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Assay Detail

CHEMBL832203

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

Binding
Inhibitory concentration against acetylcholinesterase of rat cortex homogenate
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Tissue Cortex
Confidence 9 — Direct single protein target
Curated By Expert

Target

Acetylcholinesterase (CHEMBL3199)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Bis-huperzine B: highly potent and selective acetylcholinesterase inhibitors.
Feng S, Wang Z, He X, Zheng S, Xia Y, Jiang H, Tang X, Bai D.
J Med Chem (2005) 48 : 655 -657
PubMed 15689148 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 10 6.97 8.31

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL176132 BIS(18)-HUPERZINE B 1 8.31
CHEMBL434898 BIS(16)-HUPERZINE B 1 7.73
CHEMBL368897 BIS(20)-HUPERZINE B 1 7.60
CHEMBL368899 1 7.45
CHEMBL435673 1 7.29
CHEMBL395280 HUPERZINE A 2.0 1 7.14
CHEMBL175975 BIS(12)-HUPERZINE B 1 7.12
CHEMBL367977 BIS(9)-HUPERZINE B 1 6.33
CHEMBL360092 BIS(8)-HUPERZINE B 1 5.99
CHEMBL245079 HUPERZINE B 1 4.71

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL176132 BIS(18)-HUPERZINE B IC50 = 4.93 nM 8.31
CHEMBL434898 BIS(16)-HUPERZINE B IC50 = 18.5 nM 7.73
CHEMBL368897 BIS(20)-HUPERZINE B IC50 = 25.2 nM 7.60
CHEMBL368899 IC50 = 35.9 nM 7.45
CHEMBL435673 IC50 = 50.8 nM 7.29
CHEMBL395280 HUPERZINE A IC50 = 72.4 nM 7.14
CHEMBL175975 BIS(12)-HUPERZINE B IC50 = 76.2 nM 7.12
CHEMBL367977 BIS(9)-HUPERZINE B IC50 = 471.0 nM 6.33
CHEMBL360092 BIS(8)-HUPERZINE B IC50 = 1020.0 nM 5.99
CHEMBL245079 HUPERZINE B IC50 = 19300.0 nM 4.71