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Compound Detail

CHEMBL207347

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CCC[C@H](NC(=O)[C@H](CC(C)C)C(=O)OCc1ccccc1)C(=O)c1nnc(-c2ccco2)o1

Basic Information

ChEMBL ID CHEMBL207347
Phase Preclinical
Structure Type MOL
InChI Key PUNDCXSIFPDSLX-OALUTQOASA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

467.5
MW (Da)
4.20
ALogP
8
HBA
1
HBD
124.5
PSA (Ų)
0.24
QED
0
Ro5 Violations
12
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C25H29N3O6
MW 467.52
Aromatic Rings 3
Heavy Atoms 34
NP-Likeness -0.72

Activity Summary

Ki 2 meas. best 9.0

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Procathepsin L
CHEMBL3837
Ki 9.0 9.0 1.0 1
Cathepsin B
CHEMBL4072
Ki 8.7 8.7 2.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Procathepsin L Ki = 1.0 nM 9.0 Inhibition of human cathepsin L 16546382
Cathepsin B Ki = 2.0 nM 8.7 Inhibition of human cathepsin B 16546382

Literature References

PubMed DOI Target Context # Activities
16546382 10.1016/j.bmcl.2006.03.001 Cathepsin K 1
16546382 10.1016/j.bmcl.2006.03.001 Cathepsin B 1
16546382 10.1016/j.bmcl.2006.03.001 Procathepsin L 1
16546382 10.1016/j.bmcl.2006.03.001 Cathepsin S 1

Data from ChEMBL 36 via Core Engine