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Compound Detail

CHEMBL4454706

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COc1c(C(=O)CCC2CCN(CC3CCCCC3)CC2)ccc2[nH]ccc12

Basic Information

ChEMBL ID CHEMBL4454706
Phase Preclinical
Structure Type MOL
InChI Key DZXRSFAKIAKMMD-UHFFFAOYSA-N
2
Targets
2
Activities
2
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

382.6
MW (Da)
5.43
ALogP
3
HBA
1
HBD
45.3
PSA (Ų)
0.65
QED
1
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C24H34N2O2
MW 382.55
Aromatic Rings 2
Heavy Atoms 28
NP-Likeness -0.25

Activity Summary

IC50 1 meas. best 7.4
Ki 1 meas. best 7.29

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Acetylcholinesterase
CHEMBL220
IC50 7.4 7.4 40.0 1
5-hydroxytryptamine receptor 4
CHEMBL1875
Ki 7.29 7.29 51.0 1

Activity Data Samples

Top measurements by pChEMBL value

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