | Inhibition of [3H]QNB binding to human muscarinic receptor M1 | B | 7.63 | pKi | 23.5 | nM | Ki | J Med Chem (2004) 47: 4300-4315 [PMID:15294002] |
| ChEMBL | Displacement of [3H]QNB from EGFP(delta-17)human M1 receptor expressed in HEK cells | B | 7.63 | pKi | 23.5 | nM | Ki | J Med Chem (2005) 48: 7847-7859 [PMID:16302823] |
| ChEMBL | Displacement of [3H]QNB from human muscarinic M1 receptor expressed in CHO cells | B | 7.67 | pKi | 21.38 | nM | Ki | Bioorg Med Chem (2007) 15: 7626-7637 [PMID:17889543] |
| ChEMBL | Displacement of [3H]-pyrilamine from human recombinant M1 receptor expressed in CHO cells after 60 mins by scintillation counting | B | 7.7 | pKi | 20 | nM | Ki | J Med Chem (2017) 60: 7483-7501 [PMID:28763213] |
| ChEMBL | Displacement of [3H]pirenzepine from human muscarinic M1 receptor expressed in CHO cells | B | 7.8 | pKi | 16 | nM | Ki | Eur J Med Chem (2015) 92: 221-235 [PMID:25557493] |
| ChEMBL | Inhibition of muscarinic M1 receptor (unknown origin) assessed as reduction in control ligand binding | B | 7.82 | pKi | 15 | nM | Ki | Eur J Med Chem (2015) 92: 221-235 [PMID:25557493] |
| ChEMBL | Displacement of [3H]pirenzepine from human recombinant M1 receptor expressed in CHO cells | B | 7.82 | pKi | 15 | nM | Ki | J Med Chem (2014) 57: 4543-4557 [PMID:24805037] |
| ChEMBL | Binding affinity for muscarinic acetylcholine receptor M1 by measuring displacement of [3H]QNB from guinea pig cerebral cortex | B | 7.85 | pKi | 14 | nM | Ki | J Med Chem (1995) 38: 473-487 [PMID:7853341] |
| ChEMBL | Binding affinity to human muscarinic M1 receptor by radioligand displacement assay | B | 8 | pKi | 10 | nM | Ki | Eur J Med Chem (2013) 63: 85-94 [PMID:23466604] |
| ChEMBL | Binding affinity to human M1 muscarinic receptor | B | 8.04 | pKi | 9.1 | nM | Ki | J Med Chem (2013) 56: 1693-1703 [PMID:23379472] |
| GtoPdb | - | - | 8.3 | pKi | - | - | - |
AAPS PharmSci (2001) 3: E30 [PMID:12049493]; Mol Pharmacol (1989) 35: 469-76 [PMID:2704370]; FEBS Lett (1994) 352: 91-4 [PMID:7925952]; J Pharmacol Exp Ther (1991) 256: 727-33 [PMID:1994002]; Br J Pharmacol (1997) 120: 1409-18 [PMID:9113359]; Br J Pharmacol (1991) 102: 246-50 [PMID:2043926] |
| ChEMBL | Compound was evaluated for displacement of [3H]QNB from human Muscarinic m1 receptor in CHO cells. | B | 8.34 | pKi | 4.6 | nM | Ki | Bioorg Med Chem Lett (1996) 6: 785-788 |
| ChEMBL | Displacement of [3H]N-methylscopolamine chloride from human cloned muscarinic M1 receptor expressed in CHOK1 cells | B | 8.55 | pKi | 2.82 | nM | Ki | Bioorg Med Chem (2008) 16: 7311-7320 [PMID:18595721] |
| ChEMBL | Compound was tested for its binding affinity against M1 human recombinant muscarinic receptor in CHO cells. | B | 6.92 | pIC50 | 119 | nM | IC50 | Bioorg Med Chem Lett (1999) 9: 2795-2800 [PMID:10522693] |
