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Compound Detail

CHEMBL4537101

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COc1c(C(=O)CCC2CCN(CC3CCCCC3)CC2)cc(Cl)c2[nH]ccc12

Basic Information

ChEMBL ID CHEMBL4537101
Phase Preclinical
Structure Type MOL
InChI Key DUUYHLUSDHATNS-UHFFFAOYSA-N
3
Targets
3
Activities
2
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

417.0
MW (Da)
6.09
ALogP
3
HBA
1
HBD
45.3
PSA (Ų)
0.56
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 C24H33ClN2O2
MW 416.99
Aromatic Rings 2
Heavy Atoms 29
NP-Likeness -0.40

Activity Summary

Ki 2 meas. best 8.29
IC50 1 meas. best 7.04

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Sigma non-opioid intracellular receptor 1
CHEMBL287
Ki 8.29 8.29 5.1 1
5-hydroxytryptamine receptor 4
CHEMBL1875
Ki 7.39 7.39 40.9 1
Acetylcholinesterase
CHEMBL220
IC50 7.04 7.04 91.4 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 3
30447434 10.1016/j.ejmech.2018.10.064 Acetylcholinesterase 3
30447434 10.1016/j.ejmech.2018.10.064 Sigma non-opioid intracellular receptor 1 1

Data from ChEMBL 36 via Core Engine