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Compound Detail

CHEMBL4574045

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CNC(=O)C1CCN(C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CC(C)C)C(=O)[C@@]2(C)CO2)CC1

Basic Information

ChEMBL ID CHEMBL4574045
Phase Preclinical
Structure Type MOL
InChI Key SRSPSMAIYJBQJL-PXSDZQOHSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
1
Publications
0
Known Names

Molecular Properties

599.8
MW (Da)
2.19
ALogP
6
HBA
4
HBD
149.2
PSA (Ų)
0.24
QED
1
Ro5 Violations
14
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C32H49N5O6
MW 599.77
Aromatic Rings 1
Heavy Atoms 43
NP-Likeness -0.29

Activity Summary

IC50 1 meas. best 6.63

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
20S proteasome
CHEMBL3831201
IC50 6.63 6.63 232.2 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
20S proteasome IC50 = 232.2 nM 6.63 Inhibition of human 20S proteasome preincubated for 15 mins followed by substrat... 30639896

Literature References

PubMed DOI Target Context # Activities
30639896 10.1016/j.ejmech.2018.12.064 20S proteasome 1

Data from ChEMBL 36 via Core Engine