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Compound Detail

CHEMBL130599

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CCC(NC(=O)C(CC(C)C)NC(=O)OCc1ccccc1)C(=O)C(=O)NCC(O)c1ccc(OC)cc1

Basic Information

ChEMBL ID CHEMBL130599
Phase Preclinical
Structure Type MOL
InChI Key VPRUMEOQBRFKRM-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

527.6
MW (Da)
2.65
ALogP
7
HBA
4
HBD
143.1
PSA (Ų)
0.28
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 C28H37N3O7
MW 527.62
Aromatic Rings 2
Heavy Atoms 38
NP-Likeness -0.26

Activity Summary

Ki 2 meas. best 6.92

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Cathepsin B
CHEMBL2323
Ki 6.92 6.92 120.0 1
Calpain-1 catalytic subunit
CHEMBL3891
Ki 6.62 6.62 240.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Cathepsin B Ki = 120.0 nM 6.92 Inhibition of bovine cathepsin B 8831774
Calpain-1 catalytic subunit Ki = 240.0 nM 6.62 Inhibition of the cysteine protease human Calpain 1 8831774

Literature References

PubMed DOI Target Context # Activities
8831774 10.1021/jm950541c Calpain-1 catalytic subunit 1
8831774 10.1021/jm950541c Calpain-2 catalytic subunit 1
8831774 10.1021/jm950541c Cathepsin B 1

Data from ChEMBL 36 via Core Engine