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Compound Detail

CHEMBL3984039

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COc1cc(OC)cc(N(CCCN2CCC(O)C2)c2ccc3ncc(-c4cnn(C)c4)nc3c2)c1.Cl

Basic Information

ChEMBL ID CHEMBL3984039
Phase Preclinical
Structure Type MOL
InChI Key SKARZTBSWNWMLX-UHFFFAOYSA-N
Parent Compound CHEMBL3962736
Active Moiety CHEMBL3962736
6
Targets
12
Activities
1
Assay Types
0
PK Parameters
0
Publications
0
Known Names

Molecular Properties

488.6
MW (Da)
3.64
ALogP
9
HBA
1
HBD
88.8
PSA (Ų)
0.38
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 C27H33ClN6O3
MW 525.05
Aromatic Rings 4
Heavy Atoms 36
NP-Likeness -1.32

Activity Summary

IC50 12 meas. best 9.24

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Fibroblast growth factor receptor 3
CHEMBL2742
IC50 9.24 8.7475 0.6 4
Fibroblast growth factor receptor 1
CHEMBL3650
IC50 8.87 8.295 1.3 2
Fibroblast growth factor receptor 2
CHEMBL4142
IC50 8.71 8.71 1.9 1
Fibroblast growth factor receptor 4
CHEMBL3973
IC50 8.39 8.39 4.1 1
Vascular endothelial growth factor receptor 2
CHEMBL279
IC50 8.05 7.5567 8.9 3
NON-PROTEIN TARGET
CHEMBL3879801
IC50 5.72 5.72 1905.5 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Fibroblast growth factor receptor 3 IC50 = 0.5754 nM 9.24 Inhibition of TEL-fused FGFR3 (unknown origin) transfected in mouse BA/F3 cells ... -
Fibroblast growth factor receptor 3 IC50 = 0.6457 nM 9.19 Inhibition of recombinant human N-terminal His6-tagged FGFR3 expressed in insect... -
Fibroblast growth factor receptor 1 IC50 = 1.349 nM 8.87 Inhibition of human FGFR1 using Btn-Flt3 as substrate after 60 mins by TR-FRET a... -
Fibroblast growth factor receptor 3 IC50 = 1.698 nM 8.77 Inhibition of human FGFR3 using Btn-Flt3 as substrate after 60 mins by TR-FRET a... -
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 4 IC50 = 4.074 nM 8.39 Inhibition of human FGFR4 using Btn-Flt3 as substrate after 60 mins by TR-FRET a... -
Vascular endothelial growth factor receptor 2 IC50 = 8.913 nM 8.05 Inhibition of recombinant human N-terminal His6-tagged VEGFR2 (790 end residues)... -
Vascular endothelial growth factor receptor 2 IC50 = 10.72 nM 7.97 Inhibition of human VEGFR2 using Btn-Flt3 as substrate after 120 mins by TR-FRET... -
Fibroblast growth factor receptor 3 IC50 = 16.22 nM 7.79 Inhibition of FGFR3 (unknown origin) transfected in mouse BA/F3 cells assessed a... -
Fibroblast growth factor receptor 1 IC50 = 19.05 nM 7.72 Inhibition of FGFR1 (unknown origin) transfected in mouse BA/F3 cells assessed a... -
Vascular endothelial growth factor receptor 2 IC50 = 223.87 nM 6.65 Inhibition of VEGFR2 (unknown origin) transfected in mouse BA/F3 cells assessed ... -
NON-PROTEIN TARGET IC50 = 1905.46 nM 5.72 Antiproliferative activity against mouse BA/F3 cells in presence of mouse IL3 af... -

Data from ChEMBL 36 via Core Engine