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Compound Detail

CHEMBL257126

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COc1cc(/C=C/C(=O)NCCCCCNc2c3c(nc4ccccc24)CCCC3)ccc1O

Basic Information

ChEMBL ID CHEMBL257126
Phase Preclinical
Structure Type MOL
InChI Key AULWYSXUAMRNQI-JQIJEIRASA-N
2
Targets
3
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

459.6
MW (Da)
5.24
ALogP
5
HBA
3
HBD
83.5
PSA (Ų)
0.29
QED
1
Ro5 Violations
10
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C28H33N3O3
MW 459.59
Aromatic Rings 3
Heavy Atoms 34
NP-Likeness -0.25

Activity Summary

IC50 3 meas. best 8.36

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Acetylcholinesterase
CHEMBL4078
IC50 8.36 8.36 4.4 2
Butyrylcholinesterase
CHEMBL5077
IC50 8.17 8.17 6.7 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
18406135 10.1016/j.bmcl.2008.03.073 Acetylcholinesterase 1
18406135 10.1016/j.bmcl.2008.03.073 Butyrylcholinesterase 1
18406135 10.1016/j.bmcl.2008.03.073 NON-PROTEIN TARGET 1
22472693 10.1016/j.bmcl.2012.03.046 Acetylcholinesterase 1
22472693 10.1016/j.bmcl.2012.03.046 No relevant target 1

Data from ChEMBL 36 via Core Engine