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Assay Detail

CHEMBL636829

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

Binding
In vitro inhibition against acetylcholinesterase in rat striata.
38
Total Activities
38
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Acetylcholinesterase (CHEMBL3199)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

9-Amino-1,2,3,4-tetrahydroacridin-1-ols: synthesis and evaluation as potential Alzheimer's disease therapeutics.
Shutske GM, Pierrat FA, Kapples KJ, Cornfeldt ML, Szewczak MR, Huger FP, Bores GM, Haroutunian V, Davis KL.
J Med Chem (1989) 32 : 1805 -1813
PubMed 2754707 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 38 5.11 7.93

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL298577 1 7.93
CHEMBL50309 1 6.54
CHEMBL95 TACRINE 4.0 1 6.50
CHEMBL298154 1 6.08
CHEMBL51063 1 5.89
CHEMBL50264 1 5.75
CHEMBL54086 1 5.75
CHEMBL50462 1 5.70
CHEMBL50578 1 5.47
CHEMBL51934 VELNACRINE 2.0 1 5.40
CHEMBL53978 1 5.40
CHEMBL50735 1 5.23
CHEMBL50736 1 5.22
CHEMBL298896 1 5.12
CHEMBL299771 1 5.06
CHEMBL300315 1 4.99
CHEMBL298685 1 4.96
CHEMBL1794988 1 4.90
CHEMBL52608 1 4.88
CHEMBL50263 1 4.88
CHEMBL54186 1 4.88
CHEMBL53182 1 4.88
CHEMBL53598 1 4.85
CHEMBL1794987 1 4.82
CHEMBL298674 1 4.78
CHEMBL299147 1 4.74
CHEMBL53973 1 4.70
CHEMBL53715 1 4.68
CHEMBL53239 1 4.68
CHEMBL53240 1 4.61

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL298577 IC50 = 11.7 nM 7.93
CHEMBL50309 IC50 = 292.0 nM 6.54
CHEMBL95 TACRINE IC50 = 319.0 nM 6.50
CHEMBL298154 IC50 = 823.0 nM 6.08
CHEMBL51063 IC50 = 1300.0 nM 5.89
CHEMBL50264 IC50 = 1760.0 nM 5.75
CHEMBL54086 IC50 = 1770.0 nM 5.75
CHEMBL50462 IC50 = 2000.0 nM 5.70
CHEMBL50578 IC50 = 3390.0 nM 5.47
CHEMBL51934 VELNACRINE IC50 = 4000.0 nM 5.40
CHEMBL53978 IC50 = 3980.0 nM 5.40
CHEMBL50735 IC50 = 5890.0 nM 5.23
CHEMBL50736 IC50 = 5970.0 nM 5.22
CHEMBL298896 IC50 = 7680.0 nM 5.12
CHEMBL299771 IC50 = 8630.0 nM 5.06
CHEMBL300315 IC50 = 10300.0 nM 4.99
CHEMBL298685 IC50 = 10900.0 nM 4.96
CHEMBL1794988 IC50 = 12600.0 nM 4.90
CHEMBL53182 IC50 = 13300.0 nM 4.88
CHEMBL50263 IC50 = 13300.0 nM 4.88
CHEMBL52608 IC50 = 13300.0 nM 4.88
CHEMBL54186 IC50 = 13100.0 nM 4.88
CHEMBL53598 IC50 = 14200.0 nM 4.85
CHEMBL1794987 IC50 = 15300.0 nM 4.82
CHEMBL298674 IC50 = 16700.0 nM 4.78
CHEMBL299147 IC50 = 18100.0 nM 4.74
CHEMBL53973 IC50 = 20100.0 nM 4.70
CHEMBL53715 IC50 = 21100.0 nM 4.68
CHEMBL53239 IC50 = 21000.0 nM 4.68
CHEMBL53240 IC50 = 24500.0 nM 4.61
CHEMBL51168 IC50 = 24700.0 nM 4.61
CHEMBL52181 IC50 = 27200.0 nM 4.57
CHEMBL53830 IC50 = 36000.0 nM 4.44
CHEMBL52967 IC50 = 41300.0 nM 4.38
CHEMBL53666 IC50 = 49300.0 nM 4.31
CHEMBL1794989 IC50 = 63000.0 nM 4.20
CHEMBL50410 IC50 = 68200.0 nM 4.17
CHEMBL50322 IC50 = 87800.0 nM 4.06