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

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ChEMBL ligand: CHEMBL151938 (Milameline, PD-129,409, PD-129409)
  • 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 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]