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Compound Detail

CHEMBL122561

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CC(C)CC(C(=O)NCC#N)c1cccc(-c2ccc(N3CCN(C(=O)OC(C)(C)C)CC3)cc2)c1

Basic Information

ChEMBL ID CHEMBL122561
Phase Preclinical
Structure Type MOL
InChI Key UEJZUSCGOOMJMF-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

490.6
MW (Da)
5.18
ALogP
5
HBA
1
HBD
85.7
PSA (Ų)
0.54
QED
1
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C29H38N4O3
MW 490.65
Aromatic Rings 2
Heavy Atoms 36
NP-Likeness -1.10

Activity Summary

IC50 2 meas. best 6.04

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Cathepsin K
CHEMBL268
IC50 6.04 6.04 922.0 1
Cathepsin S
CHEMBL2954
IC50 5.89 5.89 1298.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
12904076 10.1021/jm0301078 Cathepsin K 1
12904076 10.1021/jm0301078 Procathepsin L 1
12904076 10.1021/jm0301078 Cathepsin S 1
12904076 10.1021/jm0301078 Cathepsin B 1

Data from ChEMBL 36 via Core Engine