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Compound Detail

CHEMBL3143135

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

Basic Information

ChEMBL ID CHEMBL3143135
Phase Preclinical
Structure Type MOL
InChI Key QYEUFPXQJIQXLI-QKDODKLFSA-N
3
Targets
3
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

611.7
MW (Da)
3.57
ALogP
7
HBA
5
HBD
164.0
PSA (Ų)
0.16
QED
1
Ro5 Violations
14
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C32H45N5O7
MW 611.74
Aromatic Rings 2
Heavy Atoms 44
NP-Likeness -0.54

Activity Summary

Ki 3 meas. best 8.17

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Papain
CHEMBL4779
Ki 8.17 8.17 6.7 1
Cathepsin K
CHEMBL268
Ki 7.47 7.47 34.0 1
Cathepsin B
CHEMBL4072
Ki 7.4 7.4 40.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Papain Ki = 6.7 nM 8.17 In vitro inhibition of papain. 12213061
Cathepsin K Ki = 34.0 nM 7.47 Inhibition of Human Cathepsin K 12213061
Cathepsin B Ki = 40.0 nM 7.4 Inhibition of Human Cathepsin B 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