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Compound Detail

CHEMBL389192

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O=C(CCc1c[nH]c2ccccc12)NCCCCCCCCNc1c2c(nc3cc(Cl)ccc13)CCCC2

Basic Information

ChEMBL ID CHEMBL389192
Phase Preclinical
Structure Type MOL
InChI Key CANCFHBYJYSQSR-UHFFFAOYSA-N
3
Targets
3
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

531.1
MW (Da)
7.75
ALogP
3
HBA
3
HBD
69.8
PSA (Ų)
0.15
QED
2
Ro5 Violations
13
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C32H39ClN4O
MW 531.14
Aromatic Rings 4
Heavy Atoms 38
NP-Likeness -0.79

Activity Summary

IC50 3 meas. best 9.3

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Acetylcholinesterase
CHEMBL220
IC50 9.3 9.3 0.5 1
Acetylcholinesterase
CHEMBL4768
IC50 9.3 9.3 0.5 1
Cholinesterase
CHEMBL1914
IC50 8.24 8.24 5.7 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Acetylcholinesterase IC50 = 0.5 nM 9.3 Inhibition of AchE in bovine erythrocytes 16279781
Acetylcholinesterase IC50 = 0.5 nM 9.3 Inhibition of AChE 20053484
Cholinesterase IC50 = 5.7 nM 8.24 Inhibition of human serum BChE 16279781

Literature References

PubMed DOI Target Context # Activities
16279781 10.1021/jm0503289 Acetylcholinesterase 1
16279781 10.1021/jm0503289 Cholinesterase 1
16279781 10.1021/jm0503289 Unchecked 1
16279781 10.1021/jm0503289 SH-SY5Y 1
20053484 10.1016/j.ejmech.2009.12.038 Acetylcholinesterase 1

Data from ChEMBL 36 via Core Engine