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Compound Detail

CHEMBL524732

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CC(C)CNC(=O)c1ccc(-c2ccc(Cc3ccccc3)cc2C(=O)Nc2ccc(C(=N)N)cc2)c(C(=O)O)c1

Basic Information

ChEMBL ID CHEMBL524732
Phase Preclinical
Structure Type MOL
InChI Key GEJPIBYDWDPPLK-UHFFFAOYSA-N
5
Targets
5
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

548.6
MW (Da)
5.56
ALogP
4
HBA
5
HBD
145.4
PSA (Ų)
0.13
QED
2
Ro5 Violations
10
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C33H32N4O4
MW 548.64
Aromatic Rings 4
Heavy Atoms 41
NP-Likeness -0.52

Activity Summary

IC50 5 meas. best 10.68

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Coagulation factor VII/tissue factor
CHEMBL2095194
IC50 10.68 10.68 0.0 1
Unchecked
CHEMBL612545
IC50 9.24 9.24 0.6 1
Plasminogen
CHEMBL1801
IC50 9.18 9.18 0.7 1
Coagulation factor X
CHEMBL244
IC50 8.76 8.76 1.8 1
Prothrombin
CHEMBL204
IC50 8.07 8.07 8.5 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Coagulation factor VII/tissue factor IC50 = 0.021 nM 10.68 Inhibition of tissue factor/factor 7a 19409795
Unchecked IC50 = 0.57 nM 9.24 Inhibition of trypsin 19409795
Plasminogen IC50 = 0.656 nM 9.18 Inhibition of plasmin 19409795
Coagulation factor X IC50 = 1.75 nM 8.76 Inhibition of factor 10a 19409795
Prothrombin IC50 = 8.51 nM 8.07 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