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Compound Detail

CHEMBL29483

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CC(C)C[C@H](NC(=O)OCc1ccccc1)C(=O)N1CC(=O)C(NC(=O)[C@@H](CC(C)C)NC(=O)OCc2ccccc2)C1

Basic Information

ChEMBL ID CHEMBL29483
Phase Preclinical
Structure Type MOL
InChI Key GXENQLUSOCKXDN-JZGSEIKYSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

594.7
MW (Da)
3.56
ALogP
7
HBA
3
HBD
143.1
PSA (Ų)
0.32
QED
1
Ro5 Violations
13
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

Natural Product First in Class Prodrug

Extended Properties

Molecular Formula C32H42N4O7
MW 594.71
Aromatic Rings 2
Heavy Atoms 43
NP-Likeness -0.26

Activity Summary

Ki 2 meas. best 8.64

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Cathepsin K
CHEMBL268
Ki 8.64 8.64 2.3 1
Procathepsin L
CHEMBL3837
Ki 7.41 7.41 39.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Cathepsin K Ki = 2.3 nM 8.64 Inhibition of Human cathepsin K 11311061
Procathepsin L Ki = 39.0 nM 7.41 Inhibitory activity against Human cathepsin L 11311061

Literature References

PubMed DOI Target Context # Activities
11311061 10.1021/jm000481x Cathepsin K 1
11311061 10.1021/jm000481x Procathepsin L 1
11311061 10.1021/jm000481x Cathepsin B 1

Data from ChEMBL 36 via Core Engine