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Compound Detail

CHEMBL252383

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CC(C)C[C@H](N[C@@H](c1ccc(-c2ccc(S(C)(=O)=O)cc2)cc1)C(F)(F)F)C(=O)NC(C#N)(C1CC1)C1CC1

Basic Information

ChEMBL ID CHEMBL252383
Phase Preclinical
Structure Type MOL
InChI Key BHXUXLQVSXLWEI-UIOOFZCWSA-N
3
Targets
3
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

561.7
MW (Da)
5.56
ALogP
5
HBA
2
HBD
99.1
PSA (Ų)
0.37
QED
2
Ro5 Violations
11
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C29H34F3N3O3S
MW 561.67
Aromatic Rings 2
Heavy Atoms 39
NP-Likeness -0.72

Activity Summary

IC50 3 meas. best 9.52

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Cathepsin K
CHEMBL268
IC50 9.52 9.52 0.3 1
Cathepsin S
CHEMBL2954
IC50 6.58 6.58 266.0 1
Procathepsin L
CHEMBL3837
IC50 6.34 6.34 456.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Cathepsin K IC50 = 0.3 nM 9.52 Inhibition of humanized rabbit cathepsin K 18226527
Cathepsin S IC50 = 266.0 nM 6.58 Inhibition of cathepsin S 18226527
Procathepsin L IC50 = 456.0 nM 6.34 Inhibition of cathepsin L 18226527

Literature References

PubMed DOI Target Context # Activities
18226527 10.1016/j.bmcl.2007.12.047 Cathepsin K 1
18226527 10.1016/j.bmcl.2007.12.047 Cathepsin B 1
18226527 10.1016/j.bmcl.2007.12.047 Procathepsin L 1
18226527 10.1016/j.bmcl.2007.12.047 Cathepsin S 1

Data from ChEMBL 36 via Core Engine