iperoxo [Ligand Id: 6937] 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: CHEMBL3121473
  • 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!
There should be some charts here, you may need to enable JavaScript!
  • M2 receptor in Human [GtoPdb: 14] [UniProtKB: P08172]
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]
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 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]