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Compound Detail

CHEMBL1221749

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Cc1cccc(C)c1C(=O)OCC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc1ccccc1)NC(=O)OCc1ccccc1

Basic Information

ChEMBL ID CHEMBL1221749
Phase Preclinical
Structure Type MOL
InChI Key AHCLHJFPKBHMDV-SVBPBHIXSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
7
Publications
0
Known Names

Molecular Properties

601.7
MW (Da)
3.32
ALogP
7
HBA
5
HBD
172.7
PSA (Ų)
0.08
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 C33H39N5O6
MW 601.70
Aromatic Rings 3
Heavy Atoms 44
NP-Likeness -0.12

Activity Summary

IC50 1 meas. best 7.82

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Cathepsin B
CHEMBL2602
IC50 7.82 7.82 15.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Cathepsin B IC50 = 15.0 nM 7.82 Binding affinity to cathepsin B in crude rat liver homogenates using [125I]DCG-0... 16407991

Literature References

PubMed DOI Target Context # Activities
20696584 10.1016/j.bmc.2010.07.041 CAAX prenyl protease 2 1
20696584 10.1016/j.bmc.2010.07.041 Unchecked 1
16407991 10.1038/nchembio707 Cathepsin Z 1
16407991 10.1038/nchembio707 Cathepsin B 1
16407991 10.1038/nchembio707 Pro-cathepsin H 1
16407991 10.1038/nchembio707 Cathepsin J 1
16407991 10.1038/nchembio707 Dipeptidyl peptidase 1 1

Data from ChEMBL 36 via Core Engine