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Compound Detail

CHEMBL194498

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CONC(=O)c1cc(Nc2ncnn3cc(-c4nnc(C(F)F)o4)c(C(C)C)c23)c(F)cc1F

Basic Information

ChEMBL ID CHEMBL194498
Phase Preclinical
Structure Type MOL
InChI Key BPXQYAXTDCQZHB-UHFFFAOYSA-N
5
Targets
6
Activities
1
Assay Types
0
PK Parameters
13
Publications
0
Known Names

Molecular Properties

479.4
MW (Da)
4.15
ALogP
9
HBA
2
HBD
119.5
PSA (Ų)
0.30
QED
0
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C20H17F4N7O3
MW 479.39
Aromatic Rings 4
Heavy Atoms 34
NP-Likeness -1.54

Activity Summary

IC50 6 meas. best 7.77

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Vascular endothelial growth factor receptor
CHEMBL2095227
IC50 7.77 7.77 17.0 1
Fibroblast growth factor receptor
CHEMBL2095217
IC50 7.68 7.68 21.0 1
Vascular endothelial growth factor receptor 2
CHEMBL279
IC50 7.24 6.66 57.0 2
Fibroblast growth factor receptor 1
CHEMBL3650
IC50 7.0 7.0 100.0 1
Tyrosine-protein kinase Lck
CHEMBL258
IC50 4.75 4.75 18000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
15943473 10.1021/jm0501275 Mus musculus 3
15943473 10.1021/jm0501275 Vascular endothelial growth factor receptor 2 2
15943473 10.1021/jm0501275 ADMET 2
15943473 10.1021/jm0501275 Tyrosine-protein kinase Lck 1
15943473 10.1021/jm0501275 Protein kinase C alpha type 1
15943473 10.1021/jm0501275 Cyclin-dependent kinase 2 1
15943473 10.1021/jm0501275 Vascular endothelial growth factor receptor 1
15943473 10.1021/jm0501275 Fibroblast growth factor receptor 1
15943473 10.1021/jm0501275 Fibroblast growth factor receptor 1 1
15943473 10.1021/jm0501275 Epidermal growth factor receptor 1
15943473 10.1021/jm0501275 Receptor tyrosine-protein kinase erbB-2 1
15943473 10.1021/jm0501275 Platelet-derived growth factor receptor beta 1
15943473 10.1021/jm0501275 Insulin-like growth factor 1 receptor 1

Data from ChEMBL 36 via Core Engine