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Assay Detail

CHEMBL862409

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Binding
Inhibition of human AChE
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Acetylcholinesterase (CHEMBL220)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of huperzine A-tacrine hybrids as potent inhibitors of human cholinesterases targeting their midgorge recognition sites.
Gemma S, Gabellieri E, Huleatt P, Fattorusso C, Borriello M, Catalanotti B, Butini S, De Angelis M, Novellino E, Nacci V, Belinskaya T, Saxena A, Campiani G.
J Med Chem (2006) 49 : 3421 -3425
PubMed 16722663 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 6 8.09 10.59

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL208599 HUPRINE X 1 10.59
CHEMBL210453 1 8.19
CHEMBL382423 1 7.80
CHEMBL208092 1 7.78
CHEMBL395280 HUPERZINE A 2.0 1 7.33
CHEMBL95 TACRINE 4.0 1 6.86

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL208599 HUPRINE X Ki = 0.026 nM 10.59
CHEMBL210453 Ki = 6.4 nM 8.19
CHEMBL382423 Ki = 15.7 nM 7.80
CHEMBL208092 Ki = 16.5 nM 7.78
CHEMBL395280 HUPERZINE A Ki = 47.0 nM 7.33
CHEMBL95 TACRINE Ki = 137.0 nM 6.86