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Compound Detail

CHEMBL4228926

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CC(C)C[C@H](NC(=O)c1ccc(-c2ccccc2)cc1)C(=O)NC1(C#N)CCS(=O)(=O)CC1

Basic Information

ChEMBL ID CHEMBL4228926
Phase Preclinical
Structure Type MOL
InChI Key ULFKHVBAISSIOJ-QFIPXVFZSA-N
5
Targets
5
Activities
1
Assay Types
0
PK Parameters
6
Publications
0
Known Names

Molecular Properties

467.6
MW (Da)
3.09
ALogP
5
HBA
2
HBD
116.1
PSA (Ų)
0.65
QED
0
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C25H29N3O4S
MW 467.59
Aromatic Rings 2
Heavy Atoms 33
NP-Likeness -0.93

Activity Summary

IC50 5 meas. best 9.96

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Cathepsin K
CHEMBL268
IC50 9.96 9.96 0.1 1
Cathepsin S
CHEMBL2954
IC50 8.96 8.96 1.1 1
Falcipain 2
CHEMBL5800
IC50 8.1 8.1 8.0 1
Procathepsin L
CHEMBL3837
IC50 7.0 7.0 99.0 1
Cathepsin B
CHEMBL4072
IC50 5.6 5.6 2500.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
29615344 10.1016/j.bmcl.2018.03.069 Cathepsin S 1
29615344 10.1016/j.bmcl.2018.03.069 Procathepsin L 1
29615344 10.1016/j.bmcl.2018.03.069 Cathepsin K 1
29615344 10.1016/j.bmcl.2018.03.069 Cathepsin B 1
29615344 10.1016/j.bmcl.2018.03.069 Falcipain 2 1
29615344 10.1016/j.bmcl.2018.03.069 Plasmodium falciparum 1

Data from ChEMBL 36 via Core Engine