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Compound Detail

CHEMBL195505

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CC(C)CC(NC(c1ccc(-c2ccc(N3CCNCC3)cc2)cc1)C(F)(F)F)C(=O)NCC#N

Basic Information

ChEMBL ID CHEMBL195505
Phase Preclinical
Structure Type MOL
InChI Key RSIVRPBUNKODPD-UHFFFAOYSA-N
3
Targets
3
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

487.6
MW (Da)
4.01
ALogP
5
HBA
3
HBD
80.2
PSA (Ų)
0.47
QED
0
Ro5 Violations
9
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C26H32F3N5O
MW 487.57
Aromatic Rings 2
Heavy Atoms 35
NP-Likeness -0.96

Activity Summary

IC50 3 meas. best 8.34

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Cathepsin K
CHEMBL268
IC50 8.34 8.34 4.6 1
Procathepsin L
CHEMBL3837
IC50 7.17 7.17 68.0 1
Cathepsin S
CHEMBL2954
IC50 6.04 6.04 902.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
16154747 10.1016/j.bmcl.2005.07.071 Cathepsin K 1
16154747 10.1016/j.bmcl.2005.07.071 Cathepsin B 1
16154747 10.1016/j.bmcl.2005.07.071 Procathepsin L 1
16154747 10.1016/j.bmcl.2005.07.071 Cathepsin S 1

Data from ChEMBL 36 via Core Engine