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Compound Detail

CHEMBL202723

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CCCC[C@H](NC(=O)O[C@@H]1C(=O)N(C(=O)c2cccnc2)CC1(C)C)C(=O)C(=O)N[C@H](C)c1ccccc1

Basic Information

ChEMBL ID CHEMBL202723
Phase Preclinical
Structure Type MOL
InChI Key ONBHKIJPHBOPAS-RZFNWQHOSA-N
1
Targets
1
Activities
1
Assay Types
3
PK Parameters
10
Publications
0
Known Names

Molecular Properties

522.6
MW (Da)
3.19
ALogP
7
HBA
2
HBD
134.8
PSA (Ų)
0.36
QED
1
Ro5 Violations
10
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C28H34N4O6
MW 522.60
Aromatic Rings 2
Heavy Atoms 38
NP-Likeness -0.40

Activity Summary

IC50 1 meas. best 7.85

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Cathepsin K
CHEMBL268
IC50 7.85 7.85 14.0 1

Pharmacokinetic Data

Parameter Value Units Species
CL 34.0 mL.min-1.kg-1 Rattus norvegicus
F 45.0 % Rattus norvegicus
T1/2 1.567 hr Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Cathepsin K IC50 = 14.0 nM 7.85 Inhibition of recombinant human cathepsin K by fluorescence assay 16376075

Literature References

PubMed DOI Target Context # Activities
16376075 10.1016/j.bmcl.2005.11.101 Rattus norvegicus 4
16376075 10.1016/j.bmcl.2005.11.101 Cathepsin K 1
16376075 10.1016/j.bmcl.2005.11.101 Unchecked 1
16376075 10.1016/j.bmcl.2005.11.101 Cathepsin (B and K) 1
16376075 10.1016/j.bmcl.2005.11.101 Cathepsin (H and K) 1
16376075 10.1016/j.bmcl.2005.11.101 Cathepsin (L and K) 1
16376075 10.1016/j.bmcl.2005.11.101 Cathepsin (S and K) 1
16376075 10.1016/j.bmcl.2005.11.101 Cathepsin (V and K) 1
16376075 10.1016/j.bmcl.2005.11.101 MDCK 1
16376075 10.1016/j.bmcl.2005.11.101 No relevant target 1

Data from ChEMBL 36 via Core Engine