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Compound Detail

CHEMBL4435814

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CC(C)C[C@H](NC(=O)N1CCC(C(=O)Nc2ccon2)CC1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CC(C)C)C(=O)[C@@]1(C)CO1

Basic Information

ChEMBL ID CHEMBL4435814
Phase Preclinical
Structure Type MOL
InChI Key GCAGLVKLOWGBCV-CBUCOWSNSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
1
Publications
0
Known Names

Molecular Properties

652.8
MW (Da)
3.07
ALogP
8
HBA
4
HBD
175.3
PSA (Ų)
0.21
QED
1
Ro5 Violations
15
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C34H48N6O7
MW 652.79
Aromatic Rings 2
Heavy Atoms 47
NP-Likeness -0.64

Activity Summary

IC50 1 meas. best 8.19

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
20S proteasome
CHEMBL3831201
IC50 8.19 8.19 6.4 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
20S proteasome IC50 = 6.4 nM 8.19 Inhibition of human 20S proteasome preincubated for 15 mins followed by substrat... 30639896

Literature References

PubMed DOI Target Context # Activities
30639896 10.1016/j.ejmech.2018.12.064 20S proteasome 1

Data from ChEMBL 36 via Core Engine