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Compound Detail

CHEMBL4472318

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COc1ccc(NC(=O)c2ccc(N3CCOCC3=O)cc2)c(C(=O)Nc2ccc(C(C)(C)C)cc2)c1

Basic Information

ChEMBL ID CHEMBL4472318
Phase Preclinical
Structure Type MOL
InChI Key ULUYJXNPEDFMSW-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
1
Publications
0
Known Names

Molecular Properties

501.6
MW (Da)
4.86
ALogP
5
HBA
2
HBD
97.0
PSA (Ų)
0.50
QED
1
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C29H31N3O5
MW 501.58
Aromatic Rings 3
Heavy Atoms 37
NP-Likeness -1.58

Activity Summary

IC50 1 meas. best 5.68

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Coagulation factor X
CHEMBL244
IC50 5.68 5.68 2087.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Coagulation factor X IC50 = 2087.0 nM 5.68 Inhibition of human factor Xa using S-2222 as substrate preincubated for 30 mins... 30446438

Literature References

PubMed DOI Target Context # Activities
30446438 10.1016/j.bmc.2018.09.012 Coagulation factor X 1

Data from ChEMBL 36 via Core Engine