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Compound Detail

CHEMBL209216

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CCC[C@H](NC(=O)C1(NC(=O)OC(C)(C)C)CCCCC1)C(=O)c1nnc(-c2ccco2)o1

Basic Information

ChEMBL ID CHEMBL209216
Phase Preclinical
Structure Type MOL
InChI Key CMCVBOBNUPQRNQ-HNNXBMFYSA-N
4
Targets
4
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

460.5
MW (Da)
4.02
ALogP
8
HBA
2
HBD
136.6
PSA (Ų)
0.56
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 C23H32N4O6
MW 460.53
Aromatic Rings 2
Heavy Atoms 33
NP-Likeness -1.08

Activity Summary

Ki 4 meas. best 7.37

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Cathepsin K
CHEMBL268
Ki 7.37 7.37 43.0 1
Cathepsin S
CHEMBL2954
Ki 6.02 6.02 960.0 1
Cathepsin B
CHEMBL4072
Ki 5.14 5.14 7300.0 1
Procathepsin L
CHEMBL3837
Ki 4.75 4.75 18000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Cathepsin K Ki = 43.0 nM 7.37 Inhibition of human cathepsin K 16546382
Cathepsin S Ki = 960.0 nM 6.02 Inhibition of human cathepsin S 16546382
Cathepsin B Ki = 7300.0 nM 5.14 Inhibition of human cathepsin B 16546382
Procathepsin L Ki = 18000.0 nM 4.75 Inhibition of human cathepsin L 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