| ChEMBL | Antagonist activity at human M1 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by BRET based Gq protein engagement assay | B | 7.31 | pIC50 | 48.98 | nM | IC50 | J Med Chem (2014) 57: 9065-9077 [PMID:25275964] |
| ChEMBL | Displacement of radiolabeled pirenzepine from human muscarinic M1 receptor | B | 7.54 | pIC50 | 29 | nM | IC50 | J Med Chem (2008) 51: 7094-7098 [PMID:18983139] |
| ChEMBL | Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M1 using membranes from transfected CHO cells | B | 7.55 | pIC50 | 28.2 | nM | IC50 | J Med Chem (1999) 42: 356-363 [PMID:9986705] |
| ChEMBL | Displacement of [3H]pirenzepine from human recombinant Muscarinic acetylcholine receptor M1 expressed in CHO cells after 60 mins by scintillation counting | B | 7.57 | pIC50 | 27 | nM | IC50 | J Med Chem (2017) 60: 349-361 [PMID:27997171] |
| ChEMBL | Binding affinity to human muscarinic M1 receptor by radioligand displacement assay | B | 7.57 | pIC50 | 27 | nM | IC50 | Bioorg Med Chem (2013) 21: 2764-2771 [PMID:23582449] |
| ChEMBL | Percent inhibition against Muscarinic acetylcholine receptor M1 at 1 uM | B | 7.66 | pIC50 | 22 | nM | IC50 | J Med Chem (2005) 48: 6887-6896 [PMID:16250647] |
| ChEMBL | Displacement of [3H]pirenzepine from human recombinant muscarinic M1 receptor expressed in CHO cells | B | 7.68 | pIC50 | 21 | nM | IC50 | Bioorg Med Chem (2016) 24: 1793-1810 [PMID:26988801] |
| ChEMBL | Displacement of [3H]pirenzepine from human recombinant M1 receptor expressed in CHO cells measured after 60 mins by scintillation counting method | B | 7.68 | pIC50 | 21 | nM | IC50 | Bioorg Med Chem (2017) 25: 471-482 [PMID:27876250] |
| ChEMBL | Antagonist activity at human M1 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by BRET based Gq protein activation assay | B | 7.69 | pIC50 | 20.42 | nM | IC50 | J Med Chem (2014) 57: 9065-9077 [PMID:25275964] |
| ChEMBL | Inhibition of human muscarinic M1 receptor | B | 7.72 | pIC50 | 19 | nM | IC50 | Bioorg Med Chem (2010) 18: 7675-7699 [PMID:20875743] |
| ChEMBL | Inhibition of human muscarinic M1 receptor | B | 7.92 | pIC50 | 12 | nM | IC50 | J Med Chem (2008) 51: 4150-4169 [PMID:18588282] |
| ChEMBL | Binding affinity to human muscarinic M1 receptor by radioligand displacement assay | B | 7.92 | pIC50 | 12 | nM | IC50 | Eur J Med Chem (2013) 63: 85-94 [PMID:23466604] |
| ChEMBL | Antagonist activity at human M1 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by BRET based beta-arrestin engagement assay | B | 8.83 | pIC50 | 1.48 | nM | IC50 | J Med Chem (2014) 57: 9065-9077 [PMID:25275964] |
| Muscarinic acetylcholine receptor M1 in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2672] [UniProtKB: Q8WMX0] | ||||||||
| ChEMBL | Inhibition of [3H]NMS binding to cerebral cortex membranes which contain predominantly the muscarinic acetylcholine receptor M1 | B | 6.77 | pKi | 170 | nM | Ki | J Med Chem (1989) 32: 1522-1528 [PMID:2738887] |
