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Compound Detail

CHEMBL402167

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COc1ccc(-n2nc(C(F)(F)F)cc2C(=O)Cc2ccc(-c3ccccc3CN3CC[C@H](O)C3)cc2)cc1

Basic Information

ChEMBL ID CHEMBL402167
Phase Preclinical
Structure Type MOL
InChI Key MHMSYXOVNQSRJW-DEOSSOPVSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

535.6
MW (Da)
5.56
ALogP
6
HBA
1
HBD
67.6
PSA (Ų)
0.30
QED
2
Ro5 Violations
8
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C30H28F3N3O3
MW 535.57
Aromatic Rings 4
Heavy Atoms 39
NP-Likeness -1.01

Activity Summary

Ki 1 meas. best 8.48

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Coagulation factor X
CHEMBL244
Ki 8.48 8.48 3.3 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Coagulation factor X Ki = 3.3 nM 8.48 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