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Compound Detail

CHEMBL208805

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CCCCCCCCCC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)O

Basic Information

ChEMBL ID CHEMBL208805
Phase Preclinical
Structure Type MOL
InChI Key DUBNBDOVKSGEIA-SDHOMARFSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

577.7
MW (Da)
3.53
ALogP
6
HBA
6
HBD
182.1
PSA (Ų)
0.12
QED
2
Ro5 Violations
21
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C30H47N3O8
MW 577.72
Aromatic Rings 1
Heavy Atoms 41
NP-Likeness 0.30

Activity Summary

Ki 1 meas. best 4.14

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Proteasome component C5
CHEMBL4904
Ki 4.14 4.14 72000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Proteasome component C5 Ki = 72000.0 nM 4.14 Inhibition of post acid activity of yeast 20S proteasome 16630721

Literature References

PubMed DOI Target Context # Activities
16630721 10.1016/j.bmcl.2006.03.033 Proteasome Macropain subunit PRE2 1
16630721 10.1016/j.bmcl.2006.03.033 Proteasome Macropain subunit 1
16630721 10.1016/j.bmcl.2006.03.033 Proteasome component C5 1

Data from ChEMBL 36 via Core Engine