| ChEMBL | Binding affinity against Muscarinic acetylcholine receptor M1 by displacement of [3H]pirenzepine in bovine striatum | B | 8.44 | pKi | 3.6 | nM | Ki | J Med Chem (1988) 31: 1463-1466 [PMID:3385735] |
| M1 receptor/Muscarinic acetylcholine receptor M1 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL276] [GtoPdb: 13] [UniProtKB: P08482] | ||||||||
| ChEMBL | Inhibition of binding of [3H]N-methylscopolamine to muscarinic acetylcholine receptor M1 of transfected rat A9L cells. | B | 7.54 | pKi | 29 | nM | Ki | J Med Chem (1991) 34: 2133-2145 [PMID:2066986] |
| GtoPdb | - | - | 7.9 | pKi | - | - | - |
Life Sci (1992) 51: 955-71 [PMID:1325587]; Mol Pharmacol (1989) 35: 469-76 [PMID:2704370] |
| ChEMBL | Affinity constant measured against M1 muscarinic receptor in rat cortex | B | 8.19 | pKi | 6.46 | nM | Ki | J Med Chem (1993) 36: 3734-3737 [PMID:8246244] |
| ChEMBL | Tested for affinity constant against M1 muscarinic receptor in rat cortex using [3H]pirenzepine | B | 8.19 | pKi | 6.46 | nM | Ki | J Med Chem (1994) 37: 3363-3372 [PMID:7932564] |
| ChEMBL | Inhibition of binding of [3H]pirenzepine to muscarinic receptor (M1) in rat cortex homogenates | B | 8.19 | pKi | 6.46 | nM | Ki | Bioorg Med Chem Lett (1995) 5: 785-790 |
| ChEMBL | Compound was tested for inhibiting [3H]pirenzepine Binding to Muscarinic receptor (M1) receptor in Rat Cortex Homogenates | B | 8.19 | pKi | 6.46 | nM | Ki | Bioorg Med Chem Lett (1995) 5: 2325-2330 |
| ChEMBL | Ability to displace [3H]pirenzepine (PZ) from M1 receptor in rat cortex homogenate | B | 8.28 | pKi | 5.21 | nM | Ki | J Med Chem (1993) 36: 848-854 [PMID:8464039] |
| ChEMBL | Displacement of [3H]pirenzepine from muscarinic acetylcholine receptor M1 in rat cortex homogenates | B | 8.28 | pKi | 5.21 | nM | Ki | J Med Chem (1991) 34: 2984-2989 [PMID:1920350] |
| ChEMBL | Displacement of [3H]pirenzepine from muscarinic M1 receptor of rat cortex homogenates. | B | 8.28 | pKi | 5.2 | nM | Ki | Bioorg Med Chem Lett (1997) 7: 979-984 |
| ChEMBL | Binding affinity towards Muscarinic acetylcholine receptor M1 of cerebral cortex | B | 6.92 | pIC50 | 120 | nM | IC50 | J Med Chem (1988) 31: 1169-1174 [PMID:3373484] |
| ChEMBL | Displacement of [3H]pirenzepine binding to muscarinic M1 receptor in brain cortex of rat. | B | 8.42 | pIC50 | 3.8 | nM | IC50 | Bioorg Med Chem Lett (1999) 9: 3031-3034 [PMID:10571170] |
| M2 receptor/Muscarinic acetylcholine receptor M2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL211] [GtoPdb: 14] [UniProtKB: P08172] | ||||||||
| ChEMBL | Antimuscarinic activity on the acetylcholine-induced inhibition of contraction of guinea pig ileum which has Muscarinic acetylcholine receptor M2 | F | 4.3 | pKd | 50118.72 | nM | Kd | J Med Chem (1989) 32: 1522-1528 [PMID:2738887] |
| ChEMBL | Binding affinity to human M2 muscarinic receptor | B | 6.28 | pKi | 524 | nM | Ki | J Med Chem (2013) 56: 1693-1703 [PMID:23379472] |
