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Compound Detail

CHEMBL2022047

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c1ccc2oc(-c3ccc(OCCCNc4c5c(nc6ccccc46)CCCC5)cc3)nc2c1

Basic Information

ChEMBL ID CHEMBL2022047
Phase Preclinical
Structure Type MOL
InChI Key NKOMTERCWGMQCG-UHFFFAOYSA-N
2
Targets
4
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

449.6
MW (Da)
6.80
ALogP
5
HBA
1
HBD
60.2
PSA (Ų)
0.28
QED
1
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C29H27N3O2
MW 449.55
Aromatic Rings 5
Heavy Atoms 34
NP-Likeness -1.06

Activity Summary

IC50 4 meas. best 6.45

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Cholinesterase
CHEMBL5763
IC50 6.45 6.45 352.0 1
Acetylcholinesterase
CHEMBL4078
IC50 6.32 6.32 475.0 2

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
22472046 10.1016/j.bmc.2012.02.059 Unchecked 2
30503937 10.1016/j.ejmech.2018.11.049 Acetylcholinesterase 2
22472046 10.1016/j.bmc.2012.02.059 Acetylcholinesterase 1
22472046 10.1016/j.bmc.2012.02.059 Cholinesterase 1

Data from ChEMBL 36 via Core Engine