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Compound Detail

CHEMBL386294

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CCN(CC)Cc1ccccc1-c1ccc(N2CCc3c(C(F)(F)F)nn(-c4ccc5onc(N)c5c4)c3C2=O)cc1

Basic Information

ChEMBL ID CHEMBL386294
Phase Preclinical
Structure Type MOL
InChI Key UKWUFMOOIOETEJ-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

574.6
MW (Da)
6.33
ALogP
7
HBA
1
HBD
93.4
PSA (Ų)
0.24
QED
2
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C31H29F3N6O2
MW 574.61
Aromatic Rings 5
Heavy Atoms 42
NP-Likeness -1.22

Activity Summary

Ki 2 meas. best 9.96

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Coagulation factor X
CHEMBL244
Ki 9.96 9.96 0.1 1
Prothrombin
CHEMBL204
Ki 7.01 7.01 97.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Coagulation factor X Ki = 0.11 nM 9.96 Binding affinity to human F10a 16730984
Prothrombin Ki = 97.0 nM 7.01 Binding affinity to human F2a 16730984

Literature References

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

Data from ChEMBL 36 via Core Engine