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Compound Detail

CHEMBL3951714

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COc1cc(OC)cc(N(CC2CC2)c2ccc3ncc(-c4cnn(CC(=O)NCCN5CCCC5)c4)nc3c2)c1

Basic Information

ChEMBL ID CHEMBL3951714
Phase Preclinical
Structure Type MOL
InChI Key XUDRPPZFODNIIN-UHFFFAOYSA-N
6
Targets
12
Activities
1
Assay Types
0
PK Parameters
0
Publications
0
Known Names

Molecular Properties

555.7
MW (Da)
4.27
ALogP
9
HBA
1
HBD
97.6
PSA (Ų)
0.28
QED
1
Ro5 Violations
12
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C31H37N7O3
MW 555.68
Aromatic Rings 4
Heavy Atoms 41
NP-Likeness -1.62

Activity Summary

IC50 12 meas. best 8.86

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Fibroblast growth factor receptor 1
CHEMBL3650
IC50 8.86 7.275 1.4 2
Fibroblast growth factor receptor 3
CHEMBL2742
IC50 8.58 6.55 2.6 3
Fibroblast growth factor receptor 2
CHEMBL4142
IC50 8.28 8.28 5.2 1
Fibroblast growth factor receptor 4
CHEMBL3973
IC50 7.66 7.66 21.9 1
Vascular endothelial growth factor receptor 2
CHEMBL279
IC50 6.79 5.6467 162.2 3
Receptor-type tyrosine-protein kinase FLT3
CHEMBL1974
IC50 5.26 5.23 5495.4 2

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Fibroblast growth factor receptor 1 IC50 = 1.38 nM 8.86 Inhibition of human FGFR1 using Btn-Flt3 as substrate after 60 mins by TR-FRET a... -
Fibroblast growth factor receptor 3 IC50 = 2.63 nM 8.58 Inhibition of human FGFR3 using Btn-Flt3 as substrate after 60 mins by TR-FRET a... -
Fibroblast growth factor receptor 2 IC50 = 5.248 nM 8.28 Inhibition of human FGFR2 using Btn-Flt3 as substrate after 60 mins by TR-FRET a... -
Fibroblast growth factor receptor 4 IC50 = 21.88 nM 7.66 Inhibition of human FGFR4 using Btn-Flt3 as substrate after 60 mins by TR-FRET a... -
Vascular endothelial growth factor receptor 2 IC50 = 162.18 nM 6.79 Inhibition of human VEGFR2 using Btn-Flt3 as substrate after 120 mins by TR-FRET... -
Fibroblast growth factor receptor 3 IC50 = 891.25 nM 6.05 Inhibition of FGFR3 (unknown origin) transfected in mouse BA/F3 cells assessed a... -
Fibroblast growth factor receptor 1 IC50 = 2041.74 nM 5.69 Inhibition of FGFR1 (unknown origin) transfected in mouse BA/F3 cells assessed a... -
Receptor-type tyrosine-protein kinase FLT3 IC50 = 5495.41 nM 5.26 Inhibition of FLT3 (unknown origin) transfected in mouse BA/F3 cells assessed as... -
Receptor-type tyrosine-protein kinase FLT3 IC50 = 6309.57 nM 5.2 Inhibition of FLT3 (unknown origin) transfected in mouse BA/F3 cells assessed as... -
Vascular endothelial growth factor receptor 2 IC50 = 8128.31 nM 5.09 Inhibition of VEGFR2 (unknown origin) transfected in mouse BA/F3 cells assessed ... -
Vascular endothelial growth factor receptor 2 IC50 = 8709.64 nM 5.06 Inhibition of VEGFR2 (unknown origin) transfected in mouse BA/F3 cells assessed ... -
Fibroblast growth factor receptor 3 IC50 = 9549.93 nM 5.02 Inhibition of FGFR3 (unknown origin) transfected in mouse BA/F3 cells assessed a... -

Data from ChEMBL 36 via Core Engine