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Compound Detail

CHEMBL382576

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CC(C)C[C@H](N[C@@H](c1ccc(-c2ccccc2F)cc1)C(F)(F)F)C(=O)NCC#N

Basic Information

ChEMBL ID CHEMBL382576
Phase Preclinical
Structure Type MOL
InChI Key HCERRVOHXYKRJP-PMACEKPBSA-N
5
Targets
5
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

421.4
MW (Da)
4.74
ALogP
3
HBA
2
HBD
64.9
PSA (Ų)
0.48
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 C22H23F4N3O
MW 421.44
Aromatic Rings 2
Heavy Atoms 30
NP-Likeness -0.98

Activity Summary

IC50 5 meas. best 10.0

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Cathepsin K
CHEMBL268
IC50 10.0 10.0 0.1 1
Osteoclast
CHEMBL612548
IC50 7.55 7.55 28.0 1
Cathepsin S
CHEMBL2954
IC50 6.21 6.21 614.0 1
Procathepsin L
CHEMBL3837
IC50 5.78 5.78 1670.0 1
Cathepsin B
CHEMBL4072
IC50 5.22 5.22 6086.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
16413777 10.1016/j.bmcl.2005.12.071 Cathepsin B 1
16413777 10.1016/j.bmcl.2005.12.071 Procathepsin L 1
16413777 10.1016/j.bmcl.2005.12.071 Cathepsin S 1
16413777 10.1016/j.bmcl.2005.12.071 Cathepsin K 1
16413777 10.1016/j.bmcl.2005.12.071 Osteoclast 1

Data from ChEMBL 36 via Core Engine