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Compound Detail

CHEMBL194569

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[O-][n+]1ccccc1C(F)(F)CNc1nccc2oc(Cc3ccccc3N3CN=CN3)nc12

Basic Information

ChEMBL ID CHEMBL194569
Phase Preclinical
Structure Type MOL
InChI Key QGNIEHVRQPFGKU-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

451.4
MW (Da)
2.96
ALogP
8
HBA
2
HBD
105.5
PSA (Ų)
0.33
QED
0
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C22H19F2N7O2
MW 451.44
Aromatic Rings 4
Heavy Atoms 33
NP-Likeness -0.65

Activity Summary

Ki 2 meas. best 8.03

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Prothrombin
CHEMBL204
Ki 8.03 8.03 9.4 1
Coagulation factor X
CHEMBL244
Ki 7.85 7.85 14.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Prothrombin Ki = 9.4 nM 8.03 Inhibitory constant against thrombin 16137886
Coagulation factor X Ki = 14.0 nM 7.85 Inhibitory constant against human Coagulation factor Xa 16137886

Literature References

PubMed DOI Target Context # Activities
16137886 10.1016/j.bmcl.2005.07.022 Prothrombin 1
16137886 10.1016/j.bmcl.2005.07.022 NON-PROTEIN TARGET 1
16137886 10.1016/j.bmcl.2005.07.022 Coagulation factor X 1

Data from ChEMBL 36 via Core Engine