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Compound Detail

CHEMBL271495

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N=C(N)NCCC[C@H](NC(=O)CN1CCCC[C@@H](NS(=O)(=O)Cc2ccccc2)C1=O)C(=O)c1nccs1

Basic Information

ChEMBL ID CHEMBL271495
Phase Preclinical
Structure Type MOL
InChI Key OWESYYYFYGKROZ-RBUKOAKNSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

563.7
MW (Da)
0.57
ALogP
8
HBA
5
HBD
187.4
PSA (Ų)
0.10
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 C24H33N7O5S2
MW 563.71
Aromatic Rings 2
Heavy Atoms 38
NP-Likeness -0.89

Activity Summary

IC50 2 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 1
Prothrombin
CHEMBL204
IC50 7.42 7.42 38.0 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
Prothrombin IC50 = 38.0 nM 7.42 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

Data from ChEMBL 36 via Core Engine