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Compound Detail

CHEMBL3980417

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COc1cc(OC)cc(N(CC#Cc2cc(CO)ccn2)c2ccc3ncc(-c4cnn(C)c4)nc3c2)c1

Basic Information

ChEMBL ID CHEMBL3980417
Phase Preclinical
Structure Type MOL
InChI Key JVHRYVZNKJPNLU-UHFFFAOYSA-N
6
Targets
10
Activities
1
Assay Types
0
PK Parameters
0
Publications
0
Known Names

Molecular Properties

506.6
MW (Da)
4.12
ALogP
9
HBA
1
HBD
98.4
PSA (Ų)
0.33
QED
1
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C29H26N6O3
MW 506.57
Aromatic Rings 5
Heavy Atoms 38
NP-Likeness -0.96

Activity Summary

IC50 10 meas. best 8.62

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Fibroblast growth factor receptor 1
CHEMBL3650
IC50 8.62 7.36 2.4 3
Fibroblast growth factor receptor 3
CHEMBL2742
IC50 8.47 8.375 3.4 2
Fibroblast growth factor receptor 2
CHEMBL4142
IC50 8.34 8.34 4.6 1
Fibroblast growth factor receptor 4
CHEMBL3973
IC50 7.83 7.83 14.8 1
Vascular endothelial growth factor receptor 2
CHEMBL279
IC50 6.27 5.66 537.0 2
Receptor-type tyrosine-protein kinase FLT3
CHEMBL1974
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 = 2.399 nM 8.62 Inhibition of human FGFR1 using Btn-Flt3 as substrate after 60 mins by TR-FRET a... -
Fibroblast growth factor receptor 3 IC50 = 3.388 nM 8.47 Inhibition of FGFR3 (unknown origin) transfected in mouse BA/F3 cells assessed a... -
Fibroblast growth factor receptor 1 IC50 = 4.467 nM 8.35 Inhibition of FGFR1 (unknown origin) transfected in mouse BA/F3 cells assessed a... -
Fibroblast growth factor receptor 2 IC50 = 4.571 nM 8.34 Inhibition of human FGFR2 using Btn-Flt3 as substrate after 60 mins by TR-FRET a... -
Fibroblast growth factor receptor 3 IC50 = 5.248 nM 8.28 Inhibition of human FGFR3 using Btn-Flt3 as substrate after 60 mins by TR-FRET a... -
Fibroblast growth factor receptor 4 IC50 = 14.79 nM 7.83 Inhibition of human FGFR4 using Btn-Flt3 as substrate after 60 mins by TR-FRET a... -
Vascular endothelial growth factor receptor 2 IC50 = 537.03 nM 6.27 Inhibition of human VEGFR2 using Btn-Flt3 as substrate after 120 mins by TR-FRET... -
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 = 7762.47 nM 5.11 Inhibition of FGFR1 (unknown origin) transfected in mouse BA/F3 cells assessed a... -
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