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Compound Detail

CHEMBL251938

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CN(C)CCN(c1cccnc1)c1ccc(-c2ccc3c(C(N)=O)nn(-c4ccc5onc(N)c5c4)c3c2F)c(F)c1

Basic Information

ChEMBL ID CHEMBL251938
Phase Preclinical
Structure Type MOL
InChI Key LUFIRQURXPBAOK-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

568.6
MW (Da)
4.89
ALogP
9
HBA
2
HBD
132.3
PSA (Ų)
0.27
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 C30H26F2N8O2
MW 568.59
Aromatic Rings 6
Heavy Atoms 42
NP-Likeness -1.35

Activity Summary

Ki 1 meas. best 6.64

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Coagulation factor X
CHEMBL244
Ki 6.64 6.64 231.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Coagulation factor X Ki = 231.0 nM 6.64 Inhibition of human factor 10a 18159923

Literature References

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

Data from ChEMBL 36 via Core Engine