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Assay Detail

CHEMBL654400

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

Binding
Concentration that causes 50% inhibition of Butyrylcholinesterase (BChE) using human serum and BW284c51
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Cholinesterase (CHEMBL1914)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Homodimeric tacrine congeners as acetylcholinesterase inhibitors.
Hu MK, Wu LJ, Hsiao G, Yen MH.
J Med Chem (2002) 45 : 2277 -2282
PubMed 12014965 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 19 7.23 8.59

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL307908 1 8.59
CHEMBL308962 1 8.48
CHEMBL306492 1 8.42
CHEMBL75985 1 7.64
CHEMBL307004 1 7.58
CHEMBL74940 1 7.35
CHEMBL75274 1 7.28
CHEMBL32823 1 7.27
CHEMBL76173 1 7.23
CHEMBL73800 1 7.08
CHEMBL95 TACRINE 4.0 1 7.05
CHEMBL75305 1 7.03
CHEMBL312761 1 6.79
CHEMBL74827 1 6.78
CHEMBL312310 1 6.71
CHEMBL74927 1 6.59
CHEMBL421501 1 6.56
CHEMBL73160 1 6.51
CHEMBL76014 1 6.48

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL307908 IC50 = 2.6 nM 8.59
CHEMBL308962 IC50 = 3.3 nM 8.48
CHEMBL306492 IC50 = 3.8 nM 8.42
CHEMBL75985 IC50 = 23.0 nM 7.64
CHEMBL307004 IC50 = 26.0 nM 7.58
CHEMBL74940 IC50 = 45.0 nM 7.35
CHEMBL75274 IC50 = 53.0 nM 7.28
CHEMBL32823 IC50 = 54.0 nM 7.27
CHEMBL76173 IC50 = 59.0 nM 7.23
CHEMBL73800 IC50 = 83.0 nM 7.08
CHEMBL95 TACRINE IC50 = 89.0 nM 7.05
CHEMBL75305 IC50 = 93.0 nM 7.03
CHEMBL312761 IC50 = 164.0 nM 6.79
CHEMBL74827 IC50 = 165.0 nM 6.78
CHEMBL312310 IC50 = 194.0 nM 6.71
CHEMBL74927 IC50 = 257.0 nM 6.59
CHEMBL421501 IC50 = 273.0 nM 6.56
CHEMBL73160 IC50 = 312.0 nM 6.51
CHEMBL76014 IC50 = 328.0 nM 6.48