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Assay Detail

CHEMBL1051648

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

Binding
Inhibition of bovine AChE by Ellman's method
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Bos taurus
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

Acetylcholinesterase (CHEMBL4768)
Type SINGLE PROTEIN
Organism Bos taurus

Publication

Pyrano[3,2-c]quinoline-6-chlorotacrine hybrids as a novel family of acetylcholinesterase- and beta-amyloid-directed anti-Alzheimer compounds.
Camps P, Formosa X, Galdeano C, Muñoz-Torrero D, Ramírez L, Gómez E, Isambert N, Lavilla R, Badia A, Clos MV, Bartolini M, Mancini F, Andrisano V, Arce MP, Rodríguez-Franco MI, Huertas O, Dafni T, Luque FJ.
J Med Chem (2009) 52 : 5365 -5379
PubMed 19663388 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 14 7.43 8.24

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL486698 1 8.24
CHEMBL3215572 1 7.99
CHEMBL3215768 1 7.98
CHEMBL3216429 1 7.69
CHEMBL2448076 1 7.62
CHEMBL3215769 1 7.62
CHEMBL3216221 1 7.52
CHEMBL3215573 1 7.51
CHEMBL3215574 1 7.47
CHEMBL3216018 1 7.32
CHEMBL3215770 1 7.03
CHEMBL345124 PROPIDIUM 1 5.20
CHEMBL554901 1 -
CHEMBL550989 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL486698 IC50 = 5.73 nM 8.24
CHEMBL3215572 IC50 = 10.3 nM 7.99
CHEMBL3215768 IC50 = 10.4 nM 7.98
CHEMBL3216429 IC50 = 20.4 nM 7.69
CHEMBL2448076 IC50 = 23.9 nM 7.62
CHEMBL3215769 IC50 = 24.0 nM 7.62
CHEMBL3216221 IC50 = 29.9 nM 7.52
CHEMBL3215573 IC50 = 30.8 nM 7.51
CHEMBL3215574 IC50 = 34.1 nM 7.47
CHEMBL3216018 IC50 = 48.1 nM 7.32
CHEMBL3215770 IC50 = 93.7 nM 7.03
CHEMBL345124 PROPIDIUM IC50 = 6289.0 nM 5.20
CHEMBL554901 IC50 > 10000.0 nM -
CHEMBL550989 IC50 > 10000.0 nM -