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Compound Detail

CHEMBL3959345

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COc1cc(OC)cc(N(CCN2CCC(O)C2)c2ccc3ncc(-c4cnn(C)c4)nc3c2)c1.Cl

Basic Information

ChEMBL ID CHEMBL3959345
Phase Preclinical
Structure Type MOL
InChI Key ISVOAPUXDBEYPJ-UHFFFAOYSA-N
Parent Compound CHEMBL3925286
Active Moiety CHEMBL3925286
6
Targets
12
Activities
1
Assay Types
0
PK Parameters
0
Publications
0
Known Names

Molecular Properties

474.6
MW (Da)
3.25
ALogP
9
HBA
1
HBD
88.8
PSA (Ų)
0.42
QED
0
Ro5 Violations
8
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C26H31ClN6O3
MW 511.03
Aromatic Rings 4
Heavy Atoms 35
NP-Likeness -1.33

Activity Summary

IC50 12 meas. best 8.82

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Fibroblast growth factor receptor 1
CHEMBL3650
IC50 8.82 8.045 1.5 2
Fibroblast growth factor receptor 3
CHEMBL2742
IC50 8.74 8.3575 1.8 4
Fibroblast growth factor receptor 2
CHEMBL4142
IC50 8.67 8.67 2.1 1
Fibroblast growth factor receptor 4
CHEMBL3973
IC50 7.85 7.85 14.1 1
Vascular endothelial growth factor receptor 2
CHEMBL279
IC50 7.48 6.95 33.1 3
NON-PROTEIN TARGET
CHEMBL3879801
IC50 5.13 5.13 7413.1 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Fibroblast growth factor receptor 1 IC50 = 1.514 nM 8.82 Inhibition of human FGFR1 using Btn-Flt3 as substrate after 60 mins by TR-FRET a... -
Fibroblast growth factor receptor 3 IC50 = 1.82 nM 8.74 Inhibition of recombinant human N-terminal His6-tagged FGFR3 expressed in insect... -
Fibroblast growth factor receptor 2 IC50 = 2.138 nM 8.67 Inhibition of human FGFR2 using Btn-Flt3 as substrate after 60 mins by TR-FRET a... -
Fibroblast growth factor receptor 3 IC50 = 2.512 nM 8.6 Inhibition of TEL-fused FGFR3 (unknown origin) transfected in mouse BA/F3 cells ... -
Fibroblast growth factor receptor 3 IC50 = 3.02 nM 8.52 Inhibition of human FGFR3 using Btn-Flt3 as substrate after 60 mins by TR-FRET a... -
Fibroblast growth factor receptor 4 IC50 = 14.13 nM 7.85 Inhibition of human FGFR4 using Btn-Flt3 as substrate after 60 mins by TR-FRET a... -
Fibroblast growth factor receptor 3 IC50 = 26.92 nM 7.57 Inhibition of FGFR3 (unknown origin) transfected in mouse BA/F3 cells assessed a... -
Vascular endothelial growth factor receptor 2 IC50 = 33.11 nM 7.48 Inhibition of recombinant human N-terminal His6-tagged VEGFR2 (790 end residues)... -
Vascular endothelial growth factor receptor 2 IC50 = 46.77 nM 7.33 Inhibition of human VEGFR2 using Btn-Flt3 as substrate after 120 mins by TR-FRET... -
Fibroblast growth factor receptor 1 IC50 = 53.7 nM 7.27 Inhibition of FGFR1 (unknown origin) transfected in mouse BA/F3 cells assessed a... -
Vascular endothelial growth factor receptor 2 IC50 = 912.01 nM 6.04 Inhibition of VEGFR2 (unknown origin) transfected in mouse BA/F3 cells assessed ... -
NON-PROTEIN TARGET IC50 = 7413.1 nM 5.13 Antiproliferative activity against mouse BA/F3 cells in presence of mouse IL3 af... -

Data from ChEMBL 36 via Core Engine