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Compound Detail

CHEMBL255230

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C#CCN[C@@H]1CCc2cc(Cl)c(OC(=O)N(C)CCC)cc21

Basic Information

ChEMBL ID CHEMBL255230
Phase Preclinical
Structure Type MOL
InChI Key WOQRKVSECROGOP-OAHLLOKOSA-N
2
Targets
3
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

320.8
MW (Da)
3.39
ALogP
3
HBA
1
HBD
41.6
PSA (Ų)
0.85
QED
0
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C17H21ClN2O2
MW 320.82
Aromatic Rings 1
Heavy Atoms 22
NP-Likeness -0.87

Activity Summary

IC50 3 meas. best 4.5

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Amine oxidase [flavin-containing] B
CHEMBL2039
IC50 4.5 4.5 32000.0 1
Acetylcholinesterase
CHEMBL220
IC50 4.36 4.36 43900.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Amine oxidase [flavin-containing] B IC50 = 32000.0 nM 4.5 Inhibition of MAOB 18181565
Acetylcholinesterase IC50 = 43900.0 nM 4.36 Inhibition of human AchE 18181565

Literature References

PubMed DOI Target Context # Activities
18181565 10.1021/jm7009364 Acetylcholinesterase 1
18181565 10.1021/jm7009364 Amine oxidase [flavin-containing] A 1
18181565 10.1021/jm7009364 Amine oxidase [flavin-containing] B 1

Data from ChEMBL 36 via Core Engine