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Compound Detail

CHEMBL253297

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Nc1noc2ccc(-n3nc(C(F)(F)F)cc3C(=O)Cc3ccc(-c4ccccc4S(N)(=O)=O)cc3F)cc12

Basic Information

ChEMBL ID CHEMBL253297
Phase Preclinical
Structure Type MOL
InChI Key GBJUQIHMJNTHNS-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

559.5
MW (Da)
4.49
ALogP
8
HBA
2
HBD
147.1
PSA (Ų)
0.23
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 C25H17F4N5O4S
MW 559.50
Aromatic Rings 5
Heavy Atoms 39
NP-Likeness -1.45

Activity Summary

Ki 1 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

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 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 Caco-2 1

Data from ChEMBL 36 via Core Engine