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Compound Detail

CHEMBL1083620

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CCOC(=O)CNC(=O)C(=O)C(COCc1ccccc1)NC(=O)[C@H](CC1CCCCC1)NC(=O)c1ccc(Br)o1

Basic Information

ChEMBL ID CHEMBL1083620
Phase Preclinical
Structure Type MOL
InChI Key AVYKWCONGMJUNB-HMTLIYDFSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

634.5
MW (Da)
3.06
ALogP
8
HBA
3
HBD
153.0
PSA (Ų)
0.20
QED
1
Ro5 Violations
15
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C29H36BrN3O8
MW 634.52
Aromatic Rings 2
Heavy Atoms 41
NP-Likeness -0.73

Activity Summary

IC50 1 meas. best 8.64

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Cathepsin S
CHEMBL2954
IC50 8.64 8.64 2.3 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Cathepsin S IC50 = 2.3 nM 8.64 Inhibition of human recombinant cathepsin S expressed in Escherichia coli BL21 (... 20481438

Literature References

PubMed DOI Target Context # Activities
20481438 10.1021/jm100089e Cathepsin S 1
20481438 10.1021/jm100089e NON-PROTEIN TARGET 1
20481438 10.1021/jm100089e HUVEC 1

Data from ChEMBL 36 via Core Engine