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Compound Detail

CHEMBL204103

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CCCC[C@@H](/C=N/NC(=O)N1CCCC1)NC(=O)OC(C)(C)C

Basic Information

ChEMBL ID CHEMBL204103
Phase Preclinical
Structure Type MOL
InChI Key SPKPMLLMVWOADV-VLURKWGBSA-N
1
Targets
1
Activities
1
Assay Types
3
PK Parameters
4
Publications
0
Known Names

Molecular Properties

326.4
MW (Da)
2.86
ALogP
4
HBA
2
HBD
83.0
PSA (Ų)
0.58
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 C16H30N4O3
MW 326.44
Aromatic Rings 0
Heavy Atoms 23
NP-Likeness -0.88

Activity Summary

IC50 1 meas. best 7.44

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Cathepsin K
CHEMBL268
IC50 7.44 7.44 36.0 1

Pharmacokinetic Data

Parameter Value Units Species
CL 18.0 mL.min-1.kg-1 Rattus norvegicus
F - % Rattus norvegicus
T1/2 0.3 hr Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Cathepsin K IC50 = 36.0 nM 7.44 Inhibition of recombinant human cathepsin K in a fluorescence assay 16290936

Literature References

PubMed DOI Target Context # Activities
16290936 10.1016/j.bmcl.2005.10.108 Rattus norvegicus 4
16290936 10.1016/j.bmcl.2005.10.108 Cathepsin K 1
16290936 10.1016/j.bmcl.2005.10.108 MDCK 1
16290936 10.1016/j.bmcl.2005.10.108 No relevant target 1

Data from ChEMBL 36 via Core Engine