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Compound Detail

CHEMBL391804

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

Basic Information

ChEMBL ID CHEMBL391804
Phase Preclinical
Structure Type MOL
InChI Key LFQOOGATGPTOMY-JKSUJKDBSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

458.0
MW (Da)
3.35
ALogP
5
HBA
3
HBD
90.1
PSA (Ų)
0.56
QED
0
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C22H24ClN5O2S
MW 457.99
Aromatic Rings 3
Heavy Atoms 31
NP-Likeness -1.40

Activity Summary

IC50 2 meas. best 6.93

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Coagulation factor X
CHEMBL244
IC50 6.93 6.93 118.0 1
Prothrombin
CHEMBL204
IC50 4.57 4.57 27000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Coagulation factor X IC50 = 118.0 nM 6.93 Inhibition of human factor 10a after 10 seconds 17555959
Prothrombin IC50 = 27000.0 nM 4.57 Inhibition of human factor 2a after 10 seconds 17555959

Literature References

PubMed DOI Target Context # Activities
17555959 10.1016/j.bmcl.2007.05.068 Plasma 2
17555959 10.1016/j.bmcl.2007.05.068 Coagulation factor X 1
17555959 10.1016/j.bmcl.2007.05.068 Prothrombin 1

Data from ChEMBL 36 via Core Engine