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Compound Detail

CHEMBL5173174

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CC(C)(C)CNC(=O)C[C@H](NC(=O)N1CCC(NC(=O)Nc2ccc(Cl)cc2)CC1)C(=O)N[C@@H](CCc1ccccc1)C(=O)N[C@@H]1CCCc2ccccc21

Basic Information

ChEMBL ID CHEMBL5173174
Phase Preclinical
Structure Type MOL
InChI Key NSQSQZVNTUNAIU-SBPNQFBHSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
1
Publications
0
Known Names

Molecular Properties

772.4
MW (Da)
5.87
ALogP
5
HBA
6
HBD
160.8
PSA (Ų)
0.13
QED
3
Ro5 Violations
13
Rot. Bonds

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C42H54ClN7O5
MW 772.39
Aromatic Rings 3
Heavy Atoms 55
NP-Likeness -1.03

Activity Summary

IC50 1 meas. best 7.38

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
20S proteasome
CHEMBL3831201
IC50 7.38 7.38 41.2 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
20S proteasome IC50 = 41.23 nM 7.38 Inhibition of chymotrypsin-like activity of human 20S proteasome using Suc-Leu L... 35218994

Literature References

PubMed DOI Target Context # Activities
35218994 10.1016/j.ejmech.2022.114211 20S proteasome 1

Data from ChEMBL 36 via Core Engine