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Compound Detail

CHEMBL500948

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CCCc1ccc(-c2ccc(C(=O)NCC(C)C)cc2C(=O)O)c(C(=O)Nc2ccc(C(=N)N)cc2)c1

Basic Information

ChEMBL ID CHEMBL500948
Phase Preclinical
Structure Type MOL
InChI Key NDXKHAPOIIBQOC-UHFFFAOYSA-N
4
Targets
4
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

500.6
MW (Da)
4.93
ALogP
4
HBA
5
HBD
145.4
PSA (Ų)
0.20
QED
1
Ro5 Violations
10
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C29H32N4O4
MW 500.60
Aromatic Rings 3
Heavy Atoms 37
NP-Likeness -0.55

Activity Summary

IC50 4 meas. best 10.04

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Coagulation factor VII/tissue factor
CHEMBL2095194
IC50 10.04 10.04 0.1 1
Prothrombin
CHEMBL204
IC50 7.4 7.4 39.6 1
Unchecked
CHEMBL612545
IC50 7.38 7.38 41.4 1
Coagulation factor X
CHEMBL244
IC50 7.34 7.34 46.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Coagulation factor VII/tissue factor IC50 = 0.092 nM 10.04 Inhibition of tissue factor/factor 7a 19409795
Prothrombin IC50 = 39.57 nM 7.4 Inhibition of thrombin 19409795
Unchecked IC50 = 41.38 nM 7.38 Inhibition of trypsin 19409795
Coagulation factor X IC50 = 46.05 nM 7.34 Inhibition of factor 10a 19409795

Literature References

PubMed DOI Target Context # Activities
19409795 10.1016/j.bmc.2009.04.013 Unchecked 4
19409795 10.1016/j.bmc.2009.04.013 Coagulation factor VII/tissue factor 1
19409795 10.1016/j.bmc.2009.04.013 Prothrombin 1
19409795 10.1016/j.bmc.2009.04.013 Coagulation factor X 1
19409795 10.1016/j.bmc.2009.04.013 Plasminogen 1

Data from ChEMBL 36 via Core Engine