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Compound Detail

CHEMBL361846

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NCc1nccn1-c1ccc(NC(=O)c2cc(C(F)(F)F)nn2-c2ccc3onc(N)c3c2)c(F)c1

Basic Information

ChEMBL ID CHEMBL361846
Phase Preclinical
Structure Type MOL
InChI Key JPKDFYYSRDZYIY-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

500.4
MW (Da)
3.65
ALogP
9
HBA
3
HBD
142.8
PSA (Ų)
0.31
QED
1
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C22H16F4N8O2
MW 500.42
Aromatic Rings 5
Heavy Atoms 36
NP-Likeness -1.97

Activity Summary

Ki 2 meas. best 8.52

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Coagulation factor X
CHEMBL244
Ki 8.52 8.52 3.0 1
Prothrombin
CHEMBL204
Ki 5.46 5.46 3500.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Coagulation factor X Ki = 3.0 nM 8.52 Binding affinity against human Coagulation factor Xa 15771420
Prothrombin Ki = 3500.0 nM 5.46 Binding affinity against human thrombin 15771420

Literature References

PubMed DOI Target Context # Activities
15771420 10.1021/jm0497949 ADMET 2
15771420 10.1021/jm0497949 Coagulation factor X 1
15771420 10.1021/jm0497949 Prothrombin 1
15771420 10.1021/jm0497949 Caco-2 1

Data from ChEMBL 36 via Core Engine