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Assay Detail

CHEMBL1041236

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

Binding
Inhibition of human recombinant AChE in erythrocytes by Ellman's assay
29
Total Activities
29
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

Acetylcholinesterase (CHEMBL220)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis and structure-activity relationship of Huprine derivatives as human acetylcholinesterase inhibitors.
Ronco C, Sorin G, Nachon F, Foucault R, Jean L, Romieu A, Renard PY.
Bioorg Med Chem (2009) 17 : 4523 -4536
PubMed 19473849 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 29 6.04 8.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL208599 HUPRINE X 1 8.96
CHEMBL140476 HUPRINE Y 1 8.73
CHEMBL575802 1 8.40
CHEMBL575674 1 8.22
CHEMBL573095 1 8.17
CHEMBL574973 1 8.06
CHEMBL583920 1 8.02
CHEMBL574974 1 7.86
CHEMBL576385 1 7.36
CHEMBL575614 1 6.18
CHEMBL575613 1 6.09
CHEMBL584603 1 6.07
CHEMBL576004 1 5.60
CHEMBL575167 1 5.54
CHEMBL574746 1 5.32
CHEMBL573094 1 5.29
CHEMBL583776 1 5.19
CHEMBL576384 1 5.14
CHEMBL574261 1 5.11
CHEMBL575810 1 5.09
CHEMBL574267 1 4.93
CHEMBL575166 1 4.83
CHEMBL572866 1 4.72
CHEMBL572865 1 4.65
CHEMBL576189 1 4.57
CHEMBL574948 1 4.30
CHEMBL572858 1 4.30
CHEMBL584003 1 4.30
CHEMBL574747 1 4.30

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL208599 HUPRINE X IC50 = 1.1 nM 8.96
CHEMBL140476 HUPRINE Y IC50 = 1.84 nM 8.73
CHEMBL575802 IC50 = 3.95 nM 8.40
CHEMBL575674 IC50 = 5.96 nM 8.22
CHEMBL573095 IC50 = 6.75 nM 8.17
CHEMBL574973 IC50 = 8.69 nM 8.06
CHEMBL583920 IC50 = 9.66 nM 8.02
CHEMBL574974 IC50 = 13.7 nM 7.86
CHEMBL576385 IC50 = 43.3 nM 7.36
CHEMBL575614 IC50 = 664.0 nM 6.18
CHEMBL575613 IC50 = 810.0 nM 6.09
CHEMBL584603 IC50 = 855.0 nM 6.07
CHEMBL576004 IC50 = 2510.0 nM 5.60
CHEMBL575167 IC50 = 2920.0 nM 5.54
CHEMBL574746 IC50 = 4780.0 nM 5.32
CHEMBL573094 IC50 = 5100.0 nM 5.29
CHEMBL583776 IC50 = 6450.0 nM 5.19
CHEMBL576384 IC50 = 7270.0 nM 5.14
CHEMBL574261 IC50 = 7690.0 nM 5.11
CHEMBL575810 IC50 = 8080.0 nM 5.09
CHEMBL574267 IC50 = 11700.0 nM 4.93
CHEMBL575166 IC50 = 14700.0 nM 4.83
CHEMBL572866 IC50 = 19200.0 nM 4.72
CHEMBL572865 IC50 = 22400.0 nM 4.65
CHEMBL576189 IC50 = 27100.0 nM 4.57
CHEMBL574948 IC50 = 50000.0 nM 4.30
CHEMBL572858 IC50 = 50000.0 nM 4.30
CHEMBL584003 IC50 = 50000.0 nM 4.30
CHEMBL574747 IC50 = 50000.0 nM 4.30