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Compound Detail

CHEMBL505455

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CC(C)CNC(=O)c1ccc(-c2ccc(-c3ccco3)cc2C(=O)Nc2ccc(C(=N)N)cc2)c(C(=O)O)c1

Basic Information

ChEMBL ID CHEMBL505455
Phase Preclinical
Structure Type MOL
InChI Key BQDYQUZLQVWWMF-UHFFFAOYSA-N
4
Targets
5
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

524.6
MW (Da)
5.23
ALogP
5
HBA
5
HBD
158.5
PSA (Ų)
0.15
QED
2
Ro5 Violations
9
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C30H28N4O5
MW 524.58
Aromatic Rings 4
Heavy Atoms 39
NP-Likeness -0.74

Activity Summary

IC50 5 meas. best 9.79

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Plasminogen
CHEMBL1801
IC50 9.79 9.79 0.2 1
Unchecked
CHEMBL612545
IC50 9.43 9.43 0.4 1
Coagulation factor X
CHEMBL244
IC50 8.89 8.89 1.3 1
Prothrombin
CHEMBL204
IC50 7.83 7.83 14.7 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Plasminogen IC50 = 0.163 nM 9.79 Inhibition of plasmin 19409795
Unchecked IC50 = 0.37 nM 9.43 Inhibition of trypsin 19409795
Coagulation factor X IC50 = 1.3 nM 8.89 Inhibition of factor 10a 19409795
Prothrombin IC50 = 14.67 nM 7.83 Inhibition of thrombin 19409795

Literature References

PubMed DOI Target Context # Activities
19409795 10.1016/j.bmc.2009.04.013 Unchecked 5
19409795 10.1016/j.bmc.2009.04.013 Coagulation factor VII/tissue factor 1
19409795 10.1016/j.bmc.2009.04.013 Plasminogen 1
19409795 10.1016/j.bmc.2009.04.013 Coagulation factor X 1
19409795 10.1016/j.bmc.2009.04.013 Prothrombin 1

Data from ChEMBL 36 via Core Engine