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Assay Detail

CHEMBL644628

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

Binding
In vitro inhibition of human erythrocyte acetylcholinesterase.
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Acetylcholinesterase (CHEMBL220)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Methyl analogues of the experimental Alzheimer drug phenserine: synthesis and structure/activity relationships for acetyl- and butyrylcholinesterase inhibitory action.
Yu Q, Holloway HW, Flippen-Anderson JL, Hoffman B, Brossi A, Greig NH.
J Med Chem (2001) 44 : 4062 -4071
PubMed 11708910 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 21 7.00 8.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL340391 ETHYLPHENSERINE 1 8.00
CHEMBL130458 TOLSERINE 1 8.00
CHEMBL335220 1 7.85
CHEMBL130270 1 7.82
CHEMBL74926 PHENSERINE 1 7.66
CHEMBL335962 1 7.64
CHEMBL337675 1 7.58
CHEMBL94 PHYSOSTIGMINE 3.0 1 7.55
CHEMBL131598 1 7.55
CHEMBL130672 1 7.51
CHEMBL131210 1 7.11
CHEMBL130956 1 6.85
CHEMBL308043 1 6.68
CHEMBL132531 1 6.58
CHEMBL131825 1 6.16
CHEMBL129837 4-ISOPROPYLPHENSERINE 1 6.12
CHEMBL340867 1 6.11
CHEMBL130363 1 5.89
CHEMBL335167 1 5.82
CHEMBL132285 1 5.60
CHEMBL134251 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL340391 ETHYLPHENSERINE IC50 = 10.0 nM 8.00
CHEMBL130458 TOLSERINE IC50 = 10.0 nM 8.00
CHEMBL335220 IC50 = 14.0 nM 7.85
CHEMBL130270 IC50 = 15.0 nM 7.82
CHEMBL74926 PHENSERINE IC50 = 22.0 nM 7.66
CHEMBL335962 IC50 = 23.0 nM 7.64
CHEMBL337675 IC50 = 26.0 nM 7.58
CHEMBL94 PHYSOSTIGMINE IC50 = 28.0 nM 7.55
CHEMBL131598 IC50 = 28.0 nM 7.55
CHEMBL130672 IC50 = 31.0 nM 7.51
CHEMBL131210 IC50 = 78.0 nM 7.11
CHEMBL130956 IC50 = 140.0 nM 6.85
CHEMBL308043 IC50 = 210.0 nM 6.68
CHEMBL132531 IC50 = 260.0 nM 6.58
CHEMBL131825 IC50 = 690.0 nM 6.16
CHEMBL129837 4-ISOPROPYLPHENSERINE IC50 = 760.0 nM 6.12
CHEMBL340867 IC50 = 785.0 nM 6.11
CHEMBL130363 IC50 = 1300.0 nM 5.89
CHEMBL335167 IC50 = 1500.0 nM 5.82
CHEMBL132285 IC50 = 2500.0 nM 5.60
CHEMBL134251 IC50 > 10000.0 nM -