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Compound Detail

CHEMBL380431

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C[N+]1(Cc2ccccc2-c2ccc(NC(=O)c3cc(C(F)(F)F)nn3-c3ccc4onc(N)c4c3)c(F)c2)CCOCC1.[Br-]

Basic Information

ChEMBL ID CHEMBL380431
Phase Preclinical
Structure Type MOL
InChI Key GCOAXUDFACWINY-UHFFFAOYSA-N
Parent Compound CHEMBL1184957
Active Moiety CHEMBL1184957
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

595.6
MW (Da)
5.65
ALogP
7
HBA
2
HBD
108.2
PSA (Ų)
0.19
QED
2
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C30H27BrF4N6O3
MW 675.48
Aromatic Rings 5
Heavy Atoms 43
NP-Likeness -1.39

Activity Summary

Ki 1 meas. best 10.7

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Coagulation factor X
CHEMBL244
Ki 10.7 10.7 0.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Coagulation factor X Ki = 0.02 nM 10.7 Binding affinity to human factor 10a 16434195

Literature References

PubMed DOI Target Context # Activities
16434195 10.1016/j.bmcl.2006.01.010 Coagulation factor X 1
16434195 10.1016/j.bmcl.2006.01.010 Caco-2 1
16434195 10.1016/j.bmcl.2006.01.010 NON-PROTEIN TARGET 1

Data from ChEMBL 36 via Core Engine