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Compound Detail

CHEMBL225077

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O=C(CCOc1c[nH]c2ccccc12)NCCCCCCCNc1c2c(nc3cc(Cl)ccc13)CCCC2

Basic Information

ChEMBL ID CHEMBL225077
Phase Preclinical
Structure Type MOL
InChI Key QAGXISPTVQTZFB-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

533.1
MW (Da)
7.20
ALogP
4
HBA
3
HBD
79.0
PSA (Ų)
0.16
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 C31H37ClN4O2
MW 533.12
Aromatic Rings 4
Heavy Atoms 38
NP-Likeness -0.92

Activity Summary

IC50 2 meas. best 8.52

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Acetylcholinesterase
CHEMBL4768
IC50 8.52 8.52 3.0 1
Cholinesterase
CHEMBL1914
IC50 7.23 7.23 59.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Acetylcholinesterase IC50 = 3.0 nM 8.52 Inhibition of AchE in bovine erythrocytes 16279781
Cholinesterase IC50 = 59.0 nM 7.23 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

Data from ChEMBL 36 via Core Engine