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Compound Detail

CHEMBL4542373

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CC(C)C[C@H](NC(=O)N1CCC(C(=O)Nc2nncs2)CC1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CC(C)C)C(=O)[C@@]1(C)CO1

Basic Information

ChEMBL ID CHEMBL4542373
Phase Preclinical
Structure Type MOL
InChI Key PFWAXGUKYRAYAJ-DXCNDIKUSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
1
Publications
0
Known Names

Molecular Properties

669.9
MW (Da)
2.93
ALogP
9
HBA
4
HBD
175.0
PSA (Ų)
0.21
QED
1
Ro5 Violations
15
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C33H47N7O6S
MW 669.85
Aromatic Rings 2
Heavy Atoms 47
NP-Likeness -0.83

Activity Summary

IC50 1 meas. best 8.34

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
20S proteasome
CHEMBL3831201
IC50 8.34 8.34 4.6 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
20S proteasome IC50 = 4.6 nM 8.34 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