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Compound Detail

CHEMBL486112

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C=C=Cc1ccc(-c2ccc(C(=O)NCC(C)C)cc2C(=O)O)c(C(=O)Nc2ccc(C(=N)N)cc2)c1

Basic Information

ChEMBL ID CHEMBL486112
Phase Preclinical
Structure Type MOL
InChI Key MYYPVSMRQLUUCW-UHFFFAOYSA-N
3
Targets
4
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

496.6
MW (Da)
4.77
ALogP
4
HBA
5
HBD
145.4
PSA (Ų)
0.16
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 C29H28N4O4
MW 496.57
Aromatic Rings 3
Heavy Atoms 37
NP-Likeness -0.40

Activity Summary

IC50 4 meas. best 9.25

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Unchecked
CHEMBL612545
IC50 9.25 9.25 0.6 1
Coagulation factor X
CHEMBL244
IC50 8.82 8.82 1.5 1
Prothrombin
CHEMBL204
IC50 7.55 7.55 28.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Unchecked IC50 = 0.56 nM 9.25 Inhibition of trypsin 19409795
Coagulation factor X IC50 = 1.5 nM 8.82 Inhibition of factor 10a 19409795
Prothrombin IC50 = 27.96 nM 7.55 Inhibition of thrombin 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 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