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Compound Detail

CHEMBL434521

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N=C(N)c1cccc(-n2nc(C(F)(F)F)cc2C(=O)Nc2ccc(-n3cnc4cc([N+](=O)[O-])ccc43)cc2F)c1

Basic Information

ChEMBL ID CHEMBL434521
Phase Preclinical
Structure Type MOL
InChI Key WUSRGHHERUYXLJ-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

552.5
MW (Da)
4.81
ALogP
8
HBA
3
HBD
157.8
PSA (Ų)
0.09
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 C25H16F4N8O3
MW 552.45
Aromatic Rings 5
Heavy Atoms 40
NP-Likeness -2.05

Activity Summary

Ki 2 meas. best 10.1

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Coagulation factor X
CHEMBL244
Ki 10.1 10.1 0.1 1
Coagulation factor IX
CHEMBL2016
Ki 7.96 7.96 11.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Coagulation factor X Ki = 0.08 nM 10.1 Binding affinity towards human factor Xa 15454208
Coagulation factor IX Ki = 11.0 nM 7.96 Binding affinity towards human factor IXa 15454208

Literature References

PubMed DOI Target Context # Activities
15454208 10.1016/j.bmcl.2004.08.034 Coagulation factor IX 1
15454208 10.1016/j.bmcl.2004.08.034 Coagulation factor X 1
15454208 10.1016/j.bmcl.2004.08.034 Coagulation factor IX and X 1

Data from ChEMBL 36 via Core Engine