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Compound Detail

CHEMBL186693

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Cc1ccc2c(c1)ncn2-c1ccc(NC(=O)c2cc(C(F)(F)F)nn2-c2cccc(C(=N)N)c2)c(F)c1

Basic Information

ChEMBL ID CHEMBL186693
Phase Preclinical
Structure Type MOL
InChI Key QIIJPFFGWFOIHG-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

521.5
MW (Da)
5.21
ALogP
6
HBA
3
HBD
114.6
PSA (Ų)
0.17
QED
2
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C26H19F4N7O
MW 521.48
Aromatic Rings 5
Heavy Atoms 38
NP-Likeness -1.97

Activity Summary

Ki 2 meas. best 9.57

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Coagulation factor X
CHEMBL244
Ki 9.57 9.57 0.3 1
Coagulation factor IX
CHEMBL2016
Ki 8.0 8.0 10.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Coagulation factor X Ki = 0.27 nM 9.57 Binding affinity towards human factor Xa 15454208
Coagulation factor IX Ki = 10.0 nM 8.0 Binding affinity towards human factor IXa 15454208

Literature References

PubMed DOI Target Context # Activities
15454208 10.1016/j.bmcl.2004.08.034 Coagulation factor IX 1
15454208 10.1016/j.bmcl.2004.08.034 Coagulation factor X 1
15454208 10.1016/j.bmcl.2004.08.034 Coagulation factor IX and X 1

Data from ChEMBL 36 via Core Engine