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Compound Detail

CHEMBL4784875

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Cc1ccc(S(=O)(=O)N[C@@H](CCC(=O)NC(C)(C)C)C(=O)N[C@@H](C)C(=O)NCc2cccc3ccccc23)cc1

Basic Information

ChEMBL ID CHEMBL4784875
Phase Preclinical
Structure Type MOL
InChI Key YROCKOFXGKCYAZ-LVXARBLLSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

566.7
MW (Da)
3.31
ALogP
5
HBA
4
HBD
133.5
PSA (Ų)
0.28
QED
1
Ro5 Violations
11
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C30H38N4O5S
MW 566.72
Aromatic Rings 3
Heavy Atoms 40
NP-Likeness -1.12

Activity Summary

IC50 2 meas. best 9.4

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Proteasome subunit beta type-8
CHEMBL5620
IC50 9.4 9.4 0.4 1
Proteasome Macropain subunit MB1
CHEMBL4662
IC50 6.37 6.37 424.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
33095579 10.1021/acs.jmedchem.0c01520 Proteasome subunit beta type-8 1
33095579 10.1021/acs.jmedchem.0c01520 Proteasome Macropain subunit MB1 1
33095579 10.1021/acs.jmedchem.0c01520 Unchecked 1

Data from ChEMBL 36 via Core Engine