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Assay Detail

CHEMBL636701

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Binding
Compound was evaluated for the inhibition of acetylcholinesterase of bovine erythrocytes
25
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Acetylcholinesterase (CHEMBL4768)
Type SINGLE PROTEIN
Organism Bos taurus

Publication

New tacrine-huperzine A hybrids (huprines): highly potent tight-binding acetylcholinesterase inhibitors of interest for the treatment of Alzheimer's disease.
Camps P, El Achab R, Morral J, Muñoz-Torrero D, Badia A, Baños JE, Vivas NM, Barril X, Orozco M, Luque FJ.
J Med Chem (2000) 43 : 4657 -4666
PubMed 11101357 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 25 7.75 8.94

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL140476 HUPRINE Y 3 8.94
CHEMBL208599 HUPRINE X 3 8.89
CHEMBL143290 1 8.61
CHEMBL335355 1 8.58
CHEMBL143094 1 8.45
CHEMBL341658 3 8.17
CHEMBL4524111 1 8.07
CHEMBL322343 1 7.92
CHEMBL109870 1 7.91
CHEMBL139819 1 7.79
CHEMBL322106 1 7.53
CHEMBL109869 1 7.50
CHEMBL325338 1 7.42
CHEMBL357207 1 7.40
CHEMBL142491 1 7.33
CHEMBL322281 1 7.19
CHEMBL395280 HUPERZINE A 2.0 1 7.13
CHEMBL95 TACRINE 4.0 1 6.89
CHEMBL142816 1 6.59

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL140476 HUPRINE Y IC50 = 1.15 nM 8.94
CHEMBL208599 HUPRINE X IC50 = 1.3 nM 8.89
CHEMBL143290 IC50 = 2.43 nM 8.61
CHEMBL335355 IC50 = 2.62 nM 8.58
CHEMBL208599 HUPRINE X IC50 = 2.77 nM 8.56
CHEMBL143094 IC50 = 3.59 nM 8.45
CHEMBL140476 HUPRINE Y IC50 = 4.23 nM 8.37
CHEMBL341658 IC50 = 6.73 nM 8.17
CHEMBL341658 IC50 = 7.4 nM 8.13
CHEMBL4524111 IC50 = 8.5 nM 8.07
CHEMBL322343 IC50 = 12.0 nM 7.92
CHEMBL109870 IC50 = 12.4 nM 7.91
CHEMBL139819 IC50 = 16.2 nM 7.79
CHEMBL322106 IC50 = 29.8 nM 7.53
CHEMBL109869 IC50 = 31.4 nM 7.50
CHEMBL325338 IC50 = 38.5 nM 7.42
CHEMBL357207 IC50 = 39.6 nM 7.40
CHEMBL142491 IC50 = 46.4 nM 7.33
CHEMBL322281 IC50 = 65.0 nM 7.19
CHEMBL140476 HUPRINE Y IC50 = 65.0 nM 7.19
CHEMBL395280 HUPERZINE A IC50 = 74.0 nM 7.13
CHEMBL95 TACRINE IC50 = 130.0 nM 6.89
CHEMBL341658 IC50 = 139.0 nM 6.86
CHEMBL142816 IC50 = 257.0 nM 6.59
CHEMBL208599 HUPRINE X IC50 = 402.0 nM 6.40