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Compound Detail

CHEMBL1243048

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CC(C)C[C@@H](/C=C/C(=O)n1cccc1)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)OCc1ccccc1

Basic Information

ChEMBL ID CHEMBL1243048
Phase Preclinical
Structure Type MOL
InChI Key NKMZBFFPLJAUMM-WHYQKWHESA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
1
Publications
0
Known Names

Molecular Properties

566.7
MW (Da)
5.09
ALogP
6
HBA
3
HBD
118.5
PSA (Ų)
0.26
QED
2
Ro5 Violations
15
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C32H46N4O5
MW 566.74
Aromatic Rings 2
Heavy Atoms 41
NP-Likeness 0.04

Activity Summary

IC50 1 meas. best 7.04

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Unchecked
CHEMBL612545
IC50 7.04 7.04 91.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Unchecked IC50 = 91.0 nM 7.04 Inhibition of PGPH catalytic activity of 20S proteasome beta2 in human LCL cells... 20687609

Literature References

PubMed DOI Target Context # Activities
20687609 10.1021/jm100122e Unchecked 3

Data from ChEMBL 36 via Core Engine