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Compound Detail

CHEMBL3986068

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COc1cc(OC)c(Cl)c(N(CCNC(C)C)c2ccc3ncc(-c4cnn(C)c4)nc3c2)c1.Cl

Basic Information

ChEMBL ID CHEMBL3986068
Phase Preclinical
Structure Type MOL
InChI Key QGTZGRJGVNFBKB-UHFFFAOYSA-N
Parent Compound CHEMBL3990409
Active Moiety CHEMBL3990409
6
Targets
10
Activities
1
Assay Types
0
PK Parameters
0
Publications
0
Known Names

Molecular Properties

481.0
MW (Da)
4.84
ALogP
8
HBA
1
HBD
77.3
PSA (Ų)
0.37
QED
0
Ro5 Violations
9
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C25H30Cl2N6O2
MW 517.46
Aromatic Rings 4
Heavy Atoms 34
NP-Likeness -1.26

Activity Summary

IC50 10 meas. best 8.65

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Fibroblast growth factor receptor 1
CHEMBL3650
IC50 8.65 8.42 2.2 2
Fibroblast growth factor receptor 2
CHEMBL4142
IC50 8.46 8.46 3.5 1
Fibroblast growth factor receptor 3
CHEMBL2742
IC50 8.39 7.27 4.1 3
Fibroblast growth factor receptor 4
CHEMBL3973
IC50 8.27 8.27 5.4 1
Vascular endothelial growth factor receptor 2
CHEMBL279
IC50 7.75 7.355 17.8 2
Receptor-type tyrosine-protein kinase FLT3
CHEMBL1974
IC50 5.1 5.1 7943.3 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Fibroblast growth factor receptor 1 IC50 = 2.239 nM 8.65 Inhibition of human FGFR1 using Btn-Flt3 as substrate after 60 mins by TR-FRET a... -
Fibroblast growth factor receptor 2 IC50 = 3.467 nM 8.46 Inhibition of human FGFR2 using Btn-Flt3 as substrate after 60 mins by TR-FRET a... -
Fibroblast growth factor receptor 3 IC50 = 4.074 nM 8.39 Inhibition of FGFR3 (unknown origin) transfected in mouse BA/F3 cells assessed a... -
Fibroblast growth factor receptor 3 IC50 = 4.898 nM 8.31 Inhibition of human FGFR3 using Btn-Flt3 as substrate after 60 mins by TR-FRET a... -
Fibroblast growth factor receptor 4 IC50 = 5.37 nM 8.27 Inhibition of human FGFR4 using Btn-Flt3 as substrate after 60 mins by TR-FRET a... -
Fibroblast growth factor receptor 1 IC50 = 6.457 nM 8.19 Inhibition of FGFR1 (unknown origin) transfected in mouse BA/F3 cells assessed a... -
Vascular endothelial growth factor receptor 2 IC50 = 17.78 nM 7.75 Inhibition of human VEGFR2 using Btn-Flt3 as substrate after 120 mins by TR-FRET... -
Vascular endothelial growth factor receptor 2 IC50 = 109.65 nM 6.96 Inhibition of VEGFR2 (unknown origin) transfected in mouse BA/F3 cells assessed ... -
Fibroblast growth factor receptor 3 IC50 = 7762.47 nM 5.11 Inhibition of FGFR3 (unknown origin) transfected in mouse BA/F3 cells assessed a... -
Receptor-type tyrosine-protein kinase FLT3 IC50 = 7943.28 nM 5.1 Inhibition of FLT3 (unknown origin) transfected in mouse BA/F3 cells assessed as... -

Data from ChEMBL 36 via Core Engine