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Compound Detail

CHEMBL3734777

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CC(C)C[C@@H]1NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](C)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](N)CSSC[C@@H](C(=O)O)NC(=O)[C@H](CC(=O)O)NC1=O

Basic Information

ChEMBL ID CHEMBL3734777
Phase Preclinical
Structure Type BOTH
InChI Key RTBBZNOSANWPBI-ZPJKPQIISA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
10
Publications
0
Known Names

Molecular Properties

1188.3
MW (Da)

Drug Information

Molecule Type Protein
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C51H73N13O16S2
MW 1188.35

Activity Summary

Ki 2 meas. best 6.26

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Urokinase-type plasminogen activator
CHEMBL1075311
Ki 6.26 6.26 550.0 1
Serine protease 1
CHEMBL3769
Ki 4.68 4.68 20700.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
26536069 10.1021/acs.jmedchem.5b01128 Urokinase-type plasminogen activator 4
26536069 10.1021/acs.jmedchem.5b01128 Plasma kallikrein 3
26536069 10.1021/acs.jmedchem.5b01128 Plasminogen 2
26536069 10.1021/acs.jmedchem.5b01128 Prothrombin 2
26536069 10.1021/acs.jmedchem.5b01128 Tissue-type plasminogen activator 2
26536069 10.1021/acs.jmedchem.5b01128 Serine protease 1 1
26536069 10.1021/acs.jmedchem.5b01128 Coagulation factor XI 1
26536069 10.1021/acs.jmedchem.5b01128 Kallikrein-1 1
26536069 10.1021/acs.jmedchem.5b01128 Vitamin K-dependent protein C 1
26536069 10.1021/acs.jmedchem.5b01128 Suppressor of tumorigenicity 14 protein 1

Data from ChEMBL 36 via Core Engine