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Compound Detail

CHEMBL208015

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CC(C)C[C@@H](/C=C/S(C)(=O)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCC(=O)OC(C)(C)C)NC(=O)OCc1ccccc1

Basic Information

ChEMBL ID CHEMBL208015
Phase Preclinical
Structure Type MOL
InChI Key LRSBIKVQDTUNIU-DSNMTOQLSA-N
4
Targets
4
Activities
1
Assay Types
0
PK Parameters
8
Publications
0
Known Names

Molecular Properties

581.7
MW (Da)
3.00
ALogP
8
HBA
3
HBD
157.0
PSA (Ų)
0.28
QED
1
Ro5 Violations
14
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C28H43N3O8S
MW 581.73
Aromatic Rings 1
Heavy Atoms 40

Activity Summary

IC50 4 meas. best 8.21

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Proteasome Macropain subunit MB1
CHEMBL4662
IC50 8.21 8.21 6.1 1
Cathepsin S
CHEMBL2954
IC50 5.52 5.52 3000.0 1
PC-3
CHEMBL390
IC50 5.19 5.19 6500.0 1
Cathepsin B
CHEMBL4072
IC50 4.7 4.7 20000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
16686537 10.1021/jm058289o Proteasome Macropain subunit MB1 2
16686537 10.1021/jm058289o Proteasome Macropain subunit 1
16686537 10.1021/jm058289o Cathepsin B 1
16686537 10.1021/jm058289o Proteasome component C5 1
16686537 10.1021/jm058289o PC-3 1
16686537 10.1021/jm058289o Cathepsin S 1
16686537 10.1021/jm058289o Plasma 1
16686537 10.1021/jm058289o No relevant target 1

Data from ChEMBL 36 via Core Engine