blarcamesine [Ligand Id: 11586] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL4297224 (Anavex, Anavex 2-73, Blarcamesina, Blarcamesine)
  • 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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  • 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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  • sigma non-opioid intracellular receptor 1/Sigma opioid receptor in Human [ChEMBL: CHEMBL287] [GtoPdb: 2552] [UniProtKB: Q99720]
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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 Binding affinity to muscarinic acetylcholine receptor M1 (unknown origin) B 5.48 pIC50 3300 nM IC50 J Med Chem (2020) 63: 15187-15217 [PMID:33111525]
ChEMBL Binding affinity to muscarinic 1 receptor (unknown origin) B 5.48 pIC50 3300 nM IC50 Bioorg Med Chem (2022) 73: 117032-117032 [PMID:36202063]
M2 receptor/Muscarinic acetylcholine receptor M2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL211] [GtoPdb: 14] [UniProtKB: P08172]
ChEMBL Binding affinity to muscarinic acetylcholine receptor M2 (unknown origin) B 5.48 pIC50 3300 nM IC50 J Med Chem (2020) 63: 15187-15217 [PMID:33111525]
ChEMBL Binding affinity to muscarinic 2 receptor (unknown origin) B 5.48 pIC50 3300 nM IC50 Bioorg Med Chem (2022) 73: 117032-117032 [PMID:36202063]
M3 receptor/Muscarinic acetylcholine receptor M3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL245] [GtoPdb: 15] [UniProtKB: P20309]
ChEMBL Binding affinity to muscarinic acetylcholine receptor M3 (unknown origin) B 5.48 pIC50 3300 nM IC50 J Med Chem (2020) 63: 15187-15217 [PMID:33111525]
ChEMBL Binding affinity to muscarinic 3 receptor (unknown origin) B 5.48 pIC50 3300 nM IC50 Bioorg Med Chem (2022) 73: 117032-117032 [PMID:36202063]
M4 receptor/Muscarinic acetylcholine receptor M4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1821] [GtoPdb: 16] [UniProtKB: P08173]
ChEMBL Binding affinity to muscarinic acetylcholine receptor M4 (unknown origin) B 5.48 pIC50 3300 nM IC50 J Med Chem (2020) 63: 15187-15217 [PMID:33111525]
ChEMBL Binding affinity to muscarinic 4 receptor (unknown origin) B 5.48 pIC50 3300 nM IC50 Bioorg Med Chem (2022) 73: 117032-117032 [PMID:36202063]
sigma non-opioid intracellular receptor 1/Sigma opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL287] [GtoPdb: 2552] [UniProtKB: Q99720]
ChEMBL Binding affinity to sigma 1 receptor (unknown origin) assessed as inhibition constant B 8.2 pKi 6.3 nM Ki Eur J Med Chem (2023) 249: 115163-115163 [PMID:36716640]
ChEMBL Binding affinity to sigma-1 receptor (unknown origin) B 6.07 pIC50 860 nM IC50 J Med Chem (2020) 63: 15187-15217 [PMID:33111525]
ChEMBL Binding affinity to sigma 1 receptor (unknown origin) B 6.07 pIC50 860 nM IC50 Bioorg Med Chem (2022) 73: 117032-117032 [PMID:36202063]
GtoPdb - - 6.07 pIC50 860 nM IC50 J Psychopharmacol (2011) 25: 1101-17 [PMID:20829307]

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]