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Compound Detail

CHEMBL438435

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CC(C)C[C@H](NC(=O)c1cc2ccccc2o1)C(=O)N[C@H]1C[C@@H](C)CN(S(=O)(=O)c2ccccn2)CC1=O

Basic Information

ChEMBL ID CHEMBL438435
Phase Preclinical
Structure Type MOL
InChI Key MCKCVIDASJTQSU-GIVPXCGWSA-N
3
Targets
3
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

540.6
MW (Da)
2.76
ALogP
7
HBA
2
HBD
138.7
PSA (Ų)
0.45
QED
1
Ro5 Violations
8
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C27H32N4O6S
MW 540.64
Aromatic Rings 3
Heavy Atoms 38
NP-Likeness -0.86

Activity Summary

Ki 3 meas. best 7.54

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Cathepsin K
CHEMBL268
Ki 7.54 7.54 29.0 1
Procathepsin L
CHEMBL3837
Ki 6.8 6.8 160.0 1
Cathepsin S
CHEMBL2954
Ki 6.46 6.46 350.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Cathepsin K Ki = 29.0 nM 7.54 Inhibition of human cathepsin K 16509577
Procathepsin L Ki = 160.0 nM 6.8 Inhibition of human cathepsin L 16509577
Cathepsin S Ki = 350.0 nM 6.46 Inhibition of human cathepsin S 16509577

Literature References

PubMed DOI Target Context # Activities
16509577 10.1021/jm050915u Cathepsin K 2
16509577 10.1021/jm050915u Cathepsin B 1
16509577 10.1021/jm050915u Procathepsin L 1
16509577 10.1021/jm050915u Cathepsin L2 1
16509577 10.1021/jm050915u Cathepsin S 1

Data from ChEMBL 36 via Core Engine