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Compound Detail

CHEMBL3948321

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COc1cc(OC)cc(N(CC2CC2)c2ccc3ncc(-c4cnn(CC5CCN(C)CC5)c4)nc3c2)c1

Basic Information

ChEMBL ID CHEMBL3948321
Phase Preclinical
Structure Type MOL
InChI Key YWWFVNOOHJHQOP-UHFFFAOYSA-N
6
Targets
13
Activities
1
Assay Types
0
PK Parameters
0
Publications
0
Known Names

Molecular Properties

512.7
MW (Da)
5.40
ALogP
8
HBA
0
HBD
68.5
PSA (Ų)
0.30
QED
2
Ro5 Violations
9
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C30H36N6O2
MW 512.66
Aromatic Rings 4
Heavy Atoms 38
NP-Likeness -1.21

Activity Summary

IC50 13 meas. best 8.91

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Fibroblast growth factor receptor 3
CHEMBL2742
IC50 8.91 6.7433 1.2 3
Fibroblast growth factor receptor 1
CHEMBL3650
IC50 8.8 6.65 1.6 3
Fibroblast growth factor receptor 2
CHEMBL4142
IC50 8.5 8.5 3.2 1
Fibroblast growth factor receptor 4
CHEMBL3973
IC50 7.33 7.33 46.8 1
Vascular endothelial growth factor receptor 2
CHEMBL279
IC50 7.22 5.92 60.3 3
Receptor-type tyrosine-protein kinase FLT3
CHEMBL1974
IC50 5.27 5.23 5370.3 2

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Fibroblast growth factor receptor 3 IC50 = 1.23 nM 8.91 Inhibition of human FGFR3 using Btn-Flt3 as substrate after 60 mins by TR-FRET a... -
Fibroblast growth factor receptor 1 IC50 = 1.585 nM 8.8 Inhibition of human FGFR1 using Btn-Flt3 as substrate after 60 mins by TR-FRET a... -
Fibroblast growth factor receptor 2 IC50 = 3.162 nM 8.5 Inhibition of human FGFR2 using Btn-Flt3 as substrate after 60 mins by TR-FRET a... -
Fibroblast growth factor receptor 4 IC50 = 46.77 nM 7.33 Inhibition of human FGFR4 using Btn-Flt3 as substrate after 60 mins by TR-FRET a... -
Vascular endothelial growth factor receptor 2 IC50 = 60.26 nM 7.22 Inhibition of human VEGFR2 using Btn-Flt3 as substrate after 120 mins by TR-FRET... -
Fibroblast growth factor receptor 1 IC50 = 794.33 nM 6.1 Inhibition of FGFR1 (unknown origin) transfected in mouse BA/F3 cells assessed a... -
Fibroblast growth factor receptor 3 IC50 = 933.25 nM 6.03 Inhibition of FGFR3 (unknown origin) transfected in mouse BA/F3 cells assessed a... -
Fibroblast growth factor receptor 3 IC50 = 5128.61 nM 5.29 Inhibition of FGFR3 (unknown origin) transfected in mouse BA/F3 cells assessed a... -
Vascular endothelial growth factor receptor 2 IC50 = 5248.07 nM 5.28 Inhibition of VEGFR2 (unknown origin) transfected in mouse BA/F3 cells assessed ... -
Receptor-type tyrosine-protein kinase FLT3 IC50 = 5370.32 nM 5.27 Inhibition of FLT3 (unknown origin) transfected in mouse BA/F3 cells assessed as... -
Vascular endothelial growth factor receptor 2 IC50 = 5495.41 nM 5.26 Inhibition of VEGFR2 (unknown origin) transfected in mouse BA/F3 cells assessed ... -
Receptor-type tyrosine-protein kinase FLT3 IC50 = 6456.54 nM 5.19 Inhibition of FLT3 (unknown origin) transfected in mouse BA/F3 cells assessed as... -
Fibroblast growth factor receptor 1 IC50 = 8912.51 nM 5.05 Inhibition of FGFR1 (unknown origin) transfected in mouse BA/F3 cells assessed a... -

Data from ChEMBL 36 via Core Engine