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Compound Detail

CHEMBL2028909

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

Basic Information

ChEMBL ID CHEMBL2028909
Phase Preclinical
Structure Type MOL
InChI Key OILQRSUIXCAKPE-GKKOWRRISA-N
3
Targets
3
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

747.9
MW (Da)
-0.65
ALogP
9
HBA
10
HBD
303.4
PSA (Ų)
0.03
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 C34H57N11O8
MW 747.90
Aromatic Rings 1
Heavy Atoms 53
NP-Likeness -0.20

Activity Summary

Ki 3 meas. best 9.92

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Cathepsin B
CHEMBL4072
Ki 9.92 9.92 0.1 1
Papain
CHEMBL4779
Ki 9.25 9.25 0.6 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 = 0.12 nM 9.92 Inhibition of Human Cathepsin B 12213061
Papain Ki = 0.56 nM 9.25 In vitro inhibition of papain. 12213061
Cathepsin K Ki = 2.13 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