Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL3383651

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

Binding
Positive modulatory activity at human M1 receptor expressed in HEK293T cells assessed as effect on carbachol-induced response by BRET based Gq protein engagement assay
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK-293T
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Muscarinic acetylcholine receptor M1 (CHEMBL216)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis and biological evaluation of a novel series of heterobivalent muscarinic ligands based on xanomeline and 1-[3-(4-butylpiperidin-1-yl)propyl]-1,2,3,4-tetrahydroquinolin-2-one (77-LH-28-1).
Bonifazi A, Yano H, Del Bello F, Farande A, Quaglia W, Petrelli R, Matucci R, Nesi M, Vistoli G, Ferré S, Piergentili A.
J Med Chem (2014) 57 : 9065 -9077
PubMed 25275964 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 2 7.31 7.46

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3354065 1 7.46
CHEMBL3354074 1 7.16

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3354065 EC50 = 34.67 nM 7.46
CHEMBL3354074 EC50 = 69.18 nM 7.16