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Compound Detail

CHEMBL446544

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CC(C)(F)C[C@H](N[C@@H](c1ccc(-c2ccc(S(C)(=O)=O)cc2)cc1)C(F)(F)F)C(=O)NC1CCN(S(=O)(=O)c2ccccn2)CC1=O

Basic Information

ChEMBL ID CHEMBL446544
Phase Preclinical
Structure Type MOL
InChI Key XNIGRRWFJSOPGU-RRNYZTCWSA-N
1
Targets
1
Activities
1
Assay Types
2
PK Parameters
3
Publications
0
Known Names

Molecular Properties

698.8
MW (Da)
4.00
ALogP
8
HBA
2
HBD
142.6
PSA (Ų)
0.29
QED
1
Ro5 Violations
11
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C31H34F4N4O6S2
MW 698.76
Aromatic Rings 3
Heavy Atoms 47
NP-Likeness -1.03

Activity Summary

IC50 1 meas. best 8.24

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Cathepsin K
CHEMBL268
IC50 8.24 8.24 5.7 1

Pharmacokinetic Data

Parameter Value Units Species
CL 24.0 mL.min-1.kg-1 Rattus norvegicus
T1/2 0.6 hr Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Cathepsin K IC50 = 5.7 nM 8.24 Inhibition of humanized rabbit cathepsin K 19117756

Literature References

PubMed DOI Target Context # Activities
19117756 10.1016/j.bmcl.2008.12.053 Unchecked 3
19117756 10.1016/j.bmcl.2008.12.053 Rattus norvegicus 2
19117756 10.1016/j.bmcl.2008.12.053 Cathepsin K 1

Data from ChEMBL 36 via Core Engine