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Compound Detail

CHEMBL131386

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CN(CCCNc1c2c(nc3ccccc13)CCCC2)CCCNc1c2c(nc3cc(Cl)cc(Cl)c13)CCCC2

Basic Information

ChEMBL ID CHEMBL131386
Phase Preclinical
Structure Type MOL
InChI Key UBICYFGZMQMCLZ-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

576.6
MW (Da)
8.08
ALogP
5
HBA
2
HBD
53.1
PSA (Ų)
0.19
QED
2
Ro5 Violations
10
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C33H39Cl2N5
MW 576.62
Aromatic Rings 4
Heavy Atoms 40
NP-Likeness -0.83

Activity Summary

Ki 2 meas. best 8.43

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Acetylcholinesterase
CHEMBL4768
Ki 8.43 8.43 3.7 1
Butyrylcholinesterase
CHEMBL5077
Ki 7.96 7.96 11.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Acetylcholinesterase Ki = 3.7 nM 8.43 Inhibition of fetal Bovine serum AChE 12502352
Butyrylcholinesterase Ki = 11.0 nM 7.96 Inhibition of Equine Butyrylcholinesterase 12502352

Literature References

PubMed DOI Target Context # Activities
12502352 10.1021/jm0255668 Acetylcholinesterase 1
12502352 10.1021/jm0255668 Butyrylcholinesterase 1

Data from ChEMBL 36 via Core Engine