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Compound Detail

CHEMBL4567355

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COc1c(O)cc(O)c2c(=O)cc(-c3ccc(N4CCCNCC4)cc3)oc12

Basic Information

ChEMBL ID CHEMBL4567355
Phase Preclinical
Structure Type MOL
InChI Key CXASBLCGPKVNJK-UHFFFAOYSA-N
2
Targets
3
Activities
2
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

382.4
MW (Da)
2.68
ALogP
7
HBA
3
HBD
95.2
PSA (Ų)
0.64
QED
0
Ro5 Violations
3
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C21H22N2O5
MW 382.42
Aromatic Rings 3
Heavy Atoms 28
NP-Likeness 0.64

Activity Summary

IC50 2 meas. best 4.74
Kd 1 meas. best 4.36

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
HepG2
CHEMBL395
IC50 4.74 4.74 18200.0 1
Ubiquitin carboxyl-terminal hydrolase 8
CHEMBL2157854
IC50 4.5 4.5 31600.0 1
Ubiquitin carboxyl-terminal hydrolase 8
CHEMBL2157854
Kd 4.36 4.36 43600.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
35786929 10.1021/acs.jmedchem.2c00013 Ubiquitin carboxyl-terminal hydrolase 8 2
31238183 10.1016/j.ejmech.2019.06.024 CDK2/Cyclin A2 1
31238183 10.1016/j.ejmech.2019.06.024 CDK9/cyclin T1 1
31238183 10.1016/j.ejmech.2019.06.024 HepG2 1

Data from ChEMBL 36 via Core Engine