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Compound Detail

CHEMBL561725

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N#CCNC(=O)[C@H](Cc1cccc(Cl)c1)NC(=O)C1=CCCCC1

Basic Information

ChEMBL ID CHEMBL561725
Phase Preclinical
Structure Type MOL
InChI Key DPPHOBBFELMDNQ-INIZCTEOSA-N
3
Targets
3
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

345.8
MW (Da)
2.51
ALogP
3
HBA
2
HBD
82.0
PSA (Ų)
0.78
QED
0
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C18H20ClN3O2
MW 345.83
Aromatic Rings 1
Heavy Atoms 24
NP-Likeness -1.02

Activity Summary

IC50 3 meas. best 6.4

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Cathepsin L2
CHEMBL3272
IC50 6.4 6.4 398.1 1
Procathepsin L
CHEMBL3837
IC50 6.3 6.3 501.2 1
Cathepsin S
CHEMBL2954
IC50 5.7 5.7 1995.3 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Cathepsin L2 IC50 = 398.11 nM 6.4 Inhibition of cathepsin L2 19515558
Procathepsin L IC50 = 501.19 nM 6.3 Inhibition of cathepsin L 19515558
Cathepsin S IC50 = 1995.26 nM 5.7 Inhibition of cathepsin S 19515558

Literature References

PubMed DOI Target Context # Activities
19515558 10.1016/j.bmcl.2009.05.071 Procathepsin L 1
19515558 10.1016/j.bmcl.2009.05.071 Cathepsin L2 1
19515558 10.1016/j.bmcl.2009.05.071 Cathepsin S 1
19515558 10.1016/j.bmcl.2009.05.071 Cathepsin K 1
19515558 10.1016/j.bmcl.2009.05.071 Cathepsin B 1

Data from ChEMBL 36 via Core Engine