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Assay Detail

CHEMBL857186

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

Binding
Inhibitory activity was evaluated against Muscarinic acetylcholine receptor M2 expressed in A9 L cells
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type A9L
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Muscarinic acetylcholine receptor M2 (CHEMBL211)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis and biological characterization of 1-methyl-1,2,5,6-tetrahydropyridyl-1,2,5-thiadiazole derivatives as muscarinic agonists for the treatment of neurological disorders.
Cao Y, Zhang M, Wu C, Lee S, Wroblewski ME, Whipple T, Nagy PI, Takács-Novák K, Balázs A, Torös S, Messer WS.
J Med Chem (2003) 46 : 4273 -4286
PubMed 13678406 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 8.58 9.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL553058 1 9.30
CHEMBL335542 1 9.20
CHEMBL21536 XANOMELINE 4.0 1 7.90
CHEMBL14 CARBACHOL 4.0 1 7.90

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL553058 IC50 = 0.5012 nM 9.30
CHEMBL335542 IC50 = 0.631 nM 9.20
CHEMBL21536 XANOMELINE IC50 = 12.59 nM 7.90
CHEMBL14 CARBACHOL IC50 = 12.59 nM 7.90