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Compound Detail

CHEMBL20604

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Cc1cc(C(=O)Nc2ccc(-c3ccccc3S(C)(=O)=O)cc2F)n(-c2cc3ccccc3cc2S(C)(=O)=O)n1

Basic Information

ChEMBL ID CHEMBL20604
Phase Preclinical
Structure Type MOL
InChI Key FXGWYXPHUQWSQF-UHFFFAOYSA-N
1
Targets
2
Activities
2
Assay Types
4
PK Parameters
8
Publications
0
Known Names

Molecular Properties

577.7
MW (Da)
5.20
ALogP
7
HBA
1
HBD
115.2
PSA (Ų)
0.30
QED
2
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C29H24FN3O5S2
MW 577.66
Aromatic Rings 5
Heavy Atoms 40
NP-Likeness -1.41

Activity Summary

IC50 1 meas. best 8.05
Ki 1 meas. best 8.77

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Coagulation factor X
CHEMBL244
Ki 8.77 8.77 1.7 1
Coagulation factor X
CHEMBL244
IC50 8.05 8.05 9.0 1

Pharmacokinetic Data

Parameter Value Units Species
CL 41.2 mL.min-1.kg-1 Rattus norvegicus
F 18.0 % Rattus norvegicus
T1/2 0.7 hr Rattus norvegicus
Vd 2.6 L.kg-1 Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
14980670 10.1016/j.bmcl.2003.12.053 Rattus norvegicus 4
14980670 10.1016/j.bmcl.2003.12.053 Coagulation factor X 3
14980670 10.1016/j.bmcl.2003.12.053 Prothrombin 1
14980670 10.1016/j.bmcl.2003.12.053 Serine protease 1 1
14980670 10.1016/j.bmcl.2003.12.053 Tissue-type plasminogen activator 1
14980670 10.1016/j.bmcl.2003.12.053 Vitamin K-dependent protein C 1
14980670 10.1016/j.bmcl.2003.12.053 Plasminogen 1
14980670 10.1016/j.bmcl.2003.12.053 Kallikrein-1 1

Data from ChEMBL 36 via Core Engine