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Assay Detail

CHEMBL914527

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

Binding
Inhibition of human serum BChE
25
Total Activities
25
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

Cholinesterase (CHEMBL1914)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Design, synthesis, and biological evaluation of dual binding site acetylcholinesterase inhibitors: new disease-modifying agents for Alzheimer's disease.
Muñoz-Ruiz P, Rubio L, García-Palomero E, Dorronsoro I, del Monte-Millán M, Valenzuela R, Usán P, de Austria C, Bartolini M, Andrisano V, Bidon-Chanal A, Orozco M, Luque FJ, Medina M, Martínez A.
J Med Chem (2005) 48 : 7223 -7233
PubMed 16279781 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 25 8.02 10.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL224336 1 10.52
CHEMBL225198 1 10.00
CHEMBL224158 1 9.00
CHEMBL224998 1 8.77
CHEMBL225326 1 8.77
CHEMBL225567 1 8.54
CHEMBL225021 1 8.49
CHEMBL427082 1 8.25
CHEMBL389192 1 8.24
CHEMBL223549 1 8.02
CHEMBL388575 1 8.02
CHEMBL223443 1 7.93
CHEMBL223170 1 7.93
CHEMBL224335 1 7.80
CHEMBL388627 1 7.72
CHEMBL388551 1 7.67
CHEMBL223714 1 7.65
CHEMBL95 TACRINE 4.0 1 7.62
CHEMBL224051 1 7.27
CHEMBL225077 1 7.23
CHEMBL225327 1 7.22
CHEMBL224202 1 7.11
CHEMBL388615 1 7.10
CHEMBL223277 1 6.87
CHEMBL426015 1 6.69

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL224336 IC50 = 0.03 nM 10.52
CHEMBL225198 IC50 = 0.1 nM 10.00
CHEMBL224158 IC50 = 1.0 nM 9.00
CHEMBL224998 IC50 = 1.7 nM 8.77
CHEMBL225326 IC50 = 1.7 nM 8.77
CHEMBL225567 IC50 = 2.9 nM 8.54
CHEMBL225021 IC50 = 3.2 nM 8.49
CHEMBL427082 IC50 = 5.6 nM 8.25
CHEMBL389192 IC50 = 5.7 nM 8.24
CHEMBL223549 IC50 = 9.6 nM 8.02
CHEMBL388575 IC50 = 9.5 nM 8.02
CHEMBL223443 IC50 = 11.7 nM 7.93
CHEMBL223170 IC50 = 11.7 nM 7.93
CHEMBL224335 IC50 = 16.0 nM 7.80
CHEMBL388627 IC50 = 19.0 nM 7.72
CHEMBL388551 IC50 = 21.4 nM 7.67
CHEMBL223714 IC50 = 22.4 nM 7.65
CHEMBL95 TACRINE IC50 = 24.0 nM 7.62
CHEMBL224051 IC50 = 54.0 nM 7.27
CHEMBL225077 IC50 = 59.0 nM 7.23
CHEMBL225327 IC50 = 60.0 nM 7.22
CHEMBL224202 IC50 = 77.0 nM 7.11
CHEMBL388615 IC50 = 79.0 nM 7.10
CHEMBL223277 IC50 = 136.0 nM 6.87
CHEMBL426015 IC50 = 206.0 nM 6.69