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Compound Detail

CHEMBL3964762

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COc1cc(OC)cc(N(CC#Cc2cc(Cl)nc(N)n2)c2ccc3ncc(-c4cnn(C)c4)nc3c2)c1

Basic Information

ChEMBL ID CHEMBL3964762
Phase Preclinical
Structure Type MOL
InChI Key XHSUXSHBEVITPC-UHFFFAOYSA-N
6
Targets
12
Activities
1
Assay Types
0
PK Parameters
0
Publications
0
Known Names

Molecular Properties

527.0
MW (Da)
4.26
ALogP
10
HBA
1
HBD
117.1
PSA (Ų)
0.26
QED
1
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C27H23ClN8O2
MW 526.99
Aromatic Rings 5
Heavy Atoms 38
NP-Likeness -1.24

Activity Summary

IC50 12 meas. best 8.19

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Fibroblast growth factor receptor 1
CHEMBL3650
IC50 8.19 6.9833 6.5 3
Fibroblast growth factor receptor 3
CHEMBL2742
IC50 7.89 6.91 12.9 3
Fibroblast growth factor receptor 2
CHEMBL4142
IC50 7.79 7.79 16.2 1
Fibroblast growth factor receptor 4
CHEMBL3973
IC50 7.45 7.45 35.5 1
Vascular endothelial growth factor receptor 2
CHEMBL279
IC50 6.7 6.15 199.5 2
Receptor-type tyrosine-protein kinase FLT3
CHEMBL1974
IC50 5.67 5.6 2138.0 2

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Fibroblast growth factor receptor 1 IC50 = 6.457 nM 8.19 Inhibition of human FGFR1 using Btn-Flt3 as substrate after 60 mins by TR-FRET a... -
Fibroblast growth factor receptor 3 IC50 = 12.88 nM 7.89 Inhibition of human FGFR3 using Btn-Flt3 as substrate after 60 mins by TR-FRET a... -
Fibroblast growth factor receptor 2 IC50 = 16.22 nM 7.79 Inhibition of human FGFR2 using Btn-Flt3 as substrate after 60 mins by TR-FRET a... -
Fibroblast growth factor receptor 4 IC50 = 35.48 nM 7.45 Inhibition of human FGFR4 using Btn-Flt3 as substrate after 60 mins by TR-FRET a... -
Fibroblast growth factor receptor 3 IC50 = 52.48 nM 7.28 Inhibition of FGFR3 (unknown origin) transfected in mouse BA/F3 cells assessed a... -
Fibroblast growth factor receptor 1 IC50 = 85.11 nM 7.07 Inhibition of FGFR1 (unknown origin) transfected in mouse BA/F3 cells assessed a... -
Vascular endothelial growth factor receptor 2 IC50 = 199.53 nM 6.7 Inhibition of human VEGFR2 using Btn-Flt3 as substrate after 120 mins by TR-FRET... -
Fibroblast growth factor receptor 1 IC50 = 2041.74 nM 5.69 Inhibition of FGFR1 (unknown origin) transfected in mouse BA/F3 cells assessed a... -
Receptor-type tyrosine-protein kinase FLT3 IC50 = 2137.96 nM 5.67 Inhibition of FLT3 (unknown origin) transfected in mouse BA/F3 cells assessed as... -
Vascular endothelial growth factor receptor 2 IC50 = 2511.89 nM 5.6 Inhibition of VEGFR2 (unknown origin) transfected in mouse BA/F3 cells assessed ... -
Fibroblast growth factor receptor 3 IC50 = 2754.23 nM 5.56 Inhibition of FGFR3 (unknown origin) transfected in mouse BA/F3 cells assessed a... -
Receptor-type tyrosine-protein kinase FLT3 IC50 = 2951.21 nM 5.53 Inhibition of FLT3 (unknown origin) transfected in mouse BA/F3 cells assessed as... -

Data from ChEMBL 36 via Core Engine