AC-260584 [Ligand Id: 334] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL2022960
  • 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]
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  • M3 receptor/Muscarinic acetylcholine receptor M3 in Human [ChEMBL: CHEMBL245] [GtoPdb: 15] [UniProtKB: P20309]
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  • M4 receptor/Muscarinic acetylcholine receptor M4 in Human [ChEMBL: CHEMBL1821] [GtoPdb: 16] [UniProtKB: P08173]
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  • M5 receptor/Muscarinic acetylcholine receptor M5 in Human [ChEMBL: CHEMBL2035] [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]
ChEMBL Agonist activity at human muscarinic M1 receptor by calcium mobilization assay F 7.39 pEC50 41 nM EC50 Bioorg. Med. Chem. Lett. (2012) 22: 3467-3472 [PMID:22507963]
M1 receptor in Rat [GtoPdb: 13] [UniProtKB: P08482]
GtoPdb - - 5.9 pIC50 - - - Mol Pharmacol (2006) 70: 1974-83 [PMID:16959945]
M2 receptor/Muscarinic acetylcholine receptor M2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL211] [GtoPdb: 14] [UniProtKB: P08172]
ChEMBL Antagonist activity at human muscarinic M2 receptor by calcium mobilization assay F 5 pIC50 >10000 nM IC50 Bioorg. Med. Chem. Lett. (2012) 22: 3467-3472 [PMID:22507963]
M3 receptor/Muscarinic acetylcholine receptor M3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL245] [GtoPdb: 15] [UniProtKB: P20309]
ChEMBL Agonist activity at human muscarinic M3 receptor by calcium mobilization assay F 5.23 pEC50 5900 nM EC50 Bioorg. Med. Chem. Lett. (2012) 22: 3467-3472 [PMID:22507963]
M4 receptor/Muscarinic acetylcholine receptor M4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1821] [GtoPdb: 16] [UniProtKB: P08173]
ChEMBL Antagonist activity at human muscarinic M4 receptor by calcium mobilization assay F 5 pIC50 >10000 nM IC50 Bioorg. Med. Chem. Lett. (2012) 22: 3467-3472 [PMID:22507963]
M5 receptor/Muscarinic acetylcholine receptor M5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2035] [GtoPdb: 17] [UniProtKB: P08912]
ChEMBL Agonist activity at human muscarinic M5 receptor by calcium mobilization assay F 6 pEC50 1000 nM EC50 Bioorg. Med. Chem. Lett. (2012) 22: 3467-3472 [PMID:22507963]

ChEMBL data shown on this page come from version 31:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, Cibrián-Uhalte E, Davies M, Dedman N, Karlsson A, Magariños 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]