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Compound Detail

CHEMBL452524

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CCN(CC)CC1(c2ccc(N3CCc4c(C(F)(F)F)nn(-c5ccc(OC)cc5)c4C3=O)cc2)CC1

Basic Information

ChEMBL ID CHEMBL452524
Phase Preclinical
Structure Type MOL
InChI Key WRIXMSJJUBCUTJ-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
10
Publications
0
Known Names

Molecular Properties

512.6
MW (Da)
5.48
ALogP
5
HBA
0
HBD
50.6
PSA (Ų)
0.40
QED
2
Ro5 Violations
8
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C28H31F3N4O2
MW 512.58
Aromatic Rings 3
Heavy Atoms 37
NP-Likeness -0.95

Activity Summary

Ki 1 meas. best 8.72

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Plasma
CHEMBL613424
Ki 8.72 8.72 1.9 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Plasma Ki = 1.9 nM 8.72 Anticoagulant activity in human plasma assessed as concentration required to dou... 18550370

Literature References

PubMed DOI Target Context # Activities
18550370 10.1016/j.bmcl.2008.05.095 Unchecked 2
18550370 10.1016/j.bmcl.2008.05.095 Coagulation factor X 1
18550370 10.1016/j.bmcl.2008.05.095 Plasma 1
18550370 10.1016/j.bmcl.2008.05.095 Trypsin 1
18550370 10.1016/j.bmcl.2008.05.095 Coagulation factor IX 1
18550370 10.1016/j.bmcl.2008.05.095 Coagulation factor VII 1
18550370 10.1016/j.bmcl.2008.05.095 Plasminogen 1
18550370 10.1016/j.bmcl.2008.05.095 Tissue-type plasminogen activator 1
18550370 10.1016/j.bmcl.2008.05.095 Plasma kallikrein 1
18550370 10.1016/j.bmcl.2008.05.095 Vitamin K-dependent protein C 1

Data from ChEMBL 36 via Core Engine