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Compound Detail

CHEMBL212770

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CN(C)Cc1ccccc1-c1ccc(N2CNc3c(C(F)(F)F)nn(-c4ccc5onc(N)c5c4)c3C2=O)cc1

Basic Information

ChEMBL ID CHEMBL212770
Phase Preclinical
Structure Type MOL
InChI Key WNKVDNSACGSTII-UHFFFAOYSA-N
1
Targets
2
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

547.5
MW (Da)
5.37
ALogP
8
HBA
2
HBD
105.5
PSA (Ų)
0.30
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 C28H24F3N7O2
MW 547.54
Aromatic Rings 5
Heavy Atoms 40
NP-Likeness -1.06

Activity Summary

Ki 2 meas. best 9.6

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Coagulation factor X
CHEMBL244
Ki 9.6 9.6 0.2 2

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Coagulation factor X Ki = 0.25 nM 9.6 Binding affinity to human F10a 16730984
Coagulation factor X Ki = 0.25 nM 9.6 Binding affinity to human f10a 16870435

Literature References

PubMed DOI Target Context # Activities
16870435 10.1016/j.bmcl.2006.07.002 Coagulation factor X 2
16730984 10.1016/j.bmcl.2006.02.069 Coagulation factor VII/tissue factor 1
16730984 10.1016/j.bmcl.2006.02.069 Coagulation factor X 1
16870435 10.1016/j.bmcl.2006.07.002 Coagulation factor VII/tissue factor 1

Data from ChEMBL 36 via Core Engine