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Compound Detail

CHEMBL396247

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COc1cc2cc(-c3ccc(CN(CCO)Cc4ccccc4)cc3)c(=O)oc2cc1OC

Basic Information

ChEMBL ID CHEMBL396247
Phase Preclinical
Structure Type MOL
InChI Key VFAABMDLNHZKGL-UHFFFAOYSA-N
2
Targets
3
Activities
2
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

445.5
MW (Da)
4.47
ALogP
6
HBA
1
HBD
72.1
PSA (Ų)
0.38
QED
0
Ro5 Violations
9
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C27H27NO5
MW 445.52
Aromatic Rings 4
Heavy Atoms 33
NP-Likeness -0.38

Activity Summary

IC50 2 meas. best 7.31
Ki 1 meas. best 7.98

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Acetylcholinesterase
CHEMBL220
Ki 7.98 7.98 10.5 1
Acetylcholinesterase
CHEMBL220
IC50 7.31 7.31 49.3 1
Cholinesterase
CHEMBL1914
IC50 4.46 4.46 35100.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
17655212 10.1021/jm070100g Acetylcholinesterase 2
17655212 10.1021/jm070100g Cholinesterase 1
27494166 10.1016/j.ejmech.2016.07.057 Acetylcholinesterase 1

Data from ChEMBL 36 via Core Engine