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Compound Detail

CHEMBL57836

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CC(C)C[C@H](NC(=O)OCc1ccccc1)C(=O)NNC(=O)c1csc([C@H](CC(C)C)NC(=O)OCc2ccccc2)n1

Basic Information

ChEMBL ID CHEMBL57836
Phase Preclinical
Structure Type MOL
InChI Key FNMSKYFYFLZDOO-DQEYMECFSA-N
3
Targets
5
Activities
1
Assay Types
0
PK Parameters
6
Publications
0
Known Names

Molecular Properties

609.8
MW (Da)
5.26
ALogP
8
HBA
4
HBD
147.8
PSA (Ų)
0.19
QED
2
Ro5 Violations
13
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C31H39N5O6S
MW 609.75
Aromatic Rings 3
Heavy Atoms 43
NP-Likeness -0.89

Activity Summary

Ki 5 meas. best 8.0

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Cathepsin K
CHEMBL268
Ki 8.0 8.0 10.0 3
Procathepsin L
CHEMBL3837
Ki 6.16 6.16 700.0 1
Cathepsin B
CHEMBL4072
Ki 5.28 5.28 5200.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
10450951 10.1016/s0960-894x(99)00322-4 Cathepsin K 1
10669559 10.1021/jm990412m Cathepsin K 1
10669559 10.1021/jm990412m Procathepsin L 1
10669559 10.1021/jm990412m Cathepsin B 1
10669559 10.1021/jm990412m Cathepsin S 1
23350811 10.1021/jm3013932 Cathepsin K 1

Data from ChEMBL 36 via Core Engine