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Compound Detail

CHEMBL398870

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CN(C)Cc1nccn1-c1ccc(-c2ccc3c(C(N)=O)nn(-c4ccc5onc(N)c5c4)c3c2F)c(F)c1

Basic Information

ChEMBL ID CHEMBL398870
Phase Preclinical
Structure Type MOL
InChI Key MGUDDBRJHXFTEY-UHFFFAOYSA-N
2
Targets
2
Activities
2
Assay Types
0
PK Parameters
6
Publications
0
Known Names

Molecular Properties

528.5
MW (Da)
4.04
ALogP
9
HBA
2
HBD
134.0
PSA (Ų)
0.33
QED
1
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C27H22F2N8O2
MW 528.52
Aromatic Rings 6
Heavy Atoms 39
NP-Likeness -1.52

Activity Summary

EC50 1 meas. best 4.64
Ki 1 meas. best 7.8

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Coagulation factor X
CHEMBL244
Ki 7.8 7.8 15.9 1
Plasma
CHEMBL613652
EC50 4.64 4.64 23000.0 1

Activity Data Samples

Top measurements by pChEMBL value

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
18159923 10.1021/jm701217r Plasma 1
18159923 10.1021/jm701217r Liver microsomes 1
18159923 10.1021/jm701217r Caco-2 1

Data from ChEMBL 36 via Core Engine