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Compound Detail

CHEMBL77933

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FC(F)(F)c1cc(Br)cc(Nc2nnc(Cc3ccncc3)c3ccccc23)c1

Basic Information

ChEMBL ID CHEMBL77933
Phase Preclinical
Structure Type MOL
InChI Key BZGHPHUNZKSCKZ-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
2
PK Parameters
6
Publications
0
Known Names

Molecular Properties

459.3
MW (Da)
6.14
ALogP
4
HBA
1
HBD
50.7
PSA (Ų)
0.40
QED
1
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C21H14BrF3N4
MW 459.27
Aromatic Rings 4
Heavy Atoms 29
NP-Likeness -1.23

Activity Summary

IC50 2 meas. best 6.42

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Vascular endothelial growth factor receptor 2
CHEMBL279
IC50 6.42 6.42 380.0 1
Vascular endothelial growth factor receptor 1
CHEMBL1868
IC50 6.22 6.22 600.0 1

Pharmacokinetic Data

Parameter Value Units Species
Cmax 6000000.0 nM Mus musculus
Tmax 2.0 hr Mus musculus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
10882357 10.1021/jm9909443 Vascular endothelial growth factor receptor 2 2
10882357 10.1021/jm9909443 Vascular endothelial growth factor receptor 1 1
10882357 10.1021/jm9909443 Platelet-derived growth factor receptor beta 1
10882357 10.1021/jm9909443 Mast/stem cell growth factor receptor Kit 1
10882357 10.1021/jm9909443 ADMET 1
10882357 10.1021/jm9909443 Mus musculus 1

Data from ChEMBL 36 via Core Engine