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 34:

Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
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]