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Compound Detail

CHEMBL254621

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Nc1noc2ccc(-n3nc(C(F)(F)F)c4ccc(-c5ccc(N6CCCCC6=O)cc5F)c(F)c43)cc12

Basic Information

ChEMBL ID CHEMBL254621
Phase Preclinical
Structure Type MOL
InChI Key JAIIWGDOICMHHK-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

527.5
MW (Da)
6.23
ALogP
6
HBA
1
HBD
90.2
PSA (Ų)
0.28
QED
2
Ro5 Violations
3
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C26H18F5N5O2
MW 527.45
Aromatic Rings 5
Heavy Atoms 38
NP-Likeness -1.32

Activity Summary

Ki 1 meas. best 7.64

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Coagulation factor X
CHEMBL244
Ki 7.64 7.64 22.9 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Coagulation factor X Ki = 22.9 nM 7.64 Inhibition of human factor 10a 18159923

Literature References

PubMed DOI Target Context # Activities
18159923 10.1021/jm701217r Unchecked 1
18159923 10.1021/jm701217r Coagulation factor X 1
18159923 10.1021/jm701217r Trypsin 1

Data from ChEMBL 36 via Core Engine