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Compound Detail

CHEMBL4168590

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C=CC(=O)Nc1ccc(-c2ccc(NC(=O)Nc3ccc(C)c(Cl)c3)cc2)cn1

Basic Information

ChEMBL ID CHEMBL4168590
Phase Preclinical
Structure Type MOL
InChI Key UVHLKFVTSZBBCD-UHFFFAOYSA-N
2
Targets
3
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

406.9
MW (Da)
5.48
ALogP
3
HBA
3
HBD
83.1
PSA (Ų)
0.49
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 C22H19ClN4O2
MW 406.87
Aromatic Rings 3
Heavy Atoms 29
NP-Likeness -1.42

Activity Summary

IC50 3 meas. best 7.85

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Angiopoietin-1 receptor
CHEMBL4128
IC50 7.85 7.85 14.2 1
Ephrin type-B receptor 4
CHEMBL5147
IC50 7.53 7.53 29.3 1

Activity Data Samples

Top measurements by pChEMBL value

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