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Compound Detail

CHEMBL367609

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NS(=O)(=O)c1ccccc1-c1ccc(C(=O)Nc2ccccc2C(=O)Nc2ccc(Cl)cn2)cc1

Basic Information

ChEMBL ID CHEMBL367609
Phase Preclinical
Structure Type MOL
InChI Key GKCSOJWDPJQQEU-UHFFFAOYSA-N
1
Targets
2
Activities
1
Assay Types
1
PK Parameters
4
Publications
0
Known Names

Molecular Properties

507.0
MW (Da)
4.55
ALogP
5
HBA
3
HBD
131.2
PSA (Ų)
0.35
QED
1
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C25H19ClN4O4S
MW 506.97
Aromatic Rings 4
Heavy Atoms 35
NP-Likeness -1.65

Activity Summary

IC50 2 meas. best 8.17

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Coagulation factor X
CHEMBL244
IC50 8.17 8.17 6.7 2

Pharmacokinetic Data

Parameter Value Units Species
F 35.0 % Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Coagulation factor X IC50 = 6.7 nM 8.17 Inhibitory concentration against coagulation factor Xa. 15013006
Coagulation factor X IC50 = 6.7 nM 8.17 Inhibition of Factor 10a 19297158

Literature References

PubMed DOI Target Context # Activities
15013006 10.1016/j.bmcl.2003.11.079 Coagulation factor X 2
19297158 10.1016/j.bmcl.2009.02.114 Plasma 1
19297158 10.1016/j.bmcl.2009.02.114 Rattus norvegicus 1
19297158 10.1016/j.bmcl.2009.02.114 Coagulation factor X 1

Data from ChEMBL 36 via Core Engine