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Compound Detail

CHEMBL591726

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CS(=O)(=O)c1ccccc1-c1ccc(NC(=O)c2cc(C(F)(F)F)nn2-c2cccc(-c3nnc(N)[nH]3)c2)c(F)c1

Basic Information

ChEMBL ID CHEMBL591726
Phase Preclinical
Structure Type MOL
InChI Key LTKOHQXJXXVPDR-UHFFFAOYSA-N
3
Targets
3
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

585.5
MW (Da)
4.72
ALogP
8
HBA
3
HBD
148.7
PSA (Ų)
0.24
QED
1
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C26H19F4N7O3S
MW 585.54
Aromatic Rings 5
Heavy Atoms 41
NP-Likeness -1.71

Activity Summary

Ki 3 meas. best 7.82

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Coagulation factor X
CHEMBL244
Ki 7.82 7.82 15.0 1
Trypsin
CHEMBL2095204
Ki 6.8 6.8 160.0 1
Prothrombin
CHEMBL204
Ki 5.31 5.31 4900.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Coagulation factor X Ki = 15.0 nM 7.82 Inhibition of human factor 10a 20100660
Trypsin Ki = 160.0 nM 6.8 Inhibition of human trypsin 20100660
Prothrombin Ki = 4900.0 nM 5.31 Inhibition of human factor 2a 20100660

Literature References

PubMed DOI Target Context # Activities
20100660 10.1016/j.bmcl.2010.01.011 Coagulation factor X 1
20100660 10.1016/j.bmcl.2010.01.011 Prothrombin 1
20100660 10.1016/j.bmcl.2010.01.011 Trypsin 1

Data from ChEMBL 36 via Core Engine