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Compound Detail

CHEMBL402927

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Cc1nn(-c2cccc(CN)c2)c2c(F)c(-c3ccc(N4CCCC4=O)cc3)ccc12

Basic Information

ChEMBL ID CHEMBL402927
Phase Preclinical
Structure Type MOL
InChI Key JGKHUDVYQPUWSH-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

414.5
MW (Da)
4.73
ALogP
4
HBA
1
HBD
64.2
PSA (Ų)
0.53
QED
0
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C25H23FN4O
MW 414.48
Aromatic Rings 4
Heavy Atoms 31
NP-Likeness -1.31

Activity Summary

Ki 2 meas. best 6.65

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Coagulation factor X
CHEMBL244
Ki 6.65 6.65 223.0 1
Trypsin
CHEMBL2095204
Ki 6.15 6.15 702.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Coagulation factor X Ki = 223.0 nM 6.65 Inhibition of human factor 10a 18159923
Trypsin Ki = 702.0 nM 6.15 Inhibition of human trypsin 18159923

Literature References

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

Data from ChEMBL 36 via Core Engine