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Compound Detail

CHEMBL429516

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Nc1ncnc2c1N=C(c1ccc(NC(=O)Nc3ccc(F)c(C(F)(F)F)c3)cc1)CCN2

Basic Information

ChEMBL ID CHEMBL429516
Phase Preclinical
Structure Type MOL
InChI Key BYQDPWAYLMNNKF-UHFFFAOYSA-N
6
Targets
6
Activities
2
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

459.4
MW (Da)
4.80
ALogP
6
HBA
4
HBD
117.3
PSA (Ų)
0.42
QED
0
Ro5 Violations
3
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C21H17F4N7O
MW 459.41
Aromatic Rings 3
Heavy Atoms 33
NP-Likeness -1.13

Activity Summary

IC50 4 meas. best 8.3
Ki 2 meas. best 6.9

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Vascular endothelial growth factor receptor 2
CHEMBL279
IC50 8.3 8.3 5.0 1
Receptor-type tyrosine-protein kinase FLT3
CHEMBL1974
IC50 8.15 8.15 7.0 1
Mast/stem cell growth factor receptor Kit
CHEMBL1936
IC50 7.66 7.66 22.0 1
High affinity nerve growth factor receptor
CHEMBL2815
Ki 6.9 6.9 125.9 1
Vascular endothelial growth factor receptor 2
CHEMBL3337
IC50 6.46 6.46 345.0 1
Inhibitor of nuclear factor kappa-B kinase subunit epsilon
CHEMBL3529
Ki 5.5 5.5 3162.3 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
18362070 10.1016/j.bmcl.2008.03.021 Vascular endothelial growth factor receptor 2 2
18362070 10.1016/j.bmcl.2008.03.021 Receptor-type tyrosine-protein kinase FLT3 1
18362070 10.1016/j.bmcl.2008.03.021 Mast/stem cell growth factor receptor Kit 1

Data from ChEMBL 36 via Core Engine