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Compound Detail

CHEMBL252649

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COc1ccc(-n2nc(C(F)(F)F)cc2C(=O)Cc2ccc(-c3ccccc3S(N)(=O)=O)cc2)cc1

Basic Information

ChEMBL ID CHEMBL252649
Phase Preclinical
Structure Type MOL
InChI Key PXUONXFJABOVSQ-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

515.5
MW (Da)
4.64
ALogP
6
HBA
1
HBD
104.3
PSA (Ų)
0.36
QED
1
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C25H20F3N3O4S
MW 515.51
Aromatic Rings 4
Heavy Atoms 36
NP-Likeness -1.17

Activity Summary

Ki 1 meas. best 7.92

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Coagulation factor X
CHEMBL244
Ki 7.92 7.92 12.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Coagulation factor X Ki = 12.0 nM 7.92 Inhibition of human factor 10a 18054227

Literature References

PubMed DOI Target Context # Activities
18054227 10.1016/j.bmcl.2007.11.040 Plasma 2
18054227 10.1016/j.bmcl.2007.11.040 Coagulation factor X 1
18054227 10.1016/j.bmcl.2007.11.040 Trypsin 1
18054227 10.1016/j.bmcl.2007.11.040 Prothrombin 1

Data from ChEMBL 36 via Core Engine