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Compound Detail

CHEMBL468782

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COc1ccc(-n2nc(C(F)(F)F)c3c2C(=O)N(c2ccc(C4(N(C)C)CC4)cc2)CC3)cc1

Basic Information

ChEMBL ID CHEMBL468782
Phase Preclinical
Structure Type MOL
InChI Key BRWMTCCWQXNRTP-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

470.5
MW (Da)
4.65
ALogP
5
HBA
0
HBD
50.6
PSA (Ų)
0.54
QED
0
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C25H25F3N4O2
MW 470.50
Aromatic Rings 3
Heavy Atoms 34
NP-Likeness -0.88

Activity Summary

Ki 1 meas. best 10.07

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Coagulation factor X
CHEMBL244
Ki 10.07 10.07 0.1 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Coagulation factor X Ki = 0.085 nM 10.07 Binding affinity to human coagulation factor 10a 19046881

Literature References

PubMed DOI Target Context # Activities
19046881 10.1016/j.bmcl.2008.11.049 Coagulation factor X 1
19046881 10.1016/j.bmcl.2008.11.049 Plasma 1
19046881 10.1016/j.bmcl.2008.11.049 Caco-2 1

Data from ChEMBL 36 via Core Engine