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Compound Detail

CHEMBL2382115

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COc1cc(O)ccc1C(=O)/C=C/c1ccc(F)cc1

Basic Information

ChEMBL ID CHEMBL2382115
Phase Preclinical
Structure Type MOL
InChI Key FBDKBUZMOCDNPR-RUDMXATFSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
6
Publications
0
Known Names

Molecular Properties

272.3
MW (Da)
3.44
ALogP
3
HBA
1
HBD
46.5
PSA (Ų)
0.68
QED
0
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C16H13FO3
MW 272.28
Aromatic Rings 2
Heavy Atoms 20
NP-Likeness 0.09

Activity Summary

IC50 1 meas. best 4.04

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Procathepsin L
CHEMBL3837
IC50 4.04 4.04 91170.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Procathepsin L IC50 = 91170.0 nM 4.04 Inhibition of cathepsin L (unknown origin) using Z-FR-AMC as substrate after 30 ... 23608763

Literature References

PubMed DOI Target Context # Activities
23608763 10.1016/j.bmcl.2013.03.106 DNA topoisomerase 2-alpha 2
23608763 10.1016/j.bmcl.2013.03.106 DNA topoisomerase 1 2
23608763 10.1016/j.bmcl.2013.03.106 SNU-638 1
23608763 10.1016/j.bmcl.2013.03.106 T47D 1
23608763 10.1016/j.bmcl.2013.03.106 Procathepsin L 1
23608763 10.1016/j.bmcl.2013.03.106 Cathepsin B 1

Data from ChEMBL 36 via Core Engine