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Assay Detail

CHEMBL3373419

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Displacement of [3H]NMS from pig muscarinic M2 receptor after 120 mins by liquid scintillation counting
22
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Sus scrofa
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Muscarinic acetylcholine receptor M2 (CHEMBL4781)
Type SINGLE PROTEIN
Organism Sus scrofa

Publication

Semisynthetic analogues of toxiferine I and their pharmacological properties at α7 nAChRs, muscle-type nAChRs, and the allosteric binding site of muscarinic M2 receptors.
Zlotos DP, Tränkle C, Holzgrabe U, Gündisch D, Jensen AA.
J Nat Prod (2014) 77 : 2006 -2013
PubMed 25192059 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 22 7.11 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3305985 ALCURONIUM 2.0 1 8.70
CHEMBL3337858 1 8.10
CHEMBL3337859 1 7.96
CHEMBL3337863 2 7.92
CHEMBL3355097 2 7.50
CHEMBL3337867 2 7.44
CHEMBL3355098 2 7.31
CHEMBL3337857 1 7.02
CHEMBL3337866 2 6.58
CHEMBL3337862 2 6.50
CHEMBL3337860 1 6.47
CHEMBL3337861 2 6.39
CHEMBL380352 CARACURINE V 1 6.36
CHEMBL3337865 2 6.30

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3305985 ALCURONIUM EC50 = 2.0 nM 8.70
CHEMBL3337858 EC50 = 8.0 nM 8.10
CHEMBL3337859 EC50 = 11.0 nM 7.96
CHEMBL3337863 EC50 = 12.0 nM 7.92
CHEMBL3337863 EC50 = 12.3 nM 7.91
CHEMBL3355097 EC50 = 31.62 nM 7.50
CHEMBL3355097 EC50 = 32.0 nM 7.50
CHEMBL3337867 EC50 = 36.31 nM 7.44
CHEMBL3337867 EC50 = 36.0 nM 7.44
CHEMBL3355098 EC50 = 48.98 nM 7.31
CHEMBL3355098 EC50 = 49.0 nM 7.31
CHEMBL3337857 EC50 = 96.0 nM 7.02
CHEMBL3337866 EC50 = 260.0 nM 6.58
CHEMBL3337866 EC50 = 263.03 nM 6.58
CHEMBL3337862 EC50 = 320.0 nM 6.50
CHEMBL3337862 EC50 = 323.59 nM 6.49
CHEMBL3337860 EC50 = 339.0 nM 6.47
CHEMBL3337861 EC50 = 410.0 nM 6.39
CHEMBL3337861 EC50 = 407.38 nM 6.39
CHEMBL380352 CARACURINE V EC50 = 436.0 nM 6.36
CHEMBL3337865 EC50 = 500.0 nM 6.30
CHEMBL3337865 EC50 = 501.19 nM 6.30