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

CHEMBL745685

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

Functional
Effective concentration required for stimulation of phosphoinositol (PI) hydrolysis in the A9 L cell line transfected with the Muscarinic acetylcholine receptor M1.
15
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Cell Type A9L
Confidence 8 — Homologous single protein target
Curated By Expert

Target

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

Publication

1,2,5-Thiadiazole analogues of aceclidine as potent m1 muscarinic agonists.
Ward JS, Merritt L, Calligaro DO, Bymaster FP, Shannon HE, Mitch CH, Whitesitt C, Brunsting D, Sheardown MJ, Olesen PH, Swedberg MD, Jeppesen L, Sauerberg P.
J Med Chem (1998) 41 : 379 -392
PubMed 9464368 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 15 6.76 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL340435 1 9.00
CHEMBL126846 2 8.72
CHEMBL433867 1 7.65
CHEMBL341242 1 6.99
CHEMBL125732 2 6.87
CHEMBL129764 1 6.78
CHEMBL21536 XANOMELINE 4.0 1 6.70
CHEMBL126237 1 6.65
CHEMBL126332 1 6.59
CHEMBL337925 1 6.37
CHEMBL20835 ACECLIDINE 3.0 1 5.35
CHEMBL129474 1 5.31
CHEMBL340021 1 5.21

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL340435 EC50 = 1.0 nM 9.00
CHEMBL126846 EC50 = 1.9 nM 8.72
CHEMBL433867 EC50 = 22.3 nM 7.65
CHEMBL341242 EC50 = 102.0 nM 6.99
CHEMBL125732 EC50 = 135.8 nM 6.87
CHEMBL126846 EC50 = 161.7 nM 6.79
CHEMBL129764 EC50 = 164.8 nM 6.78
CHEMBL21536 XANOMELINE EC50 = 200.0 nM 6.70
CHEMBL126237 EC50 = 225.0 nM 6.65
CHEMBL126332 EC50 = 258.9 nM 6.59
CHEMBL337925 EC50 = 430.9 nM 6.37
CHEMBL125732 EC50 = 433.3 nM 6.36
CHEMBL20835 ACECLIDINE EC50 = 4466.0 nM 5.35
CHEMBL129474 EC50 = 4867.0 nM 5.31
CHEMBL340021 EC50 = 6202.0 nM 5.21