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Compound Detail

CHEMBL3971277

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COc1cc(OC)cc(N(CCCN2CCC(N3CCCCC3)C2)c2ccc3ncc(-c4cnn(C)c4)nc3c2)c1

Basic Information

ChEMBL ID CHEMBL3971277
Phase Preclinical
Structure Type MOL
InChI Key YOPGGAOPPHWDEP-UHFFFAOYSA-N
7
Targets
17
Activities
1
Assay Types
0
PK Parameters
0
Publications
0
Known Names

Molecular Properties

555.7
MW (Da)
5.14
ALogP
9
HBA
0
HBD
71.8
PSA (Ų)
0.27
QED
2
Ro5 Violations
10
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C32H41N7O2
MW 555.73
Aromatic Rings 4
Heavy Atoms 41
NP-Likeness -1.41

Activity Summary

IC50 17 meas. best 8.87

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Fibroblast growth factor receptor 3
CHEMBL2742
IC50 8.87 7.46 1.3 5
Fibroblast growth factor receptor 1
CHEMBL3650
IC50 8.8 6.6233 1.6 3
Fibroblast growth factor receptor 2
CHEMBL4142
IC50 8.68 8.68 2.1 1
Fibroblast growth factor receptor 4
CHEMBL3973
IC50 8.17 8.17 6.8 1
Vascular endothelial growth factor receptor 2
CHEMBL279
IC50 7.44 6.3475 36.3 4
NON-PROTEIN TARGET
CHEMBL3879801
IC50 6.21 6.21 616.6 1
Receptor-type tyrosine-protein kinase FLT3
CHEMBL1974
IC50 5.22 5.175 6025.6 2

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Fibroblast growth factor receptor 3 IC50 = 1.349 nM 8.87 Inhibition of recombinant human N-terminal His6-tagged FGFR3 expressed in insect... -
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 = 2.089 nM 8.68 Inhibition of human FGFR2 using Btn-Flt3 as substrate after 60 mins by TR-FRET a... -
Fibroblast growth factor receptor 3 IC50 = 3.802 nM 8.42 Inhibition of human FGFR3 using Btn-Flt3 as substrate after 60 mins by TR-FRET a... -
Fibroblast growth factor receptor 3 IC50 = 6.31 nM 8.2 Inhibition of TEL-fused FGFR3 (unknown origin) transfected in mouse BA/F3 cells ... -
Fibroblast growth factor receptor 4 IC50 = 6.761 nM 8.17 Inhibition of human FGFR4 using Btn-Flt3 as substrate after 60 mins by TR-FRET a... -
Vascular endothelial growth factor receptor 2 IC50 = 36.31 nM 7.44 Inhibition of recombinant human N-terminal His6-tagged VEGFR2 (790 end residues)... -
Vascular endothelial growth factor receptor 2 IC50 = 57.54 nM 7.24 Inhibition of human VEGFR2 using Btn-Flt3 as substrate after 120 mins by TR-FRET... -
Fibroblast growth factor receptor 3 IC50 = 229.09 nM 6.64 Inhibition of FGFR3 (unknown origin) transfected in mouse BA/F3 cells assessed a... -
NON-PROTEIN TARGET IC50 = 616.6 nM 6.21 Antiproliferative activity against mouse BA/F3 cells in presence of mouse IL3 af... -
Fibroblast growth factor receptor 1 IC50 = 912.01 nM 6.04 Inhibition of FGFR1 (unknown origin) transfected in mouse BA/F3 cells assessed a... -
Vascular endothelial growth factor receptor 2 IC50 = 2630.27 nM 5.58 Inhibition of VEGFR2 (unknown origin) transfected in mouse BA/F3 cells assessed ... -
Receptor-type tyrosine-protein kinase FLT3 IC50 = 6025.6 nM 5.22 Inhibition of FLT3 (unknown origin) transfected in mouse BA/F3 cells assessed as... -
Fibroblast growth factor receptor 3 IC50 = 6760.83 nM 5.17 Inhibition of FGFR3 (unknown origin) transfected in mouse BA/F3 cells assessed a... -
Vascular endothelial growth factor receptor 2 IC50 = 7413.1 nM 5.13 Inhibition of VEGFR2 (unknown origin) transfected in mouse BA/F3 cells assessed ... -
Receptor-type tyrosine-protein kinase FLT3 IC50 = 7413.1 nM 5.13 Inhibition of FLT3 (unknown origin) transfected in mouse BA/F3 cells assessed as... -
Fibroblast growth factor receptor 1 IC50 = 9332.54 nM 5.03 Inhibition of FGFR1 (unknown origin) transfected in mouse BA/F3 cells assessed a... -

Data from ChEMBL 36 via Core Engine