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Compound Detail

CHEMBL3962814

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COc1cc(OC)cc(N(CC2CC2)c2ccc3ncc(-c4cnn(CCN5CCCC5)c4)nc3c2)c1.Cl

Basic Information

ChEMBL ID CHEMBL3962814
Phase Preclinical
Structure Type MOL
InChI Key PAWXGXHMRSTMFA-UHFFFAOYSA-N
Parent Compound CHEMBL3991053
Active Moiety CHEMBL3991053
6
Targets
11
Activities
1
Assay Types
0
PK Parameters
0
Publications
0
Known Names

Molecular Properties

498.6
MW (Da)
5.15
ALogP
8
HBA
0
HBD
68.5
PSA (Ų)
0.30
QED
1
Ro5 Violations
10
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C29H35ClN6O2
MW 535.09
Aromatic Rings 4
Heavy Atoms 37
NP-Likeness -1.39

Activity Summary

IC50 11 meas. best 8.49

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Fibroblast growth factor receptor 3
CHEMBL2742
IC50 8.49 6.5033 3.2 3
Fibroblast growth factor receptor 2
CHEMBL4142
IC50 8.29 8.29 5.1 1
Fibroblast growth factor receptor 1
CHEMBL3650
IC50 8.27 7.055 5.4 2
Fibroblast growth factor receptor 4
CHEMBL3973
IC50 7.0 7.0 100.0 1
Vascular endothelial growth factor receptor 2
CHEMBL279
IC50 6.76 5.63 173.8 3
Receptor-type tyrosine-protein kinase FLT3
CHEMBL1974
IC50 5.24 5.24 5754.4 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Fibroblast growth factor receptor 3 IC50 = 3.236 nM 8.49 Inhibition of human FGFR3 using Btn-Flt3 as substrate after 60 mins by TR-FRET a... -
Fibroblast growth factor receptor 2 IC50 = 5.129 nM 8.29 Inhibition of human FGFR2 using Btn-Flt3 as substrate after 60 mins by TR-FRET a... -
Fibroblast growth factor receptor 1 IC50 = 5.37 nM 8.27 Inhibition of human FGFR1 using Btn-Flt3 as substrate after 60 mins by TR-FRET a... -
Fibroblast growth factor receptor 4 IC50 = 100.0 nM 7.0 Inhibition of human FGFR4 using Btn-Flt3 as substrate after 60 mins by TR-FRET a... -
Vascular endothelial growth factor receptor 2 IC50 = 173.78 nM 6.76 Inhibition of human VEGFR2 using Btn-Flt3 as substrate after 120 mins by TR-FRET... -
Fibroblast growth factor receptor 1 IC50 = 1445.44 nM 5.84 Inhibition of FGFR1 (unknown origin) transfected in mouse BA/F3 cells assessed a... -
Fibroblast growth factor receptor 3 IC50 = 1698.24 nM 5.77 Inhibition of FGFR3 (unknown origin) transfected in mouse BA/F3 cells assessed a... -
Fibroblast growth factor receptor 3 IC50 = 5623.41 nM 5.25 Inhibition of FGFR3 (unknown origin) transfected in mouse BA/F3 cells assessed a... -
Receptor-type tyrosine-protein kinase FLT3 IC50 = 5754.4 nM 5.24 Inhibition of FLT3 (unknown origin) transfected in mouse BA/F3 cells assessed as... -
Vascular endothelial growth factor receptor 2 IC50 = 8317.64 nM 5.08 Inhibition of VEGFR2 (unknown origin) transfected in mouse BA/F3 cells assessed ... -
Vascular endothelial growth factor receptor 2 IC50 = 8912.51 nM 5.05 Inhibition of VEGFR2 (unknown origin) transfected in mouse BA/F3 cells assessed ... -

Data from ChEMBL 36 via Core Engine