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Assay Detail

CHEMBL4361992

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

Binding
Inhibition of human serum BuChe by Ellman's method
12
Total Activities
12
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

Cholinesterase (CHEMBL1914)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Tacrine-O-protected phenolics heterodimers as multitarget-directed ligands against Alzheimer's disease: Selective subnanomolar BuChE inhibitors.
Roldán-Peña JM, Romero-Real V, Hicke J, Maya I, Franconetti A, Lagunes I, Padrón JM, Padrón JM, Petralla S, Poeta E, Naldi M, Bartolini M, Monti B, Bolognesi ML, López Ó, Fernández-Bolaños JG.
Eur J Med Chem (2019) 181 : 111550 -111550
PubMed 31376562 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 12 7.84 9.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4545701 1 9.30
CHEMBL4555120 1 9.29
CHEMBL4475228 1 8.54
CHEMBL4531167 1 8.22
CHEMBL4588525 1 8.16
CHEMBL4572757 1 7.64
CHEMBL4589250 1 7.45
CHEMBL4536715 1 7.38
CHEMBL95 TACRINE 4.0 1 7.36
CHEMBL4535585 1 7.13
CHEMBL4521755 1 6.92
CHEMBL4439554 1 6.71

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4545701 IC50 = 0.497 nM 9.30
CHEMBL4555120 IC50 = 0.515 nM 9.29
CHEMBL4475228 IC50 = 2.92 nM 8.54
CHEMBL4531167 IC50 = 6.06 nM 8.22
CHEMBL4588525 IC50 = 6.95 nM 8.16
CHEMBL4572757 IC50 = 22.9 nM 7.64
CHEMBL4589250 IC50 = 35.6 nM 7.45
CHEMBL4536715 IC50 = 41.5 nM 7.38
CHEMBL95 TACRINE IC50 = 44.2 nM 7.36
CHEMBL4535585 IC50 = 74.8 nM 7.13
CHEMBL4521755 IC50 = 120.0 nM 6.92
CHEMBL4439554 IC50 = 194.0 nM 6.71