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Compound Detail

CHEMBL3945872

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COc1cc(/C=C/C(=O)Nc2cccc(CN(C)Cc3ccccc3)c2)ccc1O

Basic Information

ChEMBL ID CHEMBL3945872
Phase Preclinical
Structure Type MOL
InChI Key OSLSNUMCXBJEGP-WYMLVPIESA-N
4
Targets
4
Activities
1
Assay Types
0
PK Parameters
8
Publications
0
Known Names

Molecular Properties

402.5
MW (Da)
4.68
ALogP
4
HBA
2
HBD
61.8
PSA (Ų)
0.54
QED
0
Ro5 Violations
8
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C25H26N2O3
MW 402.49
Aromatic Rings 3
Heavy Atoms 30
NP-Likeness -0.70

Activity Summary

IC50 4 meas. best 5.35

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Amine oxidase [flavin-containing] A
CHEMBL1951
IC50 5.35 5.35 4500.0 1
Cholinesterase
CHEMBL1914
IC50 5.23 5.23 5890.0 1
Acetylcholinesterase
CHEMBL220
IC50 5.22 5.22 5990.0 1
Amine oxidase [flavin-containing] B
CHEMBL2039
IC50 5.11 5.11 7700.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
27267007 10.1016/j.ejmech.2016.05.055 Cholinesterase 1
27267007 10.1016/j.ejmech.2016.05.055 Acetylcholinesterase 1
27267007 10.1016/j.ejmech.2016.05.055 Amine oxidase [flavin-containing] A 1
27267007 10.1016/j.ejmech.2016.05.055 Amine oxidase [flavin-containing] B 1
27267007 10.1016/j.ejmech.2016.05.055 No relevant target 1
27267007 10.1016/j.ejmech.2016.05.055 Beta-secretase 1 1
27267007 10.1016/j.ejmech.2016.05.055 SH-SY5Y 1
27267007 10.1016/j.ejmech.2016.05.055 NON-PROTEIN TARGET 1

Data from ChEMBL 36 via Core Engine