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]
  • This target only has 0 pki data point
  • 0
1 CHEMBL3121473_lig_chart_1 Muscarinic acetylcholine receptor M1 Human
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  • Muscarinic receptor 2 in Guinea pig [ChEMBL: CHEMBL1075061] [UniProtKB: Q8VH27]
  • This target only has 0 pki data point
  • 0
2 CHEMBL3121473_lig_chart_2 Muscarinic receptor 2 Guinea pig
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  • M2 receptor in Human [GtoPdb: 14] [UniProtKB: P08172]
  • This target only has 0 pki data point
  • 0
3 CHEMBL3121473_lig_chart_3 M2 receptor Human
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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 B 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 28:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]