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Compound Detail

CHEMBL4177333

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Nc1ncc2ccc(-c3ccc(NC(=O)C4(C(=O)Nc5cc(Br)ccc5OC(F)(F)F)CC4)cc3)cc2n1

Basic Information

ChEMBL ID CHEMBL4177333
Phase Preclinical
Structure Type MOL
InChI Key NKNUSZHAFRORBJ-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

586.4
MW (Da)
5.90
ALogP
6
HBA
3
HBD
119.2
PSA (Ų)
0.24
QED
2
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C26H19BrF3N5O3
MW 586.37
Aromatic Rings 4
Heavy Atoms 38
NP-Likeness -1.13

Activity Summary

IC50 1 meas. best 4.37

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
EA.hy 926
CHEMBL4296410
IC50 4.37 4.37 42440.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
EA.hy 926 IC50 = 42440.0 nM 4.37 Anti-angiogenic activity in human EAhy926 cells as growth inhibition after 24 hr... 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 Angiopoietin-1 receptor 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

Data from ChEMBL 36 via Core Engine