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Compound Detail

CHEMBL237242

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CCOC(=O)c1nn(-c2ccc(OC)cc2)c2c1CCN(c1ccc(-c3ccccc3CN3CC[C@@H](O)C3)cc1)C2=O

Basic Information

ChEMBL ID CHEMBL237242
Phase Preclinical
Structure Type MOL
InChI Key YALQNWIYMBHEMW-AREMUKBSSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

566.7
MW (Da)
4.49
ALogP
8
HBA
1
HBD
97.1
PSA (Ų)
0.31
QED
1
Ro5 Violations
8
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C33H34N4O5
MW 566.66
Aromatic Rings 4
Heavy Atoms 42
NP-Likeness -0.98

Activity Summary

Ki 2 meas. best 8.41

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Coagulation factor X
CHEMBL244
Ki 8.41 8.41 3.9 1
Prothrombin
CHEMBL204
Ki 6.01 6.01 980.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Coagulation factor X Ki = 3.9 nM 8.41 Binding affinity to human F10a 17914785
Prothrombin Ki = 980.0 nM 6.01 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