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Compound Detail

CHEMBL248889

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CS(=O)(=O)C[C@H](N[C@@H](c1ccc(-c2ccc(F)cc2)cc1)C(F)(F)F)C(=O)NC1(C#N)CC1

Basic Information

ChEMBL ID CHEMBL248889
Phase Preclinical
Structure Type MOL
InChI Key ZBNVNRCRULQVAR-OALUTQOASA-N
3
Targets
3
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

483.5
MW (Da)
3.27
ALogP
5
HBA
2
HBD
99.1
PSA (Ų)
0.56
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 C22H21F4N3O3S
MW 483.49
Aromatic Rings 2
Heavy Atoms 33
NP-Likeness -1.10

Activity Summary

IC50 3 meas. best 8.28

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Cathepsin K
CHEMBL268
IC50 8.28 8.28 5.3 1
Cathepsin S
CHEMBL2954
IC50 8.0 8.0 10.0 1
Cathepsin B
CHEMBL4072
IC50 6.77 6.77 170.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Cathepsin K IC50 = 5.3 nM 8.28 Inhibition of human cathepsin K 17590332
Cathepsin S IC50 = 10.0 nM 8.0 Inhibition of human cathepsin S 17590332
Cathepsin B IC50 = 170.0 nM 6.77 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