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Assay Detail

CHEMBL2395155

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

Binding
Inhibition of electric eel AChE using acetylthiocholine as substrate preincubated for 10 mins prior to substrate addition measured every 30 seconds for 30 mins by Ellman's method
32
Total Activities
32
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Electrophorus electricus
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Acetylcholinesterase (CHEMBL4078)
Type SINGLE PROTEIN
Organism Electrophorus electricus

Publication

Investigation of the role of linker moieties in bifunctional tacrine hybrids.
Eckroat TJ, Green KD, Reed RA, Bornstein JJ, Garneau-Tsodikova S.
Bioorg Med Chem (2013) 21 : 3614 -3623
PubMed 23535563 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 32 7.80 9.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2393227 1 9.30
CHEMBL2393095 1 9.22
CHEMBL2393097 1 9.19
CHEMBL2393229 1 9.11
CHEMBL2393096 1 9.03
CHEMBL2393094 1 8.94
CHEMBL2393109 1 8.94
CHEMBL2393101 1 8.64
CHEMBL2393111 1 8.53
CHEMBL2393102 1 8.29
CHEMBL2393093 1 8.27
CHEMBL2393224 1 8.18
CHEMBL2393228 1 8.16
CHEMBL2393225 1 8.10
CHEMBL2393226 1 7.96
CHEMBL2393092 1 7.96
CHEMBL2393106 1 7.87
CHEMBL59782 1 7.80
CHEMBL2393100 1 7.71
CHEMBL2393098 1 7.58
CHEMBL2393107 1 7.43
CHEMBL2393090 1 7.42
CHEMBL2393110 1 7.38
CHEMBL2393104 1 7.37
CHEMBL2393091 1 7.29
CHEMBL95 TACRINE 4.0 1 7.28
CHEMBL2393099 1 7.18
CHEMBL2393103 1 7.14
CHEMBL2390978 1 5.86
CHEMBL2393089 1 5.63

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2393227 IC50 = 0.495 nM 9.30
CHEMBL2393095 IC50 = 0.604 nM 9.22
CHEMBL2393097 IC50 = 0.648 nM 9.19
CHEMBL2393229 IC50 = 0.776 nM 9.11
CHEMBL2393096 IC50 = 0.932 nM 9.03
CHEMBL2393094 IC50 = 1.14 nM 8.94
CHEMBL2393109 IC50 = 1.14 nM 8.94
CHEMBL2393101 IC50 = 2.27 nM 8.64
CHEMBL2393111 IC50 = 2.94 nM 8.53
CHEMBL2393102 IC50 = 5.17 nM 8.29
CHEMBL2393093 IC50 = 5.37 nM 8.27
CHEMBL2393224 IC50 = 6.67 nM 8.18
CHEMBL2393228 IC50 = 6.94 nM 8.16
CHEMBL2393225 IC50 = 7.91 nM 8.10
CHEMBL2393092 IC50 = 11.1 nM 7.96
CHEMBL2393226 IC50 = 11.1 nM 7.96
CHEMBL2393106 IC50 = 13.6 nM 7.87
CHEMBL59782 IC50 = 16.0 nM 7.80
CHEMBL2393100 IC50 = 19.6 nM 7.71
CHEMBL2393098 IC50 = 26.3 nM 7.58
CHEMBL2393107 IC50 = 37.4 nM 7.43
CHEMBL2393090 IC50 = 38.0 nM 7.42
CHEMBL2393110 IC50 = 41.7 nM 7.38
CHEMBL2393104 IC50 = 42.4 nM 7.37
CHEMBL2393091 IC50 = 51.0 nM 7.29
CHEMBL95 TACRINE IC50 = 52.4 nM 7.28
CHEMBL2393099 IC50 = 65.3 nM 7.18
CHEMBL2393103 IC50 = 72.5 nM 7.14
CHEMBL2390978 IC50 = 1380.0 nM 5.86
CHEMBL2393089 IC50 = 2360.0 nM 5.63
CHEMBL2393105 IC50 = 2470.0 nM 5.61
CHEMBL2393108 IC50 = 7230.0 nM 5.14