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Assay Detail

CHEMBL2015198

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

Binding
Inhibition of human recombinant AChE using acetylthiocholine iodide as substrate preincubated for 20 mins prior substrate addition measured after 5 mins by spectrophotometry
21
Total Activities
21
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

Huprine-tacrine heterodimers as anti-amyloidogenic compounds of potential interest against Alzheimer's and prion diseases.
Galdeano C, Viayna E, Sola I, Formosa X, Camps P, Badia A, Clos MV, Relat J, Ratia M, Bartolini M, Mancini F, Andrisano V, Salmona M, Minguillón C, González-Muñoz GC, Rodríguez-Franco MI, Bidon-Chanal A, Luque FJ, Muñoz-Torrero D.
J Med Chem (2012) 55 : 661 -669
PubMed 22185619 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 21 8.56 9.51

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2011495 1 9.51
CHEMBL2011487 1 9.38
CHEMBL1994202 1 9.37
CHEMBL536047 1 9.16
CHEMBL2011491 1 9.13
CHEMBL2011483 1 9.05
CHEMBL3216777 1 8.88
CHEMBL2011496 1 8.88
CHEMBL2011488 1 8.86
CHEMBL3215882 1 8.72
CHEMBL3216556 1 8.69
CHEMBL3216778 1 8.49
CHEMBL3216116 1 8.45
CHEMBL3216555 1 8.40
CHEMBL3216554 1 8.38
CHEMBL3217208 1 8.16
CHEMBL3216779 1 8.04
CHEMBL3216557 1 7.94
CHEMBL292314 1 7.88
CHEMBL2011499 1 7.87
CHEMBL95 TACRINE 4.0 1 6.50

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2011495 IC50 = 0.31 nM 9.51
CHEMBL2011487 IC50 = 0.42 nM 9.38
CHEMBL1994202 IC50 = 0.43 nM 9.37
CHEMBL536047 IC50 = 0.69 nM 9.16
CHEMBL2011491 IC50 = 0.74 nM 9.13
CHEMBL2011483 IC50 = 0.89 nM 9.05
CHEMBL3216777 IC50 = 1.33 nM 8.88
CHEMBL2011496 IC50 = 1.32 nM 8.88
CHEMBL2011488 IC50 = 1.38 nM 8.86
CHEMBL3215882 IC50 = 1.89 nM 8.72
CHEMBL3216556 IC50 = 2.04 nM 8.69
CHEMBL3216778 IC50 = 3.26 nM 8.49
CHEMBL3216116 IC50 = 3.53 nM 8.45
CHEMBL3216555 IC50 = 4.02 nM 8.40
CHEMBL3216554 IC50 = 4.19 nM 8.38
CHEMBL3217208 IC50 = 6.84 nM 8.16
CHEMBL3216779 IC50 = 9.09 nM 8.04
CHEMBL3216557 IC50 = 11.5 nM 7.94
CHEMBL292314 IC50 = 13.2 nM 7.88
CHEMBL2011499 IC50 = 13.6 nM 7.87
CHEMBL95 TACRINE IC50 = 317.0 nM 6.50