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Compound Detail

CHEMBL221377

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COc1ccc(-n2nc(C(F)(F)F)c3c2C(=O)N(c2ccc(-c4ccccc4S(C)(=O)=O)cc2)CC3)c(C(N)=O)c1

Basic Information

ChEMBL ID CHEMBL221377
Phase Preclinical
Structure Type MOL
InChI Key JXDVPMIGKXIRMQ-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

584.6
MW (Da)
4.27
ALogP
7
HBA
1
HBD
124.6
PSA (Ų)
0.36
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 C28H23F3N4O5S
MW 584.58
Aromatic Rings 4
Heavy Atoms 41
NP-Likeness -1.16

Activity Summary

Ki 1 meas. best 9.74

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Coagulation factor X
CHEMBL244
Ki 9.74 9.74 0.2 1

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

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

Data from ChEMBL 36 via Core Engine