| ChEMBL | Binding affinity for muscarinic acetylcholine receptor M2 by measuring displacement of [3H]QNB from guinea pig heart | B | 6.57 | pKi | 270 | nM | Ki | J Med Chem (1995) 38: 473-487 [PMID:7853341] |
| ChEMBL | Compound was evaluated for displacement of [3H]-QNB from human Muscarinic m2 receptor in CHO cells. | B | 6.6 | pKi | 251 | nM | Ki | Bioorg Med Chem Lett (1996) 6: 785-788 |
| GtoPdb | - | - | 6.7 | pKi | - | - | - |
AAPS PharmSci (2001) 3: E30 [PMID:12049493]; Mol Pharmacol (1989) 35: 469-76 [PMID:2704370]; FEBS Lett (1994) 352: 91-4 [PMID:7925952]; J Pharmacol Exp Ther (1998) 284: 500-7 [PMID:9454790]; J Pharmacol Exp Ther (2006) 316: 279-88 [PMID:16188951]; J Pharmacol Exp Ther (1991) 256: 727-33 [PMID:1994002]; Br J Pharmacol (1997) 120: 1409-18 [PMID:9113359]; Br J Pharmacol (1991) 102: 246-50 [PMID:2043926] |
| ChEMBL | Displacement of [3H]N-methylscopolamine chloride from human cloned muscarinic M2 receptor expressed in CHOK1 cells | B | 6.76 | pKi | 173.78 | nM | Ki | Bioorg Med Chem (2008) 16: 7311-7320 [PMID:18595721] |
| ChEMBL | Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M2 using membranes from transfected CHO cells | B | 6.01 | pIC50 | 968.2 | nM | IC50 | J Med Chem (1999) 42: 356-363 [PMID:9986705] |
| M2 receptor/Muscarinic acetylcholine receptor M2 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL309] [GtoPdb: 14] [UniProtKB: P10980] | ||||||||
| ChEMBL | Evaluated for the inhibition of adenylate cyclase at M2 receptor in rat heart | B | 4.74 | pKi | 18300 | nM | Ki | J Med Chem (1988) 31: 1463-1466 [PMID:3385735] |
| ChEMBL | Inhibition of binding of [3H]N-methylscopolamine to muscarinic receptor (M2) in rat heart homogenates | B | 6.1 | pKi | 794.33 | nM | Ki | Bioorg Med Chem Lett (1995) 5: 785-790 |
| ChEMBL | Compound was tested for inhibiting [3H]N-Methyl-scopolamine Binding to Muscarinic receptor (M2) in Rat Heart | B | 6.1 | pKi | 794.33 | nM | Ki | Bioorg Med Chem Lett (1995) 5: 2325-2330 |
| ChEMBL | Tested for affinity constant against M2 muscarinic receptor rat heart using [3H]-NMS | B | 6.1 | pKi | 794.33 | nM | Ki | J Med Chem (1994) 37: 3363-3372 [PMID:7932564] |
| ChEMBL | Affinity constant measured against M2 muscarinic receptor in rat heart r | B | 6.1 | pKi | 794.33 | nM | Ki | J Med Chem (1993) 36: 3734-3737 [PMID:8246244] |
| ChEMBL | Inhibition of binding of [3H]N-methylscopolamine to muscarinic acetylcholine receptor M2 of rat heart tissue membrane. | B | 6.21 | pKi | 610 | nM | Ki | J Med Chem (1991) 34: 2133-2145 [PMID:2066986] |
| ChEMBL | Binding affinity against Muscarinic acetylcholine receptor M2 by displacement of [3H]QNB in rat myocardium | B | 6.42 | pKi | 377 | nM | Ki | J Med Chem (1988) 31: 1463-1466 [PMID:3385735] |
| ChEMBL | Displacement of [3H]QNB (quinuclidinyl benzylate) from muscarinic M2 receptor of rat heart homogenates. | B | 6.57 | pKi | 267 | nM | Ki | Bioorg Med Chem Lett (1997) 7: 979-984 |
