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Compound Detail

CHEMBL4456222

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O=C(/C=C/c1cccc(OCCCCN2CCc3ccccc3C2)c1)c1ccccc1O

Basic Information

ChEMBL ID CHEMBL4456222
Phase Preclinical
Structure Type MOL
InChI Key SXCBXTMLACVLPO-CCEZHUSRSA-N
3
Targets
3
Activities
1
Assay Types
0
PK Parameters
10
Publications
0
Known Names

Molecular Properties

427.5
MW (Da)
5.51
ALogP
4
HBA
1
HBD
49.8
PSA (Ų)
0.28
QED
1
Ro5 Violations
9
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C28H29NO3
MW 427.54
Aromatic Rings 3
Heavy Atoms 32
NP-Likeness -0.49

Activity Summary

IC50 3 meas. best 5.58

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Cholinesterase
CHEMBL5763
IC50 5.58 5.58 2600.0 1
Amine oxidase [flavin-containing] B
CHEMBL2039
IC50 5.28 5.28 5300.0 1
Acetylcholinesterase
CHEMBL4078
IC50 4.79 4.79 16200.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
31310916 10.1016/j.ejmech.2019.07.021 No relevant target 9
31310916 10.1016/j.ejmech.2019.07.021 PC-12 4
31310916 10.1016/j.ejmech.2019.07.021 Cholinesterase 4
31310916 10.1016/j.ejmech.2019.07.021 Unchecked 3
31310916 10.1016/j.ejmech.2019.07.021 ADMET 2
31310916 10.1016/j.ejmech.2019.07.021 Mus musculus 2
31310916 10.1016/j.ejmech.2019.07.021 Acetylcholinesterase 1
31310916 10.1016/j.ejmech.2019.07.021 Amine oxidase [flavin-containing] A 1
31310916 10.1016/j.ejmech.2019.07.021 Amine oxidase [flavin-containing] B 1
31310916 10.1016/j.ejmech.2019.07.021 Amyloid-beta precursor protein 1

Data from ChEMBL 36 via Core Engine