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Compound Detail

CHEMBL264106

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COc1ccc(-n2nc(S(C)(=O)=O)c3c2C(=O)N(c2ccc(-c4ccccc4CN4CC[C@@H](O)C4)cc2)CC3)cc1

Basic Information

ChEMBL ID CHEMBL264106
Phase Preclinical
Structure Type MOL
InChI Key OLQWKYOEBUBVRX-RUZDIDTESA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

572.7
MW (Da)
3.72
ALogP
8
HBA
1
HBD
105.0
PSA (Ų)
0.36
QED
1
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C31H32N4O5S
MW 572.69
Aromatic Rings 4
Heavy Atoms 41
NP-Likeness -0.93

Activity Summary

Ki 2 meas. best 9.6

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Coagulation factor X
CHEMBL244
Ki 9.6 9.6 0.2 1
Prothrombin
CHEMBL204
Ki 6.75 6.75 180.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Coagulation factor X Ki = 0.25 nM 9.6 Binding affinity to human F10a 17914785
Prothrombin Ki = 180.0 nM 6.75 Inhibition of human thrombin 17914785

Literature References

PubMed DOI Target Context # Activities
17914785 10.1021/jm070245n Coagulation factor X 1
17914785 10.1021/jm070245n Prothrombin 1
17914785 10.1021/jm070245n Plasma 1
17914785 10.1021/jm070245n Trypsin 1

Data from ChEMBL 36 via Core Engine