pirenzepine [Ligand Id: 328] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL9967 (Pirenzepine, Gastri p, Gastrozepin)
  • Muscarinic acetylcholine receptor DM1 in Drosophila melanogaster [ChEMBL: CHEMBL2366467] [UniProtKB: P16395]
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  • M1 receptor/Muscarinic acetylcholine receptor M1 in Human [ChEMBL: CHEMBL216] [GtoPdb: 13] [UniProtKB: P11229]
  • Muscarinic acetylcholine receptor M1 in Bovine [ChEMBL: CHEMBL2672] [UniProtKB: Q8WMX0]
  • M1 receptor/Muscarinic acetylcholine receptor M1 in Rat [ChEMBL: CHEMBL276] [GtoPdb: 13] [UniProtKB: P08482]
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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]
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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 Rat [ChEMBL: CHEMBL320] [GtoPdb: 15] [UniProtKB: P08483]
  • Muscarinic acetylcholine receptor M3 in Guinea pig [ChEMBL: CHEMBL5498] [UniProtKB: Q8VH26]
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  • M4 receptor/Muscarinic acetylcholine receptor M4 in Human [ChEMBL: CHEMBL1821] [GtoPdb: 16] [UniProtKB: P08173]
  • M4 receptor/Muscarinic acetylcholine receptor M4 in Rat [ChEMBL: CHEMBL317] [GtoPdb: 16] [UniProtKB: P08485]
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  • M5 receptor/Muscarinic acetylcholine receptor M5 in Human [ChEMBL: CHEMBL2035] [GtoPdb: 17] [UniProtKB: P08912]
  • M5 receptor in Rat [GtoPdb: 17] [UniProtKB: P08911]
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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]

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, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos 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]