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Compound Detail

CHEMBL212202

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Nc1noc2ccc(-n3nc(C(F)(F)F)c4c3C(=O)N(c3ccc(-c5ccccc5CN5CCNCC5)cc3)CC4)cc12

Basic Information

ChEMBL ID CHEMBL212202
Phase Preclinical
Structure Type MOL
InChI Key KZAQAXHOSKDNPX-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

587.6
MW (Da)
4.89
ALogP
8
HBA
2
HBD
105.5
PSA (Ų)
0.30
QED
1
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C31H28F3N7O2
MW 587.61
Aromatic Rings 5
Heavy Atoms 43
NP-Likeness -1.16

Activity Summary

Ki 2 meas. best 9.19

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Coagulation factor X
CHEMBL244
Ki 9.19 9.19 0.6 1
Prothrombin
CHEMBL204
Ki 6.55 6.55 280.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Coagulation factor X Ki = 0.64 nM 9.19 Binding affinity to human F10a 16730984
Prothrombin Ki = 280.0 nM 6.55 Binding affinity to human F2a 16730984

Literature References

PubMed DOI Target Context # Activities
16730984 10.1016/j.bmcl.2006.02.069 Prothrombin 1
16730984 10.1016/j.bmcl.2006.02.069 Coagulation factor VII/tissue factor 1
16730984 10.1016/j.bmcl.2006.02.069 Coagulation factor X 1

Data from ChEMBL 36 via Core Engine