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Compound Detail

CHEMBL3980069

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COc1cc(OC)cc(N(CCNC(C)C)c2ccc3ncc(-c4cnn(C5CCNCC5)c4)nc3c2)c1

Basic Information

ChEMBL ID CHEMBL3980069
Phase Preclinical
Structure Type MOL
InChI Key SLEJFRIKJJZQKL-UHFFFAOYSA-N
6
Targets
11
Activities
1
Assay Types
0
PK Parameters
0
Publications
0
Known Names

Molecular Properties

515.7
MW (Da)
4.57
ALogP
9
HBA
2
HBD
89.4
PSA (Ų)
0.32
QED
1
Ro5 Violations
10
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 -0.94

Activity Summary

IC50 11 meas. best 9.44

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Fibroblast growth factor receptor 1
CHEMBL3650
IC50 9.44 8.795 0.4 2
Fibroblast growth factor receptor 2
CHEMBL4142
IC50 8.54 8.54 2.9 1
Fibroblast growth factor receptor 3
CHEMBL2742
IC50 8.47 7.08 3.4 3
Fibroblast growth factor receptor 4
CHEMBL3973
IC50 8.07 8.07 8.5 1
Vascular endothelial growth factor receptor 2
CHEMBL279
IC50 7.7 6.3533 19.9 3
Receptor-type tyrosine-protein kinase FLT3
CHEMBL1974
IC50 5.24 5.24 5754.4 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Fibroblast growth factor receptor 1 IC50 = 0.3631 nM 9.44 Inhibition of human FGFR1 using Btn-Flt3 as substrate after 60 mins by TR-FRET a... -
Fibroblast growth factor receptor 2 IC50 = 2.884 nM 8.54 Inhibition of human FGFR2 using Btn-Flt3 as substrate after 60 mins by TR-FRET a... -
Fibroblast growth factor receptor 3 IC50 = 3.388 nM 8.47 Inhibition of human FGFR3 using Btn-Flt3 as substrate after 60 mins by TR-FRET a... -
Fibroblast growth factor receptor 1 IC50 = 7.079 nM 8.15 Inhibition of FGFR1 (unknown origin) transfected in mouse BA/F3 cells assessed a... -
Fibroblast growth factor receptor 4 IC50 = 8.511 nM 8.07 Inhibition of human FGFR4 using Btn-Flt3 as substrate after 60 mins by TR-FRET a... -
Vascular endothelial growth factor receptor 2 IC50 = 19.95 nM 7.7 Inhibition of human VEGFR2 using Btn-Flt3 as substrate after 120 mins by TR-FRET... -
Fibroblast growth factor receptor 3 IC50 = 22.39 nM 7.65 Inhibition of FGFR3 (unknown origin) transfected in mouse BA/F3 cells assessed a... -
Vascular endothelial growth factor receptor 2 IC50 = 1778.28 nM 5.75 Inhibition of VEGFR2 (unknown origin) transfected in mouse BA/F3 cells assessed ... -
Vascular endothelial growth factor receptor 2 IC50 = 2454.71 nM 5.61 Inhibition of VEGFR2 (unknown origin) transfected in mouse BA/F3 cells assessed ... -
Receptor-type tyrosine-protein kinase FLT3 IC50 = 5754.4 nM 5.24 Inhibition of FLT3 (unknown origin) transfected in mouse BA/F3 cells assessed as... -
Fibroblast growth factor receptor 3 IC50 = 7585.78 nM 5.12 Inhibition of FGFR3 (unknown origin) transfected in mouse BA/F3 cells assessed a... -

Data from ChEMBL 36 via Core Engine