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Compound Detail

CHEMBL5557952

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O=C1NCCCc2c1c1ccccc1n2CCCCN1CCN(CCc2ccccc2)CC1

Basic Information

ChEMBL ID CHEMBL5557952
Phase Preclinical
Structure Type MOL
InChI Key PJBVQCTVURXJBM-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

444.6
MW (Da)
3.96
ALogP
4
HBA
1
HBD
40.5
PSA (Ų)
0.53
QED
0
Ro5 Violations
8
Rot. Bonds

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C28H36N4O
MW 444.62
Aromatic Rings 3
Heavy Atoms 33
NP-Likeness -0.63

Activity Summary

IC50 1 meas. best 6.28

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Cholinesterase
CHEMBL5763
IC50 6.28 6.28 528.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Cholinesterase IC50 = 528.0 nM 6.28 Inhibition of equine serum BuChE using butyrylthiocholine iodide as substrate pr... 38579622

Literature References

PubMed DOI Target Context # Activities
38579622 10.1016/j.ejmech.2024.116353 Cholinesterase 1
38579622 10.1016/j.ejmech.2024.116353 Acetylcholinesterase 1
38579622 10.1016/j.ejmech.2024.116353 Amyloid-beta precursor protein 1

Data from ChEMBL 36 via Core Engine