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Compound Detail

CHEMBL3959787

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COc1cc(OC)cc(N(CC#Cc2cc(OC)ncn2)c2ccc3ncc(-c4cnn(C)c4)nc3c2)c1

Basic Information

ChEMBL ID CHEMBL3959787
Phase Preclinical
Structure Type MOL
InChI Key SDIZOFZVSQJIHJ-UHFFFAOYSA-N
6
Targets
12
Activities
1
Assay Types
0
PK Parameters
0
Publications
0
Known Names

Molecular Properties

507.6
MW (Da)
4.04
ALogP
10
HBA
0
HBD
100.3
PSA (Ų)
0.30
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 C28H25N7O3
MW 507.55
Aromatic Rings 5
Heavy Atoms 38
NP-Likeness -1.25

Activity Summary

IC50 12 meas. best 7.32

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Fibroblast growth factor receptor 3
CHEMBL2742
IC50 7.32 6.54 47.9 3
Fibroblast growth factor receptor 1
CHEMBL3650
IC50 7.15 6.6033 70.8 3
Fibroblast growth factor receptor 2
CHEMBL4142
IC50 7.05 7.05 89.1 1
Fibroblast growth factor receptor 4
CHEMBL3973
IC50 6.64 6.64 229.1 1
Receptor-type tyrosine-protein kinase FLT3
CHEMBL1974
IC50 5.5 5.45 3162.3 2
Vascular endothelial growth factor receptor 2
CHEMBL279
IC50 5.41 5.395 3890.4 2

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Fibroblast growth factor receptor 3 IC50 = 47.86 nM 7.32 Inhibition of FGFR3 (unknown origin) transfected in mouse BA/F3 cells assessed a... -
Fibroblast growth factor receptor 1 IC50 = 70.79 nM 7.15 Inhibition of human FGFR1 using Btn-Flt3 as substrate after 60 mins by TR-FRET a... -
Fibroblast growth factor receptor 2 IC50 = 89.13 nM 7.05 Inhibition of human FGFR2 using Btn-Flt3 as substrate after 60 mins by TR-FRET a... -
Fibroblast growth factor receptor 1 IC50 = 114.82 nM 6.94 Inhibition of FGFR1 (unknown origin) transfected in mouse BA/F3 cells assessed a... -
Fibroblast growth factor receptor 3 IC50 = 120.23 nM 6.92 Inhibition of human FGFR3 using Btn-Flt3 as substrate after 60 mins by TR-FRET a... -
Fibroblast growth factor receptor 4 IC50 = 229.09 nM 6.64 Inhibition of human FGFR4 using Btn-Flt3 as substrate after 60 mins by TR-FRET a... -
Fibroblast growth factor receptor 1 IC50 = 1905.46 nM 5.72 Inhibition of FGFR1 (unknown origin) transfected in mouse BA/F3 cells assessed a... -
Receptor-type tyrosine-protein kinase FLT3 IC50 = 3162.28 nM 5.5 Inhibition of FLT3 (unknown origin) transfected in mouse BA/F3 cells assessed as... -
Vascular endothelial growth factor receptor 2 IC50 = 3890.45 nM 5.41 Inhibition of VEGFR2 (unknown origin) transfected in mouse BA/F3 cells assessed ... -
Receptor-type tyrosine-protein kinase FLT3 IC50 = 3981.07 nM 5.4 Inhibition of FLT3 (unknown origin) transfected in mouse BA/F3 cells assessed as... -
Fibroblast growth factor receptor 3 IC50 = 4168.69 nM 5.38 Inhibition of FGFR3 (unknown origin) transfected in mouse BA/F3 cells assessed a... -
Vascular endothelial growth factor receptor 2 IC50 = 4168.69 nM 5.38 Inhibition of VEGFR2 (unknown origin) transfected in mouse BA/F3 cells assessed ... -

Data from ChEMBL 36 via Core Engine