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Compound Detail

CHEMBL520364

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C=C(C)c1ccc(-c2ccc(C(=O)NCC(C)C)cc2C(=O)O)c(C(=O)Nc2ccc(C(=N)N)cc2)c1

Basic Information

ChEMBL ID CHEMBL520364
Phase Preclinical
Structure Type MOL
InChI Key DKFBIZDHPKUBIT-UHFFFAOYSA-N
5
Targets
5
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

498.6
MW (Da)
5.01
ALogP
4
HBA
5
HBD
145.4
PSA (Ų)
0.21
QED
1
Ro5 Violations
9
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C29H30N4O4
MW 498.58
Aromatic Rings 3
Heavy Atoms 37
NP-Likeness -0.37

Activity Summary

IC50 5 meas. best 10.89

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Coagulation factor VII/tissue factor
CHEMBL2095194
IC50 10.89 10.89 0.0 1
Plasminogen
CHEMBL1801
IC50 10.15 10.15 0.1 1
Unchecked
CHEMBL612545
IC50 9.28 9.28 0.5 1
Coagulation factor X
CHEMBL244
IC50 8.93 8.93 1.2 1
Prothrombin
CHEMBL204
IC50 7.75 7.75 17.9 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Coagulation factor VII/tissue factor IC50 = 0.013 nM 10.89 Inhibition of tissue factor/factor 7a 19409795
Plasminogen IC50 = 0.07 nM 10.15 Inhibition of plasmin 19409795
Unchecked IC50 = 0.53 nM 9.28 Inhibition of trypsin 19409795
Coagulation factor X IC50 = 1.17 nM 8.93 Inhibition of factor 10a 19409795
Prothrombin IC50 = 17.9 nM 7.75 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