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Compound Detail

CHEMBL1097824

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Cn1cnc(-c2cc3nccc(Oc4ccc(NC(=O)c5cnn(-c6ccccc6)c5N)cc4F)c3s2)c1

Basic Information

ChEMBL ID CHEMBL1097824
Phase Preclinical
Structure Type MOL
InChI Key JVNNQMKXIIVSCG-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

525.6
MW (Da)
5.65
ALogP
9
HBA
2
HBD
112.9
PSA (Ų)
0.29
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 C27H20FN7O2S
MW 525.57
Aromatic Rings 6
Heavy Atoms 38
NP-Likeness -1.79

Activity Summary

IC50 2 meas. best 6.75

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Hepatocyte growth factor receptor
CHEMBL3717
IC50 6.75 6.75 180.0 1
Vascular endothelial growth factor receptor 2
CHEMBL279
IC50 6.1 6.1 800.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Hepatocyte growth factor receptor IC50 = 180.0 nM 6.75 Inhibition of c-Met 20363625
Vascular endothelial growth factor receptor 2 IC50 = 800.0 nM 6.1 Inhibition of VEGFR2 20363625

Literature References

PubMed DOI Target Context # Activities
20363625 10.1016/j.bmcl.2010.03.073 Macrophage-stimulating protein receptor 1
20363625 10.1016/j.bmcl.2010.03.073 Hepatocyte growth factor receptor 1
20363625 10.1016/j.bmcl.2010.03.073 Vascular endothelial growth factor receptor 2 1

Data from ChEMBL 36 via Core Engine