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Assay Detail

CHEMBL5047394

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

Binding
Inhibition of BuChE in mouse serum using butyrylthiocholine iodide as substrate incubated for 20 mins by Ellman's method
51
Total Activities
51
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Mus musculus
Tissue Serum
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Cholinesterase (CHEMBL2528)
Type SINGLE PROTEIN
Organism Mus musculus

Publication

The novel therapeutic strategy of vilazodone-donepezil chimeras as potent triple-target ligands for the potential treatment of Alzheimer's disease with comorbid depression.
Li X, Li J, Huang Y, Gong Q, Fu Y, Xu Y, Huang J, You H, Zhang D, Zhang D, Mao F, Zhu J, Wang H, Zhang H, Li J.
Eur J Med Chem (2022) 229 : 114045 -114045
PubMed 34922191 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 51 5.76 6.74

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5076629 1 6.74
CHEMBL5071558 1 6.49
CHEMBL5087351 1 6.47
CHEMBL5087878 1 6.46
CHEMBL5080857 1 6.30
CHEMBL5089999 1 6.26
CHEMBL5076406 1 6.20
CHEMBL5082360 1 6.16
CHEMBL5089691 1 6.13
CHEMBL5088143 1 6.05
CHEMBL5086121 1 6.04
CHEMBL5076277 1 6.01
CHEMBL5087923 1 6.01
CHEMBL5070726 1 6.00
CHEMBL5094829 1 5.95
CHEMBL5088281 1 5.94
CHEMBL5088060 1 5.92
CHEMBL5086036 1 5.92
CHEMBL5077564 1 5.88
CHEMBL5092455 1 5.87
CHEMBL5080825 1 5.85
CHEMBL5087922 1 5.83
CHEMBL5082836 1 5.83
CHEMBL5069928 1 5.78
CHEMBL5087461 1 5.78
CHEMBL5088366 1 5.75
CHEMBL5087445 1 5.73
CHEMBL5087427 1 5.72
CHEMBL5085893 1 5.70
CHEMBL5080984 1 5.70

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5076629 IC50 = 183.0 nM 6.74
CHEMBL5071558 IC50 = 325.0 nM 6.49
CHEMBL5087351 IC50 = 336.0 nM 6.47
CHEMBL5087878 IC50 = 351.0 nM 6.46
CHEMBL5080857 IC50 = 498.0 nM 6.30
CHEMBL5089999 IC50 = 551.0 nM 6.26
CHEMBL5076406 IC50 = 638.0 nM 6.20
CHEMBL5082360 IC50 = 687.0 nM 6.16
CHEMBL5089691 IC50 = 743.0 nM 6.13
CHEMBL5088143 IC50 = 883.0 nM 6.05
CHEMBL5086121 IC50 = 902.0 nM 6.04
CHEMBL5076277 IC50 = 986.0 nM 6.01
CHEMBL5087923 IC50 = 979.0 nM 6.01
CHEMBL5070726 IC50 = 1004.0 nM 6.00
CHEMBL5094829 IC50 = 1128.0 nM 5.95
CHEMBL5088281 IC50 = 1152.0 nM 5.94
CHEMBL5088060 IC50 = 1203.0 nM 5.92
CHEMBL5086036 IC50 = 1197.0 nM 5.92
CHEMBL5077564 IC50 = 1324.0 nM 5.88
CHEMBL5092455 IC50 = 1345.0 nM 5.87
CHEMBL5080825 IC50 = 1401.0 nM 5.85
CHEMBL5087922 IC50 = 1472.0 nM 5.83
CHEMBL5082836 IC50 = 1489.0 nM 5.83
CHEMBL5069928 IC50 = 1672.0 nM 5.78
CHEMBL5087461 IC50 = 1660.0 nM 5.78
CHEMBL5088366 IC50 = 1763.0 nM 5.75
CHEMBL5087445 IC50 = 1864.0 nM 5.73
CHEMBL5087427 IC50 = 1905.0 nM 5.72
CHEMBL5085893 IC50 = 2008.0 nM 5.70
CHEMBL5080984 IC50 = 1997.0 nM 5.70
CHEMBL502 DONEPEZIL IC50 = 1992.0 nM 5.70
CHEMBL5082250 IC50 = 2176.0 nM 5.66
CHEMBL5079986 IC50 = 2383.0 nM 5.62
CHEMBL5093872 IC50 = 2515.0 nM 5.60
CHEMBL5094743 IC50 = 2639.0 nM 5.58
CHEMBL5089630 IC50 = 2676.0 nM 5.57
CHEMBL5090651 IC50 = 2723.0 nM 5.57
CHEMBL5080308 IC50 = 2731.0 nM 5.56
CHEMBL5078629 IC50 = 2842.0 nM 5.55
CHEMBL5072039 IC50 = 2832.0 nM 5.55
CHEMBL5071820 IC50 = 2999.0 nM 5.52
CHEMBL5075438 IC50 = 3568.0 nM 5.45
CHEMBL5085109 IC50 = 3845.0 nM 5.42
CHEMBL5088919 IC50 = 4588.0 nM 5.34
CHEMBL5091978 IC50 = 4948.0 nM 5.31
CHEMBL5094506 IC50 = 5805.0 nM 5.24
CHEMBL5075295 IC50 = 5845.0 nM 5.23
CHEMBL5072034 IC50 = 6746.0 nM 5.17
CHEMBL5092918 IC50 = 11339.0 nM 4.95
CHEMBL5078724 IC50 = 13418.0 nM 4.87