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Compound Detail

CHEMBL4077874

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CCCCC1NC(=O)[C@@H]2CSSC[C@H](NC(=O)[C@H]([C@@H](C)CC)NC(=O)[C@@H]3CCCN3C(=O)[C@@H]3CCCN3C(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@H](Cc3ccccc3)NC1=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(N)=O)C(=O)NCC(=O)N[C@@H]([C@@H](C)O)C(=O)N2

Basic Information

ChEMBL ID CHEMBL4077874
Phase Preclinical
Structure Type MOL
InChI Key XJSYOUCCGOVDMT-RUPHBNGTSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
1
Publications
0
Known Names

Molecular Properties

1504.8
MW (Da)

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C69H97N15O19S2
MW 1504.76

Activity Summary

Ki 1 meas. best 8.96

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Cathepsin G
CHEMBL4071
Ki 8.96 8.96 1.1 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Cathepsin G Ki = 1.1 nM 8.96 Inhibition of human cathepsin G using Suc-AAPF-MCA as substrate after 30 mins 28045523

Literature References

PubMed DOI Target Context # Activities
28045523 10.1021/acs.jmedchem.6b01509 Cathepsin G 1

Data from ChEMBL 36 via Core Engine