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Compound Detail

CHEMBL450578

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O=C(N[C@H]1CCC[C@H]1NC(=O)c1ccc(Cl)s1)c1ccc(C2(CN3CCCC3)CC2)cc1

Basic Information

ChEMBL ID CHEMBL450578
Phase Preclinical
Structure Type MOL
InChI Key GSQQRIKCCGDNLT-VQTJNVASSA-N
2
Targets
3
Activities
1
Assay Types
0
PK Parameters
13
Publications
0
Known Names

Molecular Properties

472.1
MW (Da)
4.61
ALogP
4
HBA
2
HBD
61.4
PSA (Ų)
0.62
QED
0
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C25H30ClN3O2S
MW 472.05
Aromatic Rings 2
Heavy Atoms 32
NP-Likeness -1.02

Activity Summary

Ki 3 meas. best 9.29

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Coagulation factor X
CHEMBL244
Ki 9.29 9.29 0.5 2
Prothrombin
CHEMBL204
Ki 5.44 5.44 3601.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Coagulation factor X Ki = 0.51 nM 9.29 Inhibition of human factor 10a 17588746
Coagulation factor X Ki = 0.51 nM 9.29 Inhibition of factor 10a 20503967
Prothrombin Ki = 3601.0 nM 5.44 Inhibition of human thrombin 17588746

Literature References

PubMed DOI Target Context # Activities
17588746 10.1016/j.bmcl.2007.06.029 Unchecked 2
17588746 10.1016/j.bmcl.2007.06.029 Coagulation factor X 1
17588746 10.1016/j.bmcl.2007.06.029 Plasma 1
17588746 10.1016/j.bmcl.2007.06.029 Prothrombin 1
17588746 10.1016/j.bmcl.2007.06.029 Trypsin 1
17588746 10.1016/j.bmcl.2007.06.029 Coagulation factor VII 1
17588746 10.1016/j.bmcl.2007.06.029 Coagulation factor XI 1
17588746 10.1016/j.bmcl.2007.06.029 Plasminogen 1
17588746 10.1016/j.bmcl.2007.06.029 Tissue-type plasminogen activator 1
17588746 10.1016/j.bmcl.2007.06.029 Urokinase-type plasminogen activator 1
17588746 10.1016/j.bmcl.2007.06.029 Plasma kallikrein 1
20503967 10.1021/jm100146h Coagulation factor X 1
20503967 10.1021/jm100146h NON-PROTEIN TARGET 1

Data from ChEMBL 36 via Core Engine