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Compound Detail

CHEMBL378000

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CCCCCCCCCC(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1ccccc1)C(=O)O)[C@@H](C)O)C(C)C)[C@@H](C)O

Basic Information

ChEMBL ID CHEMBL378000
Phase Preclinical
Structure Type MOL
InChI Key CDTGHLYBYSXRGU-RDOWQFMTSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

912.1
MW (Da)
1.86
ALogP
11
HBA
11
HBD
298.6
PSA (Ų)
0.05
QED
3
Ro5 Violations
31
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C47H73N7O11
MW 912.14
Aromatic Rings 2
Heavy Atoms 65
NP-Likeness 0.24

Activity Summary

Ki 1 meas. best 4.14

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Proteasome Macropain subunit PRE2
CHEMBL4659
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 Macropain subunit PRE2 Ki = 72000.0 nM 4.14 Inhibition of chymotrypsin like 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