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Compound Detail

CHEMBL3218819

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Cc1ccc(CNC(=O)[C@H](CCc2ccccc2)NC(=O)[C@H](CNC(=O)CC(C)(C)C)NC(=O)C(=O)c2c[nH]c3ccccc23)cc1

Basic Information

ChEMBL ID CHEMBL3218819
Phase Preclinical
Structure Type MOL
InChI Key XPIZIYYVGLXORM-CONSDPRKSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

637.8
MW (Da)
4.13
ALogP
5
HBA
5
HBD
149.3
PSA (Ų)
0.10
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 C37H43N5O5
MW 637.78
Aromatic Rings 4
Heavy Atoms 47
NP-Likeness -0.49

Activity Summary

IC50 1 meas. best 6.04

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Proteasome Macropain subunit MB1
CHEMBL4662
IC50 6.04 6.04 910.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
- 10.1039/C2MD20060K Proteasome Macropain subunit MB1 2
- 10.1039/C2MD20060K Proteasome component C5 1
- 10.1039/C2MD20060K Proteasome Macropain subunit 1
- 10.1039/C2MD20060K Nuclear factor NF-kappa-B complex 1
- 10.1039/C2MD20060K NON-PROTEIN TARGET 1

Data from ChEMBL 36 via Core Engine