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Compound Detail

CHEMBL222044

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CCN(CCCCCCNc1ccc(-c2ccc(NCCCCCCN(CC)Cc3ccccc3OC)cc2)cc1)Cc1ccccc1OC

Basic Information

ChEMBL ID CHEMBL222044
Phase Preclinical
Structure Type MOL
InChI Key OXYGPYKFZHTXST-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

679.0
MW (Da)
10.36
ALogP
6
HBA
2
HBD
49.0
PSA (Ų)
0.07
QED
2
Ro5 Violations
25
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C44H62N4O2
MW 679.01
Aromatic Rings 4
Heavy Atoms 50
NP-Likeness -0.58

Activity Summary

IC50 2 meas. best 5.58

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Acetylcholinesterase
CHEMBL220
IC50 5.58 5.58 2630.3 1
Cholinesterase
CHEMBL1914
IC50 4.81 4.81 15488.2 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Acetylcholinesterase IC50 = 2630.27 nM 5.58 Inhibition of human recombinant AChE 15588084
Cholinesterase IC50 = 15488.17 nM 4.81 Inhibition of human recombinant BChE 15588084

Literature References

PubMed DOI Target Context # Activities
15588084 10.1021/jm0494366 Acetylcholinesterase 2
15588084 10.1021/jm0494366 Cholinesterase 1
15588084 10.1021/jm0494366 Cholinesterases; ACHE & BCHE 1
15588084 10.1021/jm0494366 Muscarinic acetylcholine receptor M2 1

Data from ChEMBL 36 via Core Engine