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Compound Detail

CHEMBL592401

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CN(C)Cc1ccccc1-c1ccc(N2CCc3c(C(F)(F)F)nn(-c4cccc(-c5n[nH]c(=O)[nH]5)c4)c3C2=O)cc1

Basic Information

ChEMBL ID CHEMBL592401
Phase Preclinical
Structure Type MOL
InChI Key XTWWNKNLOIVLSM-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

573.6
MW (Da)
4.90
ALogP
6
HBA
2
HBD
102.9
PSA (Ų)
0.30
QED
1
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C30H26F3N7O2
MW 573.58
Aromatic Rings 5
Heavy Atoms 42
NP-Likeness -1.31

Activity Summary

Ki 1 meas. best 8.96

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Coagulation factor X
CHEMBL244
Ki 8.96 8.96 1.1 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Coagulation factor X Ki = 1.1 nM 8.96 Inhibition of human factor 10a 20100660

Literature References

PubMed DOI Target Context # Activities
20100660 10.1016/j.bmcl.2010.01.011 Coagulation factor X 1
20100660 10.1016/j.bmcl.2010.01.011 Prothrombin 1
20100660 10.1016/j.bmcl.2010.01.011 Plasma 1
20100660 10.1016/j.bmcl.2010.01.011 Trypsin 1

Data from ChEMBL 36 via Core Engine