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Compound Detail

CHEMBL3917908

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COc1cc(OC)cc(N(CCNC(C)C)c2ccc3ncc(-c4cnn(C5CCN(C)CC5)c4)nc3c2)c1.Cl

Basic Information

ChEMBL ID CHEMBL3917908
Phase Preclinical
Structure Type MOL
InChI Key WWJUKYMCFMIUBZ-UHFFFAOYSA-N
Parent Compound CHEMBL3990224
Active Moiety CHEMBL3990224
6
Targets
13
Activities
1
Assay Types
0
PK Parameters
0
Publications
0
Known Names

Molecular Properties

529.7
MW (Da)
4.91
ALogP
9
HBA
1
HBD
80.6
PSA (Ų)
0.31
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 C30H40ClN7O2
MW 566.15
Aromatic Rings 4
Heavy Atoms 39
NP-Likeness -1.04

Activity Summary

IC50 13 meas. best 8.85

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Fibroblast growth factor receptor 1
CHEMBL3650
IC50 8.85 7.1667 1.4 3
Fibroblast growth factor receptor 2
CHEMBL4142
IC50 8.53 8.53 3.0 1
Fibroblast growth factor receptor 3
CHEMBL2742
IC50 8.34 6.97 4.6 3
Fibroblast growth factor receptor 4
CHEMBL3973
IC50 7.71 7.71 19.5 1
Vascular endothelial growth factor receptor 2
CHEMBL279
IC50 7.19 6.23 64.6 3
Receptor-type tyrosine-protein kinase FLT3
CHEMBL1974
IC50 5.41 5.31 3890.4 2

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Fibroblast growth factor receptor 1 IC50 = 1.413 nM 8.85 Inhibition of human FGFR1 using Btn-Flt3 as substrate after 60 mins by TR-FRET a... -
Fibroblast growth factor receptor 2 IC50 = 2.951 nM 8.53 Inhibition of human FGFR2 using Btn-Flt3 as substrate after 60 mins by TR-FRET a... -
Fibroblast growth factor receptor 3 IC50 = 4.571 nM 8.34 Inhibition of human FGFR3 using Btn-Flt3 as substrate after 60 mins by TR-FRET a... -
Fibroblast growth factor receptor 4 IC50 = 19.5 nM 7.71 Inhibition of human FGFR4 using Btn-Flt3 as substrate after 60 mins by TR-FRET a... -
Fibroblast growth factor receptor 3 IC50 = 47.86 nM 7.32 Inhibition of FGFR3 (unknown origin) transfected in mouse BA/F3 cells assessed a... -
Fibroblast growth factor receptor 1 IC50 = 52.48 nM 7.28 Inhibition of FGFR1 (unknown origin) transfected in mouse BA/F3 cells assessed a... -
Vascular endothelial growth factor receptor 2 IC50 = 64.57 nM 7.19 Inhibition of human VEGFR2 using Btn-Flt3 as substrate after 120 mins by TR-FRET... -
Vascular endothelial growth factor receptor 2 IC50 = 794.33 nM 6.1 Inhibition of VEGFR2 (unknown origin) transfected in mouse BA/F3 cells assessed ... -
Receptor-type tyrosine-protein kinase FLT3 IC50 = 3890.45 nM 5.41 Inhibition of FLT3 (unknown origin) transfected in mouse BA/F3 cells assessed as... -
Vascular endothelial growth factor receptor 2 IC50 = 3981.07 nM 5.4 Inhibition of VEGFR2 (unknown origin) transfected in mouse BA/F3 cells assessed ... -
Fibroblast growth factor receptor 1 IC50 = 4265.8 nM 5.37 Inhibition of FGFR1 (unknown origin) transfected in mouse BA/F3 cells assessed a... -
Fibroblast growth factor receptor 3 IC50 = 5623.41 nM 5.25 Inhibition of FGFR3 (unknown origin) transfected in mouse BA/F3 cells assessed a... -
Receptor-type tyrosine-protein kinase FLT3 IC50 = 6165.95 nM 5.21 Inhibition of FLT3 (unknown origin) transfected in mouse BA/F3 cells assessed as... -

Data from ChEMBL 36 via Core Engine