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Compound Detail

CHEMBL470973

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O=C[C@H](Cc1ccccc1)NC(=O)C1(NC(=O)CCc2ccccc2)CCCC1

Basic Information

ChEMBL ID CHEMBL470973
Phase Preclinical
Structure Type MOL
InChI Key QFNXOBUNAJDGBU-NRFANRHFSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

392.5
MW (Da)
2.97
ALogP
3
HBA
2
HBD
75.3
PSA (Ų)
0.64
QED
0
Ro5 Violations
9
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C24H28N2O3
MW 392.50
Aromatic Rings 2
Heavy Atoms 29
NP-Likeness -0.25

Activity Summary

Ki 2 meas. best 6.06

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Cathepsin B
CHEMBL4072
Ki 6.06 6.06 880.0 1
Calpain-1 catalytic subunit
CHEMBL4062
Ki 5.71 5.71 1940.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Cathepsin B Ki = 880.0 nM 6.06 Inhibition of human liver cathepsin B 18694642
Calpain-1 catalytic subunit Ki = 1940.0 nM 5.71 Inhibition of pig erythrocyte mu-calpain 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