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Assay Detail

CHEMBL5502894

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

Binding
Inhibition of equine serum BChE using BTC as substrate incubated for 2 mins by Ellman's method
40
Total Activities
40
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Cholinesterase (CHEMBL5763)
Type SINGLE PROTEIN
Organism Equus caballus

Publication

Discovery of 4-benzylpiperazinequinoline BChE inhibitor that suppresses neuroinflammation for the treatment of Alzheimer's disease.
Chen Y, Zhang W, Li Q, Xie H, Xing S, Lu X, Lyu W, Xiong B, Wang Y, Qu W, Liu W, Chi H, Zhang X, Feng F, Sun H.
Eur J Med Chem (2024) 272 : 116463 -116463
PubMed 38704944 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 40 6.15 7.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL95 TACRINE 4.0 1 7.70
CHEMBL5542274 1 7.22
CHEMBL5558992 1 6.89
CHEMBL5556813 1 6.85
CHEMBL5556106 1 6.80
CHEMBL5505765 1 6.77
CHEMBL5556450 1 6.75
CHEMBL5555772 1 6.75
CHEMBL5558573 1 6.75
CHEMBL5557904 1 6.68
CHEMBL5505876 1 6.64
CHEMBL5559511 1 6.55
CHEMBL5512507 1 6.52
CHEMBL5557117 1 6.44
CHEMBL5532571 1 6.40
CHEMBL5523413 1 6.40
CHEMBL5517898 1 6.38
CHEMBL5556895 1 6.37
CHEMBL5532024 1 6.36
CHEMBL5542322 1 6.34
CHEMBL5556256 1 6.23
CHEMBL5505759 1 6.22
CHEMBL5517904 1 6.16
CHEMBL5555797 1 6.11
CHEMBL5523576 1 6.02
CHEMBL5559193 1 5.93
CHEMBL5556197 1 5.90
CHEMBL5558959 1 5.89
CHEMBL5531976 1 5.80
CHEMBL5532209 1 5.65

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL95 TACRINE IC50 = 20.0 nM 7.70
CHEMBL5542274 IC50 = 60.0 nM 7.22
CHEMBL5558992 IC50 = 130.0 nM 6.89
CHEMBL5556813 IC50 = 140.0 nM 6.85
CHEMBL5556106 IC50 = 160.0 nM 6.80
CHEMBL5505765 IC50 = 170.0 nM 6.77
CHEMBL5556450 IC50 = 180.0 nM 6.75
CHEMBL5555772 IC50 = 180.0 nM 6.75
CHEMBL5558573 IC50 = 180.0 nM 6.75
CHEMBL5557904 IC50 = 210.0 nM 6.68
CHEMBL5505876 IC50 = 230.0 nM 6.64
CHEMBL5559511 IC50 = 280.0 nM 6.55
CHEMBL5512507 IC50 = 300.0 nM 6.52
CHEMBL5557117 IC50 = 360.0 nM 6.44
CHEMBL5523413 IC50 = 400.0 nM 6.40
CHEMBL5532571 IC50 = 400.0 nM 6.40
CHEMBL5517898 IC50 = 420.0 nM 6.38
CHEMBL5556895 IC50 = 430.0 nM 6.37
CHEMBL5532024 IC50 = 440.0 nM 6.36
CHEMBL5542322 IC50 = 460.0 nM 6.34
CHEMBL5556256 IC50 = 590.0 nM 6.23
CHEMBL5505759 IC50 = 600.0 nM 6.22
CHEMBL5517904 IC50 = 700.0 nM 6.16
CHEMBL5555797 IC50 = 770.0 nM 6.11
CHEMBL5523576 IC50 = 960.0 nM 6.02
CHEMBL5559193 IC50 = 1180.0 nM 5.93
CHEMBL5556197 IC50 = 1270.0 nM 5.90
CHEMBL5558959 IC50 = 1300.0 nM 5.89
CHEMBL5531976 IC50 = 1580.0 nM 5.80
CHEMBL5532209 IC50 = 2240.0 nM 5.65
CHEMBL5557514 IC50 = 2650.0 nM 5.58
CHEMBL5505928 IC50 = 3060.0 nM 5.51
CHEMBL5537076 IC50 = 3310.0 nM 5.48
CHEMBL5505894 IC50 = 3320.0 nM 5.48
CHEMBL5512557 IC50 = 4730.0 nM 5.33
CHEMBL5532046 IC50 = 6270.0 nM 5.20
CHEMBL5555535 IC50 = 7610.0 nM 5.12
CHEMBL5556303 IC50 = 9040.0 nM 5.04
CHEMBL5558875 IC50 = 11900.0 nM 4.92
CHEMBL5558423 IC50 = 15080.0 nM 4.82