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

Click here for a description of the charts and data table

Please tell us if you are using this feature and what you think!

ChEMBL ligand: CHEMBL151938 (Milameline)
  • M1 receptor/Muscarinic acetylcholine receptor M1 in Human [ChEMBL: CHEMBL216] [GtoPdb: 13] [UniProtKB: P11229]
  • 5.03
1 CHEMBL151938_lig_chart_1 Muscarinic acetylcholine receptor M1 Human
There should be some charts here, you may need to enable JavaScript!
  • M2 receptor/Muscarinic acetylcholine receptor M2 in Human [ChEMBL: CHEMBL211] [GtoPdb: 14] [UniProtKB: P08172]
  • This target only has 1 pki data point
  • 6
2 CHEMBL151938_lig_chart_2 Muscarinic acetylcholine receptor M2 Human
There should be some charts here, you may need to enable JavaScript!
  • M5 receptor/Muscarinic acetylcholine receptor M5 in Human [ChEMBL: CHEMBL2035] [GtoPdb: 17] [UniProtKB: P08912]
  • 5.45
3 CHEMBL151938_lig_chart_3 Muscarinic acetylcholine receptor M5 Human
There should be some charts here, you may need to enable JavaScript!
  • M3 receptor in Human [GtoPdb: 15] [UniProtKB: P20309]
  • This target only has 1 pki data point
  • 5.1
4 CHEMBL151938_lig_chart_4 M3 receptor Human
There should be some charts here, you may need to enable JavaScript!
  • M4 receptor in Human [GtoPdb: 16] [UniProtKB: P08173]
  • This target only has 1 pki data point
  • 5.5
5 CHEMBL151938_lig_chart_5 M4 receptor Human
There should be some charts here, you may need to enable JavaScript!
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]