| ChEMBL | Ability to displace [3H](-)-quinuclidinyl benzilate(QNB) from M2 receptor in rat heart homogenate | B | 6.57 | pKi | 267 | nM | Ki | J Med Chem (1993) 36: 848-854 [PMID:8464039] |
| ChEMBL | Displacement of [3H](-)-quinuclidinyl benzilate(QNB) from muscarinic (M2) receptor in rat heart homogenates | B | 6.57 | pKi | 267 | nM | Ki | J Med Chem (1991) 34: 2984-2989 [PMID:1920350] |
| ChEMBL | Inhibition of carbachol-induced release of alpha-amylase from pancreatic acinar cells from that of rat ileum contained the muscarinic acetylcholine receptor M2 subtypes | B | 6.92 | pKi | 120 | nM | Ki | J Med Chem (1989) 32: 1522-1528 [PMID:2738887] |
| GtoPdb | - | - | 7.4 | pKi | - | - | - |
EMBO J (1988) 7: 3031-5 [PMID:2846274]; Life Sci (1992) 51: 955-71 [PMID:1325587]; J Pharmacol Exp Ther (1998) 284: 500-7 [PMID:9454790] |
| ChEMBL | Binding affinity towards muscarinic receptor of gastric fundus containing Muscarinic acetylcholine receptor M2 | B | 5.92 | pIC50 | 1200 | nM | IC50 | J Med Chem (1988) 31: 1169-1174 [PMID:3373484] |
| ChEMBL | Binding affinity to the rat cardiac muscarinic acetylcholine receptor M2 using 0.3 nM [3H]N-methylscopolamine as radioligand | B | 6.1 | pIC50 | 800 | nM | IC50 | J Med Chem (1989) 32: 1718-1724 [PMID:2754696] |
| ChEMBL | Displacement of [3H]methylscopolamine binding to muscarinic M2 receptor in rat heart. | B | 6.16 | pIC50 | 690 | nM | IC50 | Bioorg Med Chem Lett (1999) 9: 3031-3034 [PMID:10571170] |
| M3 receptor/Muscarinic acetylcholine receptor M3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL245] [GtoPdb: 15] [UniProtKB: P20309] | ||||||||
| GtoPdb | - | - | 6.8 | pKi | - | - | - |
AAPS PharmSci (2001) 3: E30 [PMID:12049493]; Mol Pharmacol (1989) 35: 469-76 [PMID:2704370]; FEBS Lett (1994) 352: 91-4 [PMID:7925952]; J Pharmacol Exp Ther (1991) 256: 727-33 [PMID:1994002]; Br J Pharmacol (1997) 120: 1409-18 [PMID:9113359]; Br J Pharmacol (1991) 102: 246-50 [PMID:2043926] |
| ChEMBL | Binding affinity to human M3 muscarinic receptor | B | 6.8 | pKi | 158 | nM | Ki | J Med Chem (2013) 56: 1693-1703 [PMID:23379472] |
| ChEMBL | Displacement of [3H]N-methylscopolamine chloride from human cloned muscarinic M3 receptor expressed in CHOK1 cells | B | 7.32 | pKi | 47.86 | nM | Ki | Bioorg Med Chem (2008) 16: 7311-7320 [PMID:18595721] |
| ChEMBL | Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells | B | 6.02 | pIC50 | 955.6 | nM | IC50 | J Med Chem (1999) 42: 356-363 [PMID:9986705] |
| M3 receptor/Muscarinic acetylcholine receptor M3 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL320] [GtoPdb: 15] [UniProtKB: P08483] | ||||||||
| ChEMBL | Inhibition of binding of [3H]N-methylscopolamine to muscarinic acetylcholine receptor M3 of transfected rat A9L cells. | B | 6.62 | pKi | 240 | nM | Ki | J Med Chem (1991) 34: 2133-2145 [PMID:2066986] |
