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Compound Detail

CHEMBL3322232

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Cl.O=C(NCCCNc1c2c(nc3cc(Cl)ccc13)CCCC2)c1ccc2nc(-c3ccc(Cl)cc3)c3c(c2c1)NCCC3

Basic Information

ChEMBL ID CHEMBL3322232
Phase Preclinical
Structure Type MOL
InChI Key QCCKOXGFAWYVNP-UHFFFAOYSA-N
Parent Compound CHEMBL3545562
Active Moiety CHEMBL3545562
1
Targets
2
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

610.6
MW (Da)
8.23
ALogP
5
HBA
3
HBD
78.9
PSA (Ų)
0.16
QED
2
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C35H34Cl3N5O
MW 647.05
Aromatic Rings 5
Heavy Atoms 43
NP-Likeness -0.91

Activity Summary

IC50 2 meas. best 6.92

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Cholinesterase
CHEMBL1914
IC50 6.92 6.92 120.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Cholinesterase IC50 = 120.0 nM 6.92 Inhibition of human recombinant BChE using butyrylthiocholine iodide as substrat... 25016233

Literature References

PubMed DOI Target Context # Activities
25016233 10.1016/j.ejmech.2014.07.021 Amyloid-beta precursor protein 1
25016233 10.1016/j.ejmech.2014.07.021 Cholinesterase 1
25016233 10.1016/j.ejmech.2014.07.021 Acetylcholinesterase 1
25016233 10.1016/j.ejmech.2014.07.021 Microtubule-associated protein tau 1

Data from ChEMBL 36 via Core Engine