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Compound Detail

CHEMBL3968139

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COc1cc(OC)cc(N(CCCN2[C@@H](C)CC[C@@H]2C)c2ccc3ncc(-c4cnn(C)c4)nc3c2)c1.Cl

Basic Information

ChEMBL ID CHEMBL3968139
Phase Preclinical
Structure Type MOL
InChI Key NQEIXHXOMZOMCJ-GUTACTQSSA-N
Parent Compound CHEMBL3990879
Active Moiety CHEMBL3990879
6
Targets
11
Activities
1
Assay Types
0
PK Parameters
0
Publications
0
Known Names

Molecular Properties

500.6
MW (Da)
5.45
ALogP
8
HBA
0
HBD
68.5
PSA (Ų)
0.30
QED
2
Ro5 Violations
9
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C29H37ClN6O2
MW 537.11
Aromatic Rings 4
Heavy Atoms 37
NP-Likeness -1.26

Activity Summary

IC50 11 meas. best 8.71

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Fibroblast growth factor receptor 2
CHEMBL4142
IC50 8.71 8.71 1.9 1
Fibroblast growth factor receptor 1
CHEMBL3650
IC50 8.53 8.195 3.0 2
Fibroblast growth factor receptor 3
CHEMBL2742
IC50 8.39 7.1633 4.1 3
Fibroblast growth factor receptor 4
CHEMBL3973
IC50 8.13 8.13 7.4 1
Vascular endothelial growth factor receptor 2
CHEMBL279
IC50 7.18 6.03 66.1 3
Receptor-type tyrosine-protein kinase FLT3
CHEMBL1974
IC50 5.14 5.14 7244.4 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Fibroblast growth factor receptor 2 IC50 = 1.95 nM 8.71 Inhibition of human FGFR2 using Btn-Flt3 as substrate after 60 mins by TR-FRET a... -
Fibroblast growth factor receptor 1 IC50 = 2.951 nM 8.53 Inhibition of human FGFR1 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 human FGFR3 using Btn-Flt3 as substrate after 60 mins by TR-FRET a... -
Fibroblast growth factor receptor 4 IC50 = 7.413 nM 8.13 Inhibition of human FGFR4 using Btn-Flt3 as substrate after 60 mins by TR-FRET a... -
Fibroblast growth factor receptor 3 IC50 = 10.96 nM 7.96 Inhibition of FGFR3 (unknown origin) transfected in mouse BA/F3 cells assessed a... -
Fibroblast growth factor receptor 1 IC50 = 13.8 nM 7.86 Inhibition of FGFR1 (unknown origin) transfected in mouse BA/F3 cells assessed a... -
Vascular endothelial growth factor receptor 2 IC50 = 66.07 nM 7.18 Inhibition of human VEGFR2 using Btn-Flt3 as substrate after 120 mins by TR-FRET... -
Vascular endothelial growth factor receptor 2 IC50 = 1288.25 nM 5.89 Inhibition of VEGFR2 (unknown origin) transfected in mouse BA/F3 cells assessed ... -
Fibroblast growth factor receptor 3 IC50 = 7244.36 nM 5.14 Inhibition of FGFR3 (unknown origin) transfected in mouse BA/F3 cells assessed a... -
Receptor-type tyrosine-protein kinase FLT3 IC50 = 7244.36 nM 5.14 Inhibition of FLT3 (unknown origin) transfected in mouse BA/F3 cells assessed as... -
Vascular endothelial growth factor receptor 2 IC50 = 9549.93 nM 5.02 Inhibition of VEGFR2 (unknown origin) transfected in mouse BA/F3 cells assessed ... -

Data from ChEMBL 36 via Core Engine