iperoxo [Ligand Id: 6937] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL3121473
  • M1 receptor/Muscarinic acetylcholine receptor M1 in Human [ChEMBL: CHEMBL216] [GtoPdb: 13] [UniProtKB: P11229]
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  • M2 receptor in Human [GtoPdb: 14] [UniProtKB: P08172]
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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 Displacement of [3H]NMS from human muscarinic M1 acetylcholine receptor expressed in CHO cell membranes by radioligand binding assay B 5.67 pKd 2137.96 nM Kd J Med Chem (2015) 58: 560-576 [PMID:25478907]
ChEMBL Agonist activity at human muscarinic M1 receptor expressed in HEK293T cells co-expressing Galpha subunit and PLC-beta3 by split luciferase complementation assay B 8.9 pIC50 1.26 nM IC50 J Med Chem (2019) 62: 3009-3020 [PMID:30827105]
ChEMBL Partial agonist activity at human muscarinic M1 acetylcholine receptor expressed in CHO cells assessed as increase in IP1 accumulation incubated for 30 mins by FRET based HTRF assay F 8.69 pEC50 2.04 nM EC50 J Med Chem (2015) 58: 560-576 [PMID:25478907]
Muscarinic receptor 2 in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1075061] [UniProtKB: Q8VH27]
ChEMBL Agonist activity at muscarinic M3 receptor in albino guinea pig ileum assessed as stimulation of electrically-induced response B 9.78 pEC50 0.17 nM EC50 Eur J Med Chem (2014) 75: 222-232 [PMID:24534538]
ChEMBL Agonist activity at muscarinic M2 receptor in albino guinea pig left atrium assessed as stimulation of electrically-induced response B 10.1 pEC50 0.08 nM EC50 Eur J Med Chem (2014) 75: 222-232 [PMID:24534538]
M2 receptor in Human [GtoPdb: 14] [UniProtKB: P08172]
GtoPdb - - 9.8 pEC50 - - - Br J Pharmacol (2013) 169: 357-70 [PMID:23062057];
Biochem Pharmacol (2014) 90: 307-19 [PMID:24863257]

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]