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Compound Detail

CHEMBL257207

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CN1CCc2nc(C(=O)NC3CCCCC3NC(=O)c3cc4cc(Cl)ccc4[nH]3)sc2C1

Basic Information

ChEMBL ID CHEMBL257207
Phase Preclinical
Structure Type MOL
InChI Key ARPFWVKYXJZULB-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
2
PK Parameters
4
Publications
0
Known Names

Molecular Properties

472.0
MW (Da)
3.74
ALogP
5
HBA
3
HBD
90.1
PSA (Ų)
0.54
QED
0
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

Natural Product First in Class Prodrug

Extended Properties

Molecular Formula C23H26ClN5O2S
MW 472.01
Aromatic Rings 3
Heavy Atoms 32
NP-Likeness -1.38

Activity Summary

IC50 1 meas. best 7.39

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Coagulation factor X
CHEMBL244
IC50 7.39 7.39 41.0 1

Pharmacokinetic Data

Parameter Value Units Species
CL 81.0 mL.min-1.kg-1 Homo sapiens
T1/2 0.1283 hr Homo sapiens

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Coagulation factor X IC50 = 41.0 nM 7.39 Inhibition of human factor 10a 18039572

Literature References

PubMed DOI Target Context # Activities
18039572 10.1016/j.bmcl.2007.11.037 Liver microsomes 2
18039572 10.1016/j.bmcl.2007.11.037 Coagulation factor X 1
18039572 10.1016/j.bmcl.2007.11.037 No relevant target 1
18039572 10.1016/j.bmcl.2007.11.037 Plasma 1

Data from ChEMBL 36 via Core Engine