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Compound Detail

CHEMBL3985853

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COc1cc(OC)cc(N(CC2CC2)c2ccc3ncc(-c4cnn(CCN5CCNCC5)c4)nc3c2)c1.Cl

Basic Information

ChEMBL ID CHEMBL3985853
Phase Preclinical
Structure Type MOL
InChI Key UTRCUCHWVOMQOQ-UHFFFAOYSA-N
Parent Compound CHEMBL3990358
Active Moiety CHEMBL3990358
6
Targets
12
Activities
1
Assay Types
0
PK Parameters
0
Publications
0
Known Names

Molecular Properties

513.6
MW (Da)
3.96
ALogP
9
HBA
1
HBD
80.6
PSA (Ų)
0.34
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 C29H36ClN7O2
MW 550.11
Aromatic Rings 4
Heavy Atoms 38
NP-Likeness -1.34

Activity Summary

IC50 12 meas. best 8.76

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Fibroblast growth factor receptor 3
CHEMBL2742
IC50 8.76 6.65 1.7 3
Fibroblast growth factor receptor 1
CHEMBL3650
IC50 8.66 7.3 2.2 2
Fibroblast growth factor receptor 2
CHEMBL4142
IC50 8.5 8.5 3.2 1
Fibroblast growth factor receptor 4
CHEMBL3973
IC50 7.33 7.33 46.8 1
Vascular endothelial growth factor receptor 2
CHEMBL279
IC50 7.14 5.8667 72.4 3
Receptor-type tyrosine-protein kinase FLT3
CHEMBL1974
IC50 5.26 5.255 5495.4 2

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Fibroblast growth factor receptor 3 IC50 = 1.738 nM 8.76 Inhibition of human FGFR3 using Btn-Flt3 as substrate after 60 mins by TR-FRET a... -
Fibroblast growth factor receptor 1 IC50 = 2.188 nM 8.66 Inhibition of human FGFR1 using Btn-Flt3 as substrate after 60 mins by TR-FRET a... -
Fibroblast growth factor receptor 2 IC50 = 3.162 nM 8.5 Inhibition of human FGFR2 using Btn-Flt3 as substrate after 60 mins by TR-FRET a... -
Fibroblast growth factor receptor 4 IC50 = 46.77 nM 7.33 Inhibition of human FGFR4 using Btn-Flt3 as substrate after 60 mins by TR-FRET a... -
Vascular endothelial growth factor receptor 2 IC50 = 72.44 nM 7.14 Inhibition of human VEGFR2 using Btn-Flt3 as substrate after 120 mins by TR-FRET... -
Fibroblast growth factor receptor 1 IC50 = 1148.15 nM 5.94 Inhibition of FGFR1 (unknown origin) transfected in mouse BA/F3 cells assessed a... -
Fibroblast growth factor receptor 3 IC50 = 1230.27 nM 5.91 Inhibition of FGFR3 (unknown origin) transfected in mouse BA/F3 cells assessed a... -
Fibroblast growth factor receptor 3 IC50 = 5248.07 nM 5.28 Inhibition of FGFR3 (unknown origin) transfected in mouse BA/F3 cells assessed a... -
Receptor-type tyrosine-protein kinase FLT3 IC50 = 5495.41 nM 5.26 Inhibition of FLT3 (unknown origin) transfected in mouse BA/F3 cells assessed as... -
Vascular endothelial growth factor receptor 2 IC50 = 5623.41 nM 5.25 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... -
Vascular endothelial growth factor receptor 2 IC50 = 6165.95 nM 5.21 Inhibition of VEGFR2 (unknown origin) transfected in mouse BA/F3 cells assessed ... -

Data from ChEMBL 36 via Core Engine