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Compound Detail

CHEMBL3109356

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COCCOc1ccn2c(-c3ccc4cccc(O[C@@H]5CCNC[C@@H]5F)c4n3)cnc2c1

Basic Information

ChEMBL ID CHEMBL3109356
Phase Preclinical
Structure Type MOL
InChI Key PPPOUAQYRUUFNJ-GHTZIAJQSA-N
5
Targets
6
Activities
1
Assay Types
4
PK Parameters
15
Publications
0
Known Names

Molecular Properties

436.5
MW (Da)
3.65
ALogP
7
HBA
1
HBD
69.9
PSA (Ų)
0.45
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 C24H25FN4O3
MW 436.49
Aromatic Rings 4
Heavy Atoms 32
NP-Likeness -0.80

Activity Summary

IC50 6 meas. best 8.4

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Receptor-type tyrosine-protein kinase FLT3
CHEMBL1974
IC50 8.4 8.4 4.0 1
Platelet-derived growth factor receptor beta
CHEMBL2749
IC50 8.4 8.0 4.0 2
Vascular endothelial growth factor receptor 2
CHEMBL279
IC50 7.55 7.55 28.0 1
Macrophage colony-stimulating factor 1 receptor
CHEMBL1844
IC50 6.55 6.55 282.0 1
Cytochrome P450 2D6
CHEMBL289
IC50 5.23 5.23 5880.0 1

Pharmacokinetic Data

Parameter Value Units Species
AUC 730.0 ng.hr.mL-1 Rattus norvegicus
CL 28.0 mL.min-1.kg-1 Rattus norvegicus
Cmax 160.37 nM Rattus norvegicus
F 13.0 % Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
24900776 10.1021/ml4003953 Rattus norvegicus 5
24900776 10.1021/ml4003953 LLC-PK1 3
24900776 10.1021/ml4003953 Platelet-derived growth factor receptor beta 2
24900776 10.1021/ml4003953 Liver microsome 2
24900776 10.1021/ml4003953 ADMET 2
24900776 10.1021/ml4003953 No relevant target 1
24900776 10.1021/ml4003953 Cytochrome P450 3A4 1
24900776 10.1021/ml4003953 Cytochrome P450 2D6 1
24900776 10.1021/ml4003953 Cytochrome P450 2C9 1
24900776 10.1021/ml4003953 Cytochrome P450 2C19 1
24900776 10.1021/ml4003953 Cytochrome P450 1A2 1
24900776 10.1021/ml4003953 Mast/stem cell growth factor receptor Kit 1
24900776 10.1021/ml4003953 Vascular endothelial growth factor receptor 2 1
24900776 10.1021/ml4003953 Macrophage colony-stimulating factor 1 receptor 1
24900776 10.1021/ml4003953 Receptor-type tyrosine-protein kinase FLT3 1

Data from ChEMBL 36 via Core Engine