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Assay Detail

CHEMBL644101

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Binding
Inhibitory activity against human erythrocyte acetylcholinesterase
24
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Acetylcholinesterase (CHEMBL220)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

SAR of 9-amino-1,2,3,4-tetrahydroacridine-based acetylcholinesterase inhibitors: synthesis, enzyme inhibitory activity, QSAR, and structure-based CoMFA of tacrine analogues.
Recanatini M, Cavalli A, Belluti F, Piazzi L, Rampa A, Bisi A, Gobbi S, Valenti P, Andrisano V, Bartolini M, Cavrini V.
J Med Chem (2000) 43 : 2007 -2018
PubMed 10821713 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 24 6.44 8.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL292314 1 8.05
CHEMBL59782 1 7.89
CHEMBL61715 1 7.55
CHEMBL61561 1 7.35
CHEMBL61850 1 7.18
CHEMBL61533 1 7.06
CHEMBL60119 1 7.00
CHEMBL61221 1 6.89
CHEMBL59628 1 6.77
CHEMBL95 TACRINE 4.0 1 6.60
CHEMBL294525 1 6.54
CHEMBL302842 1 6.46
CHEMBL61849 1 6.41
CHEMBL61986 1 6.34
CHEMBL61930 1 6.33
CHEMBL62084 1 6.26
CHEMBL64465 1 6.12
CHEMBL418643 1 5.80
CHEMBL59977 1 5.52
CHEMBL64815 1 5.43
CHEMBL61486 1 5.42
CHEMBL61506 1 5.32
CHEMBL61929 1 5.28
CHEMBL62085 1 5.09

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL292314 IC50 = 9.0 nM 8.05
CHEMBL59782 IC50 = 13.0 nM 7.89
CHEMBL61715 IC50 = 28.0 nM 7.55
CHEMBL61561 IC50 = 45.0 nM 7.35
CHEMBL61850 IC50 = 66.0 nM 7.18
CHEMBL61533 IC50 = 87.0 nM 7.06
CHEMBL60119 IC50 = 100.0 nM 7.00
CHEMBL61221 IC50 = 130.0 nM 6.89
CHEMBL59628 IC50 = 170.0 nM 6.77
CHEMBL95 TACRINE IC50 = 250.0 nM 6.60
CHEMBL294525 IC50 = 290.0 nM 6.54
CHEMBL302842 IC50 = 350.0 nM 6.46
CHEMBL61849 IC50 = 390.0 nM 6.41
CHEMBL61986 IC50 = 460.0 nM 6.34
CHEMBL61930 IC50 = 470.0 nM 6.33
CHEMBL62084 IC50 = 550.0 nM 6.26
CHEMBL64465 IC50 = 750.0 nM 6.12
CHEMBL418643 IC50 = 1600.0 nM 5.80
CHEMBL59977 IC50 = 3000.0 nM 5.52
CHEMBL64815 IC50 = 3700.0 nM 5.43
CHEMBL61486 IC50 = 3800.0 nM 5.42
CHEMBL61506 IC50 = 4800.0 nM 5.32
CHEMBL61929 IC50 = 5200.0 nM 5.28
CHEMBL62085 IC50 = 8100.0 nM 5.09