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Compound Detail

CHEMBL1269192

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C[C@@H](O)[C@H](NC(=O)c1ccc(OCc2ccccc2)cc1)C(=O)N[C@@H](CCc1ccccc1)C(=O)NCCc1cccs1

Basic Information

ChEMBL ID CHEMBL1269192
Phase Preclinical
Structure Type MOL
InChI Key JDWNDZCJELVSRS-GTTXMTDLSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
10
Publications
0
Known Names

Molecular Properties

599.8
MW (Da)
4.28
ALogP
6
HBA
4
HBD
116.8
PSA (Ų)
0.16
QED
1
Ro5 Violations
15
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C34H37N3O5S
MW 599.75
Aromatic Rings 4
Heavy Atoms 43
NP-Likeness -0.74

Activity Summary

IC50 1 meas. best 5.5

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Unchecked
CHEMBL612545
IC50 5.5 5.5 3200.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Unchecked IC50 = 3200.0 nM 5.5 Inhibition of chymotrypsin-like activity of human 20s proteasome beta5 subunit i... 20875739

Literature References

PubMed DOI Target Context # Activities
20875739 10.1016/j.bmcl.2010.09.032 Unchecked 6
20875739 10.1016/j.bmcl.2010.09.032 Cathepsin B 1
20875739 10.1016/j.bmcl.2010.09.032 Procathepsin L 1
20875739 10.1016/j.bmcl.2010.09.032 Coagulation factor XII 1
20875739 10.1016/j.bmcl.2010.09.032 Plasminogen 1
20875739 10.1016/j.bmcl.2010.09.032 Prothrombin 1
20875739 10.1016/j.bmcl.2010.09.032 Tissue-type plasminogen activator 1
20875739 10.1016/j.bmcl.2010.09.032 Trypsin 1
20875739 10.1016/j.bmcl.2010.09.032 Calpain-1 catalytic subunit 1
20875739 10.1016/j.bmcl.2010.09.032 ADMET 1

Data from ChEMBL 36 via Core Engine