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Compound Detail

CHEMBL401175

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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)NCC(N)=O

Basic Information

ChEMBL ID CHEMBL401175
Phase Preclinical
Structure Type MOL
InChI Key YVDVDTCHSKTCEN-FPOVZHCZSA-N
3
Targets
3
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

499.6
MW (Da)
2.97
ALogP
5
HBA
3
HBD
118.4
PSA (Ų)
0.46
QED
0
Ro5 Violations
10
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C23H28F3N3O4S
MW 499.56
Aromatic Rings 2
Heavy Atoms 34
NP-Likeness -0.90

Activity Summary

IC50 3 meas. best 6.62

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Cathepsin K
CHEMBL268
IC50 6.62 6.62 238.0 1
Cathepsin S
CHEMBL2954
IC50 4.39 4.39 41082.0 1
Procathepsin L
CHEMBL3837
IC50 4.2 4.2 63060.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Cathepsin K IC50 = 238.0 nM 6.62 Inhibition of humanized rabbit cathepsin K 17544269
Cathepsin S IC50 = 41082.0 nM 4.39 Inhibition of human cathepsin S 17544269
Procathepsin L IC50 = 63060.0 nM 4.2 Inhibition of human cathepsin L 17544269

Literature References

PubMed DOI Target Context # Activities
17544269 10.1016/j.bmcl.2007.05.024 Cathepsin K 4
17544269 10.1016/j.bmcl.2007.05.024 Cathepsin B 1
17544269 10.1016/j.bmcl.2007.05.024 Procathepsin L 1
17544269 10.1016/j.bmcl.2007.05.024 Cathepsin S 1
17544269 10.1016/j.bmcl.2007.05.024 Unchecked 1

Data from ChEMBL 36 via Core Engine