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Compound Detail

CHEMBL522732

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CN1CCN(c2ccc3[nH]c(-c4c(N)c5cc(F)c(F)cc5[nH]c4=O)nc3c2)CC1

Basic Information

ChEMBL ID CHEMBL522732
Phase Preclinical
Structure Type MOL
InChI Key RWBSHLPMAISSHT-UHFFFAOYSA-N
4
Targets
4
Activities
2
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

410.4
MW (Da)
2.68
ALogP
5
HBA
3
HBD
94.0
PSA (Ų)
0.47
QED
0
Ro5 Violations
2
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C21H20F2N6O
MW 410.43
Aromatic Rings 4
Heavy Atoms 30
NP-Likeness -1.28

Activity Summary

IC50 3 meas. best 8.52
EC50 1 meas. best 6.32

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Platelet-derived growth factor receptor beta
CHEMBL1913
IC50 8.52 8.52 3.0 1
Fibroblast growth factor receptor 1
CHEMBL3650
IC50 6.96 6.96 110.0 1
Vascular endothelial growth factor receptor 2
CHEMBL279
IC50 6.72 6.72 190.0 1
NON-PROTEIN TARGET
CHEMBL3879801
EC50 6.32 6.32 480.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
19113866 10.1021/jm800790t Vascular endothelial growth factor receptor 2 1
19113866 10.1021/jm800790t Fibroblast growth factor receptor 1 1
19113866 10.1021/jm800790t Platelet-derived growth factor receptor beta 1
19113866 10.1021/jm800790t NON-PROTEIN TARGET 1

Data from ChEMBL 36 via Core Engine