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Compound Detail

CHEMBL4104466

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Nc1ncc2ccc(-c3ccc(NC(=S)Nc4ccc(Cl)cc4Cl)cc3)cc2n1

Basic Information

ChEMBL ID CHEMBL4104466
Phase Preclinical
Structure Type MOL
InChI Key JXZUQLGBYDHSAH-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

440.4
MW (Da)
5.99
ALogP
4
HBA
3
HBD
75.9
PSA (Ų)
0.34
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 C21H15Cl2N5S
MW 440.36
Aromatic Rings 4
Heavy Atoms 29
NP-Likeness -1.67

Activity Summary

IC50 1 meas. best 6.78

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Angiopoietin-1 receptor
CHEMBL4128
IC50 6.78 6.78 164.3 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Angiopoietin-1 receptor IC50 = 164.35 nM 6.78 Inhibition of TIE-2 (unknown origin) after 60 mins by ADP-Glo assay 28068599

Literature References

PubMed DOI Target Context # Activities
28068599 10.1016/j.ejmech.2016.12.059 Vascular endothelial growth factor receptor 2 1
28068599 10.1016/j.ejmech.2016.12.059 Angiopoietin-1 receptor 1
28068599 10.1016/j.ejmech.2016.12.059 Ephrin type-B receptor 4 1

Data from ChEMBL 36 via Core Engine