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, PD-129409, PD-129,409)
  • M1 receptor/Muscarinic acetylcholine receptor M1 in Human [ChEMBL: CHEMBL216] [GtoPdb: 13] [UniProtKB: P11229]
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]
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]
There should be some charts here, you may need to enable JavaScript!
  • M3 receptor in Human [GtoPdb: 15] [UniProtKB: P20309]
There should be some charts here, you may need to enable JavaScript!
  • M4 receptor in Human [GtoPdb: 16] [UniProtKB: P08173]
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 32:

Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
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]