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Compound Detail

CHEMBL4297638

PETESICATIB
🧪 Phase II
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🧪 Phase II
Cn1cc(-c2ccc(S(=O)(=O)[C@@H]3C[C@@H](C(=O)NC4(C#N)CC4)N(C(=O)C4(C(F)(F)F)CC4)C3)c(C(F)(F)F)c2)cn1

Basic Information

ChEMBL ID CHEMBL4297638
Name PETESICATIB
Phase Phase II
Structure Type MOL
InChI Key KXAAIORSMACJSI-AEFFLSMTSA-N

Known Names

Petesicatib RG-7625 Rg7625 RO-5459072 Ro5459072
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
1
Publications
5
Known Names
3
Indications
1
Mechanisms

Molecular Properties

603.5
MW (Da)
3.36
ALogP
7
HBA
1
HBD
125.2
PSA (Ų)
0.51
QED
1
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Chirality Single Enantiomer
USAN Stem -catib
USAN Year 2018

Extended Properties

Molecular Formula C25H23F6N5O4S
MW 603.55
Aromatic Rings 2
Heavy Atoms 41
NP-Likeness -1.22

Mechanism of Action

Mechanism Action Type Target Direct Efficacy
Cathepsin S inhibitor INHIBITOR Cathepsin S

Indications

Sjogren's Syndrome Autoimmune Diseases Celiac Disease

Activity Summary

IC50 1 meas. best 10.0

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Cathepsin S
CHEMBL2954
IC50 10.0 10.0 0.1 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Cathepsin S IC50 = 0.1 nM 10.0 Inhibition of Cathepsin S (unknown origin) 38894911

Literature References

PubMed DOI Target Context # Activities
38894911 10.1021/acsmedchemlett.4c00050 Cathepsin S 1

Data from ChEMBL 36 via Core Engine