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

CHEMBL4198696

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

Functional
Antagonist activity at human M1 mAChR expressed in CHO cells assessed as inhibition of oxotremorine M-stimulated calcium influx preincubated for 10 mins followed by oxotremorine M addition by Fluo-4 NW dye based fluorescence assay
25
Total Activities
25
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type CHO
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

The concept of hybrid molecules of tacrine and benzyl quinolone carboxylic acid (BQCA) as multifunctional agents for Alzheimer's disease.
Hepnarova V, Korabecny J, Matouskova L, Jost P, Muckova L, Hrabinova M, Vykoukalova N, Kerhartova M, Kucera T, Dolezal R, Nepovimova E, Spilovska K, Mezeiova E, Pham NL, Jun D, Staud F, Kaping D, Kuca K, Soukup O.
Eur J Med Chem (2018) 150 : 292 -306
PubMed 29533874 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 25 5.52 6.34

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4214668 1 6.34
CHEMBL4205374 1 6.18
CHEMBL4216601 1 5.97
CHEMBL4204913 1 5.86
CHEMBL4206484 1 5.83
CHEMBL4202784 1 5.83
CHEMBL4209755 1 5.80
CHEMBL4204901 1 5.69
CHEMBL4214900 1 5.67
CHEMBL4217126 1 5.61
CHEMBL4217346 1 5.56
CHEMBL4217660 1 5.49
CHEMBL4212151 1 5.43
CHEMBL1256415 1 5.43
CHEMBL4210729 1 5.40
CHEMBL4215154 1 5.39
CHEMBL4215217 1 5.37
CHEMBL4213591 1 5.27
CHEMBL292314 1 5.21
CHEMBL4210274 1 5.11
CHEMBL4205910 1 5.07
CHEMBL4203672 1 5.03
CHEMBL4217617 1 4.94
CHEMBL95 TACRINE 4.0 1 4.89
CHEMBL608112 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4214668 IC50 = 455.0 nM 6.34
CHEMBL4205374 IC50 = 658.0 nM 6.18
CHEMBL4216601 IC50 = 1070.0 nM 5.97
CHEMBL4204913 IC50 = 1370.0 nM 5.86
CHEMBL4206484 IC50 = 1490.0 nM 5.83
CHEMBL4202784 IC50 = 1480.0 nM 5.83
CHEMBL4209755 IC50 = 1590.0 nM 5.80
CHEMBL4204901 IC50 = 2050.0 nM 5.69
CHEMBL4214900 IC50 = 2140.0 nM 5.67
CHEMBL4217126 IC50 = 2480.0 nM 5.61
CHEMBL4217346 IC50 = 2780.0 nM 5.56
CHEMBL4217660 IC50 = 3270.0 nM 5.49
CHEMBL4212151 IC50 = 3710.0 nM 5.43
CHEMBL1256415 IC50 = 3710.0 nM 5.43
CHEMBL4210729 IC50 = 4010.0 nM 5.40
CHEMBL4215154 IC50 = 4110.0 nM 5.39
CHEMBL4215217 IC50 = 4230.0 nM 5.37
CHEMBL4213591 IC50 = 5350.0 nM 5.27
CHEMBL292314 IC50 = 6090.0 nM 5.21
CHEMBL4210274 IC50 = 7860.0 nM 5.11
CHEMBL4205910 IC50 = 8610.0 nM 5.07
CHEMBL4203672 IC50 = 9450.0 nM 5.03
CHEMBL4217617 IC50 = 11400.0 nM 4.94
CHEMBL95 TACRINE IC50 = 13000.0 nM 4.89
CHEMBL608112 IC50 - -