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Assay Detail

CHEMBL900177

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Binding
Inhibition of human Acetylcholinesterase
10
Total Activities
9
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

First gallamine-tacrine hybrid: design and characterization at cholinesterases and the M2 muscarinic receptor.
Elsinghorst PW, Cieslik JS, Mohr K, Tränkle C, Gütschow M.
J Med Chem (2007) 50 : 5685 -5695
PubMed 17944454 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 10 7.63 8.26

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL540131 1 8.26
CHEMBL555247 1 8.18
CHEMBL540132 1 8.17
CHEMBL1203985 1 8.12
CHEMBL1203986 1 7.80
CHEMBL1203984 2 7.63
CHEMBL1677 TACRINE HYDROCHLORIDE 4.0 1 6.87
CHEMBL95 TACRINE 4.0 1 6.03
CHEMBL360055 GALLAMINE 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL540131 IC50 = 5.44 nM 8.26
CHEMBL555247 IC50 = 6.54 nM 8.18
CHEMBL540132 IC50 = 6.75 nM 8.17
CHEMBL1203985 IC50 = 7.61 nM 8.12
CHEMBL1203986 IC50 = 15.8 nM 7.80
CHEMBL1203984 IC50 = 23.2 nM 7.63
CHEMBL1677 TACRINE HYDROCHLORIDE IC50 = 136.0 nM 6.87
CHEMBL95 TACRINE IC50 = 926.0 nM 6.03
CHEMBL360055 GALLAMINE IC50 = 2110000.0 nM -
CHEMBL1203984 IC50 = 1480000.0 nM -