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Compound Detail

CHEMBL3908829

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COc1cc(OC)cc(N(CC2CC2)c2ccc3ncc(-c4cnn(CCCN5CCN(CCCO)CC5)c4)nc3c2)c1.Cl

Basic Information

ChEMBL ID CHEMBL3908829
Phase Preclinical
Structure Type MOL
InChI Key RRKHYJVGAHJYAK-UHFFFAOYSA-N
Parent Compound CHEMBL3991135
Active Moiety CHEMBL3991135
6
Targets
13
Activities
1
Assay Types
0
PK Parameters
0
Publications
0
Known Names

Molecular Properties

585.8
MW (Da)
4.45
ALogP
10
HBA
1
HBD
92.0
PSA (Ų)
0.23
QED
1
Ro5 Violations
14
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C33H44ClN7O3
MW 622.21
Aromatic Rings 4
Heavy Atoms 43
NP-Likeness -1.16

Activity Summary

IC50 13 meas. best 8.54

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Fibroblast growth factor receptor 3
CHEMBL2742
IC50 8.54 6.6433 2.9 3
Fibroblast growth factor receptor 1
CHEMBL3650
IC50 8.32 6.5767 4.8 3
Fibroblast growth factor receptor 2
CHEMBL4142
IC50 8.19 8.19 6.5 1
Vascular endothelial growth factor receptor 2
CHEMBL279
IC50 7.69 6.2033 20.4 3
Fibroblast growth factor receptor 4
CHEMBL3973
IC50 7.37 7.37 42.7 1
Receptor-type tyrosine-protein kinase FLT3
CHEMBL1974
IC50 5.28 5.27 5248.1 2

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Fibroblast growth factor receptor 3 IC50 = 2.884 nM 8.54 Inhibition of human FGFR3 using Btn-Flt3 as substrate after 60 mins by TR-FRET a... -
Fibroblast growth factor receptor 1 IC50 = 4.786 nM 8.32 Inhibition of human FGFR1 using Btn-Flt3 as substrate after 60 mins by TR-FRET a... -
Fibroblast growth factor receptor 2 IC50 = 6.457 nM 8.19 Inhibition of human FGFR2 using Btn-Flt3 as substrate after 60 mins by TR-FRET a... -
Vascular endothelial growth factor receptor 2 IC50 = 20.42 nM 7.69 Inhibition of human VEGFR2 using Btn-Flt3 as substrate after 120 mins by TR-FRET... -
Fibroblast growth factor receptor 4 IC50 = 42.66 nM 7.37 Inhibition of human FGFR4 using Btn-Flt3 as substrate after 60 mins by TR-FRET a... -
Fibroblast growth factor receptor 1 IC50 = 691.83 nM 6.16 Inhibition of FGFR1 (unknown origin) transfected in mouse BA/F3 cells assessed a... -
Fibroblast growth factor receptor 3 IC50 = 870.96 nM 6.06 Inhibition of FGFR3 (unknown origin) transfected in mouse BA/F3 cells assessed a... -
Vascular endothelial growth factor receptor 2 IC50 = 2398.83 nM 5.62 Inhibition of VEGFR2 (unknown origin) transfected in mouse BA/F3 cells assessed ... -
Fibroblast growth factor receptor 3 IC50 = 4677.35 nM 5.33 Inhibition of FGFR3 (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 = 5248.07 nM 5.28 Inhibition of FLT3 (unknown origin) transfected in mouse BA/F3 cells assessed as... -
Receptor-type tyrosine-protein kinase FLT3 IC50 = 5495.41 nM 5.26 Inhibition of FLT3 (unknown origin) transfected in mouse BA/F3 cells assessed as... -
Fibroblast growth factor receptor 1 IC50 = 5623.41 nM 5.25 Inhibition of FGFR1 (unknown origin) transfected in mouse BA/F3 cells assessed a... -

Data from ChEMBL 36 via Core Engine