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Compound Detail

CHEMBL526193

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C=C(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 CHEMBL526193
Phase Preclinical
Structure Type MOL
InChI Key JFLGQUGULDSYQV-WAYWQWQTSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

524.6
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 C31H32N4O4
MW 524.62
Aromatic Rings 3
Heavy Atoms 39
NP-Likeness -0.08

Activity Summary

IC50 2 meas. best 9.89

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Coagulation factor VII/tissue factor
CHEMBL2095194
IC50 9.89 9.89 0.1 1
Coagulation factor X
CHEMBL244
IC50 9.51 9.51 0.3 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Coagulation factor VII/tissue factor IC50 = 0.13 nM 9.89 Inhibition of tissue factor/factor 7a 19409795
Coagulation factor X IC50 = 0.31 nM 9.51 Inhibition of factor 10a 19409795

Literature References

PubMed DOI Target Context # Activities
19409795 10.1016/j.bmc.2009.04.013 Unchecked 2
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