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Compound Detail

CHEMBL250121

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CS(=O)(=O)C[C@H](N[C@@H](c1cccc(F)c1)C(F)(F)F)C(=O)NC1(C#N)CC1

Basic Information

ChEMBL ID CHEMBL250121
Phase Preclinical
Structure Type MOL
InChI Key OOVJOXGELNYKFE-STQMWFEESA-N
4
Targets
4
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

407.4
MW (Da)
1.60
ALogP
5
HBA
2
HBD
99.1
PSA (Ų)
0.67
QED
0
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C16H17F4N3O3S
MW 407.39
Aromatic Rings 1
Heavy Atoms 27
NP-Likeness -1.38

Activity Summary

IC50 4 meas. best 8.19

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Cathepsin S
CHEMBL2954
IC50 8.19 8.19 6.4 1
Cathepsin K
CHEMBL268
IC50 6.5 6.5 314.0 1
Procathepsin L
CHEMBL3837
IC50 6.04 6.04 911.0 1
Cathepsin B
CHEMBL4072
IC50 5.41 5.41 3854.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Cathepsin S IC50 = 6.4 nM 8.19 Inhibition of human cathepsin S 17590332
Cathepsin K IC50 = 314.0 nM 6.5 Inhibition of human cathepsin K 17590332
Procathepsin L IC50 = 911.0 nM 6.04 Inhibition of human cathepsin L 17590332
Cathepsin B IC50 = 3854.0 nM 5.41 Inhibition of human cathepsin B 17590332

Literature References

PubMed DOI Target Context # Activities
17590332 10.1016/j.bmcl.2007.06.023 Cathepsin S 1
17590332 10.1016/j.bmcl.2007.06.023 Cathepsin K 1
17590332 10.1016/j.bmcl.2007.06.023 Cathepsin B 1
17590332 10.1016/j.bmcl.2007.06.023 Procathepsin L 1

Data from ChEMBL 36 via Core Engine