VU0255035 [Ligand Id: 3274] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL1628667
  • M1 receptor/Muscarinic acetylcholine receptor M1 in Human [ChEMBL: CHEMBL216] [GtoPdb: 13] [UniProtKB: P11229]
  • M1 receptor/Muscarinic acetylcholine receptor M1 in Rat [ChEMBL: CHEMBL276] [GtoPdb: 13] [UniProtKB: P08482]
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  • M2 receptor in Human [GtoPdb: 14] [UniProtKB: P08172]
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  • M3 receptor in Human [GtoPdb: 15] [UniProtKB: P20309]
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  • M4 receptor in Human [GtoPdb: 16] [UniProtKB: P08173]
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  • M5 receptor in Human [GtoPdb: 17] [UniProtKB: P08912]
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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]
GtoPdb - - 7.8 pKi 14.87 nM Ki Mol Pharmacol (2009) 76: 356-68 [PMID:19407080]
ChEMBL Antagonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by fluorescence assay F 6.16 pIC50 690 nM IC50 Bioorg. Med. Chem. Lett. (2012) 22: 1044-1048 [PMID:22197142]
ChEMBL Antagonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by fluorescence analysis F 6.16 pIC50 690 nM IC50 Bioorg. Med. Chem. Lett. (2012) 22: 5035-5040 [PMID:22749871]
M1 receptor/Muscarinic acetylcholine receptor M1 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL276] [GtoPdb: 13] [UniProtKB: P08482]
ChEMBL Antagonist activity at rat muscarinic M1 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by fluorescence assay F 6.62 pIC50 240 nM IC50 Bioorg. Med. Chem. Lett. (2012) 22: 1044-1048 [PMID:22197142]
M2 receptor in Human [GtoPdb: 14] [UniProtKB: P08172]
GtoPdb - - 6.2 pKi - - - Mol Pharmacol (2009) 76: 356-68 [PMID:19407080]
M3 receptor in Human [GtoPdb: 15] [UniProtKB: P20309]
GtoPdb - - 6.1 pKi - - - Mol Pharmacol (2009) 76: 356-68 [PMID:19407080]
M4 receptor in Human [GtoPdb: 16] [UniProtKB: P08173]
GtoPdb - - 5.9 pKi - - - Mol Pharmacol (2009) 76: 356-68 [PMID:19407080]
M5 receptor in Human [GtoPdb: 17] [UniProtKB: P08912]
GtoPdb - - 5.6 pKi - - - Mol Pharmacol (2009) 76: 356-68 [PMID:19407080]

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]