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Compound Detail

CHEMBL2028913

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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](Cc1c[nH]c2ccccc12)C(=O)N[C@H](C(=O)N[C@@H](C)C(N)=O)C(C)C)C(C)C

Basic Information

ChEMBL ID CHEMBL2028913
Phase Preclinical
Structure Type MOL
InChI Key TXGCKASBHJKJOM-RQNOWEOFSA-N
3
Targets
3
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

934.1
MW (Da)
0.56
ALogP
10
HBA
12
HBD
348.2
PSA (Ų)
0.03
QED
2
Ro5 Violations
24
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C45H67N13O9
MW 934.11
Aromatic Rings 3
Heavy Atoms 67
NP-Likeness -0.18

Activity Summary

Ki 3 meas. best 7.37

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Cathepsin B
CHEMBL4072
Ki 7.37 7.37 43.0 1
Cathepsin K
CHEMBL268
Ki 7.0 7.0 100.0 1
Papain
CHEMBL4779
Ki 7.0 7.0 100.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Cathepsin B Ki = 43.0 nM 7.37 Inhibition of Human Cathepsin B 12213061
Papain Ki = 100.0 nM 7.0 In vitro inhibition of papain. 12213061
Cathepsin K Ki = 100.0 nM 7.0 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