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Compound Detail

CHEMBL488778

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COc1ccc(-c2ccc(C(=O)NCC(C)C)cc2C(=O)O)c(C(=O)Nc2ccc(C(=N)N)cc2)c1

Basic Information

ChEMBL ID CHEMBL488778
Phase Preclinical
Structure Type MOL
InChI Key JVXBUVJQTIKERQ-UHFFFAOYSA-N
5
Targets
5
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

488.5
MW (Da)
3.98
ALogP
5
HBA
5
HBD
154.6
PSA (Ų)
0.23
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 C27H28N4O5
MW 488.54
Aromatic Rings 3
Heavy Atoms 36
NP-Likeness -0.58

Activity Summary

IC50 5 meas. best 10.52

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Coagulation factor VII/tissue factor
CHEMBL2095194
IC50 10.52 10.52 0.0 1
Unchecked
CHEMBL612545
IC50 9.09 9.09 0.8 1
Coagulation factor X
CHEMBL244
IC50 8.18 8.18 6.6 1
Plasminogen
CHEMBL1801
IC50 7.84 7.84 14.4 1
Prothrombin
CHEMBL204
IC50 7.83 7.83 14.9 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Coagulation factor VII/tissue factor IC50 = 0.03 nM 10.52 Inhibition of tissue factor/factor 7a 19409795
Unchecked IC50 = 0.82 nM 9.09 Inhibition of trypsin 19409795
Coagulation factor X IC50 = 6.63 nM 8.18 Inhibition of factor 10a 19409795
Plasminogen IC50 = 14.37 nM 7.84 Inhibition of plasmin 19409795
Prothrombin IC50 = 14.87 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 Coagulation factor X 1
19409795 10.1016/j.bmc.2009.04.013 Plasminogen 1
19409795 10.1016/j.bmc.2009.04.013 Prothrombin 1

Data from ChEMBL 36 via Core Engine