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Assay Detail

CHEMBL894085

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

Binding
Inhibition of human recombinant AChE
28
Total Activities
28
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

Extensive SAR and computational studies of 3-{4-[(benzylmethylamino)methyl]phenyl}-6,7-dimethoxy-2H-2-chromenone (AP2238) derivatives.
Piazzi L, Cavalli A, Belluti F, Bisi A, Gobbi S, Rizzo S, Bartolini M, Andrisano V, Recanatini M, Rampa A.
J Med Chem (2007) 50 : 4250 -4254
PubMed 17655212 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 28 6.19 7.98

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL396199 1 7.98
CHEMBL244416 1 7.74
CHEMBL75121 1 7.35
CHEMBL396247 1 7.31
CHEMBL389825 1 7.21
CHEMBL427865 1 6.91
CHEMBL244619 1 6.83
CHEMBL243532 1 6.79
CHEMBL243310 1 6.70
CHEMBL244624 1 6.55
CHEMBL413794 1 6.52
CHEMBL245046 1 6.51
CHEMBL243130 1 6.44
CHEMBL242905 1 6.43
CHEMBL245047 1 6.15
CHEMBL413793 1 6.05
CHEMBL265416 1 6.01
CHEMBL244838 1 5.91
CHEMBL388714 1 5.80
CHEMBL245054 1 5.70
CHEMBL244415 1 5.65
CHEMBL245055 1 5.64
CHEMBL243311 1 5.64
CHEMBL241827 1 5.51
CHEMBL241828 1 4.74
CHEMBL242906 1 4.61
CHEMBL244837 1 4.52
CHEMBL241830 1 4.09

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL396199 IC50 = 10.5 nM 7.98
CHEMBL244416 IC50 = 18.3 nM 7.74
CHEMBL75121 IC50 = 44.5 nM 7.35
CHEMBL396247 IC50 = 49.3 nM 7.31
CHEMBL389825 IC50 = 62.1 nM 7.21
CHEMBL427865 IC50 = 122.0 nM 6.91
CHEMBL244619 IC50 = 148.0 nM 6.83
CHEMBL243532 IC50 = 163.0 nM 6.79
CHEMBL243310 IC50 = 202.0 nM 6.70
CHEMBL244624 IC50 = 281.0 nM 6.55
CHEMBL413794 IC50 = 303.0 nM 6.52
CHEMBL245046 IC50 = 310.0 nM 6.51
CHEMBL243130 IC50 = 366.0 nM 6.44
CHEMBL242905 IC50 = 368.0 nM 6.43
CHEMBL245047 IC50 = 714.0 nM 6.15
CHEMBL413793 IC50 = 892.0 nM 6.05
CHEMBL265416 IC50 = 987.0 nM 6.01
CHEMBL244838 IC50 = 1230.0 nM 5.91
CHEMBL388714 IC50 = 1590.0 nM 5.80
CHEMBL245054 IC50 = 2020.0 nM 5.70
CHEMBL244415 IC50 = 2260.0 nM 5.65
CHEMBL245055 IC50 = 2270.0 nM 5.64
CHEMBL243311 IC50 = 2290.0 nM 5.64
CHEMBL241827 IC50 = 3100.0 nM 5.51
CHEMBL241828 IC50 = 18100.0 nM 4.74
CHEMBL242906 IC50 = 24600.0 nM 4.61
CHEMBL244837 IC50 = 30300.0 nM 4.52
CHEMBL241830 IC50 = 80500.0 nM 4.09