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Compound Detail

CHEMBL2028919

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CC[C@H](C)[C@H](NC(=O)NNC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](C)NC(=O)OCc1ccccc1)C(=O)N[C@H](C(=O)NCc1ccccc1)C(C)C

Basic Information

ChEMBL ID CHEMBL2028919
Phase Preclinical
Structure Type MOL
InChI Key XSXSYDVWNYPPNF-QJPNOCDPSA-N
3
Targets
3
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

809.0
MW (Da)
3.57
ALogP
8
HBA
8
HBD
225.0
PSA (Ų)
0.09
QED
2
Ro5 Violations
21
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C42H64N8O8
MW 809.02
Aromatic Rings 2
Heavy Atoms 58
NP-Likeness -0.57

Activity Summary

Ki 3 meas. best 9.6

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Cathepsin B
CHEMBL4072
Ki 9.6 9.6 0.2 1
Papain
CHEMBL4779
Ki 8.87 8.87 1.4 1
Cathepsin K
CHEMBL268
Ki 8.61 8.61 2.5 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Cathepsin B Ki = 0.25 nM 9.6 Inhibition of Human Cathepsin B 12213061
Papain Ki = 1.35 nM 8.87 In vitro inhibition of papain. 12213061
Cathepsin K Ki = 2.45 nM 8.61 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