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Compound Detail

CHEMBL162812

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CCCC[C@H](NC(=O)OC(C)(C)C)C(=O)C(=O)N[C@H](C)c1ccccc1

Basic Information

ChEMBL ID CHEMBL162812
Phase Preclinical
Structure Type MOL
InChI Key WPAWBLWVSDBOPB-ZBFHGGJFSA-N
1
Targets
3
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

362.5
MW (Da)
3.52
ALogP
4
HBA
2
HBD
84.5
PSA (Ų)
0.69
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 C20H30N2O4
MW 362.47
Aromatic Rings 1
Heavy Atoms 26
NP-Likeness -0.64

Activity Summary

IC50 3 meas. best 5.92

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Cathepsin K
CHEMBL268
IC50 5.92 5.92 1200.0 3

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Cathepsin K IC50 = 1200.0 nM 5.92 Inhibitory activity against human cathepsin K 14741275
Cathepsin K IC50 = 1200.0 nM 5.92 Inhibitory concentration against human cathepsin K 15837295
Cathepsin K IC50 = 1202.26 nM 5.92 Inhibition of human cathepsin K 19962796

Literature References

PubMed DOI Target Context # Activities
14741275 10.1016/j.bmcl.2003.11.029 Cathepsin K 1
15837295 10.1016/j.bmcl.2005.03.023 Cathepsin K 1
19962796 10.1016/j.ejmech.2009.11.010 Cathepsin K 1

Data from ChEMBL 36 via Core Engine