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Assay Detail

CHEMBL3772142

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

Binding
Inhibition of human AChE using acetylthiocholine iodide as substrate preincubated for 5 mins followed by substrate addition measured after 60 to 300 sec by Ellman's method
32
Total Activities
32
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Acetylcholinesterase (CHEMBL220)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Tricyclic phenothiazine and phenoselenazine derivatives as potential multi-targeting agents to treat Alzheimer's disease
Tin G, Mohamed T, Gondora N, Beazely MA, Rao PPN
Medchemcomm (2015) 6 : 1930 -1941
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 32 5.33 7.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL502 DONEPEZIL 4.0 1 7.40
CHEMBL95 TACRINE 4.0 1 6.80
CHEMBL659 GALANTAMINE 4.0 1 5.58
CHEMBL3770206 1 5.34
CHEMBL3769576 1 5.34
CHEMBL3770978 1 5.29
CHEMBL3770569 1 5.27
CHEMBL3769834 1 5.25
CHEMBL3770203 1 5.24
CHEMBL3770356 1 5.24
CHEMBL3769537 1 5.23
CHEMBL1801816 1 5.23
CHEMBL3770479 1 5.22
CHEMBL51085 EBSELEN 3.0 1 5.21
CHEMBL3769555 1 5.21
CHEMBL1327885 1 5.21
CHEMBL3769833 1 5.21
CHEMBL3770577 1 5.20
CHEMBL3769862 1 5.20
CHEMBL239618 1 5.20
CHEMBL3770803 1 5.19
CHEMBL3770071 1 5.19
CHEMBL3769811 1 5.19
CHEMBL3771233 1 5.17
CHEMBL240047 1 5.15
CHEMBL828 PHENOTHIAZINE 2.0 1 5.14
CHEMBL1411769 1 5.13
CHEMBL394753 1 5.13
CHEMBL3770516 1 5.12
CHEMBL3770866 1 5.10

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL502 DONEPEZIL IC50 = 40.0 nM 7.40
CHEMBL95 TACRINE IC50 = 160.0 nM 6.80
CHEMBL659 GALANTAMINE IC50 = 2600.0 nM 5.58
CHEMBL3770206 IC50 = 4600.0 nM 5.34
CHEMBL3769576 IC50 = 4600.0 nM 5.34
CHEMBL3770978 IC50 = 5100.0 nM 5.29
CHEMBL3770569 IC50 = 5400.0 nM 5.27
CHEMBL3769834 IC50 = 5600.0 nM 5.25
CHEMBL3770203 IC50 = 5800.0 nM 5.24
CHEMBL3770356 IC50 = 5800.0 nM 5.24
CHEMBL3769537 IC50 = 5900.0 nM 5.23
CHEMBL1801816 IC50 = 5900.0 nM 5.23
CHEMBL3770479 IC50 = 6000.0 nM 5.22
CHEMBL3769555 IC50 = 6200.0 nM 5.21
CHEMBL51085 EBSELEN IC50 = 6200.0 nM 5.21
CHEMBL3769833 IC50 = 6200.0 nM 5.21
CHEMBL1327885 IC50 = 6200.0 nM 5.21
CHEMBL3770577 IC50 = 6300.0 nM 5.20
CHEMBL3769862 IC50 = 6300.0 nM 5.20
CHEMBL239618 IC50 = 6300.0 nM 5.20
CHEMBL3770803 IC50 = 6500.0 nM 5.19
CHEMBL3770071 IC50 = 6400.0 nM 5.19
CHEMBL3769811 IC50 = 6400.0 nM 5.19
CHEMBL3771233 IC50 = 6700.0 nM 5.17
CHEMBL240047 IC50 = 7100.0 nM 5.15
CHEMBL828 PHENOTHIAZINE IC50 = 7300.0 nM 5.14
CHEMBL1411769 IC50 = 7400.0 nM 5.13
CHEMBL394753 IC50 = 7400.0 nM 5.13
CHEMBL3770516 IC50 = 7500.0 nM 5.12
CHEMBL3770866 IC50 = 7900.0 nM 5.10
CHEMBL239400 IC50 = 8000.0 nM 5.10
CHEMBL1801815 IC50 = 9900.0 nM 5.00