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Compound Detail

CHEMBL3978754

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COc1ccnc(C#CCN(c2ccc3ncc(-c4cnn(C)c4)nc3c2)c2c(F)c(OC)cc(OC)c2F)n1

Basic Information

ChEMBL ID CHEMBL3978754
Phase Preclinical
Structure Type MOL
InChI Key JYQPFNMDHXKRKL-UHFFFAOYSA-N
6
Targets
13
Activities
1
Assay Types
0
PK Parameters
0
Publications
0
Known Names

Molecular Properties

543.5
MW (Da)
4.31
ALogP
10
HBA
0
HBD
100.3
PSA (Ų)
0.28
QED
1
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C28H23F2N7O3
MW 543.53
Aromatic Rings 5
Heavy Atoms 40
NP-Likeness -1.28

Activity Summary

IC50 13 meas. best 9.42

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Fibroblast growth factor receptor 3
CHEMBL2742
IC50 9.42 7.69 0.4 3
Fibroblast growth factor receptor 1
CHEMBL3650
IC50 9.2 7.7533 0.6 3
Fibroblast growth factor receptor 4
CHEMBL3973
IC50 8.5 8.5 3.2 1
Fibroblast growth factor receptor 2
CHEMBL4142
IC50 8.47 8.47 3.4 1
Vascular endothelial growth factor receptor 2
CHEMBL279
IC50 7.58 6.4033 26.3 3
Receptor-type tyrosine-protein kinase FLT3
CHEMBL1974
IC50 5.48 5.315 3311.3 2

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Fibroblast growth factor receptor 3 IC50 = 0.3802 nM 9.42 Inhibition of FGFR3 (unknown origin) transfected in mouse BA/F3 cells assessed a... -
Fibroblast growth factor receptor 1 IC50 = 0.631 nM 9.2 Inhibition of FGFR1 (unknown origin) transfected in mouse BA/F3 cells assessed a... -
Fibroblast growth factor receptor 1 IC50 = 1.862 nM 8.73 Inhibition of human FGFR1 using Btn-Flt3 as substrate after 60 mins by TR-FRET a... -
Fibroblast growth factor receptor 3 IC50 = 2.291 nM 8.64 Inhibition of human FGFR3 using Btn-Flt3 as substrate after 60 mins by TR-FRET a... -
Fibroblast growth factor receptor 4 IC50 = 3.162 nM 8.5 Inhibition of human FGFR4 using Btn-Flt3 as substrate after 60 mins by TR-FRET a... -
Fibroblast growth factor receptor 2 IC50 = 3.388 nM 8.47 Inhibition of human FGFR2 using Btn-Flt3 as substrate after 60 mins by TR-FRET a... -
Vascular endothelial growth factor receptor 2 IC50 = 26.3 nM 7.58 Inhibition of human VEGFR2 using Btn-Flt3 as substrate after 120 mins by TR-FRET... -
Vascular endothelial growth factor receptor 2 IC50 = 467.74 nM 6.33 Inhibition of VEGFR2 (unknown origin) transfected in mouse BA/F3 cells assessed ... -
Receptor-type tyrosine-protein kinase FLT3 IC50 = 3311.31 nM 5.48 Inhibition of FLT3 (unknown origin) transfected in mouse BA/F3 cells assessed as... -
Fibroblast growth factor receptor 1 IC50 = 4677.35 nM 5.33 Inhibition of FGFR1 (unknown origin) transfected in mouse BA/F3 cells assessed a... -
Vascular endothelial growth factor receptor 2 IC50 = 5011.87 nM 5.3 Inhibition of VEGFR2 (unknown origin) transfected in mouse BA/F3 cells assessed ... -
Receptor-type tyrosine-protein kinase FLT3 IC50 = 7079.46 nM 5.15 Inhibition of FLT3 (unknown origin) transfected in mouse BA/F3 cells assessed as... -
Fibroblast growth factor receptor 3 IC50 = 9772.37 nM 5.01 Inhibition of FGFR3 (unknown origin) transfected in mouse BA/F3 cells assessed a... -

Data from ChEMBL 36 via Core Engine