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Compound Detail

CHEMBL4159125

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O=C(Nc1cccc(-c2ccc3c(=O)[nH]cnc3c2)c1)Nc1cc(C(F)(F)F)cc(C(F)(F)F)c1

Basic Information

ChEMBL ID CHEMBL4159125
Phase Preclinical
Structure Type MOL
InChI Key GSJFMLWKQMYXGD-UHFFFAOYSA-N
1
Targets
2
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

492.4
MW (Da)
6.27
ALogP
3
HBA
3
HBD
86.9
PSA (Ų)
0.29
QED
1
Ro5 Violations
3
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C23H14F6N4O2
MW 492.38
Aromatic Rings 4
Heavy Atoms 35
NP-Likeness -1.22

Activity Summary

IC50 2 meas. best 6.61

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Angiopoietin-1 receptor
CHEMBL4128
IC50 6.61 6.61 245.3 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Angiopoietin-1 receptor IC50 = 245.28 nM 6.61 Inhibition of TIE-2 (unknown origin) after 4 hrs by ADP-Glo luminescence assay 29102175

Literature References

PubMed DOI Target Context # Activities
29102175 10.1016/j.ejmech.2017.10.030 Vascular endothelial growth factor receptor 2 1
29102175 10.1016/j.ejmech.2017.10.030 EA.hy 926 1
29102175 10.1016/j.ejmech.2017.10.030 Ephrin type-B receptor 4 1
29102175 10.1016/j.ejmech.2017.10.030 Angiopoietin-1 receptor 1

Data from ChEMBL 36 via Core Engine