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Compound Detail

CHEMBL501183

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CN1CCc2nc(C(=O)N[C@@H]3CC[C@H](C(=O)O)C[C@@H]3NC(=O)c3cc4cc(Cl)ccc4[nH]3)sc2C1

Basic Information

ChEMBL ID CHEMBL501183
Phase Preclinical
Structure Type MOL
InChI Key YYXRTQKTSABROA-XZOAIXRZSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

516.0
MW (Da)
3.05
ALogP
6
HBA
4
HBD
127.4
PSA (Ų)
0.41
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 C24H26ClN5O4S
MW 516.02
Aromatic Rings 3
Heavy Atoms 35
NP-Likeness -1.08

Activity Summary

IC50 2 meas. best 7.8

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Coagulation factor X
CHEMBL244
IC50 7.8 7.8 16.0 1
Rattus norvegicus
CHEMBL376
IC50 7.8 7.8 16.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Coagulation factor X IC50 = 16.0 nM 7.8 Inhibition of human factor 10a 18675545
Rattus norvegicus IC50 = 16.0 nM 7.8 Inhibition of factor 10a in plasma of po dosed Wistar rat 18675545

Literature References

PubMed DOI Target Context # Activities
18675545 10.1016/j.bmcl.2008.07.031 Plasma 2
18675545 10.1016/j.bmcl.2008.07.031 Rattus norvegicus 2
18675545 10.1016/j.bmcl.2008.07.031 Coagulation factor X 1
18675545 10.1016/j.bmcl.2008.07.031 Liver microsomes 1

Data from ChEMBL 36 via Core Engine