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Compound Detail

CHEMBL5277927

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COc1ccccc1C(=O)N1Cc2ccc(N3C(=O)c4ccccc4C3=O)cc2CC1=O

Basic Information

ChEMBL ID CHEMBL5277927
Phase Preclinical
Structure Type MOL
InChI Key YXGNCQQSGCFRBR-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

426.4
MW (Da)
3.22
ALogP
5
HBA
0
HBD
84.0
PSA (Ų)
0.60
QED
0
Ro5 Violations
3
Rot. Bonds

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C25H18N2O5
MW 426.43
Aromatic Rings 3
Heavy Atoms 32
NP-Likeness -0.91

Activity Summary

IC50 2 meas. best 8.53

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Beta-secretase 1
CHEMBL4822
IC50 8.53 8.53 3.0 1
Acetylcholinesterase
CHEMBL220
IC50 7.09 7.09 81.7 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Beta-secretase 1 IC50 = 2.96 nM 8.53 Inhibition of BACE1 (unknown origin) 33984802
Acetylcholinesterase IC50 = 81.65 nM 7.09 Inhibition of AChE (unknown origin) 33984802

Literature References

PubMed DOI Target Context # Activities
33984802 10.1016/j.ejmech.2021.113492 Acetylcholinesterase 1
33984802 10.1016/j.ejmech.2021.113492 Beta-secretase 1 1

Data from ChEMBL 36 via Core Engine