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Compound Detail

CHEMBL2028911

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

Basic Information

ChEMBL ID CHEMBL2028911
Phase Preclinical
Structure Type MOL
InChI Key HGMOIJOFHZHWKH-ZQGXUALKSA-N
3
Targets
3
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

733.9
MW (Da)
2.42
ALogP
9
HBA
7
HBD
222.2
PSA (Ų)
0.08
QED
2
Ro5 Violations
19
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C36H59N7O9
MW 733.91
Aromatic Rings 1
Heavy Atoms 52
NP-Likeness -0.43

Activity Summary

Ki 3 meas. best 9.52

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Cathepsin B
CHEMBL4072
Ki 9.52 9.52 0.3 1
Papain
CHEMBL4779
Ki 9.02 9.02 0.9 1
Cathepsin K
CHEMBL268
Ki 8.67 8.67 2.1 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Cathepsin B Ki = 0.3 nM 9.52 Inhibition of Human Cathepsin B 12213061
Papain Ki = 0.95 nM 9.02 In vitro inhibition of papain. 12213061
Cathepsin K Ki = 2.12 nM 8.67 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