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Compound Detail

CHEMBL451304

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O=C(NCCCCCNc1c2c(nc3ccccc13)CCCC2)[C@@H]1CCCN1CCNc1c2c(nc3ccccc13)CCCC2

Basic Information

ChEMBL ID CHEMBL451304
Phase Preclinical
Structure Type MOL
InChI Key SQVWHOMDKZAUNJ-DHUJRADRSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

604.8
MW (Da)
6.82
ALogP
6
HBA
3
HBD
82.2
PSA (Ų)
0.15
QED
2
Ro5 Violations
12
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C38H48N6O
MW 604.84
Aromatic Rings 4
Heavy Atoms 45
NP-Likeness -0.74

Activity Summary

Ki 2 meas. best 8.75

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Cholinesterase
CHEMBL1914
Ki 8.75 8.75 1.8 1
Acetylcholinesterase
CHEMBL220
Ki 8.17 8.17 6.8 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Cholinesterase Ki = 1.77 nM 8.75 Inhibition of human recombinant BChE 18786825
Acetylcholinesterase Ki = 6.75 nM 8.17 Inhibition of human recombinant AChE 18786825

Literature References

PubMed DOI Target Context # Activities
18786825 10.1016/j.bmcl.2008.08.076 Acetylcholinesterase 1
18786825 10.1016/j.bmcl.2008.08.076 Cholinesterase 1

Data from ChEMBL 36 via Core Engine