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Compound Detail

CHEMBL457633

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CC(C)c1ccc(CCNS(=O)(=O)c2cc(C(=N)N)ccc2O)c(NCC(=O)O)c1

Basic Information

ChEMBL ID CHEMBL457633
Phase Preclinical
Structure Type MOL
InChI Key XIRFVOZZUZGHTD-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
1
PK Parameters
2
Publications
0
Known Names

Molecular Properties

434.5
MW (Da)
1.82
ALogP
6
HBA
6
HBD
165.6
PSA (Ų)
0.24
QED
1
Ro5 Violations
10
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C20H26N4O5S
MW 434.52
Aromatic Rings 2
Heavy Atoms 30
NP-Likeness -0.68

Activity Summary

Ki 1 meas. best 7.21

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Coagulation factor X
CHEMBL244
Ki 7.21 7.21 62.0 1

Pharmacokinetic Data

Parameter Value Units Species
CL 3.2 ml/min Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Coagulation factor X Ki = 62.0 nM 7.21 Inhibition of human factor 10a by Dixon-plot method 18667303

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

Data from ChEMBL 36 via Core Engine