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Compound Detail

CHEMBL3323040

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O=c1c2cc(OCCCN3CCc4ccccc4C3)ccc2nc2n1Cc1ccccc1-2

Basic Information

ChEMBL ID CHEMBL3323040
Phase Preclinical
Structure Type MOL
InChI Key VKOZVVGTANTLFS-UHFFFAOYSA-N
2
Targets
4
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

423.5
MW (Da)
4.25
ALogP
5
HBA
0
HBD
47.4
PSA (Ų)
0.40
QED
0
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C27H25N3O2
MW 423.52
Aromatic Rings 4
Heavy Atoms 32
NP-Likeness -0.87

Activity Summary

IC50 4 meas. best 6.64

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Acetylcholinesterase
CHEMBL4078
IC50 6.64 6.64 227.0 2
Cholinesterase
CHEMBL5763
IC50 5.76 5.76 1725.8 2

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Acetylcholinesterase IC50 = 227.0 nM 6.64 Inhibition of electric eel AChE 25047936
Acetylcholinesterase IC50 = 226.99 nM 6.64 Inhibition of electric eel AChE 25047936
Cholinesterase IC50 = 1730.0 nM 5.76 Inhibition of equine serum BChE 25047936
Cholinesterase IC50 = 1725.84 nM 5.76 Inhibition of equine serum BChE 25047936

Literature References

PubMed DOI Target Context # Activities
25047936 10.1016/j.bmc.2014.06.045 Acetylcholinesterase 2
25047936 10.1016/j.bmc.2014.06.045 Cholinesterase 2
25047936 10.1016/j.bmc.2014.06.045 Unchecked 1

Data from ChEMBL 36 via Core Engine