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Compound Detail

CHEMBL4578844

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O=C(CCC1CCN(CC2CCCCC2)CC1)c1ccc2c(ccn2Cc2ccccc2)c1

Basic Information

ChEMBL ID CHEMBL4578844
Phase Preclinical
Structure Type MOL
InChI Key ICALDSOVJLIENB-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

442.6
MW (Da)
6.94
ALogP
3
HBA
0
HBD
25.2
PSA (Ų)
0.35
QED
1
Ro5 Violations
8
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C30H38N2O
MW 442.65
Aromatic Rings 3
Heavy Atoms 33
NP-Likeness -0.95

Activity Summary

IC50 1 meas. best 6.88

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Acetylcholinesterase
CHEMBL220
IC50 6.88 6.88 133.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Acetylcholinesterase IC50 = 133.0 nM 6.88 Inhibition of human erythrocytes AChE using acetylthiocholine iodide as substrat... 30447434

Literature References

PubMed DOI Target Context # Activities
30447434 10.1016/j.ejmech.2018.10.064 5-hydroxytryptamine receptor 4 2
30447434 10.1016/j.ejmech.2018.10.064 Acetylcholinesterase 2
30447434 10.1016/j.ejmech.2018.10.064 Sigma non-opioid intracellular receptor 1 1

Data from ChEMBL 36 via Core Engine