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Compound Detail

CHEMBL425512

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Nc1noc2ccc(-n3nc(C(F)(F)F)cc3C(=O)Nc3ccc(-c4ccccc4S(N)(=O)=O)cc3F)cc12

Basic Information

ChEMBL ID CHEMBL425512
Phase Preclinical
Structure Type MOL
InChI Key QYJVSZKTSGFHME-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

560.5
MW (Da)
4.32
ALogP
8
HBA
3
HBD
159.1
PSA (Ų)
0.27
QED
1
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C24H16F4N6O4S
MW 560.49
Aromatic Rings 5
Heavy Atoms 39
NP-Likeness -1.80

Activity Summary

Ki 2 meas. best 9.8

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Coagulation factor X
CHEMBL244
Ki 9.8 9.8 0.2 1
Prothrombin
CHEMBL204
Ki 5.64 5.64 2300.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Coagulation factor X Ki = 0.16 nM 9.8 Binding affinity against human Coagulation factor Xa 15771420
Prothrombin Ki = 2300.0 nM 5.64 Binding affinity against human thrombin 15771420

Literature References

PubMed DOI Target Context # Activities
15771420 10.1021/jm0497949 Coagulation factor X 1
15771420 10.1021/jm0497949 Prothrombin 1
15771420 10.1021/jm0497949 Serine protease 1 1
15771420 10.1021/jm0497949 Caco-2 1
15771420 10.1021/jm0497949 ADMET 1

Data from ChEMBL 36 via Core Engine