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Compound Detail

CHEMBL524046

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O=C(NCc1ccccc1)O[C@H]1CO[C@H]2[C@@H]1OC[C@H]2O

Basic Information

ChEMBL ID CHEMBL524046
Phase Preclinical
Structure Type MOL
InChI Key LYJZFQNPWOVWIJ-YVECIDJPSA-N
1
Targets
2
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

279.3
MW (Da)
0.44
ALogP
5
HBA
2
HBD
77.0
PSA (Ų)
0.84
QED
0
Ro5 Violations
3
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C14H17NO5
MW 279.29
Aromatic Rings 1
Heavy Atoms 20
NP-Likeness 0.20

Activity Summary

IC50 2 meas. best 5.43

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Cholinesterase
CHEMBL1914
IC50 5.43 5.43 3700.0 2

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Cholinesterase IC50 = 3700.0 nM 5.43 Inhibition of human plasma BuchE by Ellman's method 18817366
Cholinesterase IC50 = 3700.0 nM 5.43 Inhibition of BuChE in human liver microsomes 20067290

Literature References

PubMed DOI Target Context # Activities
18817366 10.1021/jm800564y Cholinesterase 2
20067290 10.1021/jm9014845 Cholinesterase 2
18817366 10.1021/jm800564y Acetylcholinesterase 1
18817366 10.1021/jm800564y Unchecked 1

Data from ChEMBL 36 via Core Engine