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Compound Detail

CHEMBL485704

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C=Cc1ccc(-c2ccc(C(=O)NCC(C)C)cc2C(=O)O)c(C(=O)Nc2ccc(C(=N)N)cc2)c1

Basic Information

ChEMBL ID CHEMBL485704
Phase Preclinical
Structure Type MOL
InChI Key FCTCJAGJUHHZDO-UHFFFAOYSA-N
3
Targets
4
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

484.6
MW (Da)
4.62
ALogP
4
HBA
5
HBD
145.4
PSA (Ų)
0.22
QED
0
Ro5 Violations
9
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C28H28N4O4
MW 484.56
Aromatic Rings 3
Heavy Atoms 36
NP-Likeness -0.40

Activity Summary

IC50 4 meas. best 9.33

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Unchecked
CHEMBL612545
IC50 9.33 9.33 0.5 1
Coagulation factor X
CHEMBL244
IC50 8.78 8.78 1.6 1
Prothrombin
CHEMBL204
IC50 8.03 8.03 9.4 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Unchecked IC50 = 0.47 nM 9.33 Inhibition of trypsin 19409795
Coagulation factor X IC50 = 1.65 nM 8.78 Inhibition of factor 10a 19409795
Prothrombin IC50 = 9.4 nM 8.03 Inhibition of thrombin 19409795

Literature References

PubMed DOI Target Context # Activities
19409795 10.1016/j.bmc.2009.04.013 Unchecked 4
19409795 10.1016/j.bmc.2009.04.013 Coagulation factor VII/tissue factor 1
19409795 10.1016/j.bmc.2009.04.013 Coagulation factor X 1
19409795 10.1016/j.bmc.2009.04.013 Prothrombin 1
19409795 10.1016/j.bmc.2009.04.013 Plasminogen 1

Data from ChEMBL 36 via Core Engine