| GtoPdb | - | - | 6.7 | pKi | - | - | - | Life Sci (1992) 51: 955-71 [PMID:1325587] |
| ChEMBL | Affinity constant measured against M3 muscarinic receptor in rat submaxillary gland | B | 6.76 | pKi | 173.78 | nM | Ki | J Med Chem (1993) 36: 3734-3737 [PMID:8246244] |
| ChEMBL | Tested for affinity constant against M3 muscarinic receptor in rat submaxillary gland using [3H]NMS | B | 6.76 | pKi | 173.78 | nM | Ki | J Med Chem (1994) 37: 3363-3372 [PMID:7932564] |
| ChEMBL | Inhibition of binding of [3H]N-methylscopolamine to muscarinic receptor (M3) in rat submaxillary gland homogenates | B | 6.76 | pKi | 173.78 | nM | Ki | Bioorg Med Chem Lett (1995) 5: 785-790 |
| ChEMBL | Compound was tested for inhibiting [3H]N-Methyl-scopolamine Binding to Muscarinic receptor (M3) in Rat Submaxillary Gland | B | 6.76 | pKi | 173.78 | nM | Ki | Bioorg Med Chem Lett (1995) 5: 2325-2330 |
| ChEMBL | Ability to displace [3H]N-methylscopolamine (NMS) from M3 receptor in rat submaxillary gland homogenate | B | 7.55 | pKi | 28 | nM | Ki | J Med Chem (1993) 36: 848-854 [PMID:8464039] |
| ChEMBL | Binding affinity for glandular muscarinic acetylcholine receptor M3 in rat assayed using 0.3 nM [3H]N-methylscopolamine as radioligand | B | 6.22 | pIC50 | 600 | nM | IC50 | J Med Chem (1989) 32: 1718-1724 [PMID:2754696] |
| ChEMBL | Displacement of [3H]methylscopolamine binding to muscarinic M3 receptor in submaxillary salivary glands of rats. | B | 6.52 | pIC50 | 300 | nM | IC50 | Bioorg Med Chem Lett (1999) 9: 3031-3034 [PMID:10571170] |
| Muscarinic acetylcholine receptor M3 in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5498] [UniProtKB: Q8VH26] | ||||||||
| ChEMBL | Binding affinity for muscarinic acetylcholine receptor M3 by measuring displacement of [3H]QNB from guinea pig parotid gland | B | 6.96 | pKi | 110 | nM | Ki | J Med Chem (1995) 38: 473-487 [PMID:7853341] |
| M4 receptor/Muscarinic acetylcholine receptor M4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1821] [GtoPdb: 16] [UniProtKB: P08173] | ||||||||
| ChEMBL | Binding affinity to human M4 muscarinic receptor | B | 6.98 | pKi | 105 | nM | Ki | J Med Chem (2013) 56: 1693-1703 [PMID:23379472] |
| ChEMBL | Compound was tested for inhibiting [3H]N-Methyl-scopolamine Binding to Muscarinic acetylcholine receptor M4 in NG 108-15 Cell | B | 7.46 | pKi | 34.67 | nM | Ki | Bioorg Med Chem Lett (1995) 5: 2325-2330 |
| GtoPdb | - | - | 7.6 | pKi | - | - | - |
AAPS PharmSci (2001) 3: E30 [PMID:12049493]; FEBS Lett (1994) 352: 91-4 [PMID:7925952]; J Pharmacol Exp Ther (1991) 256: 727-33 [PMID:1994002]; Br J Pharmacol (1997) 120: 1409-18 [PMID:9113359]; Br J Pharmacol (1991) 102: 246-50 [PMID:2043926] |
| ChEMBL | Displacement of [3H]N-methylscopolamine chloride from human cloned muscarinic M4 receptor expressed in CHOK1 cells | B | 7.86 | pKi | 13.8 | nM | Ki | Bioorg Med Chem (2008) 16: 7311-7320 [PMID:18595721] |
