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Compound Detail

CHEMBL210702

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CCC[C@H](NC(=O)OCC(C)C)C(=O)c1nnc(-c2ccco2)o1

Basic Information

ChEMBL ID CHEMBL210702
Phase Preclinical
Structure Type MOL
InChI Key QSFFAUMRNCREGS-NSHDSACASA-N
4
Targets
4
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

335.4
MW (Da)
3.06
ALogP
7
HBA
1
HBD
107.5
PSA (Ų)
0.74
QED
0
Ro5 Violations
8
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C16H21N3O5
MW 335.36
Aromatic Rings 2
Heavy Atoms 24
NP-Likeness -1.19

Activity Summary

Ki 4 meas. best 6.42

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Cathepsin S
CHEMBL2954
Ki 6.42 6.42 380.0 1
Cathepsin K
CHEMBL268
Ki 6.3 6.3 500.0 1
Procathepsin L
CHEMBL3837
Ki 4.85 4.85 14000.0 1
Cathepsin B
CHEMBL4072
Ki 4.8 4.8 16000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Cathepsin S Ki = 380.0 nM 6.42 Inhibition of human cathepsin S 16546382
Cathepsin K Ki = 500.0 nM 6.3 Inhibition of human cathepsin K 16546382
Procathepsin L Ki = 14000.0 nM 4.85 Inhibition of human cathepsin L 16546382
Cathepsin B Ki = 16000.0 nM 4.8 Inhibition of human cathepsin B 16546382

Literature References

PubMed DOI Target Context # Activities
16546382 10.1016/j.bmcl.2006.03.001 Cathepsin K 1
16546382 10.1016/j.bmcl.2006.03.001 Cathepsin B 1
16546382 10.1016/j.bmcl.2006.03.001 Procathepsin L 1
16546382 10.1016/j.bmcl.2006.03.001 Cathepsin S 1

Data from ChEMBL 36 via Core Engine