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Compound Detail

CHEMBL513049

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CCC(CC)(NC(=O)CCc1ccccc1)C(=O)N[C@H](C=O)Cc1ccccc1

Basic Information

ChEMBL ID CHEMBL513049
Phase Preclinical
Structure Type MOL
InChI Key DPQKVMMXFBIGGX-NRFANRHFSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

394.5
MW (Da)
3.22
ALogP
3
HBA
2
HBD
75.3
PSA (Ų)
0.57
QED
0
Ro5 Violations
11
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C24H30N2O3
MW 394.52
Aromatic Rings 2
Heavy Atoms 29
NP-Likeness -0.09

Activity Summary

Ki 2 meas. best 7.1

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Calpain-1 catalytic subunit
CHEMBL4062
Ki 7.1 7.1 80.0 1
Cathepsin B
CHEMBL4072
Ki 5.54 5.54 2910.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Calpain-1 catalytic subunit Ki = 80.0 nM 7.1 Inhibition of pig erythrocyte mu-calpain 18694642
Cathepsin B Ki = 2910.0 nM 5.54 Inhibition of human liver cathepsin B 18694642

Literature References

PubMed DOI Target Context # Activities
18694642 10.1016/j.bmcl.2008.07.094 Calpain-1 catalytic subunit 1
18694642 10.1016/j.bmcl.2008.07.094 Cathepsin B 1
18694642 10.1016/j.bmcl.2008.07.094 Unchecked 1

Data from ChEMBL 36 via Core Engine