otenzepad [Ligand Id: 309] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL17045 (Otenzepad)
  • 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]
  • M1 receptor in Rat [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]
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  • M4 receptor/Muscarinic acetylcholine receptor M4 in Human [ChEMBL: CHEMBL1821] [GtoPdb: 16] [UniProtKB: P08173]
  • M4 receptor in Rat [GtoPdb: 16] [UniProtKB: P08485]
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  • M5 receptor in Human [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]AF-DX 384 from Drosophila melanogaster mAChR by scintillation counting B 5.86 pKi 1380 nM Ki J Agric Food Chem (2007) 55: 2276-2281 [PMID:17319687]
ChEMBL Displacement of [3H]QNB from Drosophila melanogaster mAChR by scintillation counting B 5.91 pKi 1220 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]
GtoPdb - - 6.2 pKd - - - Biochem Pharmacol (1996) 52: 643-58 [PMID:8759038]
ChEMBL Binding affinity to human M1 muscarinic receptor B 6.27 pKi 537 nM Ki J. Med. Chem. (2013) 56: 1693-1703 [PMID:23379472]
ChEMBL Compound was evaluated for displacement of [3H]QNB from human Muscarinic m1 receptor in CHO cells. B 6.75 pKi 179 nM Ki Bioorg. Med. Chem. Lett. (1996) 6: 785-788
M1 receptor in Rat [GtoPdb: 13] [UniProtKB: P08482]
GtoPdb - - 6.3 pKi - - - Life Sci (1992) 51: 955-71 [PMID:1325587];
Mol Pharmacol (1989) 35: 469-76 [PMID:2704370]
M2 receptor/Muscarinic acetylcholine receptor M2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL211] [GtoPdb: 14] [UniProtKB: P08172]
ChEMBL Binding affinity to human M2 muscarinic receptor B 7.09 pKi 81 nM Ki J. Med. Chem. (2013) 56: 1693-1703 [PMID:23379472]
GtoPdb - - 7.2 pKi - - - Mol Pharmacol (1989) 35: 469-76 [PMID:2704370];
J Pharmacol Exp Ther (1998) 284: 500-7 [PMID:9454790]
ChEMBL Compound was evaluated for displacement of [3H]-QNB from human Muscarinic m2 receptor in CHO cells. B 7.28 pKi 52 nM Ki Bioorg. Med. Chem. Lett. (1996) 6: 785-788
M2 receptor/Muscarinic acetylcholine receptor M2 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL309] [GtoPdb: 14] [UniProtKB: P10980]
GtoPdb - - 7.3 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 to the rat cardiac muscarinic acetylcholine receptor M2 using 0.3 nM [3H]N-methylscopolamine as radioligand B 6.4 pIC50 400 nM IC50 J. Med. Chem. (1989) 32: 1718-1724 [PMID:2754696]
ChEMBL Inhibition of muscarinic (M2) receptor isolated from rat atria B 6.4 pIC50 400 nM IC50 J. Med. Chem. (1994) 37: 3775-3788 [PMID:7966137]
ChEMBL Binding affinity to the rat cardiac muscarinic acetylcholine receptor M2 using 0.3 nM [3H]N-methylscopolamine as radioligand B 6.85 pIC50 140 nM IC50 J. Med. Chem. (1989) 32: 1718-1724 [PMID:2754696]
ChEMBL Inhibition of muscarinic (M2) receptor isolated from rat atria B 6.85 pIC50 140 nM IC50 J. Med. Chem. (1994) 37: 3775-3788 [PMID:7966137]
ChEMBL Binding affinity to the rat cardiac muscarinic acetylcholine receptor M2 using 0.3 nM [3H]N-methylscopolamine as radioligand B 7.3 pIC50 50 nM IC50 J. Med. Chem. (1989) 32: 1718-1724 [PMID:2754696]
ChEMBL Inhibition of muscarinic (M2) receptor isolated from rat atria B 7.3 pIC50 50 nM IC50 J. Med. Chem. (1994) 37: 3775-3788 [PMID:7966137]
M3 receptor/Muscarinic acetylcholine receptor M3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL245] [GtoPdb: 15] [UniProtKB: P20309]
ChEMBL Binding affinity to human M3 muscarinic receptor B 5.68 pKi 2089 nM Ki J. Med. Chem. (2013) 56: 1693-1703 [PMID:23379472]
GtoPdb - - 6.1 pKi - - - Mol Pharmacol (1989) 35: 469-76 [PMID:2704370]
M3 receptor/Muscarinic acetylcholine receptor M3 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL320] [GtoPdb: 15] [UniProtKB: P08483]
GtoPdb - - 6 pKi - - - Life Sci (1992) 51: 955-71 [PMID:1325587]
ChEMBL Binding affinity for glandular muscarinic acetylcholine receptor M3 in rat assayed using 0.3 nM [3H]N-methylscopolamine as radioligand B 5 pIC50 10000 nM IC50 J. Med. Chem. (1989) 32: 1718-1724 [PMID:2754696]
ChEMBL Inhibition of rat submandibular muscarinic (M3) receptor isolated from tissue homogenates B 5 pIC50 10000 nM IC50 J. Med. Chem. (1994) 37: 3775-3788 [PMID:7966137]
ChEMBL Binding affinity for glandular muscarinic acetylcholine receptor M3 in rat assayed using 0.3 nM [3H]N-methylscopolamine as radioligand B 5.22 pIC50 6000 nM IC50 J. Med. Chem. (1989) 32: 1718-1724 [PMID:2754696]
ChEMBL Binding affinity for glandular muscarinic acetylcholine receptor M3 in rat assayed using 0.3 nM [3H]N-methylscopolamine as radioligand B 5.22 pIC50 6000 nM IC50 J. Med. Chem. (1989) 32: 1718-1724 [PMID:2754696]
ChEMBL Inhibition of rat submandibular muscarinic (M3) receptor isolated from tissue homogenates B 5.22 pIC50 6000 nM IC50 J. Med. Chem. (1994) 37: 3775-3788 [PMID:7966137]
ChEMBL Inhibition of rat submandibular muscarinic (M3) receptor isolated from tissue homogenates B 5.22 pIC50 6000 nM IC50 J. Med. Chem. (1994) 37: 3775-3788 [PMID:7966137]
M4 receptor/Muscarinic acetylcholine receptor M4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1821] [GtoPdb: 16] [UniProtKB: P08173]
GtoPdb - - 7 pKd - - - Biochem Pharmacol (1996) 52: 643-58 [PMID:8759038]
ChEMBL Binding affinity to human M4 muscarinic receptor B 6.39 pKi 407 nM Ki J. Med. Chem. (2013) 56: 1693-1703 [PMID:23379472]
M4 receptor in Rat [GtoPdb: 16] [UniProtKB: P08485]
GtoPdb - - 6.5 pKi - - - Life Sci (1992) 51: 955-71 [PMID:1325587]
M5 receptor in Human [GtoPdb: 17] [UniProtKB: P08912]
GtoPdb - - 5.6 pKi - - - Mol Pharmacol (1989) 35: 469-76 [PMID:2704370]
M5 receptor in Rat [GtoPdb: 17] [UniProtKB: P08911]
GtoPdb - - 5.7 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]