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Compound Detail

CHEMBL4583738

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COc1c(C(=O)CCC2CCN(CC3CCCCC3)CC2)cc(Cl)c2c1ccn2S(=O)(=O)c1ccccc1.O=C(O)/C=C/C(=O)O

Basic Information

ChEMBL ID CHEMBL4583738
Phase Preclinical
Structure Type MOL
InChI Key NXHWTBJCXGLCSJ-WLHGVMLRSA-N
Parent Compound CHEMBL4596398
Active Moiety CHEMBL4596398
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

557.2
MW (Da)
6.80
ALogP
6
HBA
0
HBD
68.6
PSA (Ų)
0.27
QED
2
Ro5 Violations
9
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C34H41ClN2O8S
MW 673.23
Aromatic Rings 3
Heavy Atoms 38
NP-Likeness -0.80

Activity Summary

IC50 1 meas. best 6.25

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Acetylcholinesterase
CHEMBL220
IC50 6.25 6.25 559.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Acetylcholinesterase IC50 = 559.0 nM 6.25 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