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Compound Detail

CHEMBL5560415

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CC(=O)N[C@H]1Cc2ccc(cc2)OC/C=C\C[C@@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)c2nc3ccccc3s2)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O

Basic Information

ChEMBL ID CHEMBL5560415
Phase Preclinical
Structure Type MOL
InChI Key ZLIIZOMJAUACIT-BEJXXSQMSA-N
6
Targets
6
Activities
1
Assay Types
0
PK Parameters
6
Publications
0
Known Names

Molecular Properties

791.9
MW (Da)
3.01
ALogP
9
HBA
8
HBD
233.3
PSA (Ų)
0.03
QED
2
Ro5 Violations
11
Rot. Bonds

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C41H45N9O6S
MW 791.94
Aromatic Rings 5
Heavy Atoms 57
NP-Likeness 0.44

Activity Summary

IC50 6 meas. best 9.16

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Serine protease hepsin
CHEMBL2079849
IC50 9.16 9.16 0.7 1
Transmembrane protease serine 2
CHEMBL1795140
IC50 9.01 9.01 1.0 1
Hepatocyte growth factor activator
CHEMBL3351190
IC50 8.34 8.34 4.6 1
Suppressor of tumorigenicity 14 protein
CHEMBL3018
IC50 8.24 8.24 5.7 1
Prothrombin
CHEMBL204
IC50 5.87 5.87 1360.0 1
Coagulation factor X
CHEMBL244
IC50 4.7 4.7 19900.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
38477709 10.1021/acs.jmedchem.3c02388 Coagulation factor X 1
38477709 10.1021/acs.jmedchem.3c02388 Transmembrane protease serine 2 1
38477709 10.1021/acs.jmedchem.3c02388 Hepatocyte growth factor activator 1
38477709 10.1021/acs.jmedchem.3c02388 Suppressor of tumorigenicity 14 protein 1
38477709 10.1021/acs.jmedchem.3c02388 Serine protease hepsin 1
38477709 10.1021/acs.jmedchem.3c02388 Prothrombin 1

Data from ChEMBL 36 via Core Engine