pirenzepine [Ligand Id: 328] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL9967 (ACI-91, Gastri p, Gastrozepin, 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 | - | - | - |
Mol Pharmacol (1989) 35: 469-76 [PMID:2704370]; J Pharmacol Exp Ther (1991) 256: 727-33 [PMID:1994002]; Br J Pharmacol (1997) 120: 1409-18 [PMID:9113359]; AAPS PharmSci (2001) 3: E30 [PMID:12049493]; 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]; 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 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]
