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Compound Detail

CHEMBL2171308

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CCCOc1ccc(/C=C/C(=O)NCCCNc2c3c(nc4ccccc24)CCCC3)cc1OC

Basic Information

ChEMBL ID CHEMBL2171308
Phase Preclinical
Structure Type MOL
InChI Key MPXQSLWIVILKJD-JQIJEIRASA-N
2
Targets
3
Activities
2
Assay Types
0
PK Parameters
7
Publications
0
Known Names

Molecular Properties

473.6
MW (Da)
5.54
ALogP
5
HBA
2
HBD
72.5
PSA (Ų)
0.28
QED
1
Ro5 Violations
11
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C29H35N3O3
MW 473.62
Aromatic Rings 3
Heavy Atoms 35
NP-Likeness -0.62

Activity Summary

IC50 2 meas. best 7.39
EC50 1 meas.

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Cholinesterase
CHEMBL5763
IC50 7.39 7.39 40.3 1
Acetylcholinesterase
CHEMBL4078
IC50 7.16 7.16 69.8 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
22512543 10.1021/jm300106z Mus musculus 8
22512543 10.1021/jm300106z Acetylcholinesterase 1
22512543 10.1021/jm300106z Rattus norvegicus 1
22512543 10.1021/jm300106z Aorta 1
22512543 10.1021/jm300106z No relevant target 1
22512543 10.1021/jm300106z Unchecked 1
22512543 10.1021/jm300106z Cholinesterase 1

Data from ChEMBL 36 via Core Engine