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Compound Detail

CHEMBL252454

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Nc1noc2ccc(-n3nc(C(F)(F)F)cc3C(=O)Cc3ccc(-n4ccccc4=O)cc3F)cc12

Basic Information

ChEMBL ID CHEMBL252454
Phase Preclinical
Structure Type MOL
InChI Key BEEPJZYIKKHTQJ-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

497.4
MW (Da)
4.33
ALogP
8
HBA
1
HBD
108.9
PSA (Ų)
0.29
QED
0
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C24H15F4N5O3
MW 497.41
Aromatic Rings 5
Heavy Atoms 36
NP-Likeness -1.51

Activity Summary

Ki 2 meas. best 10.48

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Coagulation factor X
CHEMBL244
Ki 10.48 10.48 0.0 1
Prothrombin
CHEMBL204
Ki 6.46 6.46 349.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Coagulation factor X Ki = 0.033 nM 10.48 Inhibition of human factor 10a 18054227
Prothrombin Ki = 349.0 nM 6.46 Inhibition of human thrombin 18054227

Literature References

PubMed DOI Target Context # Activities
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 Plasma 1
18054227 10.1016/j.bmcl.2007.11.040 Prothrombin 1
18054227 10.1016/j.bmcl.2007.11.040 Caco-2 1

Data from ChEMBL 36 via Core Engine