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Compound Detail

CHEMBL3953833

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COc1cc(OC)cc(N(CC#Cc2nccc(OC)n2)c2ccc3ncc(-c4cnn(C)c4)nc3c2)c1

Basic Information

ChEMBL ID CHEMBL3953833
Phase Preclinical
Structure Type MOL
InChI Key MSSUJWPHHVXXFT-UHFFFAOYSA-N
6
Targets
11
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 -1.28

Activity Summary

IC50 11 meas. best 8.58

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Fibroblast growth factor receptor 1
CHEMBL3650
IC50 8.58 7.44 2.6 3
Fibroblast growth factor receptor 2
CHEMBL4142
IC50 8.13 8.13 7.4 1
Fibroblast growth factor receptor 4
CHEMBL3973
IC50 7.98 7.98 10.5 1
Fibroblast growth factor receptor 3
CHEMBL2742
IC50 7.9 7.46 12.6 2
Vascular endothelial growth factor receptor 2
CHEMBL279
IC50 6.22 5.63 602.6 2
Receptor-type tyrosine-protein kinase FLT3
CHEMBL1974
IC50 5.2 5.12 6309.6 2

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Fibroblast growth factor receptor 1 IC50 = 2.63 nM 8.58 Inhibition of human FGFR1 using Btn-Flt3 as substrate after 60 mins by TR-FRET a... -
Fibroblast growth factor receptor 1 IC50 = 2.884 nM 8.54 Inhibition of FGFR1 (unknown origin) transfected in mouse BA/F3 cells assessed a... -
Fibroblast growth factor receptor 2 IC50 = 7.413 nM 8.13 Inhibition of human FGFR2 using Btn-Flt3 as substrate after 60 mins by TR-FRET a... -
Fibroblast growth factor receptor 4 IC50 = 10.47 nM 7.98 Inhibition of human FGFR4 using Btn-Flt3 as substrate after 60 mins by TR-FRET a... -
Fibroblast growth factor receptor 3 IC50 = 12.59 nM 7.9 Inhibition of human FGFR3 using Btn-Flt3 as substrate after 60 mins by TR-FRET a... -
Fibroblast growth factor receptor 3 IC50 = 95.5 nM 7.02 Inhibition of FGFR3 (unknown origin) transfected in mouse BA/F3 cells assessed a... -
Vascular endothelial growth factor receptor 2 IC50 = 602.56 nM 6.22 Inhibition of human VEGFR2 using Btn-Flt3 as substrate after 120 mins by TR-FRET... -
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... -
Fibroblast growth factor receptor 1 IC50 = 6309.57 nM 5.2 Inhibition of FGFR1 (unknown origin) transfected in mouse BA/F3 cells assessed a... -
Vascular endothelial growth factor receptor 2 IC50 = 9120.11 nM 5.04 Inhibition of VEGFR2 (unknown origin) transfected in mouse BA/F3 cells assessed ... -
Receptor-type tyrosine-protein kinase FLT3 IC50 = 9120.11 nM 5.04 Inhibition of FLT3 (unknown origin) transfected in mouse BA/F3 cells assessed as... -

Data from ChEMBL 36 via Core Engine