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Compound Detail

CHEMBL5173789

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CC(C)(C)CNC(=O)C[C@H](NC(=O)N1CCC(C(=O)Nc2cccnc2)CC1)C(=O)N[C@@H](CCc1ccccc1)C(=O)N1CCc2ccccc2C1

Basic Information

ChEMBL ID CHEMBL5173789
Phase Preclinical
Structure Type MOL
InChI Key XGSIEVNDLXOMPH-HEVIKAOCSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
1
Publications
0
Known Names

Molecular Properties

709.9
MW (Da)
4.07
ALogP
6
HBA
4
HBD
152.8
PSA (Ų)
0.22
QED
1
Ro5 Violations
12
Rot. Bonds

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C40H51N7O5
MW 709.89
Aromatic Rings 3
Heavy Atoms 52
NP-Likeness -1.21

Activity Summary

IC50 1 meas. best 5.8

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
20S proteasome
CHEMBL3831201
IC50 5.8 5.8 1588.5 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
20S proteasome IC50 = 1588.5 nM 5.8 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