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Compound Detail

CHEMBL257080

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

Basic Information

ChEMBL ID CHEMBL257080
Phase Preclinical
Structure Type MOL
InChI Key VHBPSKASYKLQAU-QFBILLFUSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

531.0
MW (Da)
1.39
ALogP
7
HBA
4
HBD
130.7
PSA (Ų)
0.39
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 C24H27ClN6O4S
MW 531.04
Aromatic Rings 3
Heavy Atoms 36
NP-Likeness -1.35

Activity Summary

IC50 1 meas. best 8.03

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Coagulation factor X
CHEMBL244
IC50 8.03 8.03 9.3 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Coagulation factor X IC50 = 9.3 nM 8.03 Inhibition of human factor 10a 18039572

Literature References

PubMed DOI Target Context # Activities
18039572 10.1016/j.bmcl.2007.11.037 Rattus norvegicus 4
18039572 10.1016/j.bmcl.2007.11.037 No relevant target 1
18039572 10.1016/j.bmcl.2007.11.037 Coagulation factor X 1
18039572 10.1016/j.bmcl.2007.11.037 Plasma 1

Data from ChEMBL 36 via Core Engine