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Compound Detail

CHEMBL113805

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CC(C)C[C@H](C(=O)NCC(=O)CNS(=O)(=O)c1ccc(Oc2ccccc2)cc1)c1cccc(-c2ccccc2)c1

Basic Information

ChEMBL ID CHEMBL113805
Phase Preclinical
Structure Type MOL
InChI Key CNLHZZCRCBTRHI-YTTGMZPUSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

570.7
MW (Da)
5.94
ALogP
5
HBA
2
HBD
101.6
PSA (Ų)
0.21
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 C33H34N2O5S
MW 570.71
Aromatic Rings 4
Heavy Atoms 41
NP-Likeness -0.57

Activity Summary

Ki 2 meas. best 8.85

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Cathepsin K
CHEMBL268
Ki 8.85 8.85 1.4 1
Cathepsin S
CHEMBL2954
Ki 6.04 6.04 910.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Cathepsin K Ki = 1.4 nM 8.85 The apparent binding affinity against cathepsin K. 10669559
Cathepsin S Ki = 910.0 nM 6.04 The apparent binding affinity against cathepsin S. 10669559

Literature References

PubMed DOI Target Context # Activities
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

Data from ChEMBL 36 via Core Engine