| GtoPdb | - | - | 8.1 | pKi | 8 | nM | Ki | Invest Ophthalmol Vis Sci (2018) 59: 2778-2791 [PMID:29860464] |
| ChEMBL | Antagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by BRET based Gq protein engagement assay | B | 5.98 | pIC50 | 1047.13 | nM | IC50 | J Med Chem (2014) 57: 9065-9077 [PMID:25275964] |
| ChEMBL | Antagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by BRET based Gq protein activation assay | B | 5.98 | pIC50 | 1047.13 | nM | IC50 | J Med Chem (2014) 57: 9065-9077 [PMID:25275964] |
| ChEMBL | Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cells | B | 6.61 | pIC50 | 246.8 | nM | IC50 | J Med Chem (1999) 42: 356-363 [PMID:9986705] |
| ChEMBL | Antagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by beta-arrestin engagement assay | B | 8.94 | pIC50 | 1.15 | nM | IC50 | J Med Chem (2014) 57: 9065-9077 [PMID:25275964] |
| M4 receptor/Muscarinic acetylcholine receptor M4 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL317] [GtoPdb: 16] [UniProtKB: P08485] | ||||||||
| ChEMBL | Inhibition of binding of [3H]N-Methyl-scopolamine to muscarinic acetylcholine receptor M4 of rat heart NG108-15 cells | B | 6.48 | pKi | 330 | nM | Ki | J Med Chem (1991) 34: 2133-2145 [PMID:2066986] |
| GtoPdb | - | - | 7.1 | pKi | - | - | - | Life Sci (1992) 51: 955-71 [PMID:1325587] |
| ChEMBL | Affinity constant measured against M4 muscarinic receptor rat NG108-15 cells | B | 7.46 | pKi | 34.67 | nM | Ki | J Med Chem (1993) 36: 3734-3737 [PMID:8246244] |
| ChEMBL | Inhibition of binding of [3H]N-methylscopolamine to Muscarinic acetylcholine receptor M4 in NG 108-15 cell homogenates | B | 7.46 | pKi | 34.67 | nM | Ki | Bioorg Med Chem Lett (1995) 5: 785-790 |
| M5 receptor/Muscarinic acetylcholine receptor M5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2035] [GtoPdb: 17] [UniProtKB: P08912] | ||||||||
| ChEMBL | Binding affinity to human M5 muscarinic receptor | B | 6.9 | pKi | 126 | nM | Ki | J Med Chem (2013) 56: 1693-1703 [PMID:23379472] |
| GtoPdb | - | - | 7.1 | pKi | - | - | - |
FEBS Lett (1994) 352: 91-4 [PMID:7925952]; Br J Pharmacol (1997) 120: 1409-18 [PMID:9113359]; Br J Pharmacol (1991) 102: 246-50 [PMID:2043926] |
| ChEMBL | Displacement of [3H]QNB from human muscarinic M5 receptor expressed in CHO cells | B | 7.45 | pKi | 35.48 | nM | Ki | Bioorg Med Chem (2007) 15: 7626-7637 [PMID:17889543] |
| ChEMBL | Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M5 using membranes from transfected CHO cells | B | 6.47 | pIC50 | 340.6 | nM | IC50 | J Med Chem (1999) 42: 356-363 [PMID:9986705] |
| M5 receptor in Rat [GtoPdb: 17] [UniProtKB: P08911] | ||||||||
| GtoPdb | - | - | 7.1 | pKi | - | - | - | Life Sci (1992) 51: 955-71 [PMID:1325587] |
| TAS2R9 in Human [GtoPdb: 665] [UniProtKB: Q9NYW1] | ||||||||
| GtoPdb | - | - | 2.74 | pEC50 | 1800000 | nM | EC50 | PLoS One (2008) 3: e3974 [PMID:19092995] |
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]
