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Compound Detail

CHEMBL3943933

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COc1cc(OC)cc(N(CCCN2C[C@@H](C)N[C@@H](C)C2)c2ccc3ncc(-c4cnn(C)c4)nc3c2)c1

Basic Information

ChEMBL ID CHEMBL3943933
Phase Preclinical
Structure Type MOL
InChI Key IJENXCZIMOXLKN-OYRHEFFESA-N
6
Targets
13
Activities
1
Assay Types
0
PK Parameters
0
Publications
0
Known Names

Molecular Properties

515.7
MW (Da)
4.26
ALogP
9
HBA
1
HBD
80.6
PSA (Ų)
0.35
QED
1
Ro5 Violations
9
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C29H37N7O2
MW 515.66
Aromatic Rings 4
Heavy Atoms 38
NP-Likeness -1.14

Activity Summary

IC50 13 meas. best 7.94

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Fibroblast growth factor receptor 2
CHEMBL4142
IC50 7.94 7.94 11.5 1
Fibroblast growth factor receptor 1
CHEMBL3650
IC50 7.77 6.38 17.0 3
Fibroblast growth factor receptor 3
CHEMBL2742
IC50 7.47 6.3667 33.9 3
Fibroblast growth factor receptor 4
CHEMBL3973
IC50 6.73 6.73 186.2 1
Vascular endothelial growth factor receptor 2
CHEMBL279
IC50 6.63 5.7567 234.4 3
Receptor-type tyrosine-protein kinase FLT3
CHEMBL1974
IC50 5.33 5.21 4677.4 2

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Fibroblast growth factor receptor 2 IC50 = 11.48 nM 7.94 Inhibition of human FGFR2 using Btn-Flt3 as substrate after 60 mins by TR-FRET a... -
Fibroblast growth factor receptor 1 IC50 = 16.98 nM 7.77 Inhibition of human FGFR1 using Btn-Flt3 as substrate after 60 mins by TR-FRET a... -
Fibroblast growth factor receptor 3 IC50 = 33.88 nM 7.47 Inhibition of human FGFR3 using Btn-Flt3 as substrate after 60 mins by TR-FRET a... -
Fibroblast growth factor receptor 4 IC50 = 186.21 nM 6.73 Inhibition of human FGFR4 using Btn-Flt3 as substrate after 60 mins by TR-FRET a... -
Vascular endothelial growth factor receptor 2 IC50 = 234.42 nM 6.63 Inhibition of human VEGFR2 using Btn-Flt3 as substrate after 120 mins by TR-FRET... -
Fibroblast growth factor receptor 3 IC50 = 457.09 nM 6.34 Inhibition of FGFR3 (unknown origin) transfected in mouse BA/F3 cells assessed a... -
Fibroblast growth factor receptor 1 IC50 = 741.31 nM 6.13 Inhibition of FGFR1 (unknown origin) transfected in mouse BA/F3 cells assessed a... -
Vascular endothelial growth factor receptor 2 IC50 = 3548.13 nM 5.45 Inhibition of VEGFR2 (unknown origin) transfected in mouse BA/F3 cells assessed ... -
Receptor-type tyrosine-protein kinase FLT3 IC50 = 4677.35 nM 5.33 Inhibition of FLT3 (unknown origin) transfected in mouse BA/F3 cells assessed as... -
Fibroblast growth factor receptor 3 IC50 = 5128.61 nM 5.29 Inhibition of FGFR3 (unknown origin) transfected in mouse BA/F3 cells assessed a... -
Fibroblast growth factor receptor 1 IC50 = 5754.4 nM 5.24 Inhibition of FGFR1 (unknown origin) transfected in mouse BA/F3 cells assessed a... -
Vascular endothelial growth factor receptor 2 IC50 = 6456.54 nM 5.19 Inhibition of VEGFR2 (unknown origin) transfected in mouse BA/F3 cells assessed ... -
Receptor-type tyrosine-protein kinase FLT3 IC50 = 8128.31 nM 5.09 Inhibition of FLT3 (unknown origin) transfected in mouse BA/F3 cells assessed as... -

Data from ChEMBL 36 via Core Engine