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Assay Detail

CHEMBL749007

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

Binding
Binding affinity of compound labeled by [3H]QNB in CHO cells selectively expressing human Muscarinic acetylcholine receptor M2
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Design and synthesis of m1-selective muscarinic agonists: (R)-(-)-(Z)-1-Azabicyclo[2.2.1]heptan-3-one, O-(3-(3'-methoxyphenyl)-2-propynyl)oxime maleate (CI-1017), a functionally m1-selective muscarinic agonist.
Tecle H, Barrett SD, Lauffer DJ, Augelli-Szafran C, Brann MR, Callahan MJ, Caprathe BW, Davis RE, Doyle PD, Eubanks D, Lipiniski W, Mirzadegan T, Moos WH, Moreland DW, Nelson CB, Pavia MR, Raby C, Schwarz RD, Spencer CJ, Thomas AJ, Jaen JC.
J Med Chem (1998) 41 : 2524 -2536
PubMed 9651157 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 6.29 6.29

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL82378 1 6.29

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL82378 IC50 = 519.0 nM 6.29