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Compound Detail

CHEMBL3949439

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CN(Cc1ccccc1)Cc1ccc(NC(=O)/C=C/c2cccc(O)c2)cc1

Basic Information

ChEMBL ID CHEMBL3949439
Phase Preclinical
Structure Type MOL
InChI Key TXZOQRXGVMDJCJ-NTCAYCPXSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
7
Publications
0
Known Names

Molecular Properties

372.5
MW (Da)
4.68
ALogP
3
HBA
2
HBD
52.6
PSA (Ų)
0.59
QED
0
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C24H24N2O2
MW 372.47
Aromatic Rings 3
Heavy Atoms 28
NP-Likeness -0.72

Activity Summary

IC50 1 meas. best 5.46

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Acetylcholinesterase
CHEMBL220
IC50 5.46 5.46 3490.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Acetylcholinesterase IC50 = 3490.0 nM 5.46 Inhibition of human recombinant AChE using acetylthiocholine iodide as substrate... 27267007

Literature References

PubMed DOI Target Context # Activities
27267007 10.1016/j.ejmech.2016.05.055 Acetylcholinesterase 1
27267007 10.1016/j.ejmech.2016.05.055 Cholinesterase 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 SH-SY5Y 1
27267007 10.1016/j.ejmech.2016.05.055 NON-PROTEIN TARGET 1

Data from ChEMBL 36 via Core Engine