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Assay Detail

CHEMBL895408

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

Binding
Inhibition of human recombinant butyrylcholinesterase
34
Total Activities
34
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

Cholinesterase (CHEMBL1914)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Novel class of quinone-bearing polyamines as multi-target-directed ligands to combat Alzheimer's disease.
Bolognesi ML, Banzi R, Bartolini M, Cavalli A, Tarozzi A, Andrisano V, Minarini A, Rosini M, Tumiatti V, Bergamini C, Fato R, Lenaz G, Hrelia P, Cattaneo A, Recanatini M, Melchiorre C.
J Med Chem (2007) 50 : 4882 -4897
PubMed 17850125 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 34 5.53 7.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL636 RIVASTIGMINE 4.0 1 7.52
CHEMBL95 TACRINE 4.0 1 7.34
CHEMBL243269 1 6.33
CHEMBL230434 1 6.30
CHEMBL394348 1 6.29
CHEMBL218443 1 6.19
CHEMBL242836 1 6.18
CHEMBL243062 1 6.16
CHEMBL243056 1 6.10
CHEMBL243273 1 5.90
CHEMBL243055 1 5.82
CHEMBL394865 1 5.77
CHEMBL243274 1 5.68
CHEMBL396050 1 5.65
CHEMBL242661 1 5.62
CHEMBL244762 1 5.61
CHEMBL390247 1 5.55
CHEMBL243044 1 5.49
CHEMBL276444 1 5.47
CHEMBL230702 1 5.46
CHEMBL242191 1 5.29
CHEMBL502 DONEPEZIL 4.0 1 5.13
CHEMBL243271 1 5.01
CHEMBL557586 CAPROCTAMINE HCL 1 4.94
CHEMBL241974 1 4.92
CHEMBL243272 1 4.89
CHEMBL345124 PROPIDIUM 1 4.88
CHEMBL243270 1 4.78
CHEMBL242190 1 4.73
CHEMBL659 GALANTAMINE 4.0 1 4.68

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL636 RIVASTIGMINE IC50 = 30.1 nM 7.52
CHEMBL95 TACRINE IC50 = 45.8 nM 7.34
CHEMBL243269 IC50 = 462.0 nM 6.33
CHEMBL230434 IC50 = 505.0 nM 6.30
CHEMBL394348 IC50 = 518.0 nM 6.29
CHEMBL218443 IC50 = 645.0 nM 6.19
CHEMBL242836 IC50 = 660.0 nM 6.18
CHEMBL243062 IC50 = 696.0 nM 6.16
CHEMBL243056 IC50 = 800.0 nM 6.10
CHEMBL243273 IC50 = 1250.0 nM 5.90
CHEMBL243055 IC50 = 1520.0 nM 5.82
CHEMBL394865 IC50 = 1690.0 nM 5.77
CHEMBL243274 IC50 = 2080.0 nM 5.68
CHEMBL396050 IC50 = 2250.0 nM 5.65
CHEMBL242661 IC50 = 2390.0 nM 5.62
CHEMBL244762 IC50 = 2470.0 nM 5.61
CHEMBL390247 IC50 = 2790.0 nM 5.55
CHEMBL243044 IC50 = 3230.0 nM 5.49
CHEMBL276444 IC50 = 3410.0 nM 5.47
CHEMBL230702 IC50 = 3460.0 nM 5.46
CHEMBL242191 IC50 = 5110.0 nM 5.29
CHEMBL502 DONEPEZIL IC50 = 7420.0 nM 5.13
CHEMBL243271 IC50 = 9840.0 nM 5.01
CHEMBL557586 CAPROCTAMINE HCL IC50 = 11600.0 nM 4.94
CHEMBL241974 IC50 = 11900.0 nM 4.92
CHEMBL243272 IC50 = 12800.0 nM 4.89
CHEMBL345124 PROPIDIUM IC50 = 13200.0 nM 4.88
CHEMBL243270 IC50 = 16800.0 nM 4.78
CHEMBL242190 IC50 = 18500.0 nM 4.73
CHEMBL659 GALANTAMINE IC50 = 20700.0 nM 4.68
CHEMBL243057 IC50 = 45100.0 nM 4.35
CHEMBL395815 IC50 = 67100.0 nM 4.17
CHEMBL241960 IC50 = 70100.0 nM 4.15
CHEMBL429694 CONGO RED IC50 - -