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Compound Detail

CHEMBL179665

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Nc1noc2ccc(-n3nc(C(F)(F)F)cc3C(=O)Nc3ccc(-n4ccnc4CN4CCCC4)cc3F)cc12

Basic Information

ChEMBL ID CHEMBL179665
Phase Preclinical
Structure Type MOL
InChI Key GONSXYIFCYXXJP-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

554.5
MW (Da)
4.79
ALogP
9
HBA
2
HBD
120.0
PSA (Ų)
0.29
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 C26H22F4N8O2
MW 554.51
Aromatic Rings 5
Heavy Atoms 40
NP-Likeness -2.04

Activity Summary

Ki 2 meas. best 9.43

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Coagulation factor X
CHEMBL244
Ki 9.43 9.43 0.4 1
Prothrombin
CHEMBL204
Ki 6.22 6.22 600.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Coagulation factor X Ki = 0.37 nM 9.43 Binding affinity against human Coagulation factor Xa 15771420
Prothrombin Ki = 600.0 nM 6.22 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