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Compound Detail

CHEMBL5198183

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CC(C)(C)CNC(=O)C[C@H](NC(=O)N1CCN(C(=O)Nc2ccc(Cl)cc2)CC1)C(=O)N[C@@H](CCc1ccccc1)C(=O)N[C@@H]1CCCc2ccccc21

Basic Information

ChEMBL ID CHEMBL5198183
Phase Preclinical
Structure Type MOL
InChI Key QBPOBPNZSWZKFO-PLJDCMBSSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
1
Publications
0
Known Names

Molecular Properties

758.4
MW (Da)
5.43
ALogP
5
HBA
5
HBD
152.0
PSA (Ų)
0.17
QED
2
Ro5 Violations
12
Rot. Bonds

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C41H52ClN7O5
MW 758.36
Aromatic Rings 3
Heavy Atoms 54
NP-Likeness -0.87

Activity Summary

IC50 1 meas. best 7.62

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
20S proteasome
CHEMBL3831201
IC50 7.62 7.62 23.7 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
20S proteasome IC50 = 23.71 nM 7.62 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