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Assay Detail

CHEMBL2162063

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

Binding
Inhibition of human recombinant BChE using acetylthiocholine as substrate
11
Total Activities
11
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

Design, synthesis, and bioevaluation of benzamides: novel acetylcholinesterase inhibitors with multi-functions on butylcholinesterase, Aβ aggregation, and β-secretase.
Peng DY, Sun Q, Zhu XL, Lin HY, Chen Q, Yu NX, Yang WC, Yang GF.
Bioorg Med Chem (2012) 20 : 6739 -6750
PubMed 23041347 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 11 7.00 8.06

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL95 TACRINE 4.0 1 8.06
CHEMBL2159662 1 7.26
CHEMBL2159659 1 7.25
CHEMBL2159664 1 7.18
CHEMBL2159660 1 7.09
CHEMBL2159663 1 7.03
CHEMBL2159657 1 7.01
CHEMBL2159661 1 7.00
CHEMBL2159658 1 6.78
CHEMBL659 GALANTAMINE 4.0 1 6.72
CHEMBL2159656 1 5.63

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL95 TACRINE Ki = 8.72 nM 8.06
CHEMBL2159662 Ki = 55.0 nM 7.26
CHEMBL2159659 Ki = 56.0 nM 7.25
CHEMBL2159664 Ki = 66.0 nM 7.18
CHEMBL2159660 Ki = 82.0 nM 7.09
CHEMBL2159663 Ki = 93.0 nM 7.03
CHEMBL2159657 Ki = 97.0 nM 7.01
CHEMBL2159661 Ki = 99.0 nM 7.00
CHEMBL2159658 Ki = 166.0 nM 6.78
CHEMBL659 GALANTAMINE Ki = 192.47 nM 6.72
CHEMBL2159656 Ki = 2360.0 nM 5.63