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Compound Detail

CHEMBL237441

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

Basic Information

ChEMBL ID CHEMBL237441
Phase Preclinical
Structure Type MOL
InChI Key LXAASMXDKITPJA-XMMPIXPASA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

538.6
MW (Da)
4.02
ALogP
7
HBA
2
HBD
108.1
PSA (Ų)
0.37
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 C31H30N4O5
MW 538.60
Aromatic Rings 4
Heavy Atoms 40
NP-Likeness -0.92

Activity Summary

Ki 1 meas. best 8.12

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Coagulation factor X
CHEMBL244
Ki 8.12 8.12 7.6 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Coagulation factor X Ki = 7.6 nM 8.12 Binding affinity to human F10a 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