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Compound Detail

CHEMBL257068

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N=C(N)NCCC[C@H](NC(=O)Cn1cccc(NS(=O)(=O)Cc2ccccc2)c1=O)C(=O)c1nccs1

Basic Information

ChEMBL ID CHEMBL257068
Phase Preclinical
Structure Type MOL
InChI Key OXNRBEMASLTOMU-KRWDZBQOSA-N
2
Targets
3
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

545.6
MW (Da)
0.88
ALogP
9
HBA
5
HBD
189.1
PSA (Ų)
0.09
QED
1
Ro5 Violations
13
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C23H27N7O5S2
MW 545.65
Aromatic Rings 3
Heavy Atoms 37
NP-Likeness -1.23

Activity Summary

IC50 3 meas. best 8.52

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Coagulation factor X
CHEMBL244
IC50 8.52 8.52 3.0 2
Prothrombin
CHEMBL204
IC50 8.1 8.1 8.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Coagulation factor X IC50 = 3.0 nM 8.52 Inhibition of human factor 10a 18053726
Coagulation factor X IC50 = 3.0 nM 8.52 Inhibition of factor 10a 20503967
Prothrombin IC50 = 8.0 nM 8.1 Inhibition of human alpha-thrombin 18053726

Literature References

PubMed DOI Target Context # Activities
18053726 10.1016/j.bmc.2007.11.015 Coagulation factor X 1
18053726 10.1016/j.bmc.2007.11.015 Prothrombin 1
20503967 10.1021/jm100146h Coagulation factor X 1

Data from ChEMBL 36 via Core Engine