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Compound Detail

CHEMBL4091851

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COc1ccc(CCNc2c3c(nc4cc(Cl)ccc24)CCCC3)cc1OC

Basic Information

ChEMBL ID CHEMBL4091851
Phase Preclinical
Structure Type MOL
InChI Key RUXUXXGSLJSRTL-UHFFFAOYSA-N
3
Targets
3
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

396.9
MW (Da)
5.44
ALogP
4
HBA
1
HBD
43.4
PSA (Ų)
0.60
QED
1
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C23H25ClN2O2
MW 396.92
Aromatic Rings 3
Heavy Atoms 28
NP-Likeness -0.76

Activity Summary

IC50 3 meas. best 6.22

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Acetylcholinesterase
CHEMBL220
IC50 6.22 6.22 600.0 1
Cholinesterase
CHEMBL1914
IC50 5.72 5.72 1900.0 1
Cytochrome P450 1A2
CHEMBL3356
IC50 4.65 4.65 22300.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
28400237 10.1016/j.bmcl.2017.04.006 Cytochrome P450 1A2 2
28400237 10.1016/j.bmcl.2017.04.006 Acetylcholinesterase 1
28400237 10.1016/j.bmcl.2017.04.006 Cholinesterase 1

Data from ChEMBL 36 via Core Engine