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Assay Detail

CHEMBL2401048

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

Binding
Inhibition of human AchE using acetylthiocholine iodide as substrate incubated for 20 mins prior to substrate addition measured for 1 hr by Ellman's method
16
Total Activities
16
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

Synthesis, biological evaluation and molecular modeling of substituted 2-aminobenzimidazoles as novel inhibitors of acetylcholinesterase and butyrylcholinesterase.
Zhu J, Wu CF, Li X, Wu GS, Xie S, Hu QN, Deng Z, Zhu MX, Luo HR, Hong X.
Bioorg Med Chem (2013) 21 : 4218 -4224
PubMed 23719283 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 16 4.77 6.57

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL95 TACRINE 4.0 1 6.57
CHEMBL2396912 1 4.23
CHEMBL2396910 1 4.22
CHEMBL2396913 1 4.05
CHEMBL2396914 1 -
CHEMBL1429841 1 -
CHEMBL2396911 1 -
CHEMBL2396909 1 -
CHEMBL2396908 1 -
CHEMBL1572608 1 -
CHEMBL2396907 1 -
CHEMBL2396906 1 -
CHEMBL2396905 1 -
CHEMBL2396904 1 -
CHEMBL2396903 1 -
CHEMBL1376358 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL95 TACRINE IC50 = 268.0 nM 6.57
CHEMBL2396912 IC50 = 59200.0 nM 4.23
CHEMBL2396910 IC50 = 59680.0 nM 4.22
CHEMBL2396913 IC50 = 88920.0 nM 4.05
CHEMBL2396914 IC50 > 100000.0 nM -
CHEMBL1429841 IC50 > 100000.0 nM -
CHEMBL2396911 IC50 > 100000.0 nM -
CHEMBL2396909 IC50 > 100000.0 nM -
CHEMBL2396908 IC50 > 100000.0 nM -
CHEMBL1572608 IC50 > 100000.0 nM -
CHEMBL2396907 IC50 > 100000.0 nM -
CHEMBL2396906 IC50 > 100000.0 nM -
CHEMBL2396905 IC50 > 100000.0 nM -
CHEMBL2396904 IC50 > 100000.0 nM -
CHEMBL2396903 IC50 > 100000.0 nM -
CHEMBL1376358 IC50 > 100000.0 nM -