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Compound Detail

CHEMBL3960128

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COc1cc(OC)cc(N(CC2CC2)c2ccc3ncc(-c4cnn(C(C)(C)C(=O)N5CCNCC5)c4)nc3c2)c1

Basic Information

ChEMBL ID CHEMBL3960128
Phase Preclinical
Structure Type MOL
InChI Key RZRVTNNQCLYNOB-UHFFFAOYSA-N
6
Targets
12
Activities
1
Assay Types
0
PK Parameters
0
Publications
0
Known Names

Molecular Properties

555.7
MW (Da)
4.23
ALogP
9
HBA
1
HBD
97.6
PSA (Ų)
0.33
QED
1
Ro5 Violations
9
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C31H37N7O3
MW 555.68
Aromatic Rings 4
Heavy Atoms 41
NP-Likeness -1.13

Activity Summary

IC50 12 meas. best 7.93

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Fibroblast growth factor receptor 3
CHEMBL2742
IC50 7.93 6.16 11.8 3
Fibroblast growth factor receptor 1
CHEMBL3650
IC50 7.73 6.52 18.6 2
Fibroblast growth factor receptor 2
CHEMBL4142
IC50 7.73 7.73 18.6 1
Vascular endothelial growth factor receptor 2
CHEMBL279
IC50 6.34 5.5633 457.1 3
Fibroblast growth factor receptor 4
CHEMBL3973
IC50 6.12 6.12 758.6 1
Receptor-type tyrosine-protein kinase FLT3
CHEMBL1974
IC50 5.37 5.315 4265.8 2

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Fibroblast growth factor receptor 3 IC50 = 11.75 nM 7.93 Inhibition of human FGFR3 using Btn-Flt3 as substrate after 60 mins by TR-FRET a... -
Fibroblast growth factor receptor 1 IC50 = 18.62 nM 7.73 Inhibition of human FGFR1 using Btn-Flt3 as substrate after 60 mins by TR-FRET a... -
Fibroblast growth factor receptor 2 IC50 = 18.62 nM 7.73 Inhibition of human FGFR2 using Btn-Flt3 as substrate after 60 mins by TR-FRET a... -
Vascular endothelial growth factor receptor 2 IC50 = 457.09 nM 6.34 Inhibition of human VEGFR2 using Btn-Flt3 as substrate after 120 mins by TR-FRET... -
Fibroblast growth factor receptor 4 IC50 = 758.58 nM 6.12 Inhibition of human FGFR4 using Btn-Flt3 as substrate after 60 mins by TR-FRET a... -
Receptor-type tyrosine-protein kinase FLT3 IC50 = 4265.8 nM 5.37 Inhibition of FLT3 (unknown origin) transfected in mouse BA/F3 cells assessed as... -
Fibroblast growth factor receptor 1 IC50 = 4897.79 nM 5.31 Inhibition of FGFR1 (unknown origin) transfected in mouse BA/F3 cells assessed a... -
Fibroblast growth factor receptor 3 IC50 = 5128.61 nM 5.29 Inhibition of FGFR3 (unknown origin) transfected in mouse BA/F3 cells assessed a... -
Fibroblast growth factor receptor 3 IC50 = 5495.41 nM 5.26 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 = 5888.44 nM 5.23 Inhibition of VEGFR2 (unknown origin) transfected in mouse BA/F3 cells assessed ... -
Vascular endothelial growth factor receptor 2 IC50 = 7585.78 nM 5.12 Inhibition of VEGFR2 (unknown origin) transfected in mouse BA/F3 cells assessed ... -

Data from ChEMBL 36 via Core Engine