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Compound Detail

CHEMBL271441

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Cc1ccc(F)c(NC(=O)Nc2ccc(-c3cncc4[nH]nc(N)c34)cc2)c1

Basic Information

ChEMBL ID CHEMBL271441
Phase Preclinical
Structure Type MOL
InChI Key BDPBZUHWAVABDM-UHFFFAOYSA-N
11
Targets
17
Activities
2
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

376.4
MW (Da)
4.30
ALogP
4
HBA
4
HBD
108.7
PSA (Ų)
0.43
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 C20H17FN6O
MW 376.40
Aromatic Rings 4
Heavy Atoms 28
NP-Likeness -1.64

Activity Summary

Ki 11 meas. best 9.8
IC50 6 meas. best 9.0

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Vascular endothelial growth factor receptor 1
CHEMBL1868
Ki 9.8 9.8 0.2 1
Vascular endothelial growth factor receptor 3
CHEMBL1955
Ki 9.5 9.5 0.3 1
Mast/stem cell growth factor receptor Kit
CHEMBL1936
Ki 9.3 9.3 0.5 1
Receptor-type tyrosine-protein kinase FLT3
CHEMBL1974
Ki 9.3 9.3 0.5 1
Macrophage colony-stimulating factor 1 receptor
CHEMBL1844
Ki 9.1 9.1 0.8 1
Vascular endothelial growth factor receptor 2
CHEMBL279
IC50 9.0 8.84 1.0 6
Vascular endothelial growth factor receptor 2
CHEMBL279
Ki 8.7 8.7 2.0 1
Tyrosine-protein kinase Lck
CHEMBL258
Ki 7.1 7.1 79.4 1
Tyrosine-protein kinase Lyn
CHEMBL3905
Ki 7.0 7.0 100.0 1
Tyrosine-protein kinase Fyn
CHEMBL1841
Ki 6.9 6.9 125.9 1
Tyrosine-protein kinase Blk
CHEMBL2250
Ki 6.8 6.8 158.5 1
Proto-oncogene tyrosine-protein kinase Src
CHEMBL267
Ki 6.4 6.4 398.1 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Vascular endothelial growth factor receptor 1 Ki = 0.1585 nM 9.8 PUBCHEM_BIOASSAY: Navigating the Kinome. (Class of assay: other) Panel member na... -
Vascular endothelial growth factor receptor 3 Ki = 0.3162 nM 9.5 PUBCHEM_BIOASSAY: Navigating the Kinome. (Class of assay: other) Panel member na... -
Receptor-type tyrosine-protein kinase FLT3 Ki = 0.5012 nM 9.3 PUBCHEM_BIOASSAY: Navigating the Kinome. (Class of assay: other) Panel member na... -
Mast/stem cell growth factor receptor Kit Ki = 0.5012 nM 9.3 PUBCHEM_BIOASSAY: Navigating the Kinome. (Class of assay: other) Panel member na... -
Macrophage colony-stimulating factor 1 receptor Ki = 0.7943 nM 9.1 PUBCHEM_BIOASSAY: Navigating the Kinome. (Class of assay: other) Panel member na... -
Vascular endothelial growth factor receptor 2 IC50 = 1.0 nM 9.0 Inhibition of KDR (unknown origin) in cell-based assay -
Vascular endothelial growth factor receptor 2 IC50 = 1.0 nM 9.0 Inhibition of KDR (unknown origin) in cell-based assay -
Vascular endothelial growth factor receptor 2 IC50 = 1.0 nM 9.0 Inhibition of VEGF-induced human KDR phosphorylation in mouse 3T3 cells 18023347
Vascular endothelial growth factor receptor 2 Ki = 1.995 nM 8.7 PUBCHEM_BIOASSAY: Navigating the Kinome. (Class of assay: other) Panel member na... -
Vascular endothelial growth factor receptor 2 IC50 = 2.1 nM 8.68 Inhibition of KDR kinase activity (unknown origin) -
Vascular endothelial growth factor receptor 2 IC50 = 2.1 nM 8.68 Inhibition of KDR kinase activity (unknown origin) -
Vascular endothelial growth factor receptor 2 IC50 = 2.1 nM 8.68 Inhibition of KDR by HTRF assay 18023347
Tyrosine-protein kinase Lck Ki = 79.43 nM 7.1 PUBCHEM_BIOASSAY: Navigating the Kinome. (Class of assay: other) Panel member na... -
Tyrosine-protein kinase Lyn Ki = 100.0 nM 7.0 PUBCHEM_BIOASSAY: Navigating the Kinome. (Class of assay: other) Panel member na... -
Tyrosine-protein kinase Fyn Ki = 125.89 nM 6.9 PUBCHEM_BIOASSAY: Navigating the Kinome. (Class of assay: other) Panel member na... -
Tyrosine-protein kinase Blk Ki = 158.49 nM 6.8 PUBCHEM_BIOASSAY: Navigating the Kinome. (Class of assay: other) Panel member na... -
Proto-oncogene tyrosine-protein kinase Src Ki = 398.11 nM 6.4 PUBCHEM_BIOASSAY: Navigating the Kinome. (Class of assay: other) Panel member na... -

Literature References

PubMed DOI Target Context # Activities
- 10.1007/s00044-011-9926-4 Vascular endothelial growth factor receptor 2 4
18023347 10.1016/j.bmcl.2007.10.018 Vascular endothelial growth factor receptor 2 2
18023347 10.1016/j.bmcl.2007.10.018 Mus musculus 1
18023347 10.1016/j.bmcl.2007.10.018 No relevant target 1

Data from ChEMBL 36 via Core Engine