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Compound Detail

CHEMBL221913

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COc1ccc(-n2nc(C(F)(F)F)c3c2C(=O)N(c2ccc(-c4ccccc4S(C)(=O)=O)cc2)CC3)cc1

Basic Information

ChEMBL ID CHEMBL221913
Phase Preclinical
Structure Type MOL
InChI Key STFFBDBZIZWAQU-UHFFFAOYSA-N
1
Targets
2
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

541.5
MW (Da)
5.17
ALogP
6
HBA
0
HBD
81.5
PSA (Ų)
0.35
QED
2
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C27H22F3N3O4S
MW 541.55
Aromatic Rings 4
Heavy Atoms 38
NP-Likeness -1.16

Activity Summary

Ki 2 meas. best 9.74

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Coagulation factor X
CHEMBL244
Ki 9.74 9.72 0.2 2

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Coagulation factor X Ki = 0.18 nM 9.74 Binding affinity to human factor Xa 16963264
Coagulation factor X Ki = 0.1995 nM 9.7 Inhibition of human factor 10a 21443196

Literature References

PubMed DOI Target Context # Activities
16963264 10.1016/j.bmcl.2006.08.027 Coagulation factor X 1
16963264 10.1016/j.bmcl.2006.08.027 Plasma 1
21443196 10.1021/jm200026b Coagulation factor X 1

Data from ChEMBL 36 via Core Engine