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Compound Detail

CHEMBL70075

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COc1ccc(CNC(=O)[C@@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)CC2CC(=O)c3ccc(OC)cc32)cc1

Basic Information

ChEMBL ID CHEMBL70075
Phase Preclinical
Structure Type MOL
InChI Key ILCXJEYNSMZPSR-MYDYDDKHSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

565.7
MW (Da)
4.14
ALogP
6
HBA
3
HBD
122.8
PSA (Ų)
0.32
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 C32H43N3O6
MW 565.71
Aromatic Rings 2
Heavy Atoms 41
NP-Likeness -0.05

Activity Summary

IC50 1 meas. best 6.15

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Proteasome
CHEMBL612443
IC50 6.15 6.15 710.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Proteasome IC50 = 710.0 nM 6.15 Inhibition of chymotrypsin-like activity of 20S proteasome 9871656

Literature References

PubMed DOI Target Context # Activities
9871656 10.1016/s0960-894x(98)00015-8 Proteasome 1
9871656 10.1016/s0960-894x(98)00015-8 Calpain 1 1

Data from ChEMBL 36 via Core Engine