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Compound Detail

CHEMBL244416

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CCN(Cc1ccccc1)Cc1ccc(-c2cc3cc(OC)c(OC)cc3oc2=O)cc1

Basic Information

ChEMBL ID CHEMBL244416
Phase Preclinical
Structure Type MOL
InChI Key PNZIOQNBQOTGPK-UHFFFAOYSA-N

Known Names

AP-2243
2
Targets
6
Activities
2
Assay Types
0
PK Parameters
6
Publications
1
Known Names

Molecular Properties

429.5
MW (Da)
5.50
ALogP
5
HBA
0
HBD
51.9
PSA (Ų)
0.35
QED
1
Ro5 Violations
8
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C27H27NO4
MW 429.52
Aromatic Rings 4
Heavy Atoms 32
NP-Likeness -0.42

Activity Summary

IC50 5 meas. best 7.75
Ki 1 meas. best 7.98

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Acetylcholinesterase
CHEMBL220
Ki 7.98 7.98 10.5 1
Acetylcholinesterase
CHEMBL220
IC50 7.75 7.7433 18.0 3
Beta-secretase 1
CHEMBL4822
IC50 6.62 6.62 238.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
17655212 10.1021/jm070100g Acetylcholinesterase 2
17998161 10.1016/j.bmcl.2007.09.100 Beta-secretase 1 2
17655212 10.1021/jm070100g Cholinesterase 1
17998161 10.1016/j.bmcl.2007.09.100 Acetylcholinesterase 1
27519464 10.1016/j.bmc.2016.07.061 Acetylcholinesterase 1
27494166 10.1016/j.ejmech.2016.07.057 Acetylcholinesterase 1

Data from ChEMBL 36 via Core Engine