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Compound Detail

CHEMBL455932

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CS(=O)(=O)c1ccccc1-c1ccc(CCNS(=O)(=O)c2cc(C(=N)N)ccc2O)c(OCC(=O)O)c1

Basic Information

ChEMBL ID CHEMBL455932
Phase Preclinical
Structure Type MOL
InChI Key JFPVVWMDZGPJTA-UHFFFAOYSA-N
1
Targets
2
Activities
1
Assay Types
1
PK Parameters
4
Publications
0
Known Names

Molecular Properties

547.6
MW (Da)
1.73
ALogP
8
HBA
5
HBD
196.9
PSA (Ų)
0.18
QED
1
Ro5 Violations
11
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C24H25N3O8S2
MW 547.61
Aromatic Rings 3
Heavy Atoms 37
NP-Likeness -0.82

Activity Summary

Ki 2 meas. best 8.3

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Coagulation factor X
CHEMBL244
Ki 8.3 8.3 5.0 2

Pharmacokinetic Data

Parameter Value Units Species
CL 7.5 ml/min Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Coagulation factor X Ki = 5.0 nM 8.3 Inhibition of human factor 10a by Dixon-plot method 18667303
Coagulation factor X Ki = 5.0 nM 8.3 Inhibition of factor 10a 20503967

Literature References

PubMed DOI Target Context # Activities
18667303 10.1016/j.bmcl.2008.07.009 Coagulation factor X 1
18667303 10.1016/j.bmcl.2008.07.009 Rattus norvegicus 1
20503967 10.1021/jm100146h Coagulation factor X 1
20503967 10.1021/jm100146h NON-PROTEIN TARGET 1

Data from ChEMBL 36 via Core Engine