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Compound Detail

CHEMBL3927140

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

Basic Information

ChEMBL ID CHEMBL3927140
Phase Preclinical
Structure Type MOL
InChI Key AHEDUFSEDRFCTH-UHFFFAOYSA-N
6
Targets
13
Activities
1
Assay Types
0
PK Parameters
0
Publications
0
Known Names

Molecular Properties

506.6
MW (Da)
4.64
ALogP
9
HBA
0
HBD
87.4
PSA (Ų)
0.30
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 -1.07

Activity Summary

IC50 13 meas. best 8.63

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Fibroblast growth factor receptor 3
CHEMBL2742
IC50 8.63 7.33 2.3 3
Fibroblast growth factor receptor 1
CHEMBL3650
IC50 8.5 7.3933 3.2 3
Fibroblast growth factor receptor 4
CHEMBL3973
IC50 8.3 8.3 5.0 1
Fibroblast growth factor receptor 2
CHEMBL4142
IC50 8.15 8.15 7.1 1
Vascular endothelial growth factor receptor 2
CHEMBL279
IC50 5.71 5.4267 1949.8 3
Receptor-type tyrosine-protein kinase FLT3
CHEMBL1974
IC50 5.43 5.34 3715.3 2

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Fibroblast growth factor receptor 3 IC50 = 2.344 nM 8.63 Inhibition of FGFR3 (unknown origin) transfected in mouse BA/F3 cells assessed a... -
Fibroblast growth factor receptor 1 IC50 = 3.162 nM 8.5 Inhibition of human FGFR1 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 FGFR1 (unknown origin) transfected in mouse BA/F3 cells assessed a... -
Fibroblast growth factor receptor 4 IC50 = 5.012 nM 8.3 Inhibition of human FGFR4 using Btn-Flt3 as substrate after 60 mins by TR-FRET a... -
Fibroblast growth factor receptor 3 IC50 = 6.607 nM 8.18 Inhibition of human FGFR3 using Btn-Flt3 as substrate after 60 mins by TR-FRET a... -
Fibroblast growth factor receptor 2 IC50 = 7.079 nM 8.15 Inhibition of human FGFR2 using Btn-Flt3 as substrate after 60 mins by TR-FRET a... -
Vascular endothelial growth factor receptor 2 IC50 = 1949.84 nM 5.71 Inhibition of human VEGFR2 using Btn-Flt3 as substrate after 120 mins by TR-FRET... -
Receptor-type tyrosine-protein kinase FLT3 IC50 = 3715.35 nM 5.43 Inhibition of FLT3 (unknown origin) transfected in mouse BA/F3 cells assessed as... -
Fibroblast growth factor receptor 1 IC50 = 4365.16 nM 5.36 Inhibition of FGFR1 (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 ... -
Vascular endothelial growth factor receptor 2 IC50 = 5370.32 nM 5.27 Inhibition of VEGFR2 (unknown origin) transfected in mouse BA/F3 cells assessed ... -
Receptor-type tyrosine-protein kinase FLT3 IC50 = 5623.41 nM 5.25 Inhibition of FLT3 (unknown origin) transfected in mouse BA/F3 cells assessed as... -
Fibroblast growth factor receptor 3 IC50 = 6606.93 nM 5.18 Inhibition of FGFR3 (unknown origin) transfected in mouse BA/F3 cells assessed a... -

Data from ChEMBL 36 via Core Engine