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Assay Detail

CHEMBL1067130

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

Binding
Inhibition of human recombinant AChE preincubated for 20 mins before substrate addition by Ellman's method
24
Total Activities
24
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

Targeting Alzheimer's disease: Novel indanone hybrids bearing a pharmacophoric fragment of AP2238.
Rizzo S, Bartolini M, Ceccarini L, Piazzi L, Gobbi S, Cavalli A, Recanatini M, Andrisano V, Rampa A.
Bioorg Med Chem (2010) 18 : 1749 -1760
PubMed 20171894 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 24 6.20 7.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL502 DONEPEZIL 4.0 1 7.70
CHEMBL75121 1 7.36
CHEMBL599644 1 7.28
CHEMBL597188 1 7.25
CHEMBL597794 1 6.96
CHEMBL597822 1 6.75
CHEMBL604096 1 6.75
CHEMBL599057 1 6.72
CHEMBL603256 1 6.70
CHEMBL599058 1 6.42
CHEMBL598824 1 6.29
CHEMBL610779 1 6.20
CHEMBL598645 1 6.05
CHEMBL597821 1 6.05
CHEMBL598632 1 5.94
CHEMBL599254 1 5.88
CHEMBL599253 1 5.82
CHEMBL597001 1 5.79
CHEMBL604715 1 5.54
CHEMBL599252 1 5.40
CHEMBL597405 1 5.31
CHEMBL597795 1 5.27
CHEMBL597406 1 4.93
CHEMBL610219 1 4.54

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL502 DONEPEZIL IC50 = 20.0 nM 7.70
CHEMBL75121 IC50 = 44.0 nM 7.36
CHEMBL599644 IC50 = 52.0 nM 7.28
CHEMBL597188 IC50 = 56.0 nM 7.25
CHEMBL597794 IC50 = 110.0 nM 6.96
CHEMBL597822 IC50 = 180.0 nM 6.75
CHEMBL604096 IC50 = 180.0 nM 6.75
CHEMBL599057 IC50 = 190.0 nM 6.72
CHEMBL603256 IC50 = 200.0 nM 6.70
CHEMBL599058 IC50 = 380.0 nM 6.42
CHEMBL598824 IC50 = 510.0 nM 6.29
CHEMBL610779 IC50 = 630.0 nM 6.20
CHEMBL598645 IC50 = 890.0 nM 6.05
CHEMBL597821 IC50 = 890.0 nM 6.05
CHEMBL598632 IC50 = 1140.0 nM 5.94
CHEMBL599254 IC50 = 1320.0 nM 5.88
CHEMBL599253 IC50 = 1530.0 nM 5.82
CHEMBL597001 IC50 = 1610.0 nM 5.79
CHEMBL604715 IC50 = 2900.0 nM 5.54
CHEMBL599252 IC50 = 3950.0 nM 5.40
CHEMBL597405 IC50 = 4930.0 nM 5.31
CHEMBL597795 IC50 = 5380.0 nM 5.27
CHEMBL597406 IC50 = 11700.0 nM 4.93
CHEMBL610219 IC50 = 28700.0 nM 4.54