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Compound Detail

CHEMBL252453

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Nc1noc2ccc(-n3nc(C(F)(F)F)cc3C(=O)Cc3ccc(-c4ccccc4CN4CCCC4)cc3)cc12

Basic Information

ChEMBL ID CHEMBL252453
Phase Preclinical
Structure Type MOL
InChI Key AALHKJFWUSBUMO-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

545.6
MW (Da)
6.30
ALogP
7
HBA
1
HBD
90.2
PSA (Ų)
0.24
QED
2
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C30H26F3N5O2
MW 545.56
Aromatic Rings 5
Heavy Atoms 40
NP-Likeness -1.21

Activity Summary

Ki 2 meas. best 9.49

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Coagulation factor X
CHEMBL244
Ki 9.49 9.49 0.3 1
Prothrombin
CHEMBL204
Ki 6.51 6.51 310.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Coagulation factor X Ki = 0.32 nM 9.49 Inhibition of human factor 10a 18054227
Prothrombin Ki = 310.0 nM 6.51 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