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Compound Detail

CHEMBL2207591

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N#CC1(n2cc([C@@H](NC(=O)c3ccc(NC(=O)C4CC4)cc3)C3CCCCC3)nn2)CC1

Basic Information

ChEMBL ID CHEMBL2207591
Phase Preclinical
Structure Type MOL
InChI Key NEPMXTBQPHGVAE-NRFANRHFSA-N
1
Targets
1
Activities
1
Assay Types
1
PK Parameters
2
Publications
0
Known Names

Molecular Properties

432.5
MW (Da)
3.69
ALogP
6
HBA
2
HBD
112.7
PSA (Ų)
0.69
QED
0
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C24H28N6O2
MW 432.53
Aromatic Rings 2
Heavy Atoms 32
NP-Likeness -1.27

Activity Summary

IC50 1 meas. best 9.3

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Cathepsin S
CHEMBL2954
IC50 9.3 9.3 0.5 1

Pharmacokinetic Data

Parameter Value Units Species
T1/2 1.5 hr Homo sapiens

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Cathepsin S IC50 = 0.5 nM 9.3 Inhibition of cathepsin S using FR-aminoluciferin as substrate preincubated for ... 23084902

Literature References

PubMed DOI Target Context # Activities
23084902 10.1016/j.bmcl.2012.09.054 Liver microsomes 1
23084902 10.1016/j.bmcl.2012.09.054 Cathepsin S 1

Data from ChEMBL 36 via Core Engine