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Compound Detail

CHEMBL424943

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Nc1n[nH]c2cccc(-c3ccc(NC(=O)Nc4cccc(C(F)(F)F)c4)cc3)c12

Basic Information

ChEMBL ID CHEMBL424943
Phase Preclinical
Structure Type MOL
InChI Key OSIDXFCEXZWGRW-UHFFFAOYSA-N
3
Targets
6
Activities
1
Assay Types
0
PK Parameters
7
Publications
0
Known Names

Molecular Properties

411.4
MW (Da)
5.47
ALogP
3
HBA
4
HBD
95.8
PSA (Ų)
0.36
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 C21H16F3N5O
MW 411.39
Aromatic Rings 4
Heavy Atoms 30
NP-Likeness -1.30

Activity Summary

IC50 6 meas. best 8.05

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Vascular endothelial growth factor receptor 2
CHEMBL279
IC50 8.05 7.85 9.0 3
Receptor-type tyrosine-protein kinase FLT3
CHEMBL1974
IC50 8.0 8.0 10.0 1
Mast/stem cell growth factor receptor Kit
CHEMBL1936
IC50 7.39 7.39 41.0 2

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
17343372 10.1021/jm061280h Vascular endothelial growth factor receptor 2 2
17343372 10.1021/jm061280h Receptor-type tyrosine-protein kinase FLT3 1
17343372 10.1021/jm061280h Mast/stem cell growth factor receptor Kit 1
17343372 10.1021/jm061280h Mus musculus 1
17343372 10.1021/jm061280h HT-1080 1
19892442 10.1016/j.ejmech.2009.09.013 Mast/stem cell growth factor receptor Kit 1
22738639 10.1016/j.bmcl.2012.06.009 Vascular endothelial growth factor receptor 2 1

Data from ChEMBL 36 via Core Engine