milameline [Ligand Id: 301] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL151938 (Milameline)
  • M1 receptor/Muscarinic acetylcholine receptor M1 in Human [ChEMBL: CHEMBL216] [GtoPdb: 13] [UniProtKB: P11229]
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  • M2 receptor/Muscarinic acetylcholine receptor M2 in Human [ChEMBL: CHEMBL211] [GtoPdb: 14] [UniProtKB: P08172]
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  • M5 receptor/Muscarinic acetylcholine receptor M5 in Human [ChEMBL: CHEMBL2035] [GtoPdb: 17] [UniProtKB: P08912]
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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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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 - - 4.8 pKi - - - Br J Pharmacol (1999) 126: 1620-4 [PMID:10323594]
ChEMBL Binding affinity to human cloned muscarinic M1 receptor expressed in CHO cells B 5.25 pKi 5623.41 nM Ki Bioorg. Med. Chem. (2008) 16: 3049-3058 [PMID:18182302]
ChEMBL Agonist activity at human m1 muscarinic acetylcholine receptor expressed in HEK293 cells assessed as calcium mobilization by FLIPR assay F 7.68 pEC50 21 nM EC50 Bioorg. Med. Chem. Lett. (2015) 25: 1546-1551 [PMID:25765911]
M2 receptor/Muscarinic acetylcholine receptor M2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL211] [GtoPdb: 14] [UniProtKB: P08172]
ChEMBL Binding affinity to human cloned muscarinic M2 receptor expressed in CHO cells B 6 pKi 1000 nM Ki Bioorg. Med. Chem. (2008) 16: 3049-3058 [PMID:18182302]
M5 receptor/Muscarinic acetylcholine receptor M5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2035] [GtoPdb: 17] [UniProtKB: P08912]
GtoPdb - - 5.4 pKi - - - Br J Pharmacol (1999) 126: 1620-4 [PMID:10323594]
ChEMBL Binding affinity to human cloned muscarinic M5 receptor expressed in CHO cells B 5.5 pKi 3162.28 nM Ki Bioorg. Med. Chem. (2008) 16: 3049-3058 [PMID:18182302]
M3 receptor in Human [GtoPdb: 15] [UniProtKB: P20309]
GtoPdb - - 5.1 pKi - - - Br J Pharmacol (1999) 126: 1620-4 [PMID:10323594]
M4 receptor in Human [GtoPdb: 16] [UniProtKB: P08173]
GtoPdb - - 5.5 pKi - - - Br J Pharmacol (1999) 126: 1620-4 [PMID:10323594]

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]