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Compound Detail

CHEMBL2028912

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CC[C@H](C)[C@H](NC(=O)NNC(=O)[C@H](Cc1ccc(OC)cc1)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](C)NC(=O)OCc1ccccc1)C(=O)N[C@H](C(=O)OC)C(C)C

Basic Information

ChEMBL ID CHEMBL2028912
Phase Preclinical
Structure Type MOL
InChI Key QZSSZOWDSLCTPA-MAXJAHQXSA-N
3
Targets
3
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

798.0
MW (Da)
2.63
ALogP
10
HBA
7
HBD
231.4
PSA (Ų)
0.08
QED
2
Ro5 Violations
20
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C40H59N7O10
MW 797.95
Aromatic Rings 2
Heavy Atoms 57
NP-Likeness -0.42

Activity Summary

Ki 3 meas. best 9.55

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Papain
CHEMBL4779
Ki 9.55 9.55 0.3 1
Cathepsin B
CHEMBL4072
Ki 8.85 8.85 1.4 1
Cathepsin K
CHEMBL268
Ki 8.07 8.07 8.4 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Papain Ki = 0.28 nM 9.55 In vitro inhibition of papain. 12213061
Cathepsin B Ki = 1.41 nM 8.85 Inhibition of Human Cathepsin B 12213061
Cathepsin K Ki = 8.42 nM 8.07 Inhibition of Human Cathepsin K 12213061

Literature References

PubMed DOI Target Context # Activities
12213061 10.1021/jm020850k Papain 1
12213061 10.1021/jm020850k Cathepsin B 1
12213061 10.1021/jm020850k Cathepsin K 1

Data from ChEMBL 36 via Core Engine