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Compound Detail

CHEMBL30957

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CC(C)(C)O[C@@H]1NC(=O)[C@H]1NC(=O)[C@H](Cc1ccccc1)NC(=O)OCc1ccccc1

Basic Information

ChEMBL ID CHEMBL30957
Phase Preclinical
Structure Type MOL
InChI Key RHNULCWVJCENCM-JQVVWYNYSA-N
3
Targets
3
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

439.5
MW (Da)
2.28
ALogP
5
HBA
3
HBD
105.8
PSA (Ų)
0.55
QED
0
Ro5 Violations
8
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C24H29N3O5
MW 439.51
Aromatic Rings 2
Heavy Atoms 32
NP-Likeness 0.01

Activity Summary

IC50 3 meas. best 6.11

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Procathepsin L
CHEMBL3837
IC50 6.11 6.11 780.0 1
Cathepsin K
CHEMBL268
IC50 5.6 5.6 2500.0 1
Cathepsin B
CHEMBL2602
IC50 4.94 4.94 11400.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Procathepsin L IC50 = 780.0 nM 6.11 Inhibition of recombinant human Cathepsin L 12467634
Cathepsin K IC50 = 2500.0 nM 5.6 Inhibition of recombinant human Cathepsin K 12467634
Cathepsin B IC50 = 11400.0 nM 4.94 Inhibition of recombinant rat Cathepsin B 12467634

Literature References

PubMed DOI Target Context # Activities
12467634 10.1016/s0960-894x(02)00831-4 Cathepsin B 1
12467634 10.1016/s0960-894x(02)00831-4 Procathepsin L 1
12467634 10.1016/s0960-894x(02)00831-4 Cathepsin K 1
12467634 10.1016/s0960-894x(02)00831-4 Cathepsin S 1
12467634 10.1016/s0960-894x(02)00831-4 Neutrophil elastase 1

Data from ChEMBL 36 